Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

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weight		 Rot
Bonds		 H don

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 DOI
25208097 190701 3 None -1 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
CHEMBL481366 190701 3 None -1 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
3917 10702 0 None 3 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44430609 10702 0 None 3 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL409969 10702 0 None 3 4 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL1631926 215597 0 None - 1 Mouse 10.4 pEC50 = 10.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631926 215597 0 None - 1 Mouse 10.4 pEC50 = 10.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL264846 217411 0 None 12 3 Human 10.2 pEC50 = 10.2 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
44388462 168632 0 None 6 3 Human 10.2 pEC50 = 10.2 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414782 168632 0 None 6 3 Human 10.2 pEC50 = 10.2 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
16131448 9624 28 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
1681 9624 28 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
1688 9624 28 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
44361543 9624 28 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
56947112 9624 28 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
CHEMBL396460 9624 28 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Compound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no dataCompound was evaluated for increase in [35S]GTP-gamma-S, binding for human ORL1 receptor carried out in CHO cell membranes; Nd: no data
ChEMBL None None None None 10.1016/s0960-894x(02)00652-2
16131448 9624 28 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1681 9624 28 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1688 9624 28 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
44361543 9624 28 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
56947112 9624 28 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
CHEMBL396460 9624 28 None 2 5 Human 10.1 pEC50 = 10.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
44388461 166619 0 None 6 3 Human 10.0 pEC50 = 10 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL410653 166619 0 None 6 3 Human 10.0 pEC50 = 10 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
24822630 104639 0 None 8 4 Human 10.0 pEC50 = 10 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 4.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2009.07.069
CHEMBL272215 104639 0 None 8 4 Human 10.0 pEC50 = 10 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 4.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2009.07.069
CHEMBL593215 104639 0 None 8 4 Human 10.0 pEC50 = 10 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 4.1 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)c(Cl)c1 10.1016/j.bmc.2009.07.069
16131448 9624 28 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1681 9624 28 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1688 9624 28 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
44361543 9624 28 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
56947112 9624 28 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 9624 28 None 2 5 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
CHEMBL409204 219530 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL261997 217303 8 None - 1 Human 9.8 pEC50 = 9.8 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL2372052 216953 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)[C@H](CN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
16131448 9624 28 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
1681 9624 28 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
1688 9624 28 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
44361543 9624 28 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
56947112 9624 28 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
CHEMBL396460 9624 28 None 2 5 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL None None None None 10.1039/C4MD00082J
CHEMBL265801 217442 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/jm010221v
16131448 9624 28 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
1681 9624 28 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
1688 9624 28 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
44361543 9624 28 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
56947112 9624 28 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
CHEMBL396460 9624 28 None 2 5 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None None 10.1021/acs.jmedchem.5b01976
44388466 103276 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL262544 103276 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL412537 219781 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1cccc(F)c1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL405648 219351 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL1627325 215590 0 None -8 8 Human 9.6 pEC50 = 9.6 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None CSCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(C)(C)C)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)O)[C@@H](C)O 10.1021/jm900604g
CHEMBL427791 220161 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(C#N)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44388467 176184 0 None 4 2 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL442297 176184 0 None 4 2 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
1682 9627 18 None 7 3 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None None 10.1021/jm010221v
6324645 9627 18 None 7 3 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None None 10.1021/jm010221v
CHEMBL384755 9627 18 None 7 3 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None None 10.1021/jm010221v
CHEMBL1631909 215591 0 None - 1 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
CHEMBL1631909 215591 0 None - 1 Mouse 9.4 pEC50 = 9.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
16131448 9624 28 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
1681 9624 28 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
1688 9624 28 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
44361543 9624 28 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
56947112 9624 28 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
CHEMBL396460 9624 28 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Antagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilizationAntagonist activity at human recombinant NOP receptor expressed in CHO cells coexpressing alphaqi5 assessed as inhibition of N/OFQ-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
12419 9252 29 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
24800108 9252 29 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
CHEMBL481512 9252 29 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
16131448 9624 28 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
1681 9624 28 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
1688 9624 28 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
44361543 9624 28 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
56947112 9624 28 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
CHEMBL396460 9624 28 None 2 5 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
44388462 168632 0 None -6 3 Mouse 9.4 pEC50 = 9.4 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414782 168632 0 None -6 3 Mouse 9.4 pEC50 = 9.4 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL263588 217358 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
25208097 190701 3 None -1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481366 190701 3 None -1 4 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
1682 9627 18 None 7 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
6324645 9627 18 None 7 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
CHEMBL384755 9627 18 None 7 3 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.0c02062
3917 10702 0 None -3 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44430609 10702 0 None -3 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL409969 10702 0 None -3 4 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL429363 220305 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL1631923 215595 0 None - 1 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc3ccccc3)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N2)CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm101139f
CHEMBL1631923 215595 0 None - 1 Mouse 9.2 pEC50 = 9.2 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H]1NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc3ccccc3)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N2)CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O 10.1021/jm101139f
3917 10702 0 None -4 4 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44430609 10702 0 None -4 4 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL409969 10702 0 None -4 4 Guinea pig 9.2 pEC50 = 9.2 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL1162359 215296 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
44388461 166619 0 None -6 3 Mouse 9.1 pEC50 = 9.1 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL410653 166619 0 None -6 3 Mouse 9.1 pEC50 = 9.1 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414767 219933 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
1682 9627 18 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1021/jm800394v
6324645 9627 18 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1021/jm800394v
CHEMBL384755 9627 18 None 7 3 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1021/jm800394v
16131448 9624 28 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 9624 28 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 9624 28 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 9624 28 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 9624 28 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 9624 28 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL507847 221336 0 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL1631926 215597 0 None - 1 Mouse 9.0 pEC50 = 9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose in presence of compound 14 by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose in presence of compound 14 by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL428668 220244 0 None - 1 Human 9.0 pEC50 = 9 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1F)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44388467 176184 0 None -4 2 Mouse 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL442297 176184 0 None -4 2 Mouse 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
44388462 168632 0 None -14 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414782 168632 0 None -14 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
16143911 7255 16 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1689 7255 16 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL505874 7255 16 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL511107 222372 0 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16143911 7255 16 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
1689 7255 16 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL505874 7255 16 None - 1 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
16131448 9624 28 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -2 5 Rat 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 9624 28 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None 2 5 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1682 9627 18 None 7 3 Human 9.0 pEC50 = 9.0 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None None 10.1021/jm010092i
6324645 9627 18 None 7 3 Human 9.0 pEC50 = 9.0 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None None 10.1021/jm010092i
CHEMBL384755 9627 18 None 7 3 Human 9.0 pEC50 = 9.0 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None None 10.1021/jm010092i
44388461 166619 0 None -9 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL410653 166619 0 None -9 3 Guinea pig 9.0 pEC50 = 9.0 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
16131448 9624 28 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -2 5 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL506825 220992 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
25207950 190575 0 None 120 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 430 4 1 4 6.3 CC1(N2CCC(n3c(-c4cccc(CN)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL480426 190575 0 None 120 3 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 430 4 1 4 6.3 CC1(N2CCC(n3c(-c4cccc(CN)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
11956520 127343 0 None -6 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3326228 127343 0 None -6 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3545629 127343 0 None -6 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL556388 222514 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL559130 222522 0 None - 1 Rat 8.9 pEC50 = 8.9 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
25208095 197988 0 None 47 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL518950 197988 0 None 47 4 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL406097 219374 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(Br)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
16131448 9624 28 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1681 9624 28 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1688 9624 28 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
44361543 9624 28 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
56947112 9624 28 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
CHEMBL396460 9624 28 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
16131448 9624 28 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
1681 9624 28 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
1688 9624 28 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
44361543 9624 28 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
56947112 9624 28 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
CHEMBL396460 9624 28 None 2 5 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm7012979
CHEMBL1162358 215295 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CCCCNC(=O)C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
25208101 190702 0 None 181 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 479 4 0 5 6.2 CC1(N2CCC(n3c(-c4cccc(S(C)(=O)=O)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481367 190702 0 None 181 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 479 4 0 5 6.2 CC1(N2CCC(n3c(-c4cccc(S(C)(=O)=O)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
25208245 190723 0 None 478 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 453 3 0 3 7.6 CC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481547 190723 0 None 478 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 453 3 0 3 7.6 CC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
25208099 195149 0 None 8 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL501331 195149 0 None 8 4 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 422 3 0 4 6.0 CN1CCC[C@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
11464846 84369 26 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL2088035 84369 26 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL5073561 221078 0 None 107 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL264846 217411 0 None -12 3 Guinea pig 8.7 pEC50 = 8.7 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
CHEMBL437915 220518 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/jm010092i
CHEMBL5070802 221023 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL5080536 221470 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](CCc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL5093093 222185 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL504872 220964 0 None - 1 Rat 8.0 pEC50 = 8 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL262224 217313 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None Cc1ccc(C[C@H](NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)cc1 10.1021/jm010221v
9927928 97244 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 2 0 2 4.5 O=C1CCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387199 97244 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 2 0 2 4.5 O=C1CCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL507653 221223 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
44574791 185356 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 464 5 1 3 7.1 O/N=C/C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467119 185356 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 464 5 1 3 7.1 O/N=C/C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
71624265 97233 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 4 0 2 4.4 CCC[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387188 97233 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 4 0 2 4.4 CCC[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL442305 220689 0 None - 1 Rat 5.0 pEC50 = 5.0 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
CHEMBL504540 220959 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL526352 222461 0 None - 1 Rat 8.0 pEC50 = 8.0 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16131448 9624 28 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1681 9624 28 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1688 9624 28 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
44361543 9624 28 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
56947112 9624 28 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL396460 9624 28 None -14 5 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1682 9627 18 None -7 3 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
6324645 9627 18 None -7 3 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL384755 9627 18 None -7 3 Mouse 8.0 pEC50 = 8.0 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
76324308 110094 0 None 48 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 496 6 1 2 6.6 NC(=O)[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084526 110094 0 None 48 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 496 6 1 2 6.6 NC(=O)[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
16131448 9624 28 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1681 9624 28 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1688 9624 28 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
44361543 9624 28 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
56947112 9624 28 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL396460 9624 28 None -14 5 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
1682 9627 18 None -7 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
6324645 9627 18 None -7 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
CHEMBL384755 9627 18 None -7 3 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None None 10.1021/jm101139f
10406239 127338 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3326224 127338 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3326226 127338 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3545624 127338 0 None -10 2 Human 5.0 pEC50 = 5.0 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
56658044 72480 0 None -20 4 Human 7.0 pEC50 = 7.0 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 519 6 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CC4CCC1C4)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834413 72480 0 None -20 4 Human 7.0 pEC50 = 7.0 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 519 6 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CC4CCC1C4)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL5079432 221396 0 None -38 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)c1ccccc1 10.1021/acs.jmedchem.0c02062
CHEMBL442305 220689 0 None - 1 Rat 5.0 pEC50 = 5.0 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
9820782 150031 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 371 4 1 2 5.4 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL389665 150031 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 371 4 1 2 5.4 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
9848990 195944 1 None -954 7 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL2368861 195944 1 None -954 7 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL511142 195944 1 None -954 7 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
134563650 176624 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 354 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4439997 176624 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 354 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44426843 92502 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 403 6 1 4 4.8 COc1ccccc1C(c1ccccc1OC)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228964 92502 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 403 6 1 4 4.8 COc1ccccc1C(c1ccccc1OC)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
11164004 115328 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCCC3CCCCC32)CC1 10.1021/jm034249d
CHEMBL320182 115328 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCCC3CCCCC32)CC1 10.1021/jm034249d
10042904 215185 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL99738 215185 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL5078005 221306 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(-c2ccccc2)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL525604 222436 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
10385808 72916 0 None 38 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 72916 0 None 38 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
8868 10320 31 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
9887077 10320 31 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL513136 10320 31 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
49843555 64082 0 None 288 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 451 4 2 6 3.8 OCC1(N2CCC(n3c(N4CC5CNCC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650844 64082 0 None 288 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 451 4 2 6 3.8 OCC1(N2CCC(n3c(N4CC5CNCC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL438398 220549 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CCC(CC)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL437192 220487 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CCCC(CCC)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
9842289 127261 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL 369 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL354291 127261 0 None - 1 Rat 7.9 pEC50 = 7.9 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL 369 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL389521 219206 0 None -11 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
1679 7056 24 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
9963005 7056 24 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL437723 7056 24 None - 1 Human 7.9 pEC50 = 7.9 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
11956680 127336 0 None -100 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3325961 127336 0 None -100 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3545622 127336 0 None -100 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
134563655 180997 3 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4548515 180997 3 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
9803475 84370 32 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
CHEMBL2088036 84370 32 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
CHEMBL5087383 221870 0 None -7 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
90655976 117786 0 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 438 7 0 2 6.2 CCC1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262549 117786 0 None -3 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 438 7 0 2 6.2 CCC1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
118718276 122092 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 482 6 1 2 7.0 NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349260 122092 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 482 6 1 2 7.0 NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
22562137 97243 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 4.6 CC(C)C1CCC(N2CCC(N3C(=O)CCc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387198 97243 0 None -1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 4.6 CC(C)C1CCC(N2CCC(N3C(=O)CCc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
118718277 122093 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 524 7 1 2 7.2 CC(=O)NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349261 122093 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 524 7 1 2 7.2 CC(=O)NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
16131448 9624 28 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1681 9624 28 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1688 9624 28 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
44361543 9624 28 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
56947112 9624 28 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL396460 9624 28 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL389521 219206 0 None -11 2 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
25208247 190724 0 None 676 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 440 3 1 3 7.3 CC1(N2CCC(n3c(-c4ccc5cc[nH]c5c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481548 190724 0 None 676 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 440 3 1 3 7.3 CC1(N2CCC(n3c(-c4ccc5cc[nH]c5c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
11848225 7664 52 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
8866 7664 52 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL2364605 7664 52 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3545616 7664 52 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3962932 7664 52 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
16131448 9624 28 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -2 5 Rat 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 9624 28 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None 2 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL5086442 221808 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None COc1ccc(C[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)cc1 10.1021/acs.jmedchem.0c02062
44430604 175550 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL437382 175550 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
53322001 63202 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL 1601 34 25 22 -7.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@@H](CC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O)C(=O)N2 10.1021/jm101139f
CHEMBL1631924 63202 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL 1601 34 25 22 -7.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@@H](CC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O)C(=O)N2 10.1021/jm101139f
CHEMBL265392 217423 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
46227961 20892 0 None -954 4 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 460 4 3 5 3.1 Cc1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198015 20892 0 None -954 4 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 460 4 3 5 3.1 Cc1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL593214 20892 0 None -954 4 Human 6.9 pEC50 = 6.9 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 460 4 3 5 3.1 Cc1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
44574705 185566 0 None 15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 451 5 1 2 6.6 OCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL468952 185566 0 None 15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 451 5 1 2 6.6 OCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
71624269 97237 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 320 3 0 2 3.8 CC(c1ccccc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387192 97237 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 320 3 0 2 3.8 CC(c1ccccc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
129188462 183185 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4465668 183185 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4596017 183185 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
10385808 72916 0 None 38 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 72916 0 None 38 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
53322001 63202 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL 1601 34 25 22 -7.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@@H](CC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O)C(=O)N2 10.1021/jm101139f
CHEMBL1631924 63202 0 None - 1 Mouse 7.9 pEC50 = 7.9 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL 1601 34 25 22 -7.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CC(=O)NCCCC[C@@H](CC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O)C(=O)N2 10.1021/jm101139f
42629117 185328 0 None 67 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 482 5 1 2 6.3 NC(=O)C1(c2ccc(F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466921 185328 0 None 67 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 482 5 1 2 6.3 NC(=O)C1(c2ccc(F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
122179052 128173 0 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581741 128173 0 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
76331525 110124 0 None 109 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 542 6 1 3 7.7 COC(=O)N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084558 110124 0 None 109 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 542 6 1 3 7.7 COC(=O)N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44430602 151233 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL390658 151233 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL556556 151233 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL2372051 216952 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC[C@](C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL2372364 216952 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC[C@](C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
81689704 128177 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581750 128177 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
16131448 9624 28 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 9624 28 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 9624 28 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 9624 28 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 9624 28 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 9624 28 None -2 5 Rat 6.8 pEC50 = 6.8 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
9848990 195944 1 None -954 7 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL2368861 195944 1 None -954 7 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL511142 195944 1 None -954 7 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL524873 222405 0 None - 1 Rat 7.8 pEC50 = 7.8 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
46227966 20951 0 None -50 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 502 4 3 5 4.1 CC(C)(C)c1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198704 20951 0 None -50 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 502 4 3 5 4.1 CC(C)(C)c1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611932 20951 0 None -50 4 Human 7.8 pEC50 = 7.8 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 502 4 3 5 4.1 CC(C)(C)c1ccc(C(=O)N[C@@H]2CC[C@@]3(O)[C@H]4Cc5ccc(O)c6c5[C@@]3(CCN4CC3CC3)[C@H]2O6)cc1 10.1016/j.bmc.2009.07.069
CHEMBL389521 219206 0 None -11 2 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
9954388 106315 1 None -4 2 Human 5.8 pEC50 = 5.8 Functional
Effective concentration required to stimulate binding of GTPgammaS to human ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to human ORL1 receptor was determined using scintillation proximity assay
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL283480 106315 1 None -4 2 Human 5.8 pEC50 = 5.8 Functional
Effective concentration required to stimulate binding of GTPgammaS to human ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to human ORL1 receptor was determined using scintillation proximity assay
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL5081409 221526 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
134563496 181332 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 409 5 1 4 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC(O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4556227 181332 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 409 5 1 4 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC(O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
118718266 122082 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 479 6 0 3 6.6 CN(C)C[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349250 122082 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 479 6 0 3 6.6 CN(C)C[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL435511 220446 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
18782396 128462 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3585388 128462 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3586752 128462 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3ccccc31)CC2 10.1039/C4MD00082J
44394284 72961 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 365 5 1 3 3.1 CC(C)CCC(C)N1CCC(N2c3ccccc3CNS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184381 72961 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 365 5 1 3 3.1 CC(C)CCC(C)N1CCC(N2c3ccccc3CNS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
44574588 185215 0 None 44 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 443 4 1 2 6.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCC2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL466067 185215 0 None 44 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 443 4 1 2 6.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCC2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
44574585 185407 0 None 56 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 469 4 1 2 7.0 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2cccc(F)c2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL467488 185407 0 None 56 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 469 4 1 2 7.0 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2cccc(F)c2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
11451023 113999 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1021/jm034249d
CHEMBL316699 113999 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1021/jm034249d
CHEMBL268394 217529 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL396972 219280 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
44394324 72929 0 None 9 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 403 2 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184234 72929 0 None 9 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 403 2 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
129188443 176316 3 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4435280 176316 3 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
122179061 128184 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(F)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581757 128184 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(F)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
44394283 72937 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 4 1 3 3.7 CCCC1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184260 72937 0 None 1 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 4 1 3 3.7 CCCC1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
10155966 196056 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 369 4 1 2 5.3 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL511920 196056 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 369 4 1 2 5.3 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
44394375 130462 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 461 6 1 3 4.5 O=S1(=O)NCc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL362160 130462 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 461 6 1 3 4.5 O=S1(=O)NCc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
10139672 132666 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 463 5 0 5 3.4 COC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
CHEMBL364844 132666 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 463 5 0 5 3.4 COC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
53325608 64085 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 439 4 1 6 3.9 CN1CCN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CC1 10.1016/j.bmc.2010.07.034
CHEMBL1650847 64085 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 439 4 1 6 3.9 CN1CCN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CC1 10.1016/j.bmc.2010.07.034
44456216 162179 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 32 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)CC)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL403588 162179 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 32 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)CC)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL398224 219298 0 None - 1 Mouse 7.8 pEC50 = 7.8 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CCC(CC)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL5093399 222204 0 None 10 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
3655995 115522 6 None 11 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL320874 115522 6 None 11 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.03.101
3655995 115522 6 None 11 2 Human 6.8 pEC50 = 6.8 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/jm034249d
CHEMBL320874 115522 6 None 11 2 Human 6.8 pEC50 = 6.8 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/jm034249d
134563699 182855 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 440 7 2 3 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4591048 182855 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 440 7 2 3 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44456187 102416 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 985 31 15 11 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL257921 102416 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 985 31 15 11 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
76320665 110115 0 None 102 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 479 5 1 3 6.1 CC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084549 110115 0 None 102 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 479 5 1 3 6.1 CC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL5070616 221020 0 None 20 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
44456141 102129 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 1043 31 15 11 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL256687 102129 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 1043 31 15 11 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44430602 151233 0 None - 1 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL390658 151233 0 None - 1 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL556556 151233 0 None - 1 Mouse 7.7 pEC50 = 7.7 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL5081993 221560 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assayAgonist activity at human NOP receptor expressed in CHO cells assessed as dynamic mass redistribution by DMR assay
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
9905428 11181 16 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
CHEMBL101454 11181 16 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
CHEMBL505824 220976 0 None - 1 Rat 8.6 pEC50 = 8.6 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL264846 217411 0 None -17 3 Mouse 8.6 pEC50 = 8.6 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
25207948 190574 0 None 18 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 461 6 1 5 6.2 CC1(N2CCC(n3c(-c4cccc(OCCO)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL480425 190574 0 None 18 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 461 6 1 5 6.2 CC1(N2CCC(n3c(-c4cccc(OCCO)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL5074745 221109 0 None 15 2 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.0c02062
CHEMBL499157 220870 0 None - 1 Rat 8.6 pEC50 = 8.6 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL5081578 221533 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
44248674 110177 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 442 4 0 2 6.8 CN1CCCCC1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL3084677 110177 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 442 4 0 2 6.8 CN1CCCCC1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
45271534 202035 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 472 6 1 3 6.2 OCCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL551111 202035 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 472 6 1 3 6.2 OCCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
45268153 202913 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 467 5 0 3 6.7 N#CCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL561115 202913 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 467 5 0 3 6.7 N#CCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
45269032 202963 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 428 4 1 2 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@H]1CC(C1CCCCN1)C2 10.1021/jm9008218
CHEMBL561373 202963 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 428 4 1 2 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@H]1CC(C1CCCCN1)C2 10.1021/jm9008218
44247589 110097 0 None 37 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084529 110097 0 None 37 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
46227963 20948 0 None -3 4 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198701 20948 0 None -3 4 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611929 20948 0 None -3 4 Human 7.7 pEC50 = 7.7 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
9905428 11181 16 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL101454 11181 16 None 4 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
9925137 127340 0 None 2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3326222 127340 0 None 2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3545626 127340 0 None 2 2 Human 4.7 pEC50 = 4.7 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
44394419 72985 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 377 2 1 3 3.4 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184451 72985 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 377 2 1 3 3.4 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
101886205 128465 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3585402 128465 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3586792 128465 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
1684 10135 21 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
9844019 10135 21 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
CHEMBL2088034 10135 21 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assayAgonist activity at human cloned NOP receptor expressed in CHO cell membranes after 30 mins by [35S]GTPgammaS binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
16131448 9624 28 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -2 5 Rat 7.7 pEC50 = 7.7 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
86279209 117781 0 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262544 117781 0 None 2 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL405645 219348 0 None - 1 Rat 6.7 pEC50 = 6.7 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
44394381 73754 0 None 25 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 448 5 1 4 2.7 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(N)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL186822 73754 0 None 25 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 448 5 1 4 2.7 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(N)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL507269 221065 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
CHEMBL384866 219118 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CS)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(N)=O 10.1021/jm010092i
9844540 92494 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 411 4 1 2 6.1 OC1(c2ccccc2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228911 92494 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 411 4 1 2 6.1 OC1(c2ccccc2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
10274330 73447 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 430 4 0 4 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC#N)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL185415 73447 0 None 1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 430 4 0 4 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC#N)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
9863568 148867 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 148867 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 148867 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 148867 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
53316968 64079 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 453 4 2 6 4.3 CC1(C)CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
CHEMBL1650841 64079 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 453 4 2 6 4.3 CC1(C)CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
44456296 104496 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 909 31 15 11 -2.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL271478 104496 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 909 31 15 11 -2.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44456298 175582 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 33 15 11 -0.3 CCCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL437601 175582 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 33 15 11 -0.3 CCCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL2372051 216952 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC[C@](C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL2372364 216952 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC[C@](C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
122179060 128183 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 521 5 2 5 5.4 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(Cl)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581756 128183 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 521 5 2 5 5.4 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(Cl)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
122179064 128187 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 477 5 2 6 4.3 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccoc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581762 128187 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 477 5 2 6 4.3 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccoc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL405645 219348 0 None - 1 Rat 6.6 pEC50 = 6.6 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
CHEMBL427954 220175 0 None - 1 Rat 5.6 pEC50 = 5.6 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CN)C(N)=O 10.1016/j.bmcl.2006.04.086
54756990 72478 0 None -2754 3 Human 5.6 pEC50 = 5.6 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 543 7 2 5 5.7 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834411 72478 0 None -2754 3 Human 5.6 pEC50 = 5.6 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 543 7 2 5 5.7 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
16131448 9624 28 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
1681 9624 28 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
1688 9624 28 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
44361543 9624 28 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
56947112 9624 28 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
CHEMBL396460 9624 28 None 2 5 Human 7.6 pEC50 = 7.6 Functional
Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1Stimulation of [35S]GTP-gamma-S, binding against human Opioid receptor like 1
ChEMBL None None None None 10.1021/jm020078l
CHEMBL5085090 221727 0 None -1 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
134563704 183413 0 None 7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4451073 183413 0 None 7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4597933 183413 0 None 7 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
16131448 9624 28 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -2 5 Rat 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL424934 220106 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
CHEMBL415781 219979 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL262928 217332 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(N)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
10109899 92485 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 373 5 1 3 4.8 COc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228857 92485 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 373 5 1 3 4.8 COc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL5094655 222284 0 None -1 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(N)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
9803475 84370 32 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/acs.jmedchem.8b00435
CHEMBL2088036 84370 32 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assayAgonist activity at human NOPR expressed in human BHK cells assessed as inhibition of forskolin-mediated cAMP accumulation after 10 mins by radioimmuno assay
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/acs.jmedchem.8b00435
10042904 170101 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL418980 170101 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL266667 217472 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CS)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
10042904 97232 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 3 0 2 4.3 CC(C)C1CCC(N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387187 97232 0 None 2 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 3 0 2 4.3 CC(C)C1CCC(N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL5094439 222274 0 None 5 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)c1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
25235412 110095 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084527 110095 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
25235412 122108 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349276 122108 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44430588 93608 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL232245 93608 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL541911 93608 0 None - 1 Mouse 7.6 pEC50 = 7.6 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
44456220 162218 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 937 31 15 11 -1.3 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL403807 162218 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 937 31 15 11 -1.3 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
22558157 117784 0 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 374 3 0 2 4.5 CCC1C(=O)N(C2CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262547 117784 0 None -1 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 374 3 0 2 4.5 CCC1C(=O)N(C2CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
16665918 86524 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 370 2 1 1 5.9 Fc1ccc2[nH]cc(C3CCN(C4Cc5cccc6cccc4c56)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL211722 86524 0 None - 1 Human 4.6 pEC50 = 4.6 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 370 2 1 1 5.9 Fc1ccc2[nH]cc(C3CCN(C4Cc5cccc6cccc4c56)CC3)c2c1 10.1016/j.bmcl.2006.03.094
134578342 179840 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 438 8 2 4 4.7 CCNCC(=O)NCc1cn(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc12 10.1021/acs.jmedchem.9b02134
CHEMBL4519453 179840 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 438 8 2 4 4.7 CCNCC(=O)NCc1cn(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc12 10.1021/acs.jmedchem.9b02134
44181744 110150 9 None 77 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
CHEMBL3084634 110150 9 None 77 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDPAgonist activity at human NOP receptor expressed in CHO cells assessed as increase in SCH-221510-stimulated [35S]GTPgammaS binding in presence of GDP
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
11461888 11398 3 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL102900 11398 3 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
11461888 11398 3 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
CHEMBL102900 11398 3 None -1 2 Human 7.5 pEC50 = 7.5 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
CHEMBL405948 219366 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
9863568 148867 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 148867 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 148867 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 148867 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL3809510 219054 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assayAgonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 15 mins followed by forskolin addition measured for 90 mins by luciferase reporter gene assay
ChEMBL None None None CC[C@H](C)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
CHEMBL394588 219256 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CCCC(CCC)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL442113 220686 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
CHEMBL1631922 215594 0 None - 1 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@@H]2CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc3ccccc3)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N2)CCCCNC(=O)C[C@@H](C(N)=O)NC1=O 10.1021/jm101139f
CHEMBL1631922 215594 0 None - 1 Mouse 8.5 pEC50 = 8.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](NC(=O)[C@@H]2CC(=O)NCCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc3ccccc3)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc3ccccc3)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N2)CCCCNC(=O)C[C@@H](C(N)=O)NC1=O 10.1021/jm101139f
25208249 190744 0 None 1202 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 441 3 0 4 7.6 CC1(N2CCC(n3c(-c4cc5ccccc5o4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481707 190744 0 None 1202 2 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 441 3 0 4 7.6 CC1(N2CCC(n3c(-c4cc5ccccc5o4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL555757 222511 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL526333 222459 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL558807 222521 0 None - 1 Rat 8.5 pEC50 = 8.5 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
16131448 9624 28 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1681 9624 28 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1688 9624 28 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
44361543 9624 28 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
56947112 9624 28 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
CHEMBL396460 9624 28 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
44551464 20950 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 572 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(I)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198703 20950 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 572 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(I)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611931 20950 0 None 1 4 Human 8.4 pEC50 = 8.4 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 572 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(I)cc1 10.1016/j.bmc.2009.07.069
CHEMBL5079758 221417 0 None 151 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL1631921 215593 0 None - 1 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/jm101139f
1641 9505 9 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
3829 9505 9 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
5497186 9505 9 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
CHEMBL567175 9505 9 None -11 7 Human 8.4 pEC50 = 8.4 Functional
Activity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS bindingActivity at NOP expressed in HEK293 cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1016/j.bmc.2009.07.069
CHEMBL406718 219396 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(N)=O 10.1021/jm010092i
16131448 9624 28 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1681 9624 28 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1688 9624 28 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
44361543 9624 28 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
56947112 9624 28 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL396460 9624 28 None 2 5 Human 8.4 pEC50 = 8.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL455289 220781 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL1631925 215596 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631925 215596 0 None - 1 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL5081139 221505 0 None 12 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(N)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
71624387 97240 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 2 0 2 4.7 CC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387195 97240 0 None 3 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 340 2 0 2 4.7 CC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
10134217 73050 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 377 3 1 3 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184698 73050 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 377 3 1 3 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL269029 217554 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP receptor by [35S]GTPgammaS binding assayAgonist activity at human NOP receptor by [35S]GTPgammaS binding assay
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
CHEMBL269029 217554 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
CHEMBL265544 217432 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44456185 173400 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 951 32 15 11 -0.9 CCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL428076 173400 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 951 32 15 11 -0.9 CCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
5268 10428 40 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 10.1039/C4MD00082J
53 10428 40 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 10.1039/C4MD00082J
CHEMBL300555 10428 40 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 10.1039/C4MD00082J
CHEMBL505873 220978 0 None - 1 Rat 7.5 pEC50 = 7.5 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
10137876 131827 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 435 5 1 4 3.2 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCO)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL364398 131827 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 435 5 1 4 3.2 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCO)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
9863568 148867 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 148867 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 148867 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 148867 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
122179056 128179 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581752 128179 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
10110916 73036 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 389 2 1 3 4.0 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184646 73036 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 389 2 1 3 4.0 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
44394487 72220 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 512 7 1 5 2.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCNS(C)(=O)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL182967 72220 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 512 7 1 5 2.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCNS(C)(=O)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
134563466 178071 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 412 5 2 3 4.8 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4460695 178071 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 412 5 2 3 4.8 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44574789 185327 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 504 6 1 2 7.1 O=C(NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl)C1CC1 10.1016/j.bmcl.2009.03.031
CHEMBL466919 185327 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 504 6 1 2 7.1 O=C(NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl)C1CC1 10.1016/j.bmcl.2009.03.031
16131448 9624 28 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 9624 28 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 9624 28 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 9624 28 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 9624 28 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 9624 28 None -14 5 Mouse 7.5 pEC50 = 7.5 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAgonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL1631920 215592 0 None - 1 Mouse 6.5 pEC50 = 6.5 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCNC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm101139f
CHEMBL1631920 215592 0 None - 1 Mouse 6.4 pEC50 = 6.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None CC(=O)NCCCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCNC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/jm101139f
53316969 64088 0 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 357 3 2 4 3.4 O=c1[nH]c2ccccc2n1C1CCN(C2(CO)CCCCCCC2)CC1 10.1016/j.bmc.2010.07.034
CHEMBL1650851 64088 0 None 3 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 357 3 2 4 3.4 O=c1[nH]c2ccccc2n1C1CCN(C2(CO)CCCCCCC2)CC1 10.1016/j.bmc.2010.07.034
CHEMBL5091985 222118 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](CCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
10385808 72916 0 None 38 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 72916 0 None 38 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
53322245 64086 0 None 9 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 439 4 2 6 3.9 CC1CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
CHEMBL1650848 64086 0 None 9 3 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 439 4 2 6 3.9 CC1CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
9885005 64321 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL 355 3 1 3 3.6 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL166387 64321 0 None - 1 Rat 7.4 pEC50 = 7.4 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL 355 3 1 3 3.6 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
15512229 10158 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Tested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptorTested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(99)00385-6
8864 10158 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Tested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptorTested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(99)00385-6
CHEMBL355202 10158 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Tested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptorTested for potency to stimulate GTP-gamma 35S binding using membranes prepared from 293s cells transfected with the human OFQ receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(99)00385-6
1682 9627 18 None -147 3 Rat 6.4 pEC50 = 6.4 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
6324645 9627 18 None -147 3 Rat 6.4 pEC50 = 6.4 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
CHEMBL384755 9627 18 None -147 3 Rat 6.4 pEC50 = 6.4 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
CHEMBL500773 220906 0 None - 1 Rat 8.4 pEC50 = 8.4 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL1631921 215593 0 None - 1 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assayAgonist activity at NOR in mouse Neuro-2a cells assessed as stimulation of ERK phosphorylation after 30 mins post dose by Alphascreen Surefire assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/jm101139f
CHEMBL5081993 221560 0 None -2 3 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1c(C)cc(O)cc1C)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL505632 220974 0 None - 1 Rat 8.4 pEC50 = 8.4 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL1162357 215294 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CCCCNC(=O)C[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
CHEMBL443591 220705 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm010092i
CHEMBL394774 219258 0 None - 1 Mouse 8.4 pEC50 = 8.4 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
3917 10702 0 None -28 4 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44430609 10702 0 None -28 4 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL409969 10702 0 None -28 4 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44388474 167821 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 69 33 31 -15.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL411649 167821 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 69 33 31 -15.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
10022859 105946 1 None 63 2 Human 7.4 pEC50 = 7.4 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1021/jm991129q
CHEMBL281274 105946 1 None 63 2 Human 7.4 pEC50 = 7.4 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1021/jm991129q
CHEMBL5070145 221006 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
90655973 117782 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262545 117782 0 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL219144 216187 0 None - 1 Rat 6.4 pEC50 = 6.4 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
122179050 128172 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 485 5 2 5 4.5 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581740 128172 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 485 5 2 5 4.5 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
16007142 146131 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 353 2 1 2 5.2 c1cc2c3c(cccc3c1)C(N1CCC(c3c[nH]c4ncccc34)CC1)C2 10.1016/j.bmcl.2006.03.094
CHEMBL379297 146131 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 353 2 1 2 5.2 c1cc2c3c(cccc3c1)C(N1CCC(c3c[nH]c4ncccc34)CC1)C2 10.1016/j.bmcl.2006.03.094
122179585 128464 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 381 2 1 4 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3cccc(F)c31)CC2 10.1039/C4MD00082J
CHEMBL3585401 128464 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 381 2 1 4 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3cccc(F)c31)CC2 10.1039/C4MD00082J
CHEMBL3586789 128464 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 381 2 1 4 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCOc3cccc(F)c31)CC2 10.1039/C4MD00082J
12986253 127330 0 None -3 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 379 7 2 2 4.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325881 127330 0 None -3 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 379 7 2 2 4.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545610 127330 0 None -3 2 Human 4.4 pEC50 = 4.4 Functional
Agonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assayAgonist activity at human NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]-GTPgammaS binding by scintillation proximity assay
ChEMBL 379 7 2 2 4.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL406010 219370 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Efficacy for human ORL1 receptor expressing HEK293 cellsEfficacy for human ORL1 receptor expressing HEK293 cells
ChEMBL None None None C[C@@H]1NC(=O)CNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
76316935 110098 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 499 5 1 3 6.2 NC(=O)[C@@]1(c2ccc(Cl)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084530 110098 0 None 8 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 499 5 1 3 6.2 NC(=O)[C@@]1(c2ccc(Cl)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44456140 175493 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 951 31 15 11 -1.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL436852 175493 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 951 31 15 11 -1.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
134578506 181079 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 437 5 1 4 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCC(O)CC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4550088 181079 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 437 5 1 4 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCC(O)CC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
101886199 128463 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3585403 128463 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
CHEMBL3586777 128463 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assayAgonist activity at human recombinant NOP receptor expressed in CHO cells co-expressing C-terminally modifed Gaqi5 protein by Fluo-4AM dye based calcium mobilization assay
ChEMBL 363 2 1 4 2.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCOc3ccccc31)CC2 10.1039/C4MD00082J
73350483 97238 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN(C2CC[C@H]3CCCc4cccc2c43)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387193 97238 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN(C2CC[C@H]3CCCc4cccc2c43)CC1 10.1016/j.bmcl.2013.03.101
44456299 104255 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 31 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL270216 104255 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 979 31 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44430590 168103 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL412461 168103 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL557791 168103 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
155542684 179928 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 466 10 2 4 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(=O)CCCCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4521436 179928 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 466 10 2 4 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(=O)CCCCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44574629 195619 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 458 4 2 3 4.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCNC2=O)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL506634 195619 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 458 4 2 3 4.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCNC2=O)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL5072525 221061 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL5090780 222059 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
118718291 122107 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 478 6 0 2 7.2 CN(C)C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349275 122107 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human cloned nociceptin receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 478 6 0 2 7.2 CN(C)C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44394405 71341 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 505 5 0 5 4.6 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(=O)OC(C)(C)C)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL181545 71341 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 505 5 0 5 4.6 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(=O)OC(C)(C)C)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
44394344 72953 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 383 2 1 3 2.5 O=S1(=O)NCc2ccccc2N1C1CCN(C2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184328 72953 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 383 2 1 3 2.5 O=S1(=O)NCc2ccccc2N1C1CCN(C2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
16131448 9624 28 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
1681 9624 28 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
1688 9624 28 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
44361543 9624 28 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
56947112 9624 28 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 9624 28 None -7 5 Guinea pig 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of guinea pig ileumInhibition of electrically evoked contraction of guinea pig ileum
ChEMBL None None None None 10.1021/jm040106v
16131448 9624 28 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
1681 9624 28 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
1688 9624 28 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
44361543 9624 28 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
56947112 9624 28 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 9624 28 None -14 5 Mouse 8.3 pEC50 = 8.3 Functional
Inhibition of electrically evoked contraction of mouse vas deferensInhibition of electrically evoked contraction of mouse vas deferens
ChEMBL None None None None 10.1021/jm040106v
16131448 9624 28 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -2 5 Rat 8.3 pEC50 = 8.3 Functional
Agonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS bindingAgonist activity at recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells assessed as stimulation of GTPgammaS binding
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
25207946 198077 0 None 275 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 469 3 0 3 7.9 CC1(N2CCC(n3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL519100 198077 0 None 275 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 469 3 0 3 7.9 CC1(N2CCC(n3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL503512 220948 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL504587 220960 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL504587 220960 0 None - 1 Rat 8.2 pEC50 = 8.2 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL510117 222360 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
44574586 196102 0 None 33 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 453 4 1 4 5.7 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2ccncn2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL512411 196102 0 None 33 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 453 4 1 4 5.7 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2ccncn2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
44574672 196163 0 None 10 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 451 5 0 2 7.3 COC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL512950 196163 0 None 10 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 451 5 0 2 7.3 COC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL510117 222360 0 None - 1 Rat 7.3 pEC50 = 7.3 Functional
Agonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assayAgonist activity at rat ORL1 receptor expressed in african green monkey COS7 cells assessed as stimulation of [35S]GTPgammaS binding by radioligand receptor-binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
90655974 117783 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 374 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCc4ccccc43)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262546 117783 0 None -1 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 374 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCc4ccccc43)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
10714523 105883 1 None 7 2 Human 6.3 pEC50 = 6.3 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 375 2 1 3 3.8 Cc1cccc2c1CCCC2N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm991129q
CHEMBL280827 105883 1 None 7 2 Human 6.3 pEC50 = 6.3 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 375 2 1 3 3.8 Cc1cccc2c1CCCC2N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm991129q
44455999 104287 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 965 32 15 11 -0.7 CCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL270394 104287 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 965 32 15 11 -0.7 CCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
90655972 117780 0 None 14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
CHEMBL3262543 117780 0 None 14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
53319617 64087 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 441 4 1 4 5.8 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650849 64087 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 441 4 1 4 5.8 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL5073730 221081 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
134563691 177841 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 381 5 0 3 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN(C)C)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4457077 177841 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 381 5 0 3 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN(C)C)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44574743 185380 0 None 14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 494 5 1 3 7.0 COC(=O)NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467313 185380 0 None 14 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 494 5 1 3 7.0 COC(=O)NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
129188459 181947 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 326 3 0 2 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(N3CCc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4570328 181947 3 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 326 3 0 2 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(N3CCc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
71624270 97239 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 4.8 CC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387194 97239 0 None 2 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 4.8 CC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
44430588 93608 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL232245 93608 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL541911 93608 0 None - 1 Mouse 7.3 pEC50 = 7.3 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1849 63 30 26 -10.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL5086409 221807 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL413944 219882 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Inhibition of forskolin stimulated cAMP levels in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
44413442 86718 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 400 2 1 1 6.8 Cc1[nH]c2ccc(Cl)cc2c1C1CCN(C2Cc3cccc4cccc2c34)CC1 10.1016/j.bmcl.2006.03.094
CHEMBL212575 86718 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assayAgonist activity at ORL1 receptor expressed in HEK293 cells by calciun flux assay
ChEMBL 400 2 1 1 6.8 Cc1[nH]c2ccc(Cl)cc2c1C1CCN(C2Cc3cccc4cccc2c34)CC1 10.1016/j.bmcl.2006.03.094
44394559 73082 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 407 3 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184865 73082 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 407 3 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL5092388 222144 0 None -8 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
134578456 178916 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 423 5 1 4 5.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC[C@@H](O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4473045 178916 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 423 5 1 4 5.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC[C@@H](O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
1682 9627 18 None -147 3 Rat 6.2 pEC50 = 6.2 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
6324645 9627 18 None -147 3 Rat 6.2 pEC50 = 6.2 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
CHEMBL384755 9627 18 None -147 3 Rat 6.2 pEC50 = 6.2 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None None 10.1016/j.bmcl.2006.04.086
11848793 196103 0 None 63 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 464 5 1 2 6.1 NC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL512414 196103 0 None 63 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 464 5 1 2 6.1 NC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
24800107 198640 0 None 2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 437 3 1 5 5.4 CC1CN(c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)CC(C)N1 10.1021/jm7012979
CHEMBL519925 198640 0 None 2 3 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cells by [35S]GTPgammaS binding
ChEMBL 437 3 1 5 5.4 CC1CN(c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)CC(C)N1 10.1021/jm7012979
71624388 97242 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387197 97242 0 None 5 2 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
24798598 119362 11 None -23 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3301613 119362 11 None -23 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3325959 119362 11 None -23 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assayAgonist activity at human recombinant NOP receptor expressed in CHO-K1 cells assessed as stimulation of [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL5072270 221056 0 None -3 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None Cc1cc(O)cc(C)c1C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL442305 220689 0 None - 1 Rat 5.2 pEC50 = 5.2 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferensActivity against LFES-evoked contraction of Wistar rat vas deferens
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
CHEMBL427954 220175 0 None - 1 Rat 5.2 pEC50 = 5.2 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CN)C(N)=O 10.1016/j.bmcl.2006.04.086
44574631 185288 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 457 4 2 4 5.1 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2=NCCCN2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL466679 185288 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 457 4 2 4 5.1 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2=NCCCN2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
76324309 110099 0 None 6 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 543 5 1 3 6.3 NC(=O)[C@@]1(c2ccc(Br)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084531 110099 0 None 6 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 543 5 1 3 6.3 NC(=O)[C@@]1(c2ccc(Br)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL234724 216317 0 None - 1 Mouse 7.2 pEC50 = 7.2 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL5075880 221181 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](CN)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL415583 219970 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None COc1ccc(C[C@H](NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)cc1 10.1021/jm010221v
16131448 9624 28 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
1681 9624 28 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
1688 9624 28 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
44361543 9624 28 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
56947112 9624 28 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
CHEMBL396460 9624 28 None -2 5 Rat 7.2 pEC50 = 7.2 Functional
pEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptorpEC50 for its effect on stimulating GTPgammaS binding to membranes of HEK 293 cells overexpressing rat ORL-1 receptor
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
129188454 176612 0 None 46 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 367 4 1 4 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(/C=N/O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4439811 176612 0 None 46 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 367 4 1 4 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(/C=N/O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL5081432 221527 0 None 12 2 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL5092204 222131 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
146034955 181417 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assayAgonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assay
ChEMBL 399 5 1 5 3.9 CCn1c(=O)n([C@@H]2CCN(C3CCC(C(C)C)CC3)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.8b00435
CHEMBL4558048 181417 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assayAgonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assay
ChEMBL 399 5 1 5 3.9 CCn1c(=O)n([C@@H]2CCN(C3CCC(C(C)C)CC3)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.8b00435
CHEMBL410167 219582 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Inhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptorInhibition of forskolin stimulated cAMP accumulation in CHO cells stably expressing the human OP4 receptor
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(I)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
122179053 128175 0 None -33 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581743 128175 0 None -33 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
44430605 173183 0 None - 1 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1835 63 30 26 -10.9 CCC(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL427699 173183 0 None - 1 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1835 63 30 26 -10.9 CCC(C)(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
1682 9627 18 None 7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm800394v
6324645 9627 18 None 7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm800394v
CHEMBL384755 9627 18 None 7 3 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS bindingAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding
ChEMBL None None None None 10.1021/jm800394v
90655978 117788 0 None 9 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 362 6 0 2 4.6 CCC1C(=O)N(C2CCN(CCCc3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262551 117788 0 None 9 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 362 6 0 2 4.6 CCC1C(=O)N(C2CCN(CCCc3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
146034954 177788 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assayAgonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assay
ChEMBL 425 5 1 5 4.3 CCn1c(=O)n([C@@H]2CCN(CC3CCCC4CCCCC43)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.8b00435
CHEMBL4456531 177788 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assayAgonist activity at YFP-fused human NOPR expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation measured immediately by luminescence assay
ChEMBL 425 5 1 5 4.3 CCn1c(=O)n([C@@H]2CCN(CC3CCCC4CCCCC43)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.8b00435
44332117 114678 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCC[C@@H]3C2)CC1 10.1021/jm034249d
CHEMBL319307 114678 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCC[C@@H]3C2)CC1 10.1021/jm034249d
44430590 168103 0 None - 1 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL412461 168103 0 None - 1 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL557791 168103 0 None - 1 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL 1863 64 30 26 -10.2 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(CC(C)C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
44574744 196086 0 None 60 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 436 4 1 2 6.6 NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL512258 196086 0 None 60 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 436 4 1 2 6.6 NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
10160920 73747 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 447 6 0 3 5.0 CCCCN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
CHEMBL186773 73747 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1Agonist activity as stimulation of [35S]-GTP-gamma binding to human Opioid receptor like 1
ChEMBL 447 6 0 3 5.0 CCCCN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
56664973 72475 0 None -12 2 Human 7.1 pEC50 = 7.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 481 6 2 5 4.8 CCC(C)(C)[C@](C)(O)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm2003238
CHEMBL1834409 72475 0 None -12 2 Human 7.1 pEC50 = 7.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL 481 6 2 5 4.8 CCC(C)(C)[C@](C)(O)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm2003238
9997843 106441 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 347 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL284414 106441 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 347 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc31)CC2 10.1021/jm991129q
16131448 9624 28 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
1681 9624 28 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
1688 9624 28 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
44361543 9624 28 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
56947112 9624 28 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
CHEMBL396460 9624 28 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Partial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation countingPartial agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
CHEMBL436819 220467 0 None - 1 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
9799433 97241 1 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 368 4 0 2 5.2 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387196 97241 1 None -1 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 368 4 0 2 5.2 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
53324890 64080 0 None 138 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 469 4 1 4 6.6 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650842 64080 0 None 138 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 469 4 1 4 6.6 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
16131448 9624 28 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 9624 28 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 9624 28 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 9624 28 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 9624 28 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 9624 28 None -7 5 Guinea pig 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL233069 216309 0 None - 1 Mouse 8.1 pEC50 = 8.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
90655975 117785 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 373 4 1 2 4.7 CCC1C(=O)N(C2CCN(Cc3cccc4[nH]ccc34)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262548 117785 0 None -3 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 373 4 1 2 4.7 CCC1C(=O)N(C2CCN(Cc3cccc4[nH]ccc34)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
71624268 97236 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 326 3 0 2 4.0 CC(C1CCCCC1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387191 97236 0 None -2 3 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 326 3 0 2 4.0 CC(C1CCCCC1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
71624266 97234 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 368 4 0 2 5.0 CCC(C)(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387189 97234 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 368 4 0 2 5.0 CCC(C)(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL394775 219259 0 None - 1 Mouse 7.1 pEC50 = 7.1 Functional
Agonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractionsAgonist activity at NOP receptor in Swiss mouse vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CC1)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
90655971 117779 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
CHEMBL3262542 117779 0 None 4 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysisAgonist activity at human nociceptin opioid receptor transfected in CHO cell membranes assessed as stimulation of [35S]GTPgammaS binding after 60 mins by scintillation counting analysis
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
CHEMBL5081900 221553 0 None 2 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
CHEMBL504461 220957 0 None - 1 Rat 7.1 pEC50 = 7.1 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
76335144 110117 0 None 43 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 495 5 1 4 6.4 COC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084551 110117 0 None 43 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS bindingAgonist activity at human cloned ORL1 receptor assessed as stimulation of GTPgammaS binding
ChEMBL 495 5 1 4 6.4 COC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
9947044 105047 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL27460 105047 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Effective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to ORL1 receptor was determined using scintillation proximity assay
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL526142 222452 0 None - 1 Rat 6.1 pEC50 = 6.1 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
24824635 165602 0 None -12 4 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 480 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)cc1 10.1016/j.bmc.2009.07.069
CHEMBL409458 165602 0 None -12 4 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 480 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611933 165602 0 None -12 4 Human 7.1 pEC50 = 7.1 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 480 4 3 5 3.4 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Cl)cc1 10.1016/j.bmc.2009.07.069
CHEMBL524339 222383 0 None - 1 Rat 8.1 pEC50 = 8.1 Functional
Activation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assayActivation of rat ORL1 receptor expressed in african green monkey COS7 cells by [35S]GTPgammaS binding assay
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
53319615 64081 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 451 4 1 4 6.5 OCC1(N2CCC(n3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650843 64081 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation countingAgonist activity at human NOP receptor expressed in HEK293 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by liquid scintillation counting
ChEMBL 451 4 1 4 6.5 OCC1(N2CCC(n3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL5085161 221731 0 None 89 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysisAgonist activity at human NOP receptor expressed in CHO cells assessed as stimulation of calcium mobilization by Fluo-4 AM dye based analysis
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.0c02062
44574587 185214 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 496 6 1 4 6.4 COc1ccc(CC2(O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccc(C)cc2Cl)nc1 10.1016/j.bmcl.2009.03.031
CHEMBL466066 185214 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS bindingAgonist activity at human NOP assessed as stimulation of GDP-induced [35S]GTPgammaS binding
ChEMBL 496 6 1 4 6.4 COc1ccc(CC2(O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccc(C)cc2Cl)nc1 10.1016/j.bmcl.2009.03.031
11393860 11222 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 346 2 0 2 3.6 O=C1Cc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1021/jm034249d
CHEMBL101676 11222 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Concentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranesConcentration required for stimulation of [35S]GTP-gamma-S, binding to human Nociceptin receptor in cell membranes
ChEMBL 346 2 0 2 3.6 O=C1Cc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1021/jm034249d
CHEMBL442305 220689 0 None - 1 Rat 5.0 pEC50 = 5.0 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
44596170 20949 0 None -933 4 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 524 4 3 5 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Br)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198702 20949 0 None -933 4 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 524 4 3 5 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Br)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611930 20949 0 None -933 4 Human 7.0 pEC50 = 7.0 Functional
Inverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS bindingInverse agonist activity at NOP expressed in HEK293 cells assessed as inhibition of [35S]GTPgammaS binding
ChEMBL 524 4 3 5 3.5 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(Br)cc1 10.1016/j.bmc.2009.07.069
71624389 97245 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 2 0 2 5.1 CC1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387200 97245 0 None -1 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysisAgonist activity at human nociceptin receptor transfected in CHO cells assessed as stimulation of [35S]GTPgammaS binding by liquid scintillation counting analysis
ChEMBL 354 2 0 2 5.1 CC1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
134578457 180734 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 407 5 0 3 6.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCCC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4541337 180734 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at human NOP expressed in CHO cell membrane incubated for 60 mins by [35S]GTPgammaS binding assay
ChEMBL 407 5 0 3 6.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCCC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44456412 104260 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 965 30 15 11 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL270231 104260 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Activity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S bindingActivity at human ORL1-Galpha fusion receptor in COS7 cells assessed as stimulation of [35S]GTP-gamma-S binding
ChEMBL 965 30 15 11 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL219144 216187 0 None - 1 Rat 6.0 pEC50 = 6.0 Functional
Activity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxoneActivity against LFES-evoked contraction of Wistar rat vas deferens in presence of naloxone
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCN)C(N)=O 10.1016/j.bmcl.2006.04.086
16131448 9624 28 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1681 9624 28 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1688 9624 28 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
44361543 9624 28 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
56947112 9624 28 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL396460 9624 28 None -14 5 Mouse 7.7 pED50 = 7.7 Functional
Antagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contractionAntagonist activity at ORL1-Galpha fusion receptor in ICR mouse vas deferens assessed as inhibition of electrically-stimulated muscle contraction
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
11511090 80828 0 None 5888 3 Human 9.9 pIC50 = 9.9 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
CHEMBL202225 80828 0 None 5888 3 Human 9.9 pIC50 = 9.9 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
10296561 7829 26 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
7361 7829 26 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
CHEMBL201945 7829 26 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
44143431 185285 0 None 1288 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL466648 185285 0 None 1288 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.06.051
44143431 185285 0 None 1288 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
CHEMBL466648 185285 0 None 1288 3 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
44143450 195596 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 475 5 1 5 4.8 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N5CCCC5=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL506207 195596 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 475 5 1 5 4.8 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N5CCCC5=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143456 185374 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 460 5 1 7 5.0 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnco5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467279 185374 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 460 5 1 7 5.0 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnco5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
45273531 201700 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 348 5 1 4 4.3 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C(C)C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL541511 201700 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 348 5 1 4 4.3 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C(C)C)cc1F 10.1016/j.bmcl.2009.06.051
45270907 202538 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 334 5 1 4 3.7 CCn1nc(CN[C@H]2CC[C@@H](F)C2)c(C)c1-c1cnc(C)c(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL557623 202538 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 334 5 1 4 3.7 CCn1nc(CN[C@H]2CC[C@@H](F)C2)c(C)c1-c1cnc(C)c(F)c1 10.1016/j.bmcl.2009.06.051
24857819 194296 0 None 114 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL494350 194296 0 None 114 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
24857819 194296 0 None 114 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
CHEMBL494350 194296 0 None 114 4 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
24857820 103460 0 None 190 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL263918 103460 0 None 190 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
24857820 103460 0 None 190 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263918 103460 0 None 190 3 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44143432 185489 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL468302 185489 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
44143432 185489 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468302 185489 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143453 185260 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnn(C)n5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466448 185260 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnn(C)n5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143455 185239 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nc(C)no5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466252 185239 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nc(C)no5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
45273546 202554 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 353 6 1 4 3.5 COCc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL557721 202554 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 353 6 1 4 3.5 COCc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143428 185492 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL468308 185492 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
44143446 185235 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 465 5 1 6 4.5 CCOC(=O)N1CCC(C)(Sc2nc3cc(Cl)c(N4CCN(CC)CC4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466222 185235 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 465 5 1 6 4.5 CCOC(=O)N1CCC(C)(Sc2nc3cc(Cl)c(N4CCN(CC)CC4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.022
44143448 185436 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 449 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467677 185436 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 449 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143451 185494 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 449 5 2 5 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](C(=O)NC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468315 185494 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 449 5 2 5 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](C(=O)NC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143430 196166 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.8 Cc1ncc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
CHEMBL512975 196166 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.8 Cc1ncc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
9823363 185246 0 None 1047 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 418 4 2 5 3.9 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466308 185246 0 None 1047 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 418 4 2 5 3.9 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
44143433 185345 0 None 154 3 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 463 5 1 5 4.6 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N(C)C(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467057 185345 0 None 154 3 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 463 5 1 5 4.6 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N(C)C(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
1691 8888 23 None 512 3 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
5311194 8888 23 None 512 3 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
CHEMBL357076 8888 23 None 512 3 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
24894426 192546 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 404 3 1 3 5.3 O[C@H]1C[C@H](CN2CCC(c3c(Cl)cccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
CHEMBL486644 192546 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 404 3 1 3 5.3 O[C@H]1C[C@H](CN2CCC(c3c(Cl)cccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
44143449 185370 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 485 6 2 6 3.7 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NS(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467266 185370 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 485 6 2 6 3.7 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NS(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44450085 103459 0 None 47 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 408 5 2 5 4.1 CC1(Sc2nc3cc(Cl)c(N4CCN(CCO)CC4)cc3[nH]2)CCCCC1 10.1016/j.bmcl.2008.04.054
CHEMBL263917 103459 0 None 47 3 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 408 5 2 5 4.1 CC1(Sc2nc3cc(Cl)c(N4CCN(CCO)CC4)cc3[nH]2)CCCCC1 10.1016/j.bmcl.2008.04.054
44437610 152297 0 None - 1 Human 8.0 pIC50 = 8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391487 152297 0 None - 1 Human 8.0 pIC50 = 8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44561518 196233 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 363 3 1 2 5.2 Cc1ccccc1C1CCN(C[C@@H]2CCc3c(C)cccc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL513585 196233 0 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 363 3 1 2 5.2 Cc1ccccc1C1CCN(C[C@@H]2CCc3c(C)cccc3[C@@H](O)C2)CC1 10.1021/jm701590h
44437642 98528 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 536 11 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL240941 98528 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 536 11 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
46879578 12809 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 427 3 1 4 4.6 CNC(=O)CN1C(=O)OC2(CCN(C3CCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080463 12809 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 427 3 1 4 4.6 CNC(=O)CN1C(=O)OC2(CCN(C3CCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44437644 98572 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 538 12 2 8 3.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL241155 98572 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 538 12 2 8 3.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437617 161757 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 523 11 0 8 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCOC(C)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL401248 161757 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 523 11 0 8 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCOC(C)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44391133 71899 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 457 8 2 6 4.9 CCCC(Oc1cc(C)ccc1Cl)C(O)CN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/j.bmcl.2004.11.049
CHEMBL182410 71899 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 457 8 2 6 4.9 CCCC(Oc1cc(C)ccc1Cl)C(O)CN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/j.bmcl.2004.11.049
70682351 83438 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 423 5 0 3 3.4 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064158 83438 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 423 5 0 3 3.4 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.021
44391081 69380 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 471 8 2 6 5.2 Cc1ccc(Cl)c(OC(CC(C)C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL178318 69380 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 471 8 2 6 5.2 Cc1ccc(Cl)c(OC(CC(C)C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44143427 196265 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3F)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL513855 196265 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3F)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
11597677 80436 0 None 23 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 454 8 1 3 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1OCc1ccccc1 10.1021/jm0509851
CHEMBL201805 80436 0 None 23 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 454 8 1 3 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1OCc1ccccc1 10.1021/jm0509851
70690755 83426 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064130 83426 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
46879716 12813 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 460 4 1 4 3.1 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1080483 12813 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 460 4 1 4 3.1 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
53318067 63206 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2073 50 34 30 -13.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
91933707 63206 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2073 50 34 30 -13.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631930 63206 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2073 50 34 30 -13.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
44143418 194018 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 401 5 1 5 5.0 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1ccc(Cl)nc1 10.1016/j.bmcl.2009.04.116
CHEMBL492585 194018 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 401 5 1 5 5.0 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1ccc(Cl)nc1 10.1016/j.bmcl.2009.04.116
11326750 193088 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 390 3 2 4 3.3 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)Cc2cccnc21 10.1021/jm701590h
CHEMBL487458 193088 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 390 3 2 4 3.3 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)Cc2cccnc21 10.1021/jm701590h
70690760 83440 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 433 5 0 3 3.9 Cc1cccc(C)c1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064160 83440 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 433 5 0 3 3.9 Cc1cccc(C)c1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
53318067 63206 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2073 50 34 30 -13.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
91933707 63206 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2073 50 34 30 -13.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631930 63206 0 None - 1 Mouse 7.9 pIC50 = 7.9 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2073 50 34 30 -13.9 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
44437640 98007 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 536 12 1 7 4.8 CCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240086 98007 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 536 12 1 7 4.8 CCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
127034022 145781 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 333 2 0 2 4.2 c1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)CO2 10.1016/j.ejmech.2016.02.014
CHEMBL3785605 145781 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 333 2 0 2 4.2 c1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)CO2 10.1016/j.ejmech.2016.02.014
44437615 97152 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 509 10 0 8 4.4 COC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238637 97152 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 509 10 0 8 4.4 COC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437623 151958 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 523 11 0 8 4.8 COC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391234 151958 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 523 11 0 8 4.8 COC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44391094 71249 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 422 7 2 6 4.8 Cc1ccc(N)cc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL181389 71249 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 422 7 2 6 4.8 Cc1ccc(N)cc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
44437637 98672 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 529 10 0 8 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CS(C)(=O)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL241357 98672 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 529 10 0 8 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CS(C)(=O)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
45270917 201822 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 341 4 1 3 3.8 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL549439 201822 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 341 4 1 3 3.8 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2009.06.051
10159203 72384 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 421 7 1 5 5.5 Cc1ccc(C)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL183355 72384 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 421 7 1 5 5.5 Cc1ccc(C)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
70684436 83437 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064157 83437 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
44450208 102991 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3cccc(Cl)c3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL260820 102991 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3cccc(Cl)c3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
44391062 129402 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL360326 129402 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44391062 129402 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL360326 129402 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44189834 20794 0 None 1047 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.8 O=c1n(C(CO)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197240 20794 0 None 1047 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.8 O=c1n(C(CO)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL563657 20794 0 None 1047 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.8 O=c1n(C(CO)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
44391067 70233 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 425 7 1 5 5.3 Cc1cc(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)ccc1F 10.1016/j.bmcl.2004.11.049
CHEMBL179797 70233 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 425 7 1 5 5.3 Cc1cc(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)ccc1F 10.1016/j.bmcl.2004.11.049
44437628 177444 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 11 1 7 4.4 CNC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL445154 177444 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 11 1 7 4.4 CNC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
46879538 12957 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 462 5 1 4 3.0 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1081192 12957 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 462 5 1 4 3.0 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
44189733 20802 4 None 741 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197275 20802 4 None 741 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL564840 20802 4 None 741 3 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
44391157 71660 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 452 8 1 7 5.1 Cc1ccc([N+](=O)[O-])c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182202 71660 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 452 8 1 7 5.1 Cc1ccc([N+](=O)[O-])c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44437646 97119 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 534 12 1 7 4.6 C=CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238602 97119 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 534 12 1 7 4.6 C=CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437656 152493 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 10 1 6 3.7 CNC(=O)CN1CN(c2ccccc2)C2(CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)C1=O 10.1016/j.bmc.2006.11.030
CHEMBL391631 152493 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 10 1 6 3.7 CNC(=O)CN1CN(c2ccccc2)C2(CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)C1=O 10.1016/j.bmc.2006.11.030
44449766 162475 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 356 4 2 4 3.7 Cc1ccccc1CSc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL405078 162475 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 356 4 2 4 3.7 Cc1ccccc1CSc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44391103 72345 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 461 7 1 5 5.9 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.11.049
CHEMBL183135 72345 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 461 7 1 5 5.9 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.11.049
46879669 12741 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 436 4 1 4 3.4 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC4CCCCC4C3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079942 12741 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 436 4 1 4 3.4 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC4CCCCC4C3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
11462727 196159 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 366 3 2 4 3.2 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
CHEMBL512896 196159 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 366 3 2 4 3.2 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
135458466 86297 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 422 5 1 6 3.8 CN1CCN(c2[nH]ccc3nc(-c4nc(CCc5ccc(Cl)cc5)no4)cc2-3)CC1 10.1016/j.bmcl.2006.03.086
CHEMBL211390 86297 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 422 5 1 6 3.8 CN1CCN(c2[nH]ccc3nc(-c4nc(CCc5ccc(Cl)cc5)no4)cc2-3)CC1 10.1016/j.bmcl.2006.03.086
44143432 185488 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468301 185488 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
45268355 203019 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 320 4 1 4 3.2 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL561732 203019 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 320 4 1 4 3.2 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C)cc1F 10.1016/j.bmcl.2009.06.051
44576628 194506 0 None 6 4 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 382 4 2 5 3.6 C[C@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
CHEMBL495402 194506 0 None 6 4 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 382 4 2 5 3.6 C[C@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
45269358 202970 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 427 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL561397 202970 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 427 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
45268498 203480 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 413 6 1 5 4.8 CCc1c(CN[C@H]2CC[C@@H](F)C2)nc(-c2ncccc2Cl)n1-c1ccc(C)nc1 10.1016/j.bmcl.2009.06.095
CHEMBL564812 203480 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 413 6 1 5 4.8 CCc1c(CN[C@H]2CC[C@@H](F)C2)nc(-c2ncccc2Cl)n1-c1ccc(C)nc1 10.1016/j.bmcl.2009.06.095
44143437 185414 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 432 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(CC)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL467533 185414 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 432 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(CC)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
45267505 202840 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 343 4 1 3 4.0 Cn1nc(CN[C@H]2CC[C@@H](F)C2)c(Cl)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL560468 202840 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 343 4 1 3 4.0 Cn1nc(CN[C@H]2CC[C@@H](F)C2)c(Cl)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
45273537 203207 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL562932 203207 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
10199945 103461 0 None 42 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 382 6 2 5 3.6 CCC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263919 103461 0 None 42 3 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 382 6 2 5 3.6 CCC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
45102745 12815 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080485 12815 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44143438 185512 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 366 3 1 4 4.6 CCN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)[C@H](C)C1 10.1016/j.bmcl.2009.04.022
CHEMBL468504 185512 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 366 3 1 4 4.6 CCN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)[C@H](C)C1 10.1016/j.bmcl.2009.04.022
44450086 165074 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 394 5 2 5 3.8 OCCN1CCN(c2cc3[nH]c(SC4CCCCC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2008.04.054
CHEMBL408901 165074 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 394 5 2 5 3.8 OCCN1CCN(c2cc3[nH]c(SC4CCCCC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2008.04.054
10451761 44775 0 None 38 3 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cellsAntagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cells
ChEMBL 369 4 0 4 4.8 CCn1c(=O)n(C2CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1021/jm990517p
CHEMBL146013 44775 0 None 38 3 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cellsAntagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cells
ChEMBL 369 4 0 4 4.8 CCn1c(=O)n(C2CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1021/jm990517p
10783436 44975 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cellsAntagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cells
ChEMBL 341 3 1 4 4.7 Oc1nc2ccccc2n1C1CCN(CC2CCCCCCC2)CC1 10.1021/jm990517p
CHEMBL146191 44975 0 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cellsAntagonistic activity measured by GTPgammaS binding against Opioid receptor like 1 in CHO cells
ChEMBL 341 3 1 4 4.7 Oc1nc2ccccc2n1C1CCN(CC2CCCCCCC2)CC1 10.1021/jm990517p
44437648 154411 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 548 12 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL393138 154411 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 548 12 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
46879539 12266 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 448 5 1 4 3.0 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1076242 12266 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 448 5 1 4 3.0 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
22272877 102671 0 None 6 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL259185 102671 0 None 6 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
22272877 102671 0 None 6 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL259185 102671 0 None 6 3 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
11516508 145777 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 382 2 2 3 4.0 Oc1ccc(Cl)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3785560 145777 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 382 2 2 3 4.0 Oc1ccc(Cl)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
44576625 194277 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 396 7 2 5 4.0 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL494219 194277 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 396 7 2 5 4.0 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
136043779 84888 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 408 8 1 4 5.2 CCN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL210292 84888 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 408 8 1 4 5.2 CCN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
11552010 145795 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)NC2 10.1016/j.ejmech.2016.02.014
CHEMBL3785728 145795 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)NC2 10.1016/j.ejmech.2016.02.014
70690757 83431 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064139 83431 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
136043782 145442 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 380 6 1 4 4.7 CN(C)Cc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL377736 145442 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 380 6 1 4 4.7 CN(C)Cc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
44437602 97429 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239043 97429 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44391155 72042 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 475 7 1 5 6.6 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182819 72042 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 475 7 1 5 6.6 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.11.049
44391134 130091 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 425 7 1 5 5.3 Cc1ccc(F)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL361576 130091 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 425 7 1 5 5.3 Cc1ccc(F)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
11602409 145903 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 332 2 1 2 3.7 c1ccc2c(c1)CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3786899 145903 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 332 2 1 2 3.7 c1ccc2c(c1)CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
44437601 97403 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238833 97403 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
24894428 193106 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 370 3 1 3 4.6 O[C@H]1C[C@H](CN2CCC(c3ccccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
CHEMBL487485 193106 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 370 3 1 3 4.6 O[C@H]1C[C@H](CN2CCC(c3ccccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
44576627 200021 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 394 7 2 5 3.8 CCC(CC)Sc1nc2cc(Cl)c(N3C[C@@H]4C[C@H]3CN4CCO)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL523724 200021 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 394 7 2 5 3.8 CCC(CC)Sc1nc2cc(Cl)c(N3C[C@@H]4C[C@H]3CN4CCO)cc2[nH]1 10.1016/j.bmcl.2008.04.037
44450210 102993 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3c(Cl)cccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL260822 102993 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3c(Cl)cccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
46879670 12742 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 474 4 1 4 3.1 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079943 12742 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 474 4 1 4 3.1 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
127033703 145812 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 388 3 2 3 4.4 Cc1cc(F)ccc1C1CCN(CC2Cc3c(Cl)ccc(O)c3CN2)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3785952 145812 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 388 3 2 3 4.4 Cc1cc(F)ccc1C1CCN(CC2Cc3c(Cl)ccc(O)c3CN2)CC1 10.1016/j.ejmech.2016.02.014
44189735 20795 0 None 363 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197249 20795 0 None 363 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL563980 20795 0 None 363 3 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
136043759 85484 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 380 8 1 4 5.2 CN(C)CCc1cccc2[nH]c(-c3nc(CCCC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL211254 85484 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 380 8 1 4 5.2 CN(C)CCc1cccc2[nH]c(-c3nc(CCCC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
10221539 163777 0 None 10 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL407325 163777 0 None 10 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
10221539 163777 0 None 10 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL407325 163777 0 None 10 3 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44143454 195954 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnnn5C)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL511205 195954 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnnn5C)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
45270184 202049 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.6 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL551208 202049 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 399 5 1 5 4.6 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C)cn1 10.1016/j.bmcl.2009.06.095
22272974 103453 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 366 6 1 4 4.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CC)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263903 103453 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 366 6 1 4 4.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CC)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44437606 152296 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 494 10 1 7 3.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(N)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391486 152296 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 494 10 1 7 3.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(N)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
53316771 63204 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1896 66 31 27 -11.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
91933706 63204 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1896 66 31 27 -11.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
CHEMBL1631928 63204 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1896 66 31 27 -11.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
53316771 63204 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1896 66 31 27 -11.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
91933706 63204 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1896 66 31 27 -11.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
CHEMBL1631928 63204 0 None - 1 Mouse 7.5 pIC50 = 7.5 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1896 66 31 27 -11.6 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
44437652 97402 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 548 11 1 7 4.9 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CCC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238819 97402 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 548 11 1 7 4.9 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CCC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437619 98003 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 497 10 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL240074 98003 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 497 10 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
46879629 12645 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 420 4 1 4 2.5 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079417 12645 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 420 4 1 4 2.5 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
11626062 145727 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 426 2 2 3 4.1 Oc1ccc(Br)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3785095 145727 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 426 2 2 3 4.1 Oc1ccc(Br)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
44437613 153669 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 10 0 7 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)N(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL392548 153669 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 10 0 7 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)N(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
10225083 173175 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL427683 173175 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44143436 185245 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 402 4 1 5 3.7 CCN1CCN(c2cc3[nH]c(C(=O)C4(C)CCC(=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466307 185245 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 402 4 1 5 3.7 CCN1CCN(c2cc3[nH]c(C(=O)C4(C)CCC(=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
10225083 173175 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL427683 173175 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44450209 102992 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 376 4 2 4 4.1 Fc1cc2nc(SCc3ccccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL260821 102992 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 376 4 2 4 4.1 Fc1cc2nc(SCc3ccccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
53319408 63203 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1878 66 31 27 -11.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
91933705 63203 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1878 66 31 27 -11.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
CHEMBL1631927 63203 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1878 66 31 27 -11.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
53319408 63203 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1878 66 31 27 -11.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
91933705 63203 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1878 66 31 27 -11.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
CHEMBL1631927 63203 0 None - 1 Mouse 7.4 pIC50 = 7.4 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1878 66 31 27 -11.7 CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm101139f
44437610 152297 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391487 152297 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44143452 185516 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 470 5 1 6 4.2 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](S(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468524 185516 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 470 5 1 6 4.2 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](S(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
11583016 81128 0 None 1698 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 440 7 1 3 5.6 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Oc1ccccc1 10.1021/jm0509851
CHEMBL202443 81128 0 None 1698 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 440 7 1 3 5.6 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Oc1ccccc1 10.1021/jm0509851
44143429 185515 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 417 5 1 5 4.9 Cc1ccc(-c2c(C)c(CNC3CCC(F)(F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL468518 185515 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 417 5 1 5 4.9 Cc1ccc(-c2c(C)c(CNC3CCC(F)(F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
44561020 185964 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 384 3 2 4 3.4 Cc1cc(F)ccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
CHEMBL472304 185964 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 384 3 2 4 3.4 Cc1cc(F)ccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
45273679 202414 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 351 5 1 3 4.6 Cc1nc(CN[C@H]2CC[C@@H](F)C2)c(C(C)C)n1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.095
CHEMBL556300 202414 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 351 5 1 3 4.6 Cc1nc(CN[C@H]2CC[C@@H](F)C2)c(C(C)C)n1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.095
44178080 202859 2 None 1584 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 362 6 1 4 4.0 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCC#N)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL560667 202859 2 None 1584 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 362 6 1 4 4.0 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCC#N)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143419 194384 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 381 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL494767 194384 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 381 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
44437649 97401 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 534 11 1 7 4.5 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238818 97401 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 534 11 1 7 4.5 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44574003 185282 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 394 4 1 5 4.2 CC(=O)CN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)C(C)C1 10.1016/j.bmcl.2009.04.022
CHEMBL466631 185282 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 394 4 1 5 4.2 CC(=O)CN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)C(C)C1 10.1016/j.bmcl.2009.04.022
10301207 155434 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 511 11 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL393960 155434 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 511 11 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
70688697 83439 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 437 5 0 3 3.8 Cc1cc(F)ccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064159 83439 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 437 5 0 3 3.8 Cc1cc(F)ccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
11525624 140317 0 None 181 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
CHEMBL370870 140317 0 None 181 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
136043800 84565 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 428 7 1 4 5.1 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(C(F)(F)F)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL209213 84565 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 428 7 1 4 5.1 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(C(F)(F)F)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
10225083 173175 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL427683 173175 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437645 98573 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 552 13 1 8 4.0 COCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL241157 98573 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 552 13 1 8 4.0 COCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437605 97663 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 507 11 0 7 5.2 CCC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239260 97663 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 507 11 0 7 5.2 CCC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
70696991 83436 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064156 83436 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
46879478 12259 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 413 4 1 4 3.9 CNC(=O)CN1C(=O)OC2(CCN(C3CCC(C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1076208 12259 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 413 4 1 4 3.9 CNC(=O)CN1C(=O)OC2(CCN(C3CCC(C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
136043780 146046 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 438 10 1 5 4.8 CN(C)CCOCCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL379048 146046 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 438 10 1 5 4.8 CN(C)CCOCCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
44574053 185401 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 451 5 2 6 4.1 CCN1CCN(c2cc3[nH]c(SC4(C)CCC(NC(=O)OC)C4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467473 185401 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 451 5 2 6 4.1 CCN1CCN(c2cc3[nH]c(SC4(C)CCC(NC(=O)OC)C4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143406 194278 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 407 5 1 3 6.3 Cc1c(CNC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL494230 194278 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 407 5 1 3 6.3 Cc1c(CNC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
70686573 83428 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 406 5 0 4 2.2 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064133 83428 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation countingAntagonist activity at human recombinant ORL1 receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding to alpha-unit of G-protein after 1.5 hrs by scintillation counting
ChEMBL 406 5 0 4 2.2 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCN(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
11188910 196222 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 404 3 2 4 3.7 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)CCc2cccnc21 10.1021/jm701590h
CHEMBL513423 196222 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 404 3 2 4 3.7 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)CCc2cccnc21 10.1021/jm701590h
46879580 12640 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 476 4 1 4 3.7 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079400 12640 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 476 4 1 4 3.7 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
44143435 185221 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 441 5 2 6 3.5 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2C)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466112 185221 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 441 5 2 6 3.5 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2C)CC1 10.1016/j.bmcl.2009.04.023
44517710 203302 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 393 8 1 4 5.0 COCCc1nc(CN[C@H]2CC[C@@H](F)C2)n(C(C)C)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL563593 203302 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 393 8 1 4 5.0 COCCc1nc(CN[C@H]2CC[C@@H](F)C2)n(C(C)C)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
1691 8888 23 None 512 3 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cellsAntagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
5311194 8888 23 None 512 3 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cellsAntagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
CHEMBL357076 8888 23 None 512 3 Human 8.3 pIC50 = 8.3 Functional
Antagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cellsAntagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
11152739 196024 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 364 3 1 3 4.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1C 10.1021/jm701590h
CHEMBL511658 196024 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 364 3 1 3 4.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1C 10.1021/jm701590h
44391138 72237 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 445 7 1 5 5.7 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1cc(F)ccc1Cl 10.1016/j.bmcl.2004.11.049
CHEMBL182995 72237 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 445 7 1 5 5.7 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1cc(F)ccc1Cl 10.1016/j.bmcl.2004.11.049
46879537 12956 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 424 5 1 4 3.3 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1081191 12956 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 424 5 1 4 3.3 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
11544795 145794 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1cccc2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3785718 145794 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1cccc2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
44437654 152513 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 451 8 1 5 4.2 COc1ccc(C)c(OC(CCN2CCC3(CC2)C(=O)NCN3c2ccccc2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391650 152513 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 451 8 1 5 4.2 COc1ccc(C)c(OC(CCN2CCC3(CC2)C(=O)NCN3c2ccccc2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437647 97118 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 584 12 1 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCc4ccccc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238600 97118 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 584 12 1 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCc4ccccc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
127034292 145857 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 338 3 1 2 4.0 Cc1cc(F)ccc1C1CCN(CC2Cc3ccccc3CN2)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3786469 145857 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 338 3 1 2 4.0 Cc1cc(F)ccc1C1CCN(CC2Cc3ccccc3CN2)CC1 10.1016/j.ejmech.2016.02.014
45102745 12814 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080484 12814 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44576626 200145 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 410 7 2 5 4.4 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL525054 200145 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at human ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 410 7 2 5 4.4 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
44143442 185281 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 391 4 1 5 4.5 C[C@@H]1CN(CCC#N)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL466630 185281 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 391 4 1 5 4.5 C[C@@H]1CN(CCC#N)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
45270082 202024 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL551002 202024 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.06.051
44437602 97429 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239043 97429 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
53323365 63205 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1395 47 24 20 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm101139f
CHEMBL1631929 63205 0 None - 1 Mouse 6.2 pIC50 = 6.2 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1395 47 24 20 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm101139f
136043819 84712 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 394 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL209537 84712 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 394 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
10225083 173175 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL427683 173175 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
127034023 145932 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 331 2 0 1 4.8 c1ccc2c(c1)CCC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3787174 145932 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assayAntagonist activity at human NOP receptor expressed in HEK293 cells assessed as inhibition of N/OFQ-induced [35S]GTPgammaS binding after 1.5 hrs by scintillation proximity assay
ChEMBL 331 2 0 1 4.8 c1ccc2c(c1)CCC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
46879667 12739 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 438 4 1 4 3.7 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079940 12739 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 438 4 1 4 3.7 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
17858448 102733 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 322 5 2 4 3.4 CCC(CC)Sc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL259452 102733 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 322 5 2 4 3.4 CCC(CC)Sc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44143457 185375 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnc(C)o5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467280 185375 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnc(C)o5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
11372427 185934 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 380 4 2 4 3.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1CO 10.1021/jm701590h
CHEMBL472125 185934 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 380 4 2 4 3.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1CO 10.1021/jm701590h
46879581 12672 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 462 4 1 4 3.7 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079571 12672 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 462 4 1 4 3.7 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
44143434 185295 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 461 5 2 6 3.8 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466702 185295 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against ORL1 receptor by [S35]GTPgammaS bindingAntagonist activity against ORL1 receptor by [S35]GTPgammaS binding
ChEMBL 461 5 2 6 3.8 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
53320710 63207 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
91933708 63207 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631931 63207 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
11633324 79453 0 None 724 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 392 7 2 3 3.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H](O)Cc1ccccc1 10.1021/jm0509851
CHEMBL199639 79453 0 None 724 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 392 7 2 3 3.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H](O)Cc1ccccc1 10.1021/jm0509851
53320710 63207 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
91933708 63207 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631931 63207 0 None - 1 Mouse 8.1 pIC50 = 8.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
45272626 202543 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 306 4 2 3 3.2 Cc1ncc(-c2[nH]nc(CN[C@H]3CC[C@@H](F)C3)c2C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL557653 202543 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at ORL1 receptor by [35S]GTPgammaS binding assayAntagonist activity at ORL1 receptor by [35S]GTPgammaS binding assay
ChEMBL 306 4 2 3 3.2 Cc1ncc(-c2[nH]nc(CN[C@H]3CC[C@@H](F)C3)c2C)cc1F 10.1016/j.bmcl.2009.06.051
44437610 152297 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391487 152297 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
53323365 63205 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1395 47 24 20 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm101139f
CHEMBL1631929 63205 0 None - 1 Mouse 6.1 pIC50 = 6.1 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by Alphascreen Surefire assay
ChEMBL 1395 47 24 20 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm101139f
44437630 152340 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 481 10 1 7 4.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391518 152340 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 481 10 1 7 4.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437602 97429 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239043 97429 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44450151 102567 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 329 5 2 5 3.1 CCC(CC)Sc1nc2cc(C#N)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL258711 102567 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 329 5 2 5 3.1 CCC(CC)Sc1nc2cc(C#N)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44391104 71788 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 491 7 2 6 5.5 Cc1ccc(Cl)c(OC(c2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182328 71788 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 491 7 2 6 5.5 Cc1ccc(Cl)c(OC(c2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44437636 152217 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 513 10 0 7 4.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(C[S+](C)[O-])c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391422 152217 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 513 10 0 7 4.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(C[S+](C)[O-])c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
11619553 168499 1 None 407 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 424 6 1 2 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1-c1ccccc1 10.1021/jm0509851
CHEMBL413571 168499 1 None 407 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cellsAntagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
ChEMBL 424 6 1 2 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1-c1ccccc1 10.1021/jm0509851
44143445 185234 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 439 7 2 6 4.0 CCN1CCN(c2cc3[nH]c(SC(C)(C)CCNC(=O)OC)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466221 185234 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS bindingAntagonist activity at ORL1 receptor expressed in CHO cells assessed as inhibition of NC/OFQ-stimulated [35S]GTPgammaS binding
ChEMBL 439 7 2 6 4.0 CCN1CCN(c2cc3[nH]c(SC(C)(C)CCNC(=O)OC)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44391124 103213 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 457 8 1 6 5.5 COc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL262104 103213 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 457 8 1 6 5.5 COc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44437601 97403 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238833 97403 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437626 97398 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 11 0 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCN(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238795 97398 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 508 11 0 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCN(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
136043788 146121 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 420 5 1 4 5.5 CN1CCC(c2cccc3[nH]c(-c4nc(CCc5ccc(Cl)cc5)no4)cc23)CC1 10.1016/j.bmcl.2006.03.086
CHEMBL379284 146121 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against ORL1 receptor by GTPgammaS assayAntagonist activity against ORL1 receptor by GTPgammaS assay
ChEMBL 420 5 1 4 5.5 CN1CCC(c2cccc3[nH]c(-c4nc(CCc5ccc(Cl)cc5)no4)cc23)CC1 10.1016/j.bmcl.2006.03.086
11187225 185944 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL472168 185944 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS bindingAntagonist activity at human ORL1 expressed in CHO cells assessed as effect on nociceptin-induced GTPgammaS binding
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
22273044 102566 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 338 5 2 4 3.9 CCC(CC)Sc1nc2cc(Cl)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL258710 102566 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 338 5 2 4 3.9 CCC(CC)Sc1nc2cc(Cl)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
46879579 12810 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 438 4 1 4 4.0 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCCCCCCCC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1080464 12810 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 438 4 1 4 4.0 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCCCCCCCC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
45269357 202969 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 409 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CNC3CCCC3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL561396 202969 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS bindingAntagonist activity at human cloned ORL1 receptor expressed in CHO cells assessed as inhibition of nociceptin/orphanin FQ-stimulated [35S]GTPgammaS binding
ChEMBL 409 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CNC3CCCC3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
44437639 98006 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 11 1 7 4.4 CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240085 98006 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 522 11 1 7 4.4 CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437604 97430 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 5.2 CCOCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239045 97430 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 495 11 0 7 5.2 CCOCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
22272900 103449 1 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 348 4 2 4 3.8 Fc1cc2nc(SCC3CCCCC3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL263889 103449 1 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assayAntagonist activity at human ORL1 receptor expressed in CHO cell membrane by [35S]GTP-gamma-S binding assay
ChEMBL 348 4 2 4 3.8 Fc1cc2nc(SCC3CCCCC3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
44390989 172670 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 483 6 2 6 5.5 Cc1ccc(Cl)c(OC2(C(O)CN3CCC(n4c(O)nc5ccccc54)CC3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL424971 172670 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 483 6 2 6 5.5 Cc1ccc(Cl)c(OC2(C(O)CN3CCC(n4c(O)nc5ccccc54)CC3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
44391052 136447 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 425 7 1 5 5.3 Cc1cc(F)ccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL367367 136447 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
Inhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptorInhibitory concentration measured by cellular decreases in forskolin stimulated cAMP in CHO cells stably transfected with hORL1 receptor
ChEMBL 425 7 1 5 5.3 Cc1cc(F)ccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
44437638 98005 0 None - 1 Human 7.0 pIC50 = 7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 494 11 1 7 4.5 CNCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240084 98005 0 None - 1 Human 7.0 pIC50 = 7 Functional
Agonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrsAgonist activity at human NOP receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production after 2 hrs
ChEMBL 494 11 1 7 4.5 CNCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
25001412 69425 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant NOP expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human recombinant NOP expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL1783826 69425 0 None - 0 Human 9.9 pKd = 9.9 Functional
Antagonist activity at human recombinant NOP expressed in CHO cells by [35S]GTPgammaS binding assayAntagonist activity at human recombinant NOP expressed in CHO cells by [35S]GTPgammaS binding assay
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL2372052 216953 0 None - 1 Guinea pig 9.5 pKd = 9.5 Functional
Antagonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAntagonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)[C@H](CN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL2372052 216953 0 None - 1 Rat 9.2 pKd = 9.2 Functional
Antagonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAntagonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)[C@H](CN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL2372052 216953 0 None - 1 Mouse 9.1 pKd = 9.1 Functional
Antagonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAntagonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)[C@H](CN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
53320710 63207 0 None - 1 Mouse 8.7 pKd = 8.7 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by competitive inhibition assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by competitive inhibition assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
91933708 63207 0 None - 1 Mouse 8.7 pKd = 8.7 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by competitive inhibition assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by competitive inhibition assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
CHEMBL1631931 63207 0 None - 1 Mouse 8.7 pKd = 8.7 Functional
Antagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by competitive inhibition assayAntagonist activity at NOR in mouse Neuro-2a cells assessed as inhibition of nociceptin-induced ERK phosphorylation administered for 15 mins before nociceptin challenge by competitive inhibition assay
ChEMBL 2091 50 34 30 -13.8 C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNC(=O)c1ccccc1)C(=O)NCC(=O)N[C@H]1CCCCNC(=O)C[C@@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]2CCCCNC(=O)C[C@@H](C(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC2=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC1=O 10.1021/jm101139f
25001412 69425 0 None - 0 Mouse 8.0 pKd = 8 Functional
Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitchesAntagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL1783826 69425 0 None - 0 Mouse 8.0 pKd = 8 Functional
Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitchesAntagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
127043001 147144 0 None - 1 Human 6.0 pKd = 6 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1577 43 25 17 -1.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL3808398 147144 0 None - 1 Human 6.0 pKd = 6 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1577 43 25 17 -1.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL269068 217556 0 None - 0 Human 8.7 pKd = 8.7 Functional
Antagonist activity at human NOP receptor expressed in CHO cells by [35S]GTP-gamma-S binding assayAntagonist activity at human NOP receptor expressed in CHO cells by [35S]GTP-gamma-S binding assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL269068 217556 0 None - 0 Mouse 7.5 pKd = 7.5 Functional
Antagonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assayAntagonist activity at NOP receptor in Swiss mouse vas deferens by [35S]GTP-gamma-S binding assay
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
127044528 147146 0 None - 1 Human 5.4 pKd = 5.4 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1474 43 23 18 -1.9 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCN1Cc2ccccc2C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
CHEMBL3808415 147146 0 None - 1 Human 5.4 pKd = 5.4 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1474 43 23 18 -1.9 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCN1Cc2ccccc2C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
CHEMBL269068 217556 0 None - 0 Guinea pig 7.3 pKd = 7.3 Functional
Antagonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractionsAntagonist activity at NOP receptor in Albino guinea pig ileum assessed as effect on electrically stimulated contractions
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
10296561 7829 26 None - 3 Mouse 8.2 pKd = 8.2 Functional
Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitchesAntagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
7361 7829 26 None - 3 Mouse 8.2 pKd = 8.2 Functional
Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitchesAntagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
CHEMBL201945 7829 26 None - 3 Mouse 8.2 pKd = 8.2 Functional
Antagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitchesAntagonist activity at nociceptin receptor in Swiss mouse vas deferens assessed as inhibition of electrically evoked twitches
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
127043559 147288 0 None - 1 Human 6.3 pKd = 6.3 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1603 43 26 18 -1.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL3810104 147288 0 None - 1 Human 6.3 pKd = 6.3 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1603 43 26 18 -1.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL269068 217556 0 None - 0 Rat 7.1 pKd = 7.1 Functional
Antagonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractionsAntagonist activity at NOP receptor in Sprague-Dawley rat vas deferens assessed as effect on electrically stimulated contractions
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
127043364 147156 0 None - 1 Human 6.0 pKd = 6.0 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1575 43 26 18 -2.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL3808523 147156 0 None - 1 Human 6.0 pKd = 6.0 Functional
Antagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assayAntagonist activity at human nociceptin receptor expressed in HEK293 cells assessed as inhibition of OFQ/nociceptin-induced suppression of cAMP accumulation at 2 to 20 uM preincubated for 15 mins followed by OFQ/nociceptin addition by luciferase reporter gene assay
ChEMBL 1575 43 26 18 -2.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
44339596 16568 3 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 3 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL113684 16568 3 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 3 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
11743914 116442 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 439 6 1 2 6.2 OC1(c2cccc(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL322515 116442 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 439 6 1 2 6.2 OC1(c2cccc(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(03)00665-6
44339424 16110 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 3 1 2 5.2 CC(C)C1CCC(N2CCC(O)(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL111192 16110 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 3 1 2 5.2 CC(C)C1CCC(N2CCC(O)(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/s0960-894x(03)00665-6
44339695 16138 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 381 2 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(C2CCC3CCCCC3C2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL111347 16138 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 381 2 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(C2CCC3CCCCC3C2)CC1 10.1016/s0960-894x(03)00665-6
44339425 15455 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 4 1 2 5.3 CCCC1CCC(N2CCC(O)(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL109563 15455 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 369 4 1 2 5.3 CCCC1CCC(N2CCC(O)(c3cccc(C(F)(F)F)c3)CC2)CC1 10.1016/s0960-894x(03)00665-6
44339374 117374 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 473 6 1 2 6.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL325536 117374 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 473 6 1 2 6.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/s0960-894x(03)00665-6
44339423 16116 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 403 3 1 2 5.9 CC(C)C1CCC(N2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL111230 16116 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 403 3 1 2 5.9 CC(C)C1CCC(N2CCC(O)(c3ccc(Cl)c(C(F)(F)F)c3)CC2)CC1 10.1016/s0960-894x(03)00665-6
46227963 20948 0 None -3 4 Human 8.4 pKi = 8.4 Functional
Antagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS bindingAntagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
CHEMBL1198701 20948 0 None -3 4 Human 8.4 pKi = 8.4 Functional
Antagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS bindingAntagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
CHEMBL611929 20948 0 None -3 4 Human 8.4 pKi = 8.4 Functional
Antagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS bindingAntagonist activity at NOP expressed in HEK293 cells assessed as inhibition of compound 15-induced [35S]GTPgammaS binding
ChEMBL 514 4 3 5 3.8 O=C(N[C@@H]1CC[C@@]2(O)[C@H]3Cc4ccc(O)c5c4[C@@]2(CCN3CC2CC2)[C@H]1O5)c1ccc(C(F)(F)F)cc1 10.1016/j.bmc.2009.07.069
44339576 15500 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 403 3 1 2 6.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL109598 15500 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 403 3 1 2 6.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
44339504 115621 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 335 3 1 2 5.0 OC1(c2ccc(Cl)cc2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL320991 115621 0 None - 0 Human 6.3 pKi = 6.3 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 335 3 1 2 5.0 OC1(c2ccc(Cl)cc2)CCN(CC2CCCCCCC2)CC1 10.1016/s0960-894x(03)00665-6
44339684 16451 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 395 2 1 2 4.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(C2Cc3ccccc3C2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL112974 16451 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonistic activity against orphan FQ receptorAntagonistic activity against orphan FQ receptor
ChEMBL 395 2 1 2 4.8 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(C2Cc3ccccc3C2)CC1 10.1016/s0960-894x(03)00665-6
10499 10624 0 None - 1 Mouse 7.8 pA2 = 7.8 Functional
Antagonism of the electrically induced twitch response in mouse vas deferens stimulated by N/OFQ as agonist.Antagonism of the electrically induced twitch response in mouse vas deferens stimulated by N/OFQ as agonist.
Guide to Pharmacology 397 5 1 5 4.1 OCC1=C(CCN(C1)CC1CCCCCCC1)n1c(=O)n(c2c1cccc2)CC 16202610
11494970 10624 0 None - 1 Mouse 7.8 pA2 = 7.8 Functional
Antagonism of the electrically induced twitch response in mouse vas deferens stimulated by N/OFQ as agonist.Antagonism of the electrically induced twitch response in mouse vas deferens stimulated by N/OFQ as agonist.
Guide to Pharmacology 397 5 1 5 4.1 OCC1=C(CCN(C1)CC1CCCCCCC1)n1c(=O)n(c2c1cccc2)CC 16202610
CHEMBL3182208 10624 0 None - 1 Mouse 7.8 pA2 = 7.8 Functional
Antagonism of the electrically induced twitch response in mouse vas deferens stimulated by N/OFQ as agonist.Antagonism of the electrically induced twitch response in mouse vas deferens stimulated by N/OFQ as agonist.
Guide to Pharmacology 397 5 1 5 4.1 OCC1=C(CCN(C1)CC1CCCCCCC1)n1c(=O)n(c2c1cccc2)CC 16202610
66553195 99920 34 None 1 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 386 7 1 5 4.7 COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1 None
CHEMBL2443262 99920 34 None 1 4 Human 8.1 pEC50 = 8.1 Functional
NoneNone
Drug Central 386 7 1 5 4.7 COc1ccsc1CNCC[C@@]1(c2ccccn2)CCOC2(CCCC2)C1 None
12419 9252 29 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Potency determined in a functional assay; [35S]GTPγS recruitmentPotency determined in a functional assay; [35S]GTPγS recruitment
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
24800108 9252 29 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Potency determined in a functional assay; [35S]GTPγS recruitmentPotency determined in a functional assay; [35S]GTPγS recruitment
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
CHEMBL481512 9252 29 None 87 4 Human 9.4 pEC50 = 9.4 Functional
Potency determined in a functional assay; [35S]GTPγS recruitmentPotency determined in a functional assay; [35S]GTPγS recruitment
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
1684 10135 21 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP&gamma;<sup>35</sup>S bindingStimulation of GTP&gamma;<sup>35</sup>S binding
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
9844019 10135 21 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP&gamma;<sup>35</sup>S bindingStimulation of GTP&gamma;<sup>35</sup>S binding
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
CHEMBL2088034 10135 21 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP&gamma;<sup>35</sup>S bindingStimulation of GTP&gamma;<sup>35</sup>S binding
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
1686 9847 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 15743186
1679 7056 24 None - 1 Human 5.1 pEC50 = 5.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 9353393
9963005 7056 24 None - 1 Human 5.1 pEC50 = 5.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 9353393
CHEMBL437723 7056 24 None - 1 Human 5.1 pEC50 = 5.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 9353393
11597355 10327 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 439 4 1 4 5.4 Clc1ccccc1C(c1ccccc1Cl)N1[C@@H]2CC[C@H]1CC(C2)(O)c1ncccn1 20006596
8869 10327 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 439 4 1 4 5.4 Clc1ccccc1C(c1ccccc1Cl)N1[C@@H]2CC[C@H]1CC(C2)(O)c1ncccn1 20006596
49843739 10440 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 386 2 0 2 5.0 O=C1Cc2c(N1C1CCN(CC1)C1CCC3c4c1cccc4CCC3)cccc2 19773529
8867 10440 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 386 2 0 2 5.0 O=C1Cc2c(N1C1CCN(CC1)C1CCC3c4c1cccc4CCC3)cccc2 19773529
CHEMBL3262554 10440 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 386 2 0 2 5.0 O=C1Cc2c(N1C1CCN(CC1)C1CCC3c4c1cccc4CCC3)cccc2 19773529
15512229 10158 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10476866
8864 10158 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10476866
CHEMBL355202 10158 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10476866
11848225 7664 52 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8866 7664 52 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL2364605 7664 52 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3545616 7664 52 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3962932 7664 52 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8868 10320 31 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
9887077 10320 31 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
CHEMBL513136 10320 31 None 57 2 Human 7.9 pEC50 = 7.9 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
8865 10012 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Stimulation of GTP-&gamma;<sup>35</sup>S bindingStimulation of GTP-&gamma;<sup>35</sup>S binding
Guide to Pharmacology None None None None 24903280
1680 7057 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
3917 10702 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
3917 10702 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
44430609 10702 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
44430609 10702 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
CHEMBL409969 10702 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17532097
CHEMBL409969 10702 0 None 3 4 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19183962
16131448 9624 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 9624 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 9624 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 9624 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 9624 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 9624 28 None 2 5 Human 9.1 pEC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1691 8888 23 None 512 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10602690
5311194 8888 23 None 512 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10602690
CHEMBL357076 8888 23 None 512 3 Human 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10602690
10047612 10302 15 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
10047612 10302 15 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
1693 10302 15 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
1693 10302 15 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
CHEMBL559569 10302 15 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
CHEMBL559569 10302 15 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
10296561 7829 26 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 16451050
10296561 7829 26 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
7361 7829 26 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 16451050
7361 7829 26 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
CHEMBL201945 7829 26 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 16451050
CHEMBL201945 7829 26 None 13182 3 Human 9.8 pIC50 = 9.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
10500 9601 0 None - 1 Human 7.4 pKB = 7.4 Functional
Antagonism of N/OFQ-induced calcium mobilisation in CHO cells expressing hNOP.Antagonism of N/OFQ-induced calcium mobilisation in CHO cells expressing hNOP.
Guide to Pharmacology 512 6 1 5 3.8 NC(=O)Cn1c(C(=O)N2CCOCC2)c(c2c1cccc2)CN1CCC(CC1)c1c(F)cccc1Cl 22994368
24889797 9601 0 None - 1 Human 7.4 pKB = 7.4 Functional
Antagonism of N/OFQ-induced calcium mobilisation in CHO cells expressing hNOP.Antagonism of N/OFQ-induced calcium mobilisation in CHO cells expressing hNOP.
Guide to Pharmacology 512 6 1 5 3.8 NC(=O)Cn1c(C(=O)N2CCOCC2)c(c2c1cccc2)CN1CCC(CC1)c1c(F)cccc1Cl 22994368


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay
Type		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

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 DOI
CHEMBL414542 219917 0 None - 1 Human 10.2 pEC50 = 10.2 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
44388462 168632 0 None - 0 Human 10.1 pEC50 = 10.1 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414782 168632 0 None - 0 Human 10.1 pEC50 = 10.1 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1970 68 33 31 -15.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL266191 217458 0 None - 1 Human 10.1 pEC50 = 10.1 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
162662480 188834 0 None - 0 Human 10.1 pEC50 = 10.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2434 92 38 37 -12.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4781235 188834 0 None - 0 Human 10.1 pEC50 = 10.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2434 92 38 37 -12.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL408356 219487 0 None - 1 Human 9.9 pEC50 = 9.9 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
44388461 166619 0 None - 0 Human 9.9 pEC50 = 9.9 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL410653 166619 0 None - 0 Human 9.9 pEC50 = 9.9 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1952 68 33 31 -15.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL415845 219983 0 None - 1 Human 9.7 pEC50 = 9.7 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
44388467 176184 0 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL442297 176184 0 None - 1 Human 9.7 pEC50 = 9.7 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL264084 217384 0 None - 1 Human 9.6 pEC50 = 9.6 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
162662934 188806 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1789 67 24 23 -3.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4780822 188806 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1789 67 24 23 -3.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
162676761 190295 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1848 68 26 25 -5.3 CCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4799815 190295 0 None - 0 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1848 68 26 25 -5.3 CCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
124565311 180849 0 None 165 2 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assay
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/acs.jmedchem.5b01499
CHEMBL4544227 180849 0 None 165 2 Human 9.5 pEC50 = 9.5 Binding
Agonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assay
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/acs.jmedchem.5b01499
CHEMBL264846 217411 0 None - 1 Human 9.5 pEC50 = 9.5 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
44388474 167821 0 None - 1 Human 9.4 pEC50 = 9.4 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing human NOP receptor (CHOhNOP) Agonist potency against GTPgammaS binding in CHO cell membranes expressing human NOP receptor (CHOhNOP)
ChEMBL 1970 69 33 31 -15.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL411649 167821 0 None - 1 Human 9.4 pEC50 = 9.4 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing human NOP receptor (CHOhNOP) Agonist potency against GTPgammaS binding in CHO cell membranes expressing human NOP receptor (CHOhNOP)
ChEMBL 1970 69 33 31 -15.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
162676231 190105 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1805 68 25 24 -4.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4797388 190105 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1805 68 25 24 -4.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
16131448 9624 28 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
1681 9624 28 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
1688 9624 28 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
44361543 9624 28 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
56947112 9624 28 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
CHEMBL396460 9624 28 None 1 6 Human 9.4 pEC50 = 9.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
162656512 187686 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1399 47 24 20 -8.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(F)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4757730 187686 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1399 47 24 20 -8.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(F)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL410979 219634 0 None - 1 Human 9.3 pEC50 = 9.3 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
162651080 186999 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1720 64 22 23 -3.2 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4749802 186999 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1720 64 22 23 -3.2 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
162650489 186813 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1876 70 26 25 -4.5 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4747497 186813 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1876 70 26 25 -4.5 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
162669053 189506 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1365 46 23 19 -7.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4789749 189506 0 None - 0 Human 9.3 pEC50 = 9.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1365 46 23 19 -7.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL438537 220553 0 None - 1 Human 9.1 pEC50 = 9.1 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
162676138 190177 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2861 104 44 43 -15.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4798159 190177 0 None - 0 Human 9.1 pEC50 = 9.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2861 104 44 43 -15.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL263588 217358 0 None - 1 Human 9.1 pEC50 = 9.1 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
44388466 103276 0 None - 1 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL262544 103276 0 None - 1 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL415584 219971 0 None - 1 Human 9.0 pEC50 = 9 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
16131448 9624 28 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1681 9624 28 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
1688 9624 28 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
44361543 9624 28 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
56947112 9624 28 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 9624 28 None 1 6 Human 9.0 pEC50 = 9.0 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None None 10.1021/jm040106v
162661740 188623 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2777 104 44 43 -17.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4778484 188623 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2777 104 44 43 -17.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL406905 219408 0 None - 1 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)CC1CCCCC1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162670125 189378 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4788218 189378 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162670701 189663 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1748 64 24 23 -4.1 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4792010 189663 0 None - 0 Human 8.9 pEC50 = 8.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1748 64 24 23 -4.1 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
10276738 179040 0 None 54 2 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes by GTPgamma(35)S binding assay
ChEMBL 466 5 2 3 6.1 NCc1ccccc1C1(O)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
CHEMBL4474536 179040 0 None 54 2 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes by GTPgamma(35)S binding assay
ChEMBL 466 5 2 3 6.1 NCc1ccccc1C1(O)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
162645148 186196 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1904 72 26 25 -3.7 CCCCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4740203 186196 0 None - 0 Human 8.8 pEC50 = 8.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1904 72 26 25 -3.7 CCCCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL265801 217442 0 None - 1 Human 8.7 pEC50 = 8.7 Binding
Binding of compound to cell membranes expressing human ORL1 receptor in HEk-293 cells using [32S]GTP-gamma-SBinding of compound to cell membranes expressing human ORL1 receptor in HEk-293 cells using [32S]GTP-gamma-S
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/jm010092i
1682 9627 18 None 3 2 Human 8.0 pEC50 = 8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
6324645 9627 18 None 3 2 Human 8.0 pEC50 = 8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
CHEMBL384755 9627 18 None 3 2 Human 8.0 pEC50 = 8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
CHEMBL405212 219329 0 None - 1 Human 8.0 pEC50 = 8.0 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
CHEMBL439528 220623 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162653778 187260 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1379 47 23 19 -7.5 CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4753041 187260 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1379 47 23 19 -7.5 CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162652312 187099 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4751132 187099 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/acs.jmedchem.9b02057
162649797 186810 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2830 92 44 43 -18.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4747450 186810 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2830 92 44 43 -18.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162650108 186920 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2101 80 29 34 -12.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCOCCOCC(=O)NCCOCCOCC(=O)NCCOCCOCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4748849 186920 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2101 80 29 34 -12.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCOCCOCC(=O)NCCOCCOCC(=O)NCCOCCOCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
11848225 7664 52 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
8866 7664 52 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL2364605 7664 52 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL3545616 7664 52 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL3962932 7664 52 None -4 7 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assayAgonist activity at recombinant human nociceptin opioid receptor expressed in CHOK1 cell membranes after 45 mins by GTPgamma(35)S binding assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
162659015 188169 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4763461 188169 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162652312 187099 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4751132 187099 0 None - 0 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL412479 219774 0 None - 1 Human 7.9 pEC50 = 7.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL None None None CC(C)C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.9b02057
162661740 188623 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2777 104 44 43 -17.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4778484 188623 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2777 104 44 43 -17.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
11804490 188594 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1296 43 21 19 -8.1 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4778171 188594 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1296 43 21 19 -8.1 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL2403216 217196 0 None - 0 Rat 5.9 pEC50 = 5.9 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None COc1ccc2[nH]cc([C@H](CNC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(N)=O)c2c1 10.1016/j.bmcl.2013.05.064
162650108 186920 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2101 80 29 34 -12.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCOCCOCC(=O)NCCOCCOCC(=O)NCCOCCOCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4748849 186920 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2101 80 29 34 -12.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCOCCOCC(=O)NCCOCCOCC(=O)NCCOCCOCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL2403218 217198 19 None - 0 Rat 7.8 pEC50 = 7.8 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmcl.2013.05.064
11137032 188217 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4764102 188217 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
25208097 190701 3 None 5 4 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-2 recruitmentAgonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-2 recruitment
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
CHEMBL481366 190701 3 None 5 4 Human 5.8 pEC50 = 5.8 Binding
Agonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-2 recruitmentAgonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-2 recruitment
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
162661631 188657 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4778926 188657 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL2403216 217196 0 None - 0 Rat 5.8 pEC50 = 5.8 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction in presence of naloxoneActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction in presence of naloxone
ChEMBL None None None COc1ccc2[nH]cc([C@H](CNC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(N)=O)c2c1 10.1016/j.bmcl.2013.05.064
162676138 190177 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2861 104 44 43 -15.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4798159 190177 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2861 104 44 43 -15.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162650867 186982 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2698 92 44 43 -21.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4749620 186982 0 None - 0 Human 7.8 pEC50 = 7.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2698 92 44 43 -21.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
5311327 187216 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4752457 187216 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162662934 188806 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1789 67 24 23 -3.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4780822 188806 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1789 67 24 23 -3.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
162665903 189108 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC1(C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)CCCC1 10.1021/acs.jmedchem.9b02057
CHEMBL4784371 189108 0 None - 0 Human 8.6 pEC50 = 8.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC1(C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)CCCC1 10.1021/acs.jmedchem.9b02057
9905428 11181 16 None 21 3 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assay
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b01499
CHEMBL101454 11181 16 None 21 3 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assay
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b01499
162659601 187978 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1393 47 24 20 -8.7 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4761103 187978 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1393 47 24 20 -8.7 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162646448 186478 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4743726 186478 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162651080 186999 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1720 64 22 23 -3.2 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4749802 186999 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1720 64 22 23 -3.2 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
11137032 188217 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4764102 188217 0 None - 0 Human 7.7 pEC50 = 7.7 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162655432 187460 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1420 47 25 20 -8.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4755353 187460 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1420 47 25 20 -8.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162655941 187521 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4755981 187521 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162648427 186740 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2782 92 44 43 -19.4 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4746696 186740 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2782 92 44 43 -19.4 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.9b02057
162676761 190295 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1848 68 26 25 -5.3 CCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4799815 190295 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1848 68 26 25 -5.3 CCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
25208097 190701 3 None 5 4 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-1 recruitmentAgonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-1 recruitment
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
CHEMBL481366 190701 3 None 5 4 Human 5.6 pEC50 = 5.6 Binding
Agonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-1 recruitmentAgonist activity at human NOPR expressed in human BHK cells assessed as increase in beta-arrestin-1 recruitment
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/acs.jmedchem.8b00435
10832076 44825 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cellsAgonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 355 3 1 4 4.8 CC(c1ccccc1Cl)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm990517p
CHEMBL146054 44825 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cellsAgonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 355 3 1 4 4.8 CC(c1ccccc1Cl)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm990517p
10534521 189830 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4794113 189830 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162650635 186875 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1394 48 24 20 -9.3 C[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4748275 186875 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1394 48 24 20 -9.3 C[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162659601 187978 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1393 47 24 20 -8.7 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4761103 187978 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1393 47 24 20 -8.7 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162671943 189713 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1776 57 26 25 -7.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NC2CCCCCCC2)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4792616 189713 0 None - 0 Human 7.6 pEC50 = 7.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1776 57 26 25 -7.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NC2CCCCCCC2)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162659015 188169 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4763461 188169 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162673971 189929 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4795259 189929 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162669053 189506 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1365 46 23 19 -7.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4789749 189506 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1365 46 23 19 -7.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162671943 189713 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1776 57 26 25 -7.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NC2CCCCCCC2)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4792616 189713 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1776 57 26 25 -7.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NC2CCCCCCC2)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162656512 187686 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1399 47 24 20 -8.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(F)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4757730 187686 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1399 47 24 20 -8.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(F)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162670125 189378 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4788218 189378 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162676231 190105 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1805 68 25 24 -4.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4797388 190105 0 None - 0 Human 7.5 pEC50 = 7.5 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1805 68 25 24 -4.0 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
10763594 168056 1 None 120 4 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human nociceptin opioid receptor by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor by GTPgamma(35)S binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1021/acs.jmedchem.5b01499
CHEMBL412098 168056 1 None 120 4 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human nociceptin opioid receptor by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor by GTPgamma(35)S binding assay
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1021/acs.jmedchem.5b01499
15512228 74530 0 None 8 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assay
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1Cc3cccc4cccc1c34)CC2 10.1021/acs.jmedchem.5b01499
CHEMBL1907858 74530 0 None 8 3 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in HEK293 cell membranes by GTPgamma(35)S binding assay
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1Cc3cccc4cccc1c34)CC2 10.1021/acs.jmedchem.5b01499
162661152 188304 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4765138 188304 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162649797 186810 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2830 92 44 43 -18.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4747450 186810 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2830 92 44 43 -18.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(=O)NCC(=O)N[C@@H](Cc2cnc[nH]2)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162648962 186569 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4744757 186569 0 None - 0 Human 8.4 pEC50 = 8.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162657281 187753 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4758592 187753 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162655941 187521 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4755981 187521 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL414541 219916 0 None - 1 Human 6.4 pEC50 = 6.4 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
162653778 187260 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1379 47 23 19 -7.5 CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4753041 187260 0 None - 0 Human 7.4 pEC50 = 7.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1379 47 23 19 -7.5 CC(C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL413429 219846 0 None - 0 Human 6.4 pEC50 = 6.4 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
155544763 180135 0 None 7 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assay
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@H]3CCCc4cccc2c43)CC1 10.1021/acs.jmedchem.5b01499
CHEMBL4527189 180135 0 None 7 2 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by GTPgamma(35)S binding assay
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@H]3CCCc4cccc2c43)CC1 10.1021/acs.jmedchem.5b01499
162645845 186454 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2032 78 28 27 -4.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4743479 186454 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2032 78 28 27 -4.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
11804490 188594 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1296 43 21 19 -8.1 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4778171 188594 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1296 43 21 19 -8.1 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162650867 186982 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2698 92 44 43 -21.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4749620 186982 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2698 92 44 43 -21.7 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162658205 187908 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4760586 187908 0 None - 0 Human 6.3 pEC50 = 6.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162645845 186454 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2032 78 28 27 -4.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4743479 186454 0 None - 0 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2032 78 28 27 -4.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL406905 219408 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)CC1CCCCC1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL414767 219933 0 None 154 2 Human 8.3 pEC50 = 8.3 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP)
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
CHEMBL436732 220466 0 None - 1 Human 8.3 pEC50 = 8.3 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
162657281 187753 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4758592 187753 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL413944 219882 0 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP) at 1 uMAgonist potency against GTPgammaS binding in CHO cell membranes expressing the human NOP receptor (CHOhNOP) at 1 uM
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
10593778 106018 0 None 10 4 Human 6.3 pEC50 = 6.3 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL 347 2 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(C1Cc3ccccc3C1)CC2 10.1021/jm991129q
CHEMBL28172 106018 0 None 10 4 Human 6.3 pEC50 = 6.3 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL 347 2 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(C1Cc3ccccc3C1)CC2 10.1021/jm991129q
1682 9627 18 None - 2 Rat 7.3 pEC50 = 7.3 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None None 10.1016/j.bmcl.2013.05.064
6324645 9627 18 None - 2 Rat 7.3 pEC50 = 7.3 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None None 10.1016/j.bmcl.2013.05.064
CHEMBL384755 9627 18 None - 2 Rat 7.3 pEC50 = 7.3 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contractionActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction
ChEMBL None None None None 10.1016/j.bmcl.2013.05.064
CHEMBL414543 219918 0 None - 1 Human 7.3 pEC50 = 7.3 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
5311327 187216 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4752457 187216 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162650489 186813 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1876 70 26 25 -4.5 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4747497 186813 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1876 70 26 25 -4.5 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
162670701 189663 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1748 64 24 23 -4.1 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4792010 189663 0 None - 0 Human 7.3 pEC50 = 7.3 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1748 64 24 23 -4.1 CCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
162672438 190006 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2215 89 29 28 -2.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4796153 190006 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2215 89 29 28 -2.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162662480 188834 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2434 92 38 37 -12.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4781235 188834 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2434 92 38 37 -12.5 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
162665903 189108 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC1(C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)CCCC1 10.1021/acs.jmedchem.9b02057
CHEMBL4784371 189108 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC1(C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O)CCCC1 10.1021/acs.jmedchem.9b02057
CHEMBL2403218 217198 19 None - 0 Rat 8.2 pEC50 = 8.2 Binding
Activity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction in presence of naloxoneActivity at Wistar rat NOP receptor assessed as inhibition of low-frequency electrically-stimulated vas deferens contraction in presence of naloxone
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmcl.2013.05.064
162648962 186569 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4744757 186569 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)NC(C)(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162672438 190006 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2215 89 29 28 -2.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4796153 190006 0 None - 0 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2215 89 29 28 -2.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CSC1CC(=O)N(CCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(=O)NCCCCCCCCCCC(N)=O)C1=O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL412479 219774 0 None - 1 Human 8.2 pEC50 = 8.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None CC(C)C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O 10.1021/acs.jmedchem.9b02057
162645148 186196 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1904 72 26 25 -3.7 CCCCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
CHEMBL4740203 186196 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1904 72 26 25 -3.7 CCCCCCCCCCCCCCCCCC(=O)NCCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O 10.1021/acs.jmedchem.9b02057
16131448 9624 28 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
1681 9624 28 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
1688 9624 28 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
44361543 9624 28 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
56947112 9624 28 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
CHEMBL396460 9624 28 None 1 6 Human 7.2 pEC50 = 7.2 Binding
Effective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assayEffective concentration required to stimulate binding of GTPgammaS to Opioid receptor like 1 was determined using scintillation proximity assay
ChEMBL None None None None 10.1021/jm991129q
162655432 187460 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1420 47 25 20 -8.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4755353 187460 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1420 47 25 20 -8.3 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
10534521 189830 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4794113 189830 0 None - 0 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
416359 108637 21 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cellsAgonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1021/jm990517p
CHEMBL300616 108637 21 None - 0 Human 5.2 pEC50 = 5.2 Binding
Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cellsAgonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1021/jm990517p
162661631 188657 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4778926 188657 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1324 43 23 19 -8.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162671290 189607 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2914 92 44 43 -16.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4791156 189607 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 2914 92 44 43 -16.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(N)=O 10.1021/acs.jmedchem.9b02057
162673058 189905 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4795008 189905 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162673058 189905 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4795008 189905 0 None - 0 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1421 47 24 20 -7.9 C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C1(NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162661152 188304 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4765138 188304 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162645528 186413 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1351 46 23 19 -8.2 C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4742892 186413 0 None - 0 Human 6.1 pEC50 = 6.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1351 46 23 19 -8.2 C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162645528 186413 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1351 46 23 19 -8.2 C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4742892 186413 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1351 46 23 19 -8.2 C[C@H](NC(=O)CNC(=O)[C@H](C)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
11583008 182642 5 None 213 2 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 30 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 30 mins by GTPgamma(35)S binding assay
ChEMBL 439 4 1 4 5.4 OC1(c2ncccn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
CHEMBL4585935 182642 5 None 213 2 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 30 mins by GTPgamma(35)S binding assayAgonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 30 mins by GTPgamma(35)S binding assay
ChEMBL 439 4 1 4 5.4 OC1(c2ncccn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
162646448 186478 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4743726 186478 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 1395 47 24 20 -8.4 C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
1682 9627 18 None 3 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
6324645 9627 18 None 3 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
CHEMBL384755 9627 18 None 3 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.9b02057
CHEMBL410396 219597 17 None 1 2 Human 8.1 pEC50 = 8.1 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162650635 186875 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1394 48 24 20 -9.3 C[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4748275 186875 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1394 48 24 20 -9.3 C[C@H](NC(=O)CNC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162671290 189607 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2914 92 44 43 -16.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4791156 189607 0 None - 0 Human 8.0 pEC50 = 8.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2914 92 44 43 -16.5 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1cnc[nH]1)C(N)=O 10.1021/acs.jmedchem.9b02057
162673971 189929 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4795259 189929 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162648427 186740 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2782 92 44 43 -19.4 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4746696 186740 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as induction of beta-arrestin2 activation incubated for 15 mins by BRET assay
ChEMBL 2782 92 44 43 -19.4 C[C@H](NC(=O)CCCN1C(=O)CC(SC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(N)=O)C1=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL429239 220297 0 None - 0 Human 6.0 pEC50 = 6.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL427617 220135 0 None - 1 Human 7.0 pEC50 = 7.0 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
162658205 187908 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4760586 187908 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
Agonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assayAgonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as induction of G protein activation incubated for 15 mins by BRET assay
ChEMBL 1381 47 24 20 -8.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
24882570 121909 0 None - 1 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343946 121909 0 None - 1 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343947 121909 0 None - 1 Human 10.5 pIC50 = 10.5 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL414736 219931 0 None - 0 Human 10.3 pIC50 = 10.3 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCCNC(=O)CNC(=O)CNC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2006.06.060
101354795 121911 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 967 31 16 12 -1.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343949 121911 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 967 31 16 12 -1.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
44416445 176131 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL 1847 62 28 25 -8.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCCNC(=O)CNC(=O)CNC(=O)CCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2006.06.060
CHEMBL441930 176131 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL 1847 62 28 25 -8.2 CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)NCC(=O)NCC(=O)N[C@@H](CCCCNC(=O)CNC(=O)CNC(=O)CCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2006.06.060
16131448 9624 28 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1681 9624 28 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1688 9624 28 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44361543 9624 28 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
56947112 9624 28 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL396460 9624 28 None 1 6 Human 10.1 pIC50 = 10.1 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor high affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL443591 220705 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm010092i
CHEMBL511107 222372 0 None - 0 Rat 9.8 pIC50 = 9.8 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16143911 7255 16 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1689 7255 16 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL505874 7255 16 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL506825 220992 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16143911 7255 16 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
1689 7255 16 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL505874 7255 16 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
16131448 9624 28 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None 1 6 Human 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
11511090 80828 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
CHEMBL202225 80828 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
16131448 9624 28 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 9624 28 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -1 6 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL556388 222514 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL559130 222522 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
10296561 7829 26 None 23 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
7361 7829 26 None 23 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
CHEMBL201945 7829 26 None 23 2 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1021/jm0509851
CHEMBL507847 221336 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL265801 217442 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/jm010092i
16131448 9624 28 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
1681 9624 28 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
1688 9624 28 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
44361543 9624 28 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
56947112 9624 28 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
CHEMBL396460 9624 28 None 1 6 Human 9.5 pIC50 = 9.5 Binding
Binding affinity to ORL1 receptor (unknown origin) by radioligand displacement assayBinding affinity to ORL1 receptor (unknown origin) by radioligand displacement assay
ChEMBL None None None None 10.1016/j.bmc.2013.03.016
CHEMBL555757 222511 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL526333 222459 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL558807 222521 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL500773 220906 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1682 9627 18 None 3 2 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None None 10.1021/jm010092i
6324645 9627 18 None 3 2 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None None 10.1021/jm010092i
CHEMBL384755 9627 18 None 3 2 Human 9.5 pIC50 = 9.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None None 10.1021/jm010092i
CHEMBL503512 220948 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL504587 220960 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL505632 220974 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL504587 220960 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
CHEMBL505824 220976 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16131448 9624 28 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL406718 219396 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(N)=O 10.1021/jm010092i
CHEMBL504872 220964 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
44143431 185285 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL466648 185285 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.06.051
44143431 185285 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
CHEMBL466648 185285 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 417 5 1 5 4.7 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
CHEMBL437915 220518 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(N)=O 10.1021/jm010092i
CHEMBL499157 220870 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16131448 9624 28 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -1 6 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 9624 28 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1681 9624 28 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
1688 9624 28 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
44361543 9624 28 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
56947112 9624 28 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL396460 9624 28 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
155569742 183431 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 415 6 1 5 3.6 O=c1n(CCF)c2ccccc2n1[C@H]1CCN(C[C@H]2CCCCC23CC3)C[C@@H]1CO 10.1021/acs.jmedchem.5b01499
CHEMBL4454908 183431 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 415 6 1 5 3.6 O=c1n(CCF)c2ccccc2n1[C@H]1CCN(C[C@H]2CCCCC23CC3)C[C@@H]1CO 10.1021/acs.jmedchem.5b01499
CHEMBL4598052 183431 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 415 6 1 5 3.6 O=c1n(CCF)c2ccccc2n1[C@H]1CCN(C[C@H]2CCCCC23CC3)C[C@@H]1CO 10.1021/acs.jmedchem.5b01499
16131448 9624 28 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1681 9624 28 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1688 9624 28 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44361543 9624 28 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
56947112 9624 28 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL396460 9624 28 None 1 6 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
16131448 9624 28 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -1 6 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44456296 104496 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 909 31 15 11 -2.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL271478 104496 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 909 31 15 11 -2.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
16131448 9624 28 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None 1 6 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 9624 28 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1681 9624 28 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1688 9624 28 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
44361543 9624 28 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
56947112 9624 28 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL396460 9624 28 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1679 7056 24 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.06.060
9963005 7056 24 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.06.060
CHEMBL437723 7056 24 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmcl.2006.06.060
44416444 168371 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL 1604 53 23 20 -3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2006.06.060
CHEMBL412939 168371 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL 1604 53 23 20 -3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCNC(=O)CCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2006.06.060
1679 7056 24 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
9963005 7056 24 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
CHEMBL437723 7056 24 None 1 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2007.11.043
44143437 185414 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 432 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(CC)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL467533 185414 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 432 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(CC)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
16131448 9624 28 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -1 6 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44143433 185345 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 463 5 1 5 4.6 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N(C)C(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL467057 185345 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 463 5 1 5 4.6 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N(C)C(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
44143433 185345 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 463 5 1 5 4.6 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N(C)C(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467057 185345 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 463 5 1 5 4.6 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N(C)C(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL269029 217554 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
16131448 9624 28 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
45273531 201700 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 348 5 1 4 4.3 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C(C)C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL541511 201700 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 348 5 1 4 4.3 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C(C)C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL504461 220957 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
72548703 168346 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor after 60 mins by scintillation counting analysisDisplacement of [3H]nociceptin from human recombinant NOP receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 168346 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor after 60 mins by scintillation counting analysisDisplacement of [3H]nociceptin from human recombinant NOP receptor after 60 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
44143451 185494 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 449 5 2 5 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](C(=O)NC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468315 185494 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 449 5 2 5 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](C(=O)NC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL505873 220978 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL525604 222436 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
16131448 9624 28 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -1 6 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assayDisplacement of [3H]nociceptin from recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by competitive receptor binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1679 7056 24 None 1 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
9963005 7056 24 None 1 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL437723 7056 24 None 1 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44143456 185374 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 460 5 1 7 5.0 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnco5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467279 185374 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 460 5 1 7 5.0 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnco5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44576628 194506 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 4 2 5 3.6 C[C@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
CHEMBL495402 194506 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 4 2 5 3.6 C[C@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
44143430 196166 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 399 5 1 5 4.8 Cc1ncc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
CHEMBL512975 196166 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 399 5 1 5 4.8 Cc1ncc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cc1F 10.1016/j.bmcl.2009.04.116
CHEMBL504540 220959 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL524339 222383 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL524873 222405 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
24857820 103460 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263918 103460 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
24857820 103460 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL263918 103460 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 396 7 2 5 4.0 CCC(C)(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL389521 219206 0 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in HEK293 cells measured after 60 mins by scintillation counting method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2016.11.014
16131448 9624 28 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
1681 9624 28 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
1688 9624 28 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
44361543 9624 28 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
56947112 9624 28 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
CHEMBL396460 9624 28 None 1 6 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cellsDisplacement of [3H]nociceptin from human recombinant Nociceptin receptor expressed in HEK293 cells
ChEMBL None None None None 10.1016/j.bmc.2016.03.006
118717442 121910 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 953 31 16 12 -1.6 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2014.09.018
CHEMBL3343948 121910 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 953 31 16 12 -1.6 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2014.09.018
9823363 185246 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 418 4 2 5 3.9 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466308 185246 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 418 4 2 5 3.9 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
45273546 202554 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 353 6 1 4 3.5 COCc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL557721 202554 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 353 6 1 4 3.5 COCc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143450 195596 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 475 5 1 5 4.8 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N5CCCC5=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL506207 195596 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 475 5 1 5 4.8 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](N5CCCC5=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
45269358 202970 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 427 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL561397 202970 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 427 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
16131448 9624 28 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
1681 9624 28 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
1688 9624 28 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
44361543 9624 28 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
56947112 9624 28 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
CHEMBL396460 9624 28 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
CHEMBL526352 222461 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
101354795 121911 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 967 31 16 12 -1.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343949 121911 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 967 31 16 12 -1.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
44143455 185239 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nc(C)no5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466252 185239 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nc(C)no5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44456220 162218 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 937 31 15 11 -1.3 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL403807 162218 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 937 31 15 11 -1.3 CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
16131448 9624 28 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
1681 9624 28 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
1688 9624 28 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
44361543 9624 28 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
56947112 9624 28 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
CHEMBL396460 9624 28 None 1 6 Human 8.8 pIC50 = 8.8 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
44450085 103459 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 408 5 2 5 4.1 CC1(Sc2nc3cc(Cl)c(N4CCN(CCO)CC4)cc3[nH]2)CCCCC1 10.1016/j.bmcl.2008.04.054
CHEMBL263917 103459 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 408 5 2 5 4.1 CC1(Sc2nc3cc(Cl)c(N4CCN(CCO)CC4)cc3[nH]2)CCCCC1 10.1016/j.bmcl.2008.04.054
44143457 185375 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnc(C)o5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467280 185375 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 7 5.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnc(C)o5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
16131448 9624 28 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1681 9624 28 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1688 9624 28 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44361543 9624 28 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
56947112 9624 28 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL396460 9624 28 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]isoVa-RYYRIK-NH2 from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44456185 173400 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 951 32 15 11 -0.9 CCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL428076 173400 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 951 32 15 11 -0.9 CCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
44143448 185436 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 449 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467677 185436 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 449 5 2 5 4.3 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(C)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44189735 20795 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197249 20795 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL563980 20795 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
11619553 168499 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 424 6 1 2 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1-c1ccccc1 10.1021/jm0509851
CHEMBL413571 168499 1 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 424 6 1 2 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1-c1ccccc1 10.1021/jm0509851
22272974 103453 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 366 6 1 4 4.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CC)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263903 103453 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 366 6 1 4 4.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CC)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
15982795 78926 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 426 4 0 4 4.4 COC(=O)CN1C(=O)C2(CCN(CC3CCC(C(C)(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL197942 78926 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 426 4 0 4 4.4 COC(=O)CN1C(=O)C2(CCN(CC3CCC(C(C)(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44404679 175213 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 398 4 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL434944 175213 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 398 4 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44406497 142786 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 439 3 2 4 3.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL373170 142786 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 439 3 2 4 3.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2005.09.067
44406604 147399 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 419 3 2 4 3.6 Cc1ccccc1[C@]1(O)CCCC[C@H]1N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2005.09.067
CHEMBL381419 147399 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 419 3 2 4 3.6 Cc1ccccc1[C@]1(O)CCCC[C@H]1N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2005.09.067
44406603 172842 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 423 3 2 4 3.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(F)cc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL425753 172842 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 423 3 2 4 3.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(F)cc1)CC2 10.1016/j.bmcl.2005.09.067
15982659 79074 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 440 5 0 4 4.4 COC(=O)CN1C(=O)C2(CCN(Cc3ccc(-c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL198322 79074 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 440 5 0 4 4.4 COC(=O)CN1C(=O)C2(CCN(Cc3ccc(-c4ccccc4)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44404706 141981 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 378 4 0 4 3.3 COC(=O)CN1C(=O)C2(CCN(C(C)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL372135 141981 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 378 4 0 4 3.3 COC(=O)CN1C(=O)C2(CCN(C(C)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
15983065 142139 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 446 5 0 5 4.5 COC(=O)CN1C(=O)C2(CCN(Cc3ccccc3-c3ccsc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL372779 142139 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 446 5 0 5 4.5 COC(=O)CN1C(=O)C2(CCN(Cc3ccccc3-c3ccsc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
15982796 147671 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 442 12 0 4 5.3 CCCCCCC(CCCC)CN1CCC2(CC1)C(=O)N(CC(=O)OC)c1ccccc12 10.1016/j.bmcl.2005.08.009
CHEMBL382086 147671 0 None - 0 Human 5.0 pIC50 = 5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 442 12 0 4 5.3 CCCCCCC(CCCC)CN1CCC2(CC1)C(=O)N(CC(=O)OC)c1ccccc12 10.1016/j.bmcl.2005.08.009
44406587 79622 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 473 3 2 4 4.6 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(Cl)c(Cl)c1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL200227 79622 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 473 3 2 4 4.6 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(Cl)c(Cl)c1)CC2 10.1016/j.bmcl.2005.09.067
44406503 175429 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 441 3 2 4 3.5 O=C1NCN(c2ccc(F)cc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(F)cc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL436295 175429 0 None - 0 Human 5.0 pIC50 = 5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 441 3 2 4 3.5 O=C1NCN(c2ccc(F)cc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(F)cc1)CC2 10.1016/j.bmcl.2005.09.067
44406543 142037 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 457 3 2 4 4.0 O=C1NCN(c2ccc(F)cc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL372567 142037 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 457 3 2 4 4.0 O=C1NCN(c2ccc(F)cc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2005.09.067
44404711 139791 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 404 3 0 4 3.1 COC(=O)CN1C(=O)C2(CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL370226 139791 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 404 3 0 4 3.1 COC(=O)CN1C(=O)C2(CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44143418 194018 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 401 5 1 5 5.0 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1ccc(Cl)nc1 10.1016/j.bmcl.2009.04.116
CHEMBL492585 194018 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 401 5 1 5 5.0 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1ccc(Cl)nc1 10.1016/j.bmcl.2009.04.116
45271041 203163 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 331 5 1 3 5.1 Cc1nc(CNC2CCCC2)n(C(C)C)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL562663 203163 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 331 5 1 3 5.1 Cc1nc(CNC2CCCC2)n(C(C)C)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL404792 219312 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cellsDisplacement of [3H]NOC from human ORL1 receptor expressed in HEK293 cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCN=C(N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCNC(=O)[C@H](CO)NC(=O)[C@@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2006.06.060
52915518 67351 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 511 13 4 6 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1760025 67351 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 511 13 4 6 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52915270 67709 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 468 10 3 5 5.8 CCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762398 67709 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 468 10 3 5 5.8 CCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
15982938 140296 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 454 4 0 4 5.5 COC(=O)CN1C(=O)C2(CCN(CC3CCCCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL370782 140296 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 454 4 0 4 5.5 COC(=O)CN1C(=O)C2(CCN(CC3CCCCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
52916471 67689 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 930 21 4 10 12.1 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762378 67689 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 930 21 4 10 12.1 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52916266 67723 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 412 6 3 5 4.4 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762412 67723 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 412 6 3 5 4.4 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
11633324 79453 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 392 7 2 3 3.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H](O)Cc1ccccc1 10.1021/jm0509851
CHEMBL199639 79453 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 392 7 2 3 3.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H](O)Cc1ccccc1 10.1021/jm0509851
11619363 81213 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 452 7 1 3 5.0 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1C(=O)c1ccccc1 10.1021/jm0509851
CHEMBL202715 81213 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 452 7 1 3 5.0 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1C(=O)c1ccccc1 10.1021/jm0509851
45273547 202575 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 365 6 1 4 3.7 CC(=O)Cn1nc(CN[C@H]2CC[C@@H](F)C2)c(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL557925 202575 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 365 6 1 4 3.7 CC(=O)Cn1nc(CN[C@H]2CC[C@@H](F)C2)c(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
15982661 140220 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 512 9 2 6 3.0 O=C1N(CC(O)CNCCN2CCOCC2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
CHEMBL370613 140220 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 512 9 2 6 3.0 O=C1N(CC(O)CNCCN2CCOCC2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
44404670 141985 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 416 4 0 2 5.9 O=C1N(Cc2ccccc2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
CHEMBL372184 141985 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 416 4 0 2 5.9 O=C1N(Cc2ccccc2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
22273116 103454 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 354 5 2 5 2.8 CC(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263904 103454 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 354 5 2 5 2.8 CC(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
136043786 84147 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 421 5 1 5 4.4 CN1CCN(c2cccc3[nH]c(-c4nc(CCc5ccc(Cl)cc5)no4)cc23)CC1 10.1016/j.bmcl.2006.03.086
CHEMBL208602 84147 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 421 5 1 5 4.4 CN1CCN(c2cccc3[nH]c(-c4nc(CCc5ccc(Cl)cc5)no4)cc23)CC1 10.1016/j.bmcl.2006.03.086
52915390 67711 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 496 12 3 5 6.6 CCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762400 67711 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 496 12 3 5 6.6 CCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL405948 219366 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
44143422 194304 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 381 5 1 5 4.6 Cc1cncc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)c1 10.1016/j.bmcl.2009.04.116
CHEMBL494406 194304 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 381 5 1 5 4.6 Cc1cncc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)c1 10.1016/j.bmcl.2009.04.116
CHEMBL526142 222452 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
45273662 202629 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 419 5 1 3 6.5 Clc1ccc(-c2cc(CNC3CCCC3)nn2-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL558524 202629 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 419 5 1 3 6.5 Clc1ccc(-c2cc(CNC3CCCC3)nn2-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2009.06.095
44406621 79667 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 405 3 2 4 3.2 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@@]1(O)c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL200371 79667 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 405 3 2 4 3.2 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@@]1(O)c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
44407084 147138 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 477 7 1 5 3.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1COCN1C(=O)OCc1ccccc1 10.1021/jm0509851
CHEMBL380786 147138 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 477 7 1 5 3.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1COCN1C(=O)OCc1ccccc1 10.1021/jm0509851
44404653 148086 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 446 5 0 3 5.9 COc1ccc(CN2C(=O)C3(CCN(CC4CCCCCCC4)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.08.009
CHEMBL383371 148086 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 446 5 0 3 5.9 COc1ccc(CN2C(=O)C3(CCN(CC4CCCCCCC4)CC3)c3ccccc32)cc1 10.1016/j.bmcl.2005.08.009
44406557 79750 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 406 3 2 5 2.6 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1cccnc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL200695 79750 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 406 3 2 5 2.6 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1cccnc1)CC2 10.1016/j.bmcl.2005.09.067
118726267 124013 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 594 11 2 6 5.6 Cc1ccccc1CNC[C@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
CHEMBL3394749 124013 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 594 11 2 6 5.6 Cc1ccccc1CNC[C@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
44456187 102416 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 985 31 15 11 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL257921 102416 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 985 31 15 11 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)c1ccccc1)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44456412 104260 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 30 15 11 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL270231 104260 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 30 15 11 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
15982658 103474 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 432 4 0 4 3.8 COC(=O)CN1C(=O)C2(CCN(Cc3cccc(C(F)(F)F)c3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL264066 103474 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 432 4 0 4 3.8 COC(=O)CN1C(=O)C2(CCN(Cc3cccc(C(F)(F)F)c3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44449771 162429 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 342 4 2 4 3.4 Fc1cc2nc(SCc3ccccc3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL404771 162429 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 342 4 2 4 3.4 Fc1cc2nc(SCc3ccccc3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
136043771 84966 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 366 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3nc(CCC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL210504 84966 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 366 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3nc(CCC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
52915147 67704 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 508 12 2 5 7.3 CCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762393 67704 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 508 12 2 5 7.3 CCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
52915635 67720 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 539 15 4 6 6.3 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762409 67720 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 539 15 4 6 6.3 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52915266 67705 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 522 13 2 5 7.7 CCCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762394 67705 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 522 13 2 5 7.7 CCCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
44450151 102567 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 329 5 2 5 3.1 CCC(CC)Sc1nc2cc(C#N)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL258711 102567 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 329 5 2 5 3.1 CCC(CC)Sc1nc2cc(C#N)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
45270917 201822 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 341 4 1 3 3.8 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL549439 201822 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 341 4 1 3 3.8 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)c(F)c(F)c1 10.1016/j.bmcl.2009.06.051
45270928 202367 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 353 6 2 4 3.1 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCO)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL555354 202367 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 353 6 2 4 3.1 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCO)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
24847114 162165 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1(c3ccccc3)CCCCC1)CC2 10.1016/j.bmcl.2006.05.063
CHEMBL403515 162165 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1(c3ccccc3)CCCCC1)CC2 10.1016/j.bmcl.2006.05.063
44404695 79273 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 354 2 0 2 4.7 Cc1ccc2c(c1)N(C)C(=O)C21CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2005.08.009
CHEMBL199011 79273 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 354 2 0 2 4.7 Cc1ccc2c(c1)N(C)C(=O)C21CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2005.08.009
44143408 185317 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 435 7 1 3 6.9 Cc1c(CNCCC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL466843 185317 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 435 7 1 3 6.9 Cc1c(CNCCC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
44143407 199997 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 421 6 1 3 6.6 Cc1c(CNCC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL523530 199997 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 421 6 1 3 6.6 Cc1c(CNCC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
44406538 79615 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 405 3 2 4 3.2 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL200204 79615 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 405 3 2 4 3.2 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
44406551 140607 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 406 3 2 5 2.6 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccccn1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL371550 140607 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 406 3 2 5 2.6 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1ccccn1)CC2 10.1016/j.bmcl.2005.09.067
18441735 86286 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]NOP from human NOP receptors expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptors expressed in HEK293 cells
ChEMBL 405 3 2 4 3.2 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1(O)c1ccccc1)CC2 10.1016/j.bmcl.2006.05.058
CHEMBL211373 86286 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Displacement of [3H]NOP from human NOP receptors expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptors expressed in HEK293 cells
ChEMBL 405 3 2 4 3.2 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1(O)c1ccccc1)CC2 10.1016/j.bmcl.2006.05.058
52915637 67722 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 567 17 4 6 7.1 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762411 67722 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 567 17 4 6 7.1 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52915267 67706 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 536 14 2 5 8.1 CCCCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762395 67706 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 536 14 2 5 8.1 CCCCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
52915515 67716 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 469 10 4 6 4.4 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762405 67716 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 469 10 4 6 4.4 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44574053 185401 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 451 5 2 6 4.1 CCN1CCN(c2cc3[nH]c(SC4(C)CCC(NC(=O)OC)C4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467473 185401 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 451 5 2 6 4.1 CCN1CCN(c2cc3[nH]c(SC4(C)CCC(NC(=O)OC)C4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44456299 104255 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 31 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL270216 104255 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 31 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
118726265 124011 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 586 11 2 7 5.3 O=C1N(C[C@@H](O)CNCc2cccs2)CN(c2ccccc2)C12CCN(CCc1ccccc1-c1cccs1)CC2 10.1016/j.bmcl.2014.12.015
CHEMBL3394747 124011 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 586 11 2 7 5.3 O=C1N(C[C@@H](O)CNCc2cccs2)CN(c2ccccc2)C12CCN(CCc1ccccc1-c1cccs1)CC2 10.1016/j.bmcl.2014.12.015
45271902 202305 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 465 7 1 3 7.2 FCCn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL554058 202305 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 465 7 1 3 7.2 FCCn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
45269372 203440 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 489 8 1 3 8.6 CCC(CC)n1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL564484 203440 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 489 8 1 3 8.6 CCC(CC)n1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
45268503 203481 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 447 6 1 3 7.2 CCn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL564837 203481 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 447 6 1 3 7.2 CCn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
118726264 124010 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 636 14 1 6 6.8 CCCCN(Cc1ccccc1)C[C@@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
CHEMBL3394746 124010 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 636 14 1 6 6.8 CCCCN(Cc1ccccc1)C[C@@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
22272877 102671 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL259185 102671 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
22272900 103449 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 348 4 2 4 3.8 Fc1cc2nc(SCC3CCCCC3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL263889 103449 1 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 348 4 2 4 3.8 Fc1cc2nc(SCC3CCCCC3)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
45268356 203317 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 339 4 1 3 4.2 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(Cl)c1 10.1016/j.bmcl.2009.06.051
CHEMBL563686 203317 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 339 4 1 3 4.2 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(Cl)c1 10.1016/j.bmcl.2009.06.051
22272877 102671 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL259185 102671 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 368 4 2 5 3.2 CC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
44407070 80704 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 394 7 1 3 4.3 O=C(CSc1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL202059 80704 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 394 7 1 3 4.3 O=C(CSc1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
118726273 124020 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 649 11 2 6 5.3 Cc1ccc(CN(C[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)C(=O)[C@H](N)C(C)C)cc1 10.1016/j.bmcl.2014.12.015
CHEMBL3394756 124020 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 649 11 2 6 5.3 Cc1ccc(CN(C[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)C(=O)[C@H](N)C(C)C)cc1 10.1016/j.bmcl.2014.12.015
44576627 200021 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 394 7 2 5 3.8 CCC(CC)Sc1nc2cc(Cl)c(N3C[C@@H]4C[C@H]3CN4CCO)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL523724 200021 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 394 7 2 5 3.8 CCC(CC)Sc1nc2cc(Cl)c(N3C[C@@H]4C[C@H]3CN4CCO)cc2[nH]1 10.1016/j.bmcl.2008.04.037
44404731 142819 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 412 5 0 4 4.3 CC(=O)OCCN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL373190 142819 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 412 5 0 4 4.3 CC(=O)OCCN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44449767 102797 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 356 4 2 4 3.7 Cc1cccc(CSc2nc3cc(F)c(N4CCNCC4)cc3[nH]2)c1 10.1016/j.bmcl.2008.04.054
CHEMBL259764 102797 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 356 4 2 4 3.7 Cc1cccc(CSc2nc3cc(F)c(N4CCNCC4)cc3[nH]2)c1 10.1016/j.bmcl.2008.04.054
52915268 67707 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 550 15 2 5 8.5 CCCCCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762396 67707 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 550 15 2 5 8.5 CCCCCCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
52915145 67702 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 480 10 2 5 6.6 CCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762391 67702 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 480 10 2 5 6.6 CCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
10004950 16821 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 470 5 1 6 2.5 CNC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cc4c(cc3Cl)OCO4)CC2)C1=O 10.1021/jm010878g
CHEMBL115222 16821 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 470 5 1 6 2.5 CNC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cc4c(cc3Cl)OCO4)CC2)C1=O 10.1021/jm010878g
45271885 203403 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 459 6 1 3 7.5 Clc1ccc(-c2c(-c3ccc(Cl)cc3Cl)nc(CNC3CCCC3)n2C2CC2)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL564225 203403 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 459 6 1 3 7.5 Clc1ccc(-c2c(-c3ccc(Cl)cc3Cl)nc(CNC3CCCC3)n2C2CC2)cc1 10.1016/j.bmcl.2009.06.095
44342270 16702 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
CHEMBL114484 16702 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 355 3 1 4 4.5 Cc1ccc(CN2CCC(n3c(O)nc4ccccc43)CC2)c(Cl)c1 10.1021/jm010878g
44143435 185221 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 441 5 2 6 3.5 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2C)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466112 185221 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 441 5 2 6 3.5 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2C)CC1 10.1016/j.bmcl.2009.04.023
45270907 202538 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 334 5 1 4 3.7 CCn1nc(CN[C@H]2CC[C@@H](F)C2)c(C)c1-c1cnc(C)c(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL557623 202538 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 334 5 1 4 3.7 CCn1nc(CN[C@H]2CC[C@@H](F)C2)c(C)c1-c1cnc(C)c(F)c1 10.1016/j.bmcl.2009.06.051
22273044 102566 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 338 5 2 4 3.9 CCC(CC)Sc1nc2cc(Cl)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL258710 102566 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 338 5 2 4 3.9 CCC(CC)Sc1nc2cc(Cl)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44143449 185370 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 485 6 2 6 3.7 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NS(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL467266 185370 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 485 6 2 6 3.7 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NS(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL510117 222360 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
CHEMBL510117 222360 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assayDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells by competitive binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.06.015
16131448 9624 28 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
1681 9624 28 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
1688 9624 28 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
44361543 9624 28 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
56947112 9624 28 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
CHEMBL396460 9624 28 None 1 6 Human 8.7 pIC50 = 8.7 Binding
Inhibition of human ORL1 receptorInhibition of human ORL1 receptor
ChEMBL None None None None 10.1021/jm701575k
24882570 121909 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]isoVa-RYYRIK-NH2 from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]isoVa-RYYRIK-NH2 from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343946 121909 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]isoVa-RYYRIK-NH2 from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]isoVa-RYYRIK-NH2 from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343947 121909 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [3H]isoVa-RYYRIK-NH2 from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]isoVa-RYYRIK-NH2 from human ORL1 receptor expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
44143453 185260 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnn(C)n5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466448 185260 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnn(C)n5)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL455289 220781 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cellsDisplacement of [3H]nociceptin from rat ORL1 receptor expressed in african green monkey COS7 cells
ChEMBL None None None None 10.1016/j.bmc.2008.09.014
1691 8888 23 None - 1 Human 8.6 pIC50 = 8.6 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
5311194 8888 23 None - 1 Human 8.6 pIC50 = 8.6 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
CHEMBL357076 8888 23 None - 1 Human 8.6 pIC50 = 8.6 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm990517p
1691 8888 23 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm900581g
5311194 8888 23 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm900581g
CHEMBL357076 8888 23 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm900581g
44189834 20794 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.8 O=c1n(C(CO)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197240 20794 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.8 O=c1n(C(CO)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL563657 20794 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.8 O=c1n(C(CO)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
44189733 20802 4 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL1197275 20802 4 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
CHEMBL564840 20802 4 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 425 6 2 6 2.6 O=c1n(C[C@@H](O)CO)c2ccccc2n1C1CCN(C[C@H]2[C@H]3CC[C@H](C3)C23CC3)CC1 10.1021/jm900581g
1691 8888 23 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
5311194 8888 23 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
CHEMBL357076 8888 23 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm0509851
44143432 185489 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL468302 185489 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
44143432 185489 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468302 185489 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44143428 185492 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL468308 185492 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
24857819 194296 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
24857819 194296 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL494350 194296 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2008.04.037
CHEMBL494350 194296 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 4 2 5 3.6 C[C@@H]1CN(CCO)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
44456140 175493 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 951 31 15 11 -1.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL436852 175493 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 951 31 15 11 -1.1 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44450086 165074 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 394 5 2 5 3.8 OCCN1CCN(c2cc3[nH]c(SC4CCCCC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2008.04.054
CHEMBL408901 165074 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 394 5 2 5 3.8 OCCN1CCN(c2cc3[nH]c(SC4CCCCC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2008.04.054
416359 108637 21 None - 0 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]-Tyr14 at nociceptin (NOP) receptorAbility to displace [125I]-Tyr14 at nociceptin (NOP) receptor
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2003.09.068
CHEMBL300616 108637 21 None - 0 Human 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]-Tyr14 at nociceptin (NOP) receptorAbility to displace [125I]-Tyr14 at nociceptin (NOP) receptor
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2003.09.068
416359 108637 21 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1021/jm990517p
CHEMBL300616 108637 21 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 307 3 1 4 3.6 Oc1nc2ccccc2n1C1CCN(Cc2ccccc2)CC1 10.1021/jm990517p
45267616 203066 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 432 5 1 2 7.4 Cc1c(CNC2CCCC2)cc(-c2ccc(Cl)cc2Cl)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL562077 203066 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 432 5 1 2 7.4 Cc1c(CNC2CCCC2)cc(-c2ccc(Cl)cc2Cl)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
52915517 67718 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 497 12 4 6 5.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762407 67718 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 497 12 4 6 5.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52916174 67724 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 411 6 2 5 4.8 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(C=O)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762413 67724 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 411 6 2 5 4.8 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(C=O)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52915146 67703 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 494 11 2 5 7.0 CCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762392 67703 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 494 11 2 5 7.0 CCCCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
44407116 80977 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 438 7 1 2 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Cc1ccccc1 10.1021/jm0509851
CHEMBL202322 80977 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 438 7 1 2 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Cc1ccccc1 10.1021/jm0509851
44143445 185234 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 439 7 2 6 4.0 CCN1CCN(c2cc3[nH]c(SC(C)(C)CCNC(=O)OC)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466221 185234 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 439 7 2 6 4.0 CCN1CCN(c2cc3[nH]c(SC(C)(C)CCNC(=O)OC)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44455999 104287 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 32 15 11 -0.7 CCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL270394 104287 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 32 15 11 -0.7 CCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
44456339 175672 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 34 15 11 -0.1 CCCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL438383 175672 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 34 15 11 -0.1 CCCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
45269228 202710 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 373 4 1 3 4.5 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL559402 202710 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 373 4 1 3 4.5 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(C(F)(F)F)c1 10.1016/j.bmcl.2009.06.051
136043790 84836 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 408 8 1 4 5.2 CN(C)CCCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL210000 84836 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 408 8 1 4 5.2 CN(C)CCCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
52915636 67721 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 553 16 4 6 6.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762410 67721 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 553 16 4 6 6.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL444110 220707 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44143444 185206 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 352 3 1 4 4.2 CCN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466020 185206 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 352 3 1 4 4.2 CCN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
579 9918 18 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to ORL1 receptorBinding affinity to ORL1 receptor
ChEMBL None None None None 10.1016/j.bmcl.2006.07.036
6918468 9918 18 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to ORL1 receptorBinding affinity to ORL1 receptor
ChEMBL None None None None 10.1016/j.bmcl.2006.07.036
CHEMBL41547 9918 18 None - 0 Human 5.7 pIC50 = 5.7 Binding
Binding affinity to ORL1 receptorBinding affinity to ORL1 receptor
ChEMBL None None None None 10.1016/j.bmcl.2006.07.036
11710187 78855 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 358 2 0 2 4.5 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2cc(F)ccc21 10.1016/j.bmcl.2005.08.009
CHEMBL197727 78855 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 358 2 0 2 4.5 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2cc(F)ccc21 10.1016/j.bmcl.2005.08.009
44450209 102992 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 376 4 2 4 4.1 Fc1cc2nc(SCc3ccccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL260821 102992 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 376 4 2 4 4.1 Fc1cc2nc(SCc3ccccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
44143439 179529 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 402 4 1 4 4.9 C[C@@H]1CN(CC(F)F)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL450887 179529 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 402 4 1 4 4.9 C[C@@H]1CN(CC(F)F)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
44407085 80820 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 439 7 2 3 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Nc1ccccc1 10.1021/jm0509851
CHEMBL202220 80820 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 439 7 2 3 5.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Nc1ccccc1 10.1021/jm0509851
136043796 85795 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 374 7 1 4 4.4 Cc1ccc(CCc2noc(-c3cc4c(CCN(C)C)cccc4[nH]3)n2)cc1 10.1016/j.bmcl.2006.03.086
CHEMBL211310 85795 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 374 7 1 4 4.4 Cc1ccc(CCc2noc(-c3cc4c(CCN(C)C)cccc4[nH]3)n2)cc1 10.1016/j.bmcl.2006.03.086
44407133 81176 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 447 7 1 4 3.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1COC(=O)N1Cc1ccccc1 10.1021/jm0509851
CHEMBL202492 81176 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 447 7 1 4 3.5 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1COC(=O)N1Cc1ccccc1 10.1021/jm0509851
44450180 163542 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 442 4 2 5 3.4 O=S(=O)(Cc1cccc(Cl)c1Cl)c1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL407068 163542 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 442 4 2 5 3.4 O=S(=O)(Cc1cccc(Cl)c1Cl)c1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44404684 147407 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 370 3 0 3 4.4 COc1ccc2c(c1)N(C)C(=O)C21CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2005.08.009
CHEMBL381429 147407 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 370 3 0 3 4.4 COc1ccc2c(c1)N(C)C(=O)C21CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2005.08.009
11811722 16837 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 413 5 1 4 4.4 O=C1NCN(c2ccccc2)C12CCN(Cc1cccc(Oc3ccccc3)c1)CC2 10.1021/jm010878g
CHEMBL115280 16837 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 413 5 1 4 4.4 O=C1NCN(c2ccccc2)C12CCN(Cc1cccc(Oc3ccccc3)c1)CC2 10.1021/jm010878g
52915634 67719 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 525 14 4 6 6.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762408 67719 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 525 14 4 6 6.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
11411841 67682 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 835 16 0 6 10.4 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)N(CCCCCCCCCN2CN(c4ccccc4)C4(CCN([C@H]5CC[C@@H](C(C)C)CC5)CC4)C2=O)CN3c2ccccc2)CC1 10.1016/j.ejmech.2011.01.040
CHEMBL1762371 67682 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 835 16 0 6 10.4 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)N(CCCCCCCCCN2CN(c4ccccc4)C4(CCN([C@H]5CC[C@@H](C(C)C)CC5)CC4)C2=O)CN3c2ccccc2)CC1 10.1016/j.ejmech.2011.01.040
15982935 177053 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 414 4 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(Cc3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL444620 177053 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 414 4 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(Cc3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
118726268 124014 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 594 11 2 6 5.6 Cc1ccccc1CNC[C@@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
CHEMBL3394750 124014 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 594 11 2 6 5.6 Cc1ccccc1CNC[C@@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
45271015 202317 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 381 5 1 5 4.6 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CNC3CCCC3)c2C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL554299 202317 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 381 5 1 5 4.6 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CNC3CCCC3)c2C)cn1 10.1016/j.bmcl.2009.06.095
44404689 175097 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 356 2 1 3 4.1 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccc(O)cc21 10.1016/j.bmcl.2005.08.009
CHEMBL434179 175097 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 356 2 1 3 4.1 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccc(O)cc21 10.1016/j.bmcl.2005.08.009
9823363 196032 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 418 4 2 5 3.9 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL511742 196032 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 418 4 2 5 3.9 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@](C)(O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
44143442 185281 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 391 4 1 5 4.5 C[C@@H]1CN(CCC#N)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL466630 185281 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 391 4 1 5 4.5 C[C@@H]1CN(CCC#N)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
44143421 194279 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 435 5 1 5 5.3 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1ccc(C(F)(F)F)nc1 10.1016/j.bmcl.2009.04.116
CHEMBL494231 194279 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 435 5 1 5 5.3 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1ccc(C(F)(F)F)nc1 10.1016/j.bmcl.2009.04.116
CHEMBL268145 217519 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CS)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
15983067 79305 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 384 4 0 3 4.8 CCN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccc(OC)cc21 10.1016/j.bmcl.2005.08.009
CHEMBL199095 79305 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 384 4 0 3 4.8 CCN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccc(OC)cc21 10.1016/j.bmcl.2005.08.009
44143413 196150 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 433 5 1 3 6.8 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL512827 196150 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 433 5 1 3 6.8 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
44143413 196150 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.8 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL512827 196150 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.8 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
45267601 202877 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.8 Cc1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL560875 202877 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.8 Cc1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)n1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
52915031 67698 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 949 24 6 10 11.8 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762387 67698 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 949 24 6 10 11.8 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
10949380 170802 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 399 3 1 6 4.3 Cc1ccc2nc(O)n(C3CCN(Cc4cc5c(cc4Cl)OCO5)CC3)c2c1 10.1021/jm010878g
CHEMBL420863 170802 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 399 3 1 6 4.3 Cc1ccc2nc(O)n(C3CCN(Cc4cc5c(cc4Cl)OCO5)CC3)c2c1 10.1021/jm010878g
44404646 147074 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 370 4 1 3 3.7 O=C1N(CCO)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
CHEMBL380603 147074 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 370 4 1 3 3.7 O=C1N(CCO)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
44407086 80446 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 451 7 1 5 4.9 O=C(CSc1nc2ccccc2s1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL201826 80446 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 451 7 1 5 4.9 O=C(CSc1nc2ccccc2s1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
44449793 164438 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 266 2 2 4 1.8 CSc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL408148 164438 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 266 2 2 4 1.8 CSc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44450207 166232 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 426 4 2 4 3.7 [O-][S+](Cc1cccc(Cl)c1Cl)c1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL410124 166232 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 426 4 2 4 3.7 [O-][S+](Cc1cccc(Cl)c1Cl)c1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL442113 220686 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)[C@H](CS)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
CHEMBL435511 220446 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
45273537 203207 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL562932 203207 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
45268498 203480 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 413 6 1 5 4.8 CCc1c(CN[C@H]2CC[C@@H](F)C2)nc(-c2ncccc2Cl)n1-c1ccc(C)nc1 10.1016/j.bmcl.2009.06.095
CHEMBL564812 203480 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 413 6 1 5 4.8 CCc1c(CN[C@H]2CC[C@@H](F)C2)nc(-c2ncccc2Cl)n1-c1ccc(C)nc1 10.1016/j.bmcl.2009.06.095
44456141 102129 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 1043 31 15 11 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL256687 102129 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 1043 31 15 11 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
118726269 124015 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 654 14 2 8 5.3 COc1ccc(CCNC[C@@H](O)CN2CN(c3ccccc3)C3(CCN(CCc4ccccc4-c4cccs4)CC3)C2=O)cc1OC 10.1016/j.bmcl.2014.12.015
CHEMBL3394751 124015 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 654 14 2 8 5.3 COc1ccc(CCNC[C@@H](O)CN2CN(c3ccccc3)C3(CCN(CCc4ccccc4-c4cccs4)CC3)C2=O)cc1OC 10.1016/j.bmcl.2014.12.015
44407044 147355 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 447 7 2 4 3.2 O=C1N[C@@H](Cc2ccccc2)[C@@H](C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)O1 10.1021/jm0509851
CHEMBL381287 147355 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 447 7 2 4 3.2 O=C1N[C@@H](Cc2ccccc2)[C@@H](C(=O)NCCCN2CCC3(CCc4ccccc43)CC2)O1 10.1021/jm0509851
1692 8935 29 None 12 4 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1016/j.ejmech.2011.01.040
5311340 8935 29 None 12 4 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1016/j.ejmech.2011.01.040
CHEMBL140979 8935 29 None 12 4 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1016/j.ejmech.2011.01.040
52916714 67696 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 920 22 6 10 11.1 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762385 67696 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 920 22 6 10 11.1 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44406618 140377 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
CHEMBL371267 140377 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
52915393 67714 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 538 15 3 5 7.8 CCCCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762403 67714 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 538 15 3 5 7.8 CCCCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
52915144 67701 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 466 9 2 5 6.2 CCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762390 67701 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 466 9 2 5 6.2 CCCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
44449764 164031 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 356 4 2 4 3.7 Cc1ccc(CSc2nc3cc(F)c(N4CCNCC4)cc3[nH]2)cc1 10.1016/j.bmcl.2008.04.054
CHEMBL407653 164031 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 356 4 2 4 3.7 Cc1ccc(CSc2nc3cc(F)c(N4CCNCC4)cc3[nH]2)cc1 10.1016/j.bmcl.2008.04.054
52915030 67697 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 934 23 6 10 11.4 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762386 67697 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 934 23 6 10 11.4 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44406618 140377 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL371267 140377 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
22273255 164302 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 346 6 2 5 3.5 CCC(CC)Sc1nc2cc(C(C)=O)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL407991 164302 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 346 6 2 5 3.5 CCC(CC)Sc1nc2cc(C(C)=O)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
11544654 77044 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 340 2 0 2 4.4 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL194200 77044 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 340 2 0 2 4.4 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
52915032 67699 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 963 25 6 10 12.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762388 67699 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 963 25 6 10 12.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
15982791 79149 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 531 9 1 4 5.9 CCN(Cc1ccc(C)cc1)CC(O)CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL198604 79149 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 531 9 1 4 5.9 CCN(Cc1ccc(C)cc1)CC(O)CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
17858339 103448 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 304 5 2 4 3.3 CCC(CC)Sc1nc2ccc(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263888 103448 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 304 5 2 4 3.3 CCC(CC)Sc1nc2ccc(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
45267506 202841 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 415 7 1 5 3.2 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCS(C)(=O)=O)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL560469 202841 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 415 7 1 5 3.2 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCS(C)(=O)=O)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143423 194308 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 361 5 1 5 4.3 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2C)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL494413 194308 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 361 5 1 5 4.3 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2C)cn1 10.1016/j.bmcl.2009.04.116
45268504 202890 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 461 6 1 3 7.8 CC(C)n1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL560937 202890 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 461 6 1 3 7.8 CC(C)n1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
44407140 81190 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 415 6 2 3 3.8 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)C(=O)c1c[nH]c2ccccc12 10.1021/jm0509851
CHEMBL202604 81190 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 415 6 2 3 3.8 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)C(=O)c1c[nH]c2ccccc12 10.1021/jm0509851
23542099 124006 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 592 12 1 5 6.3 CCCCN(Cc1ccccc1)C[C@H](O)CN1CN(c2ccc(F)cc2)C2(CCN(CC3CCCCCCC3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
CHEMBL3394742 124006 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 592 12 1 5 6.3 CCCCN(Cc1ccccc1)C[C@H](O)CN1CN(c2ccc(F)cc2)C2(CCN(CC3CCCCCCC3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
44407112 80713 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 454 8 1 3 5.5 O=C(Cc1cccc(Oc2ccccc2)c1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL202091 80713 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 454 8 1 3 5.5 O=C(Cc1cccc(Oc2ccccc2)c1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
10948527 118132 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 365 3 1 5 2.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3c(c1)OCO3)CC2 10.1021/jm010878g
CHEMBL326962 118132 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 365 3 1 5 2.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3c(c1)OCO3)CC2 10.1021/jm010878g
52916358 67685 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 874 17 4 10 10.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762374 67685 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 874 17 4 10 10.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44404721 78968 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 426 3 0 4 4.0 COC(=O)CN1C(=O)C2(CCN(c3ccc4c5c(cccc35)CC4)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL198046 78968 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 426 3 0 4 4.0 COC(=O)CN1C(=O)C2(CCN(c3ccc4c5c(cccc35)CC4)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
11523972 172943 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 390 8 1 2 4.5 O=C(CCCc1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL426303 172943 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 390 8 1 2 4.5 O=C(CCCc1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
44143406 194278 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 407 5 1 3 6.3 Cc1c(CNC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL494230 194278 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 407 5 1 3 6.3 Cc1c(CNC(C)C)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
44143424 199505 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 415 5 1 5 5.0 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2C(F)(F)F)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL522021 199505 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 415 5 1 5 5.0 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2C(F)(F)F)cn1 10.1016/j.bmcl.2009.04.116
44407048 80714 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 415 7 2 2 4.6 O=C(CCc1c[nH]c2ccccc12)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL202094 80714 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 415 7 2 2 4.6 O=C(CCc1c[nH]c2ccccc12)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
15983063 148119 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 328 4 0 4 2.0 COC(=O)CN1C(=O)C2(CCN(CC3CC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL383561 148119 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 328 4 0 4 2.0 COC(=O)CN1C(=O)C2(CCN(CC3CC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44404699 175569 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 354 2 0 2 4.7 Cc1cccc2c1C1(CCN(CC3CCCCCCC3)CC1)C(=O)N2C 10.1016/j.bmcl.2005.08.009
CHEMBL437505 175569 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 354 2 0 2 4.7 Cc1cccc2c1C1(CCN(CC3CCCCCCC3)CC1)C(=O)N2C 10.1016/j.bmcl.2005.08.009
118726272 124018 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 553 8 1 5 6.1 Cc1cccc(SC[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)c1 10.1016/j.bmcl.2014.12.015
CHEMBL3394754 124018 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 553 8 1 5 6.1 Cc1cccc(SC[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)c1 10.1016/j.bmcl.2014.12.015
44143415 185565 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 400 5 1 4 5.6 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1cccnc1 10.1016/j.bmcl.2009.04.116
CHEMBL468937 185565 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 400 5 1 4 5.6 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1cccnc1 10.1016/j.bmcl.2009.04.116
CHEMBL384866 219118 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CS)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CS)C(N)=O 10.1021/jm010092i
11406629 148116 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
CHEMBL383539 148116 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
44574003 185282 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 394 4 1 5 4.2 CC(=O)CN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)C(C)C1 10.1016/j.bmcl.2009.04.022
CHEMBL466631 185282 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 394 4 1 5 4.2 CC(=O)CN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)C(C)C1 10.1016/j.bmcl.2009.04.022
10937901 16682 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 385 3 1 6 4.0 Oc1nc2ccccc2n1C1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1021/jm010878g
CHEMBL114379 16682 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 385 3 1 6 4.0 Oc1nc2ccccc2n1C1CCN(Cc2cc3c(cc2Cl)OCO3)CC1 10.1021/jm010878g
44404652 79351 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 326 2 1 2 4.3 O=C1Nc2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
CHEMBL199248 79351 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 326 2 1 2 4.3 O=C1Nc2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
44406540 79785 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 439 3 2 4 3.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL200882 79785 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 439 3 2 4 3.9 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCC[C@@]1(O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL406010 219370 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@@H]1NC(=O)CNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](N)CSSC[C@@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
44143419 194384 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 381 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL494767 194384 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 381 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
118726262 124008 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 610 12 2 7 5.3 COc1ccc(CNC[C@@H](O)CN2CN(c3ccccc3)C3(CCN(CCc4ccccc4-c4cccs4)CC3)C2=O)cc1 10.1016/j.bmcl.2014.12.015
CHEMBL3394744 124008 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 610 12 2 7 5.3 COc1ccc(CNC[C@@H](O)CN2CN(c3ccccc3)C3(CCN(CCc4ccccc4-c4cccs4)CC3)C2=O)cc1 10.1016/j.bmcl.2014.12.015
45268355 203019 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 320 4 1 4 3.2 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL561732 203019 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 320 4 1 4 3.2 Cc1ncc(-c2c(C)c(CN[C@H]3CC[C@@H](F)C3)nn2C)cc1F 10.1016/j.bmcl.2009.06.051
44143446 185235 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 465 5 1 6 4.5 CCOC(=O)N1CCC(C)(Sc2nc3cc(Cl)c(N4CCN(CC)CC4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL466222 185235 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 465 5 1 6 4.5 CCOC(=O)N1CCC(C)(Sc2nc3cc(Cl)c(N4CCN(CC)CC4)cc3[nH]2)CC1 10.1016/j.bmcl.2009.04.022
10763594 168056 1 None 120 4 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1016/j.ejmech.2011.01.040
CHEMBL412098 168056 1 None 120 4 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1016/j.ejmech.2011.01.040
17858448 102733 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 322 5 2 4 3.4 CCC(CC)Sc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL259452 102733 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 322 5 2 4 3.4 CCC(CC)Sc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
45269357 202969 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 409 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CNC3CCCC3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL561396 202969 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 409 6 1 5 5.4 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CNC3CCCC3)c2C(C)C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL424934 220106 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@@H]1NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)CSSC[C@@H](C(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm010092i
135458466 86297 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 422 5 1 6 3.8 CN1CCN(c2[nH]ccc3nc(-c4nc(CCc5ccc(Cl)cc5)no4)cc2-3)CC1 10.1016/j.bmcl.2006.03.086
CHEMBL211390 86297 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 422 5 1 6 3.8 CN1CCN(c2[nH]ccc3nc(-c4nc(CCc5ccc(Cl)cc5)no4)cc2-3)CC1 10.1016/j.bmcl.2006.03.086
118726270 124016 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 546 9 2 6 4.8 CC(C)(C)NC[C@@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
CHEMBL3394752 124016 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 546 9 2 6 4.8 CC(C)(C)NC[C@@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
44406719 172875 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 423 3 1 3 4.8 O=C1NCN(c2ccc(Cl)cc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
CHEMBL425929 172875 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 423 3 1 3 4.8 O=C1NCN(c2ccc(Cl)cc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
52915514 67715 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 552 16 3 5 8.2 CCCCCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762404 67715 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 552 16 3 5 8.2 CCCCCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
136043824 86706 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 396 7 1 5 4.6 CN(C)CCc1cccc2[nH]c(-c3nc(COc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL212520 86706 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 396 7 1 5 4.6 CN(C)CCc1cccc2[nH]c(-c3nc(COc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
10905740 117447 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 413 3 1 6 2.9 O=c1[nH]c2ccccc2n(C2CCN(Cc3cc4c(cc3Cl)OCO4)CC2)c1=O 10.1021/jm010878g
CHEMBL325945 117447 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 413 3 1 6 2.9 O=c1[nH]c2ccccc2n(C2CCN(Cc3cc4c(cc3Cl)OCO4)CC2)c1=O 10.1021/jm010878g
136043756 85158 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 378 7 1 4 4.7 CN(C)CCc1cccc2[nH]c(-c3nc(CCC4CC5CCC4C5)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL211053 85158 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 378 7 1 4 4.7 CN(C)CCc1cccc2[nH]c(-c3nc(CCC4CC5CCC4C5)no3)cc12 10.1016/j.bmcl.2006.03.086
136043767 86507 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 352 6 1 4 4.4 CN(C)CCc1cccc2[nH]c(-c3nc(CC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL211617 86507 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 352 6 1 4 4.4 CN(C)CCc1cccc2[nH]c(-c3nc(CC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
44456216 162179 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 32 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)CC)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL403588 162179 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 32 15 11 -0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)CC)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44404698 139519 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 354 2 0 2 4.7 Cc1ccc2c(c1)C1(CCN(CC3CCCCCCC3)CC1)C(=O)N2C 10.1016/j.bmcl.2005.08.009
CHEMBL369945 139519 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 354 2 0 2 4.7 Cc1ccc2c(c1)C1(CCN(CC3CCCCCCC3)CC1)C(=O)N2C 10.1016/j.bmcl.2005.08.009
136043795 84859 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 378 7 1 4 4.2 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(F)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL210140 84859 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 378 7 1 4 4.2 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(F)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
136043817 86615 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 380 6 1 4 4.6 CN(C)CCc1cccc2[nH]c(-c3nc(Cc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL212161 86615 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 380 6 1 4 4.6 CN(C)CCc1cccc2[nH]c(-c3nc(Cc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
11525624 140317 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
CHEMBL370870 140317 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 431 7 1 3 4.1 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@@H]1CCCN1Cc1ccccc1 10.1021/jm0509851
44456298 175582 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 33 15 11 -0.3 CCCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL437601 175582 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 33 15 11 -0.3 CCCC(C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
44404694 79172 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 414 4 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(Cc3cccc4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL198678 79172 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 414 4 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(Cc3cccc4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
52916267 67684 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 860 16 4 10 10.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762373 67684 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 860 16 4 10 10.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52915392 67713 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 524 14 3 5 7.4 CCCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762402 67713 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 524 14 3 5 7.4 CCCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
136043800 84565 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 428 7 1 4 5.1 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(C(F)(F)F)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL209213 84565 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 428 7 1 4 5.1 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(C(F)(F)F)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
155533462 178612 0 None 15 2 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 2.5 hrs by GTPgamma(35)S binding assayAntagonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 2.5 hrs by GTPgamma(35)S binding assay
ChEMBL 385 4 1 5 3.8 CCn1c(=O)n([C@@H]2CCN(C3CCCCCCC3)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.5b01499
CHEMBL4468676 178612 0 None 15 2 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 2.5 hrs by GTPgamma(35)S binding assayAntagonist activity at human nociceptin opioid receptor expressed in CHO cell membranes after 2.5 hrs by GTPgamma(35)S binding assay
ChEMBL 385 4 1 5 3.8 CCn1c(=O)n([C@@H]2CCN(C3CCCCCCC3)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.5b01499
11191683 67683 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 524 13 0 4 6.6 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)N(CCCCCCCCCN(C)C)CN3c2ccccc2)CC1 10.1016/j.ejmech.2011.01.040
CHEMBL1762372 67683 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 524 13 0 4 6.6 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)N(CCCCCCCCCN(C)C)CN3c2ccccc2)CC1 10.1016/j.ejmech.2011.01.040
10199945 103461 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 382 6 2 5 3.6 CCC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL263919 103461 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 382 6 2 5 3.6 CCC(C)(C)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
44456101 104610 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 33 15 11 -0.5 CCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL272084 104610 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 33 15 11 -0.5 CCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
44143434 185295 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 461 5 2 6 3.8 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466702 185295 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 461 5 2 6 3.8 CCN1CCN(c2cc3[nH]c(C(=O)[C@]4(C)CC[C@@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
10832076 44825 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 355 3 1 4 4.8 CC(c1ccccc1Cl)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm990517p
CHEMBL146054 44825 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 355 3 1 4 4.8 CC(c1ccccc1Cl)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm990517p
44407129 80803 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 445 7 1 3 3.7 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1CCC(=O)N1Cc1ccccc1 10.1021/jm0509851
CHEMBL202204 80803 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 445 7 1 3 3.7 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)[C@H]1CCC(=O)N1Cc1ccccc1 10.1021/jm0509851
52916359 67686 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 888 18 4 10 10.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762375 67686 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 888 18 4 10 10.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
45270203 203229 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 483 7 1 3 7.5 FC(F)Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL563073 203229 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 483 7 1 3 7.5 FC(F)Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
15982524 173061 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 384 4 0 4 3.5 COC(=O)CN1C(=O)C2(CCN(CC3CCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL427010 173061 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 384 4 0 4 3.5 COC(=O)CN1C(=O)C2(CCN(CC3CCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
45271862 201908 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.7 Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL550117 201908 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.7 Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
44143414 185564 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 400 5 1 4 5.6 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccccn1 10.1016/j.bmcl.2009.04.116
CHEMBL468936 185564 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 400 5 1 4 5.6 Cc1c(CNC2CCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccccn1 10.1016/j.bmcl.2009.04.116
45270196 202174 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 473 6 1 3 7.9 Clc1ccc(-c2c(-c3ccc(Cl)cc3Cl)nc(CNC3CCCC3)n2C2CCC2)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL552011 202174 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 473 6 1 3 7.9 Clc1ccc(-c2c(-c3ccc(Cl)cc3Cl)nc(CNC3CCCC3)n2C2CCC2)cc1 10.1016/j.bmcl.2009.06.095
11559820 172750 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 374 6 1 2 4.2 O=C(/C=C/c1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL425225 172750 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 374 6 1 2 4.2 O=C(/C=C/c1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
45270202 202230 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 475 7 1 3 7.9 CC(C)Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL552417 202230 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 475 7 1 3 7.9 CC(C)Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
44450210 102993 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3c(Cl)cccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL260822 102993 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3c(Cl)cccc3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
52916599 67693 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 878 19 6 10 9.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762382 67693 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 878 19 6 10 9.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44143412 185237 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 433 4 0 3 6.8 Cc1c(CN2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL466226 185237 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 433 4 0 3 6.8 Cc1c(CN2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
136043797 84269 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 390 8 1 5 4.1 COc1ccc(CCc2noc(-c3cc4c(CCN(C)C)cccc4[nH]3)n2)cc1 10.1016/j.bmcl.2006.03.086
CHEMBL208725 84269 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 390 8 1 5 4.1 COc1ccc(CCc2noc(-c3cc4c(CCN(C)C)cccc4[nH]3)n2)cc1 10.1016/j.bmcl.2006.03.086
136043781 84775 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 420 7 1 4 5.3 Clc1ccc(CCc2noc(-c3cc4c(CCN5CCCC5)cccc4[nH]3)n2)cc1 10.1016/j.bmcl.2006.03.086
CHEMBL209728 84775 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 420 7 1 4 5.3 Clc1ccc(CCc2noc(-c3cc4c(CCN5CCCC5)cccc4[nH]3)n2)cc1 10.1016/j.bmcl.2006.03.086
136043779 84888 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 408 8 1 4 5.2 CCN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL210292 84888 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 408 8 1 4 5.2 CCN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
11676849 80291 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 454 7 2 3 4.9 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1C(O)c1ccccc1 10.1021/jm0509851
CHEMBL201694 80291 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 454 7 2 3 4.9 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1C(O)c1ccccc1 10.1021/jm0509851
136043765 86502 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 352 7 1 4 4.4 CN(C)CCc1cccc2[nH]c(-c3nc(CCC4CCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL211592 86502 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 352 7 1 4 4.4 CN(C)CCc1cccc2[nH]c(-c3nc(CCC4CCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
44406550 142830 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 435 4 2 5 3.3 COc1cccc([C@]2(O)CCCC[C@H]2N2CCC3(CC2)C(=O)NCN3c2ccccc2)c1 10.1016/j.bmcl.2005.09.067
CHEMBL373198 142830 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 435 4 2 5 3.3 COc1cccc([C@]2(O)CCCC[C@H]2N2CCC3(CC2)C(=O)NCN3c2ccccc2)c1 10.1016/j.bmcl.2005.09.067
44450208 102991 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3cccc(Cl)c3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
CHEMBL260820 102991 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 410 4 2 4 4.7 Fc1cc2nc(SCc3cccc(Cl)c3Cl)[nH]c2cc1N1CCNCC1 10.1016/j.bmcl.2008.04.054
45270082 202024 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL551002 202024 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 323 4 1 3 3.7 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(C)c1-c1ccc(F)c(F)c1 10.1016/j.bmcl.2009.06.051
10451761 44775 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cellsInhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cells
ChEMBL 369 4 0 4 4.8 CCn1c(=O)n(C2CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1021/jm990517p
CHEMBL146013 44775 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cellsInhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cells
ChEMBL 369 4 0 4 4.8 CCn1c(=O)n(C2CCN(CC3CCCCCCC3)CC2)c2ccccc21 10.1021/jm990517p
10783436 44975 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cellsInhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cells
ChEMBL 341 3 1 4 4.7 Oc1nc2ccccc2n1C1CCN(CC2CCCCCCC2)CC1 10.1021/jm990517p
CHEMBL146191 44975 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cellsInhibition of [125I]Tyr14-nociceptin binding to human Opioid receptor like 1 (opioid receptor like 1) in CHO cells
ChEMBL 341 3 1 4 4.7 Oc1nc2ccccc2n1C1CCN(CC2CCCCCCC2)CC1 10.1021/jm990517p
44143452 185516 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 470 5 1 6 4.2 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](S(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468524 185516 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 470 5 1 6 4.2 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](S(C)(=O)=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
15982530 79148 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 408 2 0 2 5.4 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2005.08.009
CHEMBL198600 79148 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 408 2 0 2 5.4 CN1C(=O)C2(CCN(CC3CCCCCCC3)CC2)c2cc(C(F)(F)F)ccc21 10.1016/j.bmcl.2005.08.009
136043792 84148 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 394 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3noc(CCc4ccc(Cl)cc4)n3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL208603 84148 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 394 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3noc(CCc4ccc(Cl)cc4)n3)cc12 10.1016/j.bmcl.2006.03.086
44406489 148129 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
44406489 148129 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
44406489 148129 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2006.05.064
CHEMBL383610 148129 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.067
CHEMBL383610 148129 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2005.09.075
CHEMBL383610 148129 7 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCC[C@H]1c1ccccc1)CC2 10.1016/j.bmcl.2006.05.064
15965865 145141 5 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptors expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptors expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1c1ccccc1)CC2 10.1016/j.bmcl.2006.05.058
CHEMBL377140 145141 5 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptors expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptors expressed in HEK293 cells
ChEMBL 389 3 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1c1ccccc1)CC2 10.1016/j.bmcl.2006.05.058
118726261 124007 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 610 12 2 7 5.3 COc1ccc(CNC[C@H](O)CN2CN(c3ccccc3)C3(CCN(CCc4ccccc4-c4cccs4)CC3)C2=O)cc1 10.1016/j.bmcl.2014.12.015
CHEMBL3394743 124007 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 610 12 2 7 5.3 COc1ccc(CNC[C@H](O)CN2CN(c3ccccc3)C3(CCN(CCc4ccccc4-c4cccs4)CC3)C2=O)cc1 10.1016/j.bmcl.2014.12.015
44143441 185253 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 377 3 1 5 4.1 C[C@@H]1CN(CC#N)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL466427 185253 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 377 3 1 5 4.1 C[C@@H]1CN(CC#N)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
44143417 193993 12 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 367 5 1 5 4.3 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1cccnc1 10.1016/j.bmcl.2009.04.116
CHEMBL492396 193993 12 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 367 5 1 5 4.3 Cc1c(CNC2CCCC2)nn(-c2ncccc2Cl)c1-c1cccnc1 10.1016/j.bmcl.2009.04.116
11372671 145145 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 388 3 1 2 4.8 O=C1NCC(c2ccccc2)C12CCN(C1(c3ccccc3)CCCCC1)CC2 10.1016/j.bmcl.2006.05.063
CHEMBL377164 145145 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 388 3 1 2 4.8 O=C1NCC(c2ccccc2)C12CCN(C1(c3ccccc3)CCCCC1)CC2 10.1016/j.bmcl.2006.05.063
136043782 145442 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 380 6 1 4 4.7 CN(C)Cc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL377736 145442 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 380 6 1 4 4.7 CN(C)Cc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
136043788 146121 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 420 5 1 4 5.5 CN1CCC(c2cccc3[nH]c(-c4nc(CCc5ccc(Cl)cc5)no4)cc23)CC1 10.1016/j.bmcl.2006.03.086
CHEMBL379284 146121 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 420 5 1 4 5.5 CN1CCC(c2cccc3[nH]c(-c4nc(CCc5ccc(Cl)cc5)no4)cc23)CC1 10.1016/j.bmcl.2006.03.086
45270174 201976 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 419 5 1 3 6.5 Clc1ccc(-c2nc(CNC3CCCC3)cn2-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL550601 201976 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 419 5 1 3 6.5 Clc1ccc(-c2nc(CNC3CCCC3)cn2-c2ccc(Cl)cc2Cl)cc1 10.1016/j.bmcl.2009.06.095
44449822 102643 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 360 4 2 4 3.5 Fc1ccc(CSc2nc3cc(F)c(N4CCNCC4)cc3[nH]2)cc1 10.1016/j.bmcl.2008.04.054
CHEMBL259065 102643 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 360 4 2 4 3.5 Fc1ccc(CSc2nc3cc(F)c(N4CCNCC4)cc3[nH]2)cc1 10.1016/j.bmcl.2008.04.054
52916470 67688 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 916 20 4 10 11.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762377 67688 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 916 20 4 10 11.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44407013 81184 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 430 6 1 2 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)C1(c2ccccc2)CCCCC1 10.1021/jm0509851
CHEMBL202575 81184 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 430 6 1 2 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)C1(c2ccccc2)CCCCC1 10.1021/jm0509851
44143440 185434 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 420 3 1 4 5.2 C[C@@H]1CN(CC(F)(F)F)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
CHEMBL467669 185434 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 420 3 1 4 5.2 C[C@@H]1CN(CC(F)(F)F)CCN1c1cc2[nH]c(SC(C)(C)C)nc2cc1Cl 10.1016/j.bmcl.2009.04.022
52915391 67712 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 510 13 3 5 7.0 CCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762401 67712 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 510 13 3 5 7.0 CCCCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
44143420 194385 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 395 6 1 5 4.9 CCc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL494768 194385 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 395 6 1 5 4.9 CCc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
15982526 78858 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 422 4 0 2 6.3 O=C1N(CC2CCCCC2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
CHEMBL197735 78858 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 422 4 0 2 6.3 O=C1N(CC2CCCCC2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
44143427 196265 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3F)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL513855 196265 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 399 5 1 5 4.6 Cc1ccc(-c2c(C)c(CNC3CCCC3F)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
44143454 195954 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnnn5C)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL511205 195954 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 474 5 1 8 4.1 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@@H](c5nnnn5C)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
44456028 162378 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 32 15 11 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
CHEMBL404530 162378 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 965 32 15 11 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2007.11.043
44517710 203302 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 393 8 1 4 5.0 COCCc1nc(CN[C@H]2CC[C@@H](F)C2)n(C(C)C)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL563593 203302 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 393 8 1 4 5.0 COCCc1nc(CN[C@H]2CC[C@@H](F)C2)n(C(C)C)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
44406539 141953 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 435 4 2 5 3.3 COc1ccc([C@]2(O)CCCC[C@H]2N2CCC3(CC2)C(=O)NCN3c2ccccc2)cc1 10.1016/j.bmcl.2005.09.067
CHEMBL371966 141953 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [3H]NOP from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]NOP from human NOP receptor expressed in HEK293 cells
ChEMBL 435 4 2 5 3.3 COc1ccc([C@]2(O)CCCC[C@H]2N2CCC3(CC2)C(=O)NCN3c2ccccc2)cc1 10.1016/j.bmcl.2005.09.067
136043759 85484 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 380 8 1 4 5.2 CN(C)CCc1cccc2[nH]c(-c3nc(CCCC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL211254 85484 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 380 8 1 4 5.2 CN(C)CCc1cccc2[nH]c(-c3nc(CCCC4CCCCC4)no3)cc12 10.1016/j.bmcl.2006.03.086
52916713 67695 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 906 21 6 10 10.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762384 67695 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 906 21 6 10 10.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44404693 142871 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 398 4 0 4 3.4 COC(=O)CN1C(=O)C2(CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL373222 142871 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 398 4 0 4 3.4 COC(=O)CN1C(=O)C2(CCN(Cc3ccc(Cl)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44143425 194309 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 425 6 1 7 3.4 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2S(C)(=O)=O)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL494414 194309 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 425 6 1 7 3.4 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncccc2S(C)(=O)=O)cn1 10.1016/j.bmcl.2009.04.116
44576626 200145 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 410 7 2 5 4.4 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL525054 200145 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 410 7 2 5 4.4 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
11603249 79965 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 376 7 1 2 4.1 O=C(CCc1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL201181 79965 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 376 7 1 2 4.1 O=C(CCc1ccccc1)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
52915389 67710 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 482 11 3 5 6.2 CCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762399 67710 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 482 11 3 5 6.2 CCCCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
15982529 78917 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 382 3 0 2 5.5 CC(C)c1ccc2c(c1)C1(CCN(CC3CCCCCCC3)CC1)C(=O)N2C 10.1016/j.bmcl.2005.08.009
CHEMBL197895 78917 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 382 3 0 2 5.5 CC(C)c1ccc2c(c1)C1(CCN(CC3CCCCCCC3)CC1)C(=O)N2C 10.1016/j.bmcl.2005.08.009
44143409 185344 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 447 5 1 3 7.2 Cc1c(CNC2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
CHEMBL467049 185344 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 447 5 1 3 7.2 Cc1c(CNC2CCCCC2)nn(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.04.116
10981761 117415 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 379 3 1 6 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3nsnc3c1)CC2 10.1021/jm010878g
CHEMBL325750 117415 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 379 3 1 6 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccc3nsnc3c1)CC2 10.1021/jm010878g
52916712 67694 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 892 20 6 10 10.3 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762383 67694 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 892 20 6 10 10.3 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52916598 67692 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 864 18 6 10 9.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762381 67692 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 864 18 6 10 9.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCNCc4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
44449766 162475 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 356 4 2 4 3.7 Cc1ccccc1CSc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL405078 162475 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 356 4 2 4 3.7 Cc1ccccc1CSc1nc2cc(F)c(N3CCNCC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
52915516 67717 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 483 11 4 6 4.8 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762406 67717 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 483 11 4 6 4.8 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(CNCCCCN)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
118726266 124012 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 586 11 2 7 5.3 O=C1N(C[C@H](O)CNCc2cccs2)CN(c2ccccc2)C12CCN(CCc1ccccc1-c1cccs1)CC2 10.1016/j.bmcl.2014.12.015
CHEMBL3394748 124012 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 586 11 2 7 5.3 O=C1N(C[C@H](O)CNCc2cccs2)CN(c2ccccc2)C12CCN(CCc1ccccc1-c1cccs1)CC2 10.1016/j.bmcl.2014.12.015
44576625 194277 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 396 7 2 5 4.0 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL494219 194277 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 396 7 2 5 4.0 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)C(C)C3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
11583016 81128 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 440 7 1 3 5.6 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Oc1ccccc1 10.1021/jm0509851
CHEMBL202443 81128 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 440 7 1 3 5.6 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1Oc1ccccc1 10.1021/jm0509851
44178080 202859 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 362 6 1 4 4.0 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCC#N)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL560667 202859 2 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 362 6 1 4 4.0 Cc1c(CN[C@H]2CC[C@@H](F)C2)nn(CCC#N)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143426 185491 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 415 5 1 5 5.3 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncc(Cl)cc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL468307 185491 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 415 5 1 5 5.3 Cc1ccc(-c2c(C)c(CNC3CCCC3)nn2-c2ncc(Cl)cc2Cl)cn1 10.1016/j.bmcl.2009.04.116
24882570 121909 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343946 121909 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343947 121909 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysisDisplacement of [3H]]nociceptin from human ORL1 receptor low affinity binding site expressed in African green monkey COS7 cells after 90 mins by topcount analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
45273679 202414 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 351 5 1 3 4.6 Cc1nc(CN[C@H]2CC[C@@H](F)C2)c(C(C)C)n1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.095
CHEMBL556300 202414 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 351 5 1 3 4.6 Cc1nc(CN[C@H]2CC[C@@H](F)C2)c(C(C)C)n1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.095
CHEMBL266667 217472 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@@H](O)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)C(=O)NCC(=O)N[C@@H](CS)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
118726271 124017 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 610 12 2 7 4.8 COc1ccc(CCNC[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)cc1OC 10.1016/j.bmcl.2014.12.015
CHEMBL3394753 124017 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 610 12 2 7 4.8 COc1ccc(CCNC[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)cc1OC 10.1016/j.bmcl.2014.12.015
15983062 78989 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 370 4 0 4 3.1 COC(=O)CN1C(=O)C2(CCN(CC3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL198099 78989 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 370 4 0 4 3.1 COC(=O)CN1C(=O)C2(CCN(CC3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
23542106 124019 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 611 12 1 7 5.3 COc1ccc(CCOC[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)cc1OC 10.1016/j.bmcl.2014.12.015
CHEMBL3394755 124019 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 611 12 1 7 5.3 COc1ccc(CCOC[C@H](O)CN2CN(c3ccc(F)cc3)C3(CCN(CC4CCCCCCC4)CC3)C2=O)cc1OC 10.1016/j.bmcl.2014.12.015
52916597 67691 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 958 23 4 10 12.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762380 67691 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 958 23 4 10 12.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
52916472 67690 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 944 22 4 10 12.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762379 67690 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 944 22 4 10 12.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
15982797 79015 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 358 7 0 4 3.1 CCCCCCN1CCC2(CC1)C(=O)N(CC(=O)OC)c1ccccc12 10.1016/j.bmcl.2005.08.009
CHEMBL198167 79015 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 358 7 0 4 3.1 CCCCCCN1CCC2(CC1)C(=O)N(CC(=O)OC)c1ccccc12 10.1016/j.bmcl.2005.08.009
9887195 45317 6 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 CCn1c(=O)n([C@H]2CCN(CC3CCCCCCC3)C[C@@H]2CO)c2ccccc21 10.1021/jm990517p
CHEMBL146462 45317 6 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptinBinding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
ChEMBL 399 5 1 5 4.0 CCn1c(=O)n([C@H]2CCN(CC3CCCCCCC3)C[C@@H]2CO)c2ccccc21 10.1021/jm990517p
44449850 168020 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 450 6 1 4 5.5 Fc1ccc(CSc2nc3cc(F)c(N4CCN(Cc5ccccc5)CC4)cc3[nH]2)cc1 10.1016/j.bmcl.2008.04.054
CHEMBL411890 168020 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 450 6 1 4 5.5 Fc1ccc(CSc2nc3cc(F)c(N4CCN(Cc5ccccc5)CC4)cc3[nH]2)cc1 10.1016/j.bmcl.2008.04.054
15982660 79231 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 382 4 0 3 4.1 O=C1N(CC2CO2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
CHEMBL198867 79231 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 382 4 0 3 4.1 O=C1N(CC2CO2)c2ccccc2C12CCN(CC1CCCCCCC1)CC2 10.1016/j.bmcl.2005.08.009
11597677 80436 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 454 8 1 3 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1OCc1ccccc1 10.1021/jm0509851
CHEMBL201805 80436 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 454 8 1 3 5.4 O=C(NCCCN1CCC2(CCc3ccccc32)CC1)c1ccccc1OCc1ccccc1 10.1021/jm0509851
52915269 67708 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 454 9 3 5 5.5 CCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762397 67708 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 454 9 3 5 5.5 CCCNCc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
52916360 67687 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 902 19 4 10 11.3 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
CHEMBL1762376 67687 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 902 19 4 10 11.3 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(/C=N/CCCCCC/N=C/c4ccc(OCc5ccccc5C(=O)Nc5ccc6nc(C)cc(N)c6c5)cc4)cc3)ccc2n1 10.1016/j.ejmech.2011.01.040
45271014 202239 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.7 Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2)c1-c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2009.06.095
CHEMBL552482 202239 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 433 5 1 3 6.7 Cn1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2)c1-c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2009.06.095
44407020 80741 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 440 7 1 3 5.0 CC(C)(Oc1ccc(Cl)cc1)C(=O)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL202152 80741 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 440 7 1 3 5.0 CC(C)(Oc1ccc(Cl)cc1)C(=O)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL405451 219341 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membraneDisplacement of [3H]NC from human ORL1 receptor expressing HEK293 cell membrane
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@@H]1CSSC[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010092i
15982657 78915 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 432 4 0 4 3.8 COC(=O)CN1C(=O)C2(CCN(Cc3ccc(C(F)(F)F)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL197880 78915 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 432 4 0 4 3.8 COC(=O)CN1C(=O)C2(CCN(Cc3ccc(C(F)(F)F)cc3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
45270184 202049 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 399 5 1 5 4.6 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C)cn1 10.1016/j.bmcl.2009.06.095
CHEMBL551208 202049 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 399 5 1 5 4.6 Cc1ccc(-n2c(-c3ncccc3Cl)nc(CN[C@H]3CC[C@@H](F)C3)c2C)cn1 10.1016/j.bmcl.2009.06.095
44143438 185512 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 366 3 1 4 4.6 CCN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)[C@H](C)C1 10.1016/j.bmcl.2009.04.022
CHEMBL468504 185512 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 366 3 1 4 4.6 CCN1CCN(c2cc3[nH]c(SC(C)(C)C)nc3cc2Cl)[C@H](C)C1 10.1016/j.bmcl.2009.04.022
45267505 202840 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 343 4 1 3 4.0 Cn1nc(CN[C@H]2CC[C@@H](F)C2)c(Cl)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
CHEMBL560468 202840 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 343 4 1 3 4.0 Cn1nc(CN[C@H]2CC[C@@H](F)C2)c(Cl)c1-c1cc(F)cc(F)c1 10.1016/j.bmcl.2009.06.051
44143429 185515 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 417 5 1 5 4.9 Cc1ccc(-c2c(C)c(CNC3CCC(F)(F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
CHEMBL468518 185515 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 417 5 1 5 4.9 Cc1ccc(-c2c(C)c(CNC3CCC(F)(F)C3)nn2-c2ncccc2Cl)cn1 10.1016/j.bmcl.2009.04.116
44143432 185488 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
CHEMBL468301 185488 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 465 5 2 6 4.5 CCN1CCN(c2cc3[nH]c(S[C@]4(C)CC[C@H](NC(=O)OC)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.022
10221539 163777 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
CHEMBL407325 163777 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.054
10221539 163777 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
CHEMBL407325 163777 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr14-NC/OFQ from human ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from human ORL1 receptor
ChEMBL 382 7 2 5 3.6 CCC(CC)Sc1nc2cc(Cl)c(N3CCN(CCO)CC3)cc2[nH]1 10.1016/j.bmcl.2008.04.037
44143436 185245 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 402 4 1 5 3.7 CCN1CCN(c2cc3[nH]c(C(=O)C4(C)CCC(=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
CHEMBL466307 185245 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 402 4 1 5 3.7 CCN1CCN(c2cc3[nH]c(C(=O)C4(C)CCC(=O)CC4)nc3cc2Cl)CC1 10.1016/j.bmcl.2009.04.023
45272626 202543 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 306 4 2 3 3.2 Cc1ncc(-c2[nH]nc(CN[C@H]3CC[C@@H](F)C3)c2C)cc1F 10.1016/j.bmcl.2009.06.051
CHEMBL557653 202543 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr14-NC/OFQ from ORL1 receptorDisplacement of [125I]Tyr14-NC/OFQ from ORL1 receptor
ChEMBL 306 4 2 3 3.2 Cc1ncc(-c2[nH]nc(CN[C@H]3CC[C@@H](F)C3)c2C)cc1F 10.1016/j.bmcl.2009.06.051
15982937 147055 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 410 3 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(C3CCC4CCCCC4C3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
CHEMBL380580 147055 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cellsBinding affinity determined by the ability to compete with [125I]-Tyr14- nociceptin from binding to human opiate receptor-like 1 expressed in HEK293 cells
ChEMBL 410 3 0 4 3.9 COC(=O)CN1C(=O)C2(CCN(C3CCC4CCCCC4C3)CC2)c2ccccc21 10.1016/j.bmcl.2005.08.009
44407156 148107 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 392 7 1 3 3.9 CC(Oc1ccccc1)C(=O)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
CHEMBL383489 148107 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cellsDisplacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
ChEMBL 392 7 1 3 3.9 CC(Oc1ccccc1)C(=O)NCCCN1CCC2(CCc3ccccc32)CC1 10.1021/jm0509851
44449851 102569 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 374 4 1 4 3.9 CN1CCN(c2cc3[nH]c(SCc4ccc(F)cc4)nc3cc2F)CC1 10.1016/j.bmcl.2008.04.054
CHEMBL258746 102569 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membraneDisplacement of [125I]Tyr14-NC from human ORL1 receptor expressed in CHO cell membrane
ChEMBL 374 4 1 4 3.9 CN1CCN(c2cc3[nH]c(SCc4ccc(F)cc4)nc3cc2F)CC1 10.1016/j.bmcl.2008.04.054
44456217 176459 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 33 15 11 -0.3 CCC(CC)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
CHEMBL443765 176459 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cellsDisplacement of [3H]nociceptin from human ORL1-Galpha fusion receptor in COS7 cells
ChEMBL 979 33 15 11 -0.3 CCC(CC)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)CC 10.1016/j.bmc.2007.11.043
136043819 84712 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 394 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL209537 84712 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 394 7 1 4 4.8 CN(C)CCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
45273702 202556 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 497 8 1 3 7.7 FCC(CF)n1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
CHEMBL557729 202556 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cellsDisplacement of [125I]Tyr14-nociceptin from human ORL1 receptor expressed in CHO cells
ChEMBL 497 8 1 3 7.7 FCC(CF)n1c(CNC2CCCC2)nc(-c2ccc(Cl)cc2Cl)c1-c1ccc(Cl)cc1 10.1016/j.bmcl.2009.06.095
136043780 146046 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 438 10 1 5 4.8 CN(C)CCOCCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
CHEMBL379048 146046 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cellsDisplacement of [125I][Tyr14]N/OFQ from ORL1 receptor transfected in CHO cells
ChEMBL 438 10 1 5 4.8 CN(C)CCOCCc1cccc2[nH]c(-c3nc(CCc4ccc(Cl)cc4)no3)cc12 10.1016/j.bmcl.2006.03.086
11143820 16894 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 399 3 1 5 3.0 O=C1NCN(c2ccccc2)C12CCN(Cc1cc3c(cc1Cl)OCO3)CC2 10.1021/jm010878g
CHEMBL115652 16894 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibition of human ORL1 orphanin receptorInhibition of human ORL1 orphanin receptor
ChEMBL 399 3 1 5 3.0 O=C1NCN(c2ccccc2)C12CCN(Cc1cc3c(cc1Cl)OCO3)CC2 10.1021/jm010878g
52915143 67700 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 452 8 2 5 5.8 CCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
CHEMBL1762389 67700 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
ChEMBL 452 8 2 5 5.8 CCC/N=C/c1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1016/j.ejmech.2011.01.040
118726263 124009 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 636 14 1 6 6.8 CCCCN(Cc1ccccc1)C[C@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
CHEMBL3394745 124009 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr14-nociceptin from human ORL1 expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 636 14 1 6 6.8 CCCCN(Cc1ccccc1)C[C@H](O)CN1CN(c2ccccc2)C2(CCN(CCc3ccccc3-c3cccs3)CC2)C1=O 10.1016/j.bmcl.2014.12.015
16131448 9624 28 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -1 6 Rat 10.1 pKd = 10.1 Binding
Binding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Gln205Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
Binding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 9624 28 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
1681 9624 28 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
1688 9624 28 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
44361543 9624 28 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
56947112 9624 28 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
CHEMBL396460 9624 28 None -1 6 Rat 10.0 pKd = 10 Binding
Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Compound was tested for inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL None None None None 10.1016/s0960-894x(00)00111-6
16131448 9624 28 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1681 9624 28 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
1688 9624 28 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
44361543 9624 28 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
56947112 9624 28 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
CHEMBL396460 9624 28 None 1 6 Human 9.7 pKd = 9.7 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL None None None None 10.1016/j.bmc.2014.09.018
16131448 9624 28 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -1 6 Rat 9.3 pKd = 9.3 Binding
Binding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Trp208Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 9624 28 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Asp206Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
16131448 9624 28 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1681 9624 28 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
1688 9624 28 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
44361543 9624 28 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
56947112 9624 28 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
CHEMBL396460 9624 28 None -1 6 Rat 9.2 pKd = 9.2 Binding
Binding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assayBinding affinity to recombinant ORL1 receptor Tyr207Ala mutant expressed in COS7 cells by saturation binding assay
ChEMBL None None None None 10.1016/j.bmc.2009.10.026
24882570 121909 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343946 121909 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
CHEMBL3343947 121909 0 None - 1 Human 8.9 pKd = 8.9 Binding
Binding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysisBinding affinity to human ORL1 receptor expressed in African green monkey COS7 cells assessed per mg protein after 90 mins by Scatchard plot analysis
ChEMBL 981 32 16 12 -1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CC(C)C)C(=O)N[C@@H](CCCCN)C(N)=O 10.1016/j.bmc.2014.09.018
101232765 186603 0 None - 1 Human 7.0 pKd = 7.0 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1384 48 23 20 -7.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CSC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4745049 186603 0 None - 1 Human 7.0 pKd = 7.0 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1384 48 23 20 -7.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CSC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162657543 187914 0 None - 1 Human 7.9 pKd = 7.9 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1395 48 24 20 -8.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CN[C@@H](C)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4760649 187914 0 None - 1 Human 7.9 pKd = 7.9 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1395 48 24 20 -8.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CN[C@@H](C)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
101232765 186603 0 None - 1 Human 6.9 pKd = 6.9 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1384 48 23 20 -7.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CSC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4745049 186603 0 None - 1 Human 6.9 pKd = 6.9 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1384 48 23 20 -7.2 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CSC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL410396 219597 17 None 1 2 Human 7.8 pKd = 7.8 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
162657543 187914 0 None - 1 Human 7.7 pKd = 7.7 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1395 48 24 20 -8.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CN[C@@H](C)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL4760649 187914 0 None - 1 Human 7.7 pKd = 7.7 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL 1395 48 24 20 -8.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CN[C@@H](C)c1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
10654047 219409 18 None 2 2 Human 7.5 pKd = 7.5 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL406946 219409 18 None 2 2 Human 7.5 pKd = 7.5 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL410396 219597 17 None 1 2 Human 8.2 pKd = 8.2 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing Gbeta1-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of G protein activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
10654047 219409 18 None 2 2 Human 7.1 pKd = 7.1 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
CHEMBL406946 219409 18 None 2 2 Human 7.1 pKd = 7.1 Binding
Antagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assayAntagonist activity at NOP (unknown origin) expressed in HEK293 cell membranes co-expressing beta-arrestin2-RGFP protein assessed as reduction in N/OFQ(1-13)-NH2-induced induction of beta-arrestin2 activation pre-incubated for 15 mins before stimulation with N/OFQ(1-13)-NH2 for 15 mins by BRET assay
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.9b02057
44388467 176184 0 None - 1 Human 10.7 pKi = 10.7 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL442297 176184 0 None - 1 Human 10.7 pKi = 10.7 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1956 69 33 31 -14.8 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL415845 219983 0 None - 1 Human 10.7 pKi = 10.7 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
CHEMBL264846 217411 0 None - 1 Human 10.7 pKi = 10.7 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
44388474 167821 0 None - 1 Human 10.6 pKi = 10.6 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1970 69 33 31 -15.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL411649 167821 0 None - 1 Human 10.6 pKi = 10.6 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1970 69 33 31 -15.0 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
3917 10702 0 None 154 4 Human 10.6 pKi = 10.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44430609 10702 0 None 154 4 Human 10.6 pKi = 10.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL409969 10702 0 None 154 4 Human 10.6 pKi = 10.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1641 9505 9 None 2 12 Human 10.5 pKi = 10.5 Binding
Binding affinity against delta-opioid receptor in guinea pig brain membranesBinding affinity against delta-opioid receptor in guinea pig brain membranes
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1021/jm00038a019
3829 9505 9 None 2 12 Human 10.5 pKi = 10.5 Binding
Binding affinity against delta-opioid receptor in guinea pig brain membranesBinding affinity against delta-opioid receptor in guinea pig brain membranes
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1021/jm00038a019
5497186 9505 9 None 2 12 Human 10.5 pKi = 10.5 Binding
Binding affinity against delta-opioid receptor in guinea pig brain membranesBinding affinity against delta-opioid receptor in guinea pig brain membranes
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1021/jm00038a019
CHEMBL567175 9505 9 None 2 12 Human 10.5 pKi = 10.5 Binding
Binding affinity against delta-opioid receptor in guinea pig brain membranesBinding affinity against delta-opioid receptor in guinea pig brain membranes
ChEMBL 414 2 3 4 3.6 Oc1ccc2c3c1O[C@@H]1[C@@]43CCN([C@H](C2)[C@]4(O)Cc2c1[nH]c1c2cccc1)CC1CC1 10.1021/jm00038a019
44388466 103276 0 None - 1 Human 10.5 pKi = 10.5 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL262544 103276 0 None - 1 Human 10.5 pKi = 10.5 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1938 69 33 31 -14.9 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
70689062 84377 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 438 5 1 4 4.3 NC(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2088054 84377 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 438 5 1 4 4.3 NC(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL3810319 219056 0 None - 1 Human 10.4 pKi = 10.4 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c(C)cc(O)cc1C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.5b01976
CHEMBL263588 217358 0 None - 1 Human 10.3 pKi = 10.3 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
16131448 9624 28 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
1681 9624 28 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
1688 9624 28 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
44361543 9624 28 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
56947112 9624 28 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
CHEMBL396460 9624 28 None 1 6 Human 10.3 pKi = 10.3 Binding
Binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsBinding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None None 10.1021/jm040106v
CHEMBL266191 217458 0 None - 1 Human 10.3 pKi = 10.3 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
CHEMBL414542 219917 0 None - 1 Human 10.3 pKi = 10.3 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
CHEMBL3808650 219053 0 None - 1 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acs.jmedchem.5b01976
CHEMBL2372052 216953 0 None 5 7 Human 10.3 pKi = 10.3 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)[C@H](CN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
CHEMBL438537 220553 0 None - 1 Human 10.2 pKi = 10.2 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
16131448 9624 28 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
1681 9624 28 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
1688 9624 28 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
44361543 9624 28 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
56947112 9624 28 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
CHEMBL396460 9624 28 None 1 6 Human 10.2 pKi = 10.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL None None None None 10.1016/j.bmcl.2003.09.068
68182754 119466 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 472 5 0 6 4.6 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3236476 119466 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 472 5 0 6 4.6 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3304248 119466 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 472 5 0 6 4.6 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
70684842 84382 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 460 6 0 4 4.4 CN(C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12)C1CC1 10.1021/jm201629q
CHEMBL2088061 84382 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 460 6 0 4 4.4 CN(C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12)C1CC1 10.1021/jm201629q
68182860 119480 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 433 3 0 5 4.7 Cc1nn(-c2c(F)cccc2F)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3236474 119480 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 433 3 0 5 4.7 Cc1nn(-c2c(F)cccc2F)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3304364 119480 0 None - 1 Human 10.2 pKi = 10.2 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 433 3 0 5 4.7 Cc1nn(-c2c(F)cccc2F)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
9885005 64321 0 None 40 3 Rat 10.1 pKi = 10.1 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 3 1 3 3.6 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL166387 64321 0 None 40 3 Rat 10.1 pKi = 10.1 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 3 1 3 3.6 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL408356 219487 0 None - 1 Human 10.1 pKi = 10.1 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
16131448 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
1681 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
1688 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
44361543 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
56947112 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
CHEMBL396460 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm2003238
9842289 127261 0 None 8 3 Rat 10.1 pKi = 10.1 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 369 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL354291 127261 0 None 8 3 Rat 10.1 pKi = 10.1 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 369 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
12419 9252 29 None 12 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
24800108 9252 29 None 12 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
CHEMBL481512 9252 29 None 12 3 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 10.1021/jm7012979
58268629 85100 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 450 5 0 4 4.4 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2088055 85100 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 450 5 0 4 4.4 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2109704 85100 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 450 5 0 4 4.4 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
52951809 90370 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 436 5 1 4 4.0 CNC(=O)[C@@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2204347 90370 0 None - 1 Human 10.1 pKi = 10.1 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 436 5 1 4 4.0 CNC(=O)[C@@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
70684841 84380 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 436 5 1 4 4.0 CNC(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088058 84380 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 436 5 1 4 4.0 CNC(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
58268628 119428 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 0 7 4.5 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCCc2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3236478 119428 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 0 7 4.5 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCCc2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3303098 119428 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 5 0 7 4.5 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCCc2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
58268566 116897 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 516 4 1 7 5.3 Cc1nn(-c2ncccc2-c2ncc[nH]2)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236486 116897 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 516 4 1 7 5.3 Cc1nn(-c2ncccc2-c2ncc[nH]2)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
58268647 119392 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 0 7 4.0 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCCc2cc(F)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3236479 119392 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 0 7 4.0 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCCc2cc(F)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3302393 119392 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 442 5 0 7 4.0 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCCc2cc(F)sc23)c(C)n1 10.1021/jm500117r
68182857 119472 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 4 1 6 3.7 Cc1nn(-c2c(F)cccc2C(N)=O)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3236475 119472 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 4 1 6 3.7 Cc1nn(-c2c(F)cccc2C(N)=O)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3304315 119472 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 458 4 1 6 3.7 Cc1nn(-c2c(F)cccc2C(N)=O)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
67168385 119478 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 510 5 1 6 5.4 CNCc1cccc(F)c1-n1cc(CN2CCC3(CC2)OCC(F)(F)c2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3236485 119478 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 510 5 1 6 5.4 CNCc1cccc(F)c1-n1cc(CN2CCC3(CC2)OCC(F)(F)c2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3304360 119478 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 510 5 1 6 5.4 CNCc1cccc(F)c1-n1cc(CN2CCC3(CC2)OCC(F)(F)c2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL264084 217384 0 None - 1 Human 10.0 pKi = 10 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
16131448 9624 28 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
1681 9624 28 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
1688 9624 28 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
44361543 9624 28 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
56947112 9624 28 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
CHEMBL396460 9624 28 None 1 6 Human 10.0 pKi = 10 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None None 10.1021/jm020078l
CHEMBL1162359 215296 0 None - 1 Human 10.0 pKi = 10 Binding
Binding affinity to human NOP receptorBinding affinity to human NOP receptor
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
25208097 190701 3 None 5 4 Human 10.0 pKi = 10 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481366 190701 3 None 5 4 Human 10.0 pKi = 10 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 408 3 1 4 5.6 CC1(N2CCC(n3c([C@H]4CCCNC4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
10406239 127338 0 None 2 4 Human 10.0 pKi = 10 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3326224 127338 0 None 2 4 Human 10.0 pKi = 10 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3326226 127338 0 None 2 4 Human 10.0 pKi = 10 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3545624 127338 0 None 2 4 Human 10.0 pKi = 10 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
52951675 90373 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 422 5 1 4 3.7 NC(=O)[C@@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2204353 90373 0 None - 1 Human 10.0 pKi = 10 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 422 5 1 4 3.7 NC(=O)[C@@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
52914971 9186 37 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 10.1021/jm500117r
9462 9186 37 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 10.1021/jm500117r
CHEMBL3304244 9186 37 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 10.1021/jm500117r
DB16048 9186 37 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 10.1021/jm500117r
52951807 84155 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 1 4 3.2 NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2086410 84155 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 1 4 3.2 NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
52951807 84155 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 406 5 1 4 3.2 NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2086410 84155 0 None - 1 Human 10.0 pKi = 10.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 406 5 1 4 3.2 NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
68182737 119394 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 4 1 6 5.1 Cc1nn(-c2c(F)cccc2CO)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236484 119394 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 4 1 6 5.1 Cc1nn(-c2c(F)cccc2CO)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3302404 119394 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 497 4 1 6 5.1 Cc1nn(-c2c(F)cccc2CO)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
60154264 84162 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 434 5 0 4 3.8 CN(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2086648 84162 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 434 5 0 4 3.8 CN(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088060 84162 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 434 5 0 4 3.8 CN(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
16131448 9624 28 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1681 9624 28 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
1688 9624 28 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
44361543 9624 28 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
56947112 9624 28 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
CHEMBL396460 9624 28 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL None None None None 10.1016/j.bmc.2014.02.047
68182789 119400 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 488 5 0 6 5.2 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236477 119400 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 488 5 0 6 5.2 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3302591 119400 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 488 5 0 6 5.2 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm500117r
70697390 84376 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 452 5 1 4 4.5 CNC(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2088053 84376 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 452 5 1 4 4.5 CNC(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
70689063 84378 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 436 5 1 4 4.0 CNC(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2088056 84378 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 436 5 1 4 4.0 CNC(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
44388473 166245 0 None - 1 Human 9.9 pKi = 9.9 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1952 69 33 31 -15.1 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL410145 166245 0 None - 1 Human 9.9 pKi = 9.9 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL 1952 69 33 31 -15.1 C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)N(N)N)C(=O)NN 10.1021/jm040106v
CHEMBL414767 219933 0 None 154 2 Human 9.9 pKi = 9.9 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
44253565 149190 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 5 0 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2cccc(F)c2)CC1 nan
CHEMBL3889835 149190 0 None 1 2 Human 9.9 pKi = 9.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 5 0 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2cccc(F)c2)CC1 nan
16131448 9624 28 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
1681 9624 28 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
1688 9624 28 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
44361543 9624 28 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
56947112 9624 28 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
CHEMBL396460 9624 28 None 1 6 Human 9.9 pKi = 9.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7009606
70697391 84379 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 450 5 0 4 4.4 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088057 84379 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 450 5 0 4 4.4 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
52951808 84364 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088029 84364 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
52951808 84364 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2088029 84364 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
58268595 119479 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 3 0 6 4.0 Cc1nn(-c2ncccc2F)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3236473 119479 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 3 0 6 4.0 Cc1nn(-c2ncccc2F)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
CHEMBL3304363 119479 0 None - 1 Human 9.9 pKi = 9.9 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 416 3 0 6 4.0 Cc1nn(-c2ncccc2F)cc1CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm500117r
68182794 119393 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 524 5 0 6 5.7 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236482 119393 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 524 5 0 6 5.7 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3302403 119393 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 524 5 0 6 5.7 Cc1nn(-c2c(F)cccc2CN(C)C)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL410979 219634 0 None - 1 Human 9.8 pKi = 9.8 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
25208101 190702 0 None 41 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 479 4 0 5 6.2 CC1(N2CCC(n3c(-c4cccc(S(C)(=O)=O)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481367 190702 0 None 41 2 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 479 4 0 5 6.2 CC1(N2CCC(n3c(-c4cccc(S(C)(=O)=O)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
53319615 64081 0 None 1174 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 451 4 1 4 6.5 OCC1(N2CCC(n3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650843 64081 0 None 1174 3 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 451 4 1 4 6.5 OCC1(N2CCC(n3c(-c4ccc(Cl)cc4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
52951810 84368 1 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 420 5 1 4 3.5 CNC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2088033 84368 1 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 420 5 1 4 3.5 CNC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
70695375 85110 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 466 5 0 4 4.9 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2088052 85110 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 466 5 0 4 4.9 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
CHEMBL2109867 85110 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 466 5 0 4 4.9 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(Cl)sc12 10.1021/jm201629q
68182775 119412 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 3 0 5 5.8 Cc1nn(-c2c(F)cccc2F)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236480 119412 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 3 0 5 5.8 Cc1nn(-c2c(F)cccc2F)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3302759 119412 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 485 3 0 5 5.8 Cc1nn(-c2c(F)cccc2F)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
52951810 84368 1 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 420 5 1 4 3.5 CNC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088033 84368 1 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 420 5 1 4 3.5 CNC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
58268569 119463 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 468 3 0 6 5.0 Cc1nn(-c2ncccc2F)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236481 119463 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 468 3 0 6 5.0 Cc1nn(-c2ncccc2F)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3304234 119463 0 None - 1 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 468 3 0 6 5.0 Cc1nn(-c2ncccc2F)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL269068 217556 0 None 56 5 Human 9.8 pKi = 9.8 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)C(C)(C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1016/j.bmc.2007.04.026
25207950 190575 0 None 109 4 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 430 4 1 4 6.3 CC1(N2CCC(n3c(-c4cccc(CN)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL480426 190575 0 None 109 4 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 430 4 1 4 6.3 CC1(N2CCC(n3c(-c4cccc(CN)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
16131448 9624 28 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1681 9624 28 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
1688 9624 28 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
44361543 9624 28 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
56947112 9624 28 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
CHEMBL396460 9624 28 None 1 6 Human 9.7 pKi = 9.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL None None None None 10.1016/j.bmcl.2004.08.001
58268591 119410 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 5 0 7 5.1 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCC(F)(F)c2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3236488 119410 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 5 0 7 5.1 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCC(F)(F)c2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
CHEMBL3302755 119410 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 494 5 0 7 5.1 COCc1cccnc1-n1cc(CN2CCC3(CC2)OCC(F)(F)c2cc(Cl)sc23)c(C)n1 10.1021/jm500117r
11956520 127343 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3326228 127343 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3545629 127343 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 359 2 2 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)NCCc1c3ccccc3[nH]c12 10.1021/ml500117c
70682760 84383 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 476 6 0 4 4.9 CN(C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12)C1CC1 10.1021/jm201629q
CHEMBL2088062 84383 0 None - 1 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 476 6 0 4 4.9 CN(C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12)C1CC1 10.1021/jm201629q
25208095 197988 0 None 18 3 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 6.0 CN1CCC[C@@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL518950 197988 0 None 18 3 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 6.0 CN1CCC[C@@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
46880032 14382 0 None 54 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 4 1 5 4.1 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1088036 14382 0 None 54 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 4 1 5 4.1 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
124565311 180849 0 None 165 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in HEK293 cell membranes after 60 minsDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in HEK293 cell membranes after 60 mins
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/acs.jmedchem.5b01499
CHEMBL4544227 180849 0 None 165 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in HEK293 cell membranes after 60 minsDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in HEK293 cell membranes after 60 mins
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/acs.jmedchem.5b01499
16131448 9624 28 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
1681 9624 28 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
1688 9624 28 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
44361543 9624 28 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
56947112 9624 28 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
CHEMBL396460 9624 28 None 1 6 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL None None None None 10.1021/jm500117r
25208245 190723 0 None 204 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 453 3 0 3 7.6 CC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481547 190723 0 None 204 2 Human 9.7 pKi = 9.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 453 3 0 3 7.6 CC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
52951674 84365 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088030 84365 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
52951674 84365 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2088030 84365 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
10296561 7829 26 None 23 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
7361 7829 26 None 23 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
CHEMBL201945 7829 26 None 23 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 10.1016/j.bmc.2009.05.068
CHEMBL413944 219882 0 None - 1 Human 9.6 pKi = 9.6 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
25208099 195149 0 None 41 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 6.0 CN1CCC[C@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
CHEMBL501331 195149 0 None 41 4 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 422 3 0 4 6.0 CN1CCC[C@H](c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)C1 10.1021/jm7012979
9885004 176001 1 None 13 3 Rat 9.6 pKi = 9.6 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL440928 176001 1 None 13 3 Rat 9.6 pKi = 9.6 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
70691173 85109 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 0 6 2.4 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1cc(F)sc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088051 85109 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 0 6 2.4 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1cc(F)sc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2109866 85109 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 0 6 2.4 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1cc(F)sc12)Cn1cccn1 10.1021/jm201629q
15512229 10158 0 None 1 7 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(99)00385-6
8864 10158 0 None 1 7 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(99)00385-6
CHEMBL355202 10158 0 None 1 7 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(99)00385-6
10047612 10302 15 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm201629q
1693 10302 15 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm201629q
CHEMBL559569 10302 15 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm201629q
10047612 10302 15 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm101487v
1693 10302 15 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm101487v
CHEMBL559569 10302 15 None 173 2 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/jm101487v
CHEMBL1162358 215295 0 None - 1 Human 9.6 pKi = 9.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CCCCNC(=O)C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
16131448 9624 28 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
1681 9624 28 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
1688 9624 28 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
44361543 9624 28 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
56947112 9624 28 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
CHEMBL396460 9624 28 None 1 6 Human 9.5 pKi = 9.5 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm0202021
8868 10320 31 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
9887077 10320 31 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL513136 10320 31 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
44438983 153962 0 None 16 4 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 379 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3cccc(F)c31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL392798 153962 0 None 16 4 Human 9.5 pKi = 9.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 379 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3cccc(F)c31)CC2 10.1016/j.bmcl.2007.01.069
134563655 180997 3 None 7 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4548515 180997 3 None 7 3 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 353 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
25207948 190574 0 None 31 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 461 6 1 5 6.2 CC1(N2CCC(n3c(-c4cccc(OCCO)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL480425 190574 0 None 31 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 461 6 1 5 6.2 CC1(N2CCC(n3c(-c4cccc(OCCO)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
10406239 127338 0 None 2 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3326224 127338 0 None 2 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3326226 127338 0 None 2 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
CHEMBL3545624 127338 0 None 2 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 360 2 1 2 5.0 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500116x
44414890 145961 0 None 1 3 Guinea pig 9.5 pKi = 9.5 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 445 4 3 6 2.5 C=CCN1CCC23c4c5ccc(O)c4O[C@@H]2/C(=N/NC(=O)c2ccccc2)CCC3(O)C1C5 10.1016/j.bmcl.2006.05.060
CHEMBL378753 145961 0 None 1 3 Guinea pig 9.5 pKi = 9.5 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 445 4 3 6 2.5 C=CCN1CCC23c4c5ccc(O)c4O[C@@H]2/C(=N/NC(=O)c2ccccc2)CCC3(O)C1C5 10.1016/j.bmcl.2006.05.060
CHEMBL409204 219530 0 None - 1 Mouse 9.5 pKi = 9.5 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
15512237 211937 0 None 12 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 401 2 1 3 4.0 O=C1NCN(c2cccc(F)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL78156 211937 0 None 12 4 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 401 2 1 3 4.0 O=C1NCN(c2cccc(F)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
16131448 9624 28 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1681 9624 28 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
1688 9624 28 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
44361543 9624 28 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
56947112 9624 28 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
CHEMBL396460 9624 28 None 1 6 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1016/j.bmc.2007.04.026
10047612 10302 15 None 173 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/acs.jmedchem.5b01499
1693 10302 15 None 173 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/acs.jmedchem.5b01499
CHEMBL559569 10302 15 None 173 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 10.1021/acs.jmedchem.5b01499
11464846 84369 26 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL2088035 84369 26 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 440 4 1 5 3.6 CNC(=O)Cn1c(=O)n(C2CCN([C@@H]3Cc4cccc5cccc3c45)CC2)c2ccccc21 10.1021/jm201629q
CHEMBL1162357 215294 0 None - 1 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CCCCNC(=O)C[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
1682 9627 18 None 3 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human NOP receptorBinding affinity to human NOP receptor
ChEMBL None None None None 10.1021/jm800394v
6324645 9627 18 None 3 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human NOP receptorBinding affinity to human NOP receptor
ChEMBL None None None None 10.1021/jm800394v
CHEMBL384755 9627 18 None 3 2 Human 9.5 pKi = 9.5 Binding
Binding affinity to human NOP receptorBinding affinity to human NOP receptor
ChEMBL None None None None 10.1021/jm800394v
58268645 119422 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 5 0 7 5.0 Cc1nn(-c2ncccc2CN(C)C)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3236483 119422 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 5 0 7 5.0 Cc1nn(-c2ncccc2CN(C)C)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
CHEMBL3302938 119422 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]-nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 507 5 0 7 5.0 Cc1nn(-c2ncccc2CN(C)C)cc1CN1CCC2(CC1)OCC(F)(F)c1cc(Cl)sc12 10.1021/jm500117r
10276738 179040 0 None 54 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 466 5 2 3 6.1 NCc1ccccc1C1(O)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
CHEMBL4474536 179040 0 None 54 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 466 5 2 3 6.1 NCc1ccccc1C1(O)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
10763594 168056 1 None 120 4 Human 9.4 pKi = 9.4 Binding
Binding affinity to human nociceptin opioid receptorBinding affinity to human nociceptin opioid receptor
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1021/acs.jmedchem.5b01499
CHEMBL412098 168056 1 None 120 4 Human 9.4 pKi = 9.4 Binding
Binding affinity to human nociceptin opioid receptorBinding affinity to human nociceptin opioid receptor
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1021/acs.jmedchem.5b01499
10763594 168056 1 None 120 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1021/jm7009606
CHEMBL412098 168056 1 None 120 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 401 2 1 3 4.4 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CC[C@H]3CCCc4cccc1c43)CC2 10.1021/jm7009606
16131448 9624 28 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
1681 9624 28 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
1688 9624 28 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
44361543 9624 28 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
56947112 9624 28 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
CHEMBL396460 9624 28 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL None None None None 10.1021/jm7012979
16131448 9624 28 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1681 9624 28 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
1688 9624 28 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
44361543 9624 28 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
56947112 9624 28 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
CHEMBL396460 9624 28 None 1 6 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL None None None None 10.1016/j.bmc.2010.07.034
60154200 84381 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 434 5 0 4 3.8 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088059 84381 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 434 5 0 4 3.8 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL261997 217303 8 None - 1 Mouse 9.4 pKi = 9.4 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44430038 94142 0 None 5 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 352 7 2 3 4.4 CCCCC(c1ccccc1)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233326 94142 0 None 5 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 352 7 2 3 4.4 CCCCC(c1ccccc1)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
23383556 186136 0 None 25 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 9 1 4 5.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL473700 186136 0 None 25 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 9 1 4 5.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190623 196492 0 None 204 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 502 8 1 4 5.6 CC(C)CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL515575 196492 0 None 204 4 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 502 8 1 4 5.6 CC(C)CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
118662460 177907 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 354 4 0 2 4.4 CN(C)C1(c2ccccc2)CCC2(CCN(C(=O)CC3CCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
CHEMBL4458273 177907 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 354 4 0 2 4.4 CN(C)C1(c2ccccc2)CCC2(CCN(C(=O)CC3CCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
10156591 127337 0 None 22 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 379 6 2 2 4.8 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccc(F)cc23)CC1 10.1021/ml500116x
CHEMBL3326223 127337 0 None 22 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 379 6 2 2 4.8 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccc(F)cc23)CC1 10.1021/ml500116x
CHEMBL3545623 127337 0 None 22 2 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 379 6 2 2 4.8 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccc(F)cc23)CC1 10.1021/ml500116x
1691 8888 23 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm201629q
5311194 8888 23 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm201629q
CHEMBL357076 8888 23 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1021/jm201629q
15512229 10158 0 None -1 7 Rat 9.4 pKi = 9.4 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(00)00111-6
8864 10158 0 None -1 7 Rat 9.4 pKi = 9.4 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(00)00111-6
CHEMBL355202 10158 0 None -1 7 Rat 9.4 pKi = 9.4 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10.1016/s0960-894x(00)00111-6
CHEMBL411621 219731 0 None 301 2 Human 9.4 pKi = 9.4 Binding
Receptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cellsReceptor binding affinity for recombinant human N/OFQ peptide receptor (NOP) expressed in chinese hamster ovary cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm040106v
11004121 113820 0 None 60 4 Human 9.4 pKi = 9.4 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 409 2 0 3 5.4 CN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN(C2CCCCCCCCC2)CC1 10.1021/jm0209174
CHEMBL315551 113820 0 None 60 4 Human 9.4 pKi = 9.4 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 409 2 0 3 5.4 CN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN(C2CCCCCCCCC2)CC1 10.1021/jm0209174
60154191 84374 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088041 84374 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088042 84374 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
24894426 192546 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 404 3 1 3 5.3 O[C@H]1C[C@H](CN2CCC(c3c(Cl)cccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
CHEMBL486644 192546 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 404 3 1 3 5.3 O[C@H]1C[C@H](CN2CCC(c3c(Cl)cccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
CHEMBL415584 219971 0 None - 1 Human 9.3 pKi = 9.3 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
16131448 9624 28 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
1681 9624 28 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
1688 9624 28 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
44361543 9624 28 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
56947112 9624 28 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
CHEMBL396460 9624 28 None 1 6 Human 9.3 pKi = 9.3 Binding
Binding affinity to human NOP receptor by radioligand displacement assayBinding affinity to human NOP receptor by radioligand displacement assay
ChEMBL None None None None 10.1016/j.ejmech.2013.01.044
44297539 201459 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 394 3 0 2 5.6 CC(C)C1CCC(N2CCC3(CC2)C(c2ccccc2)C[C@H]2CN(C)C[C@H]23)CC1 10.1016/j.bmcl.2003.09.068
CHEMBL53256 201459 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 394 3 0 2 5.6 CC(C)C1CCC(N2CCC3(CC2)C(c2ccccc2)C[C@H]2CN(C)C[C@H]23)CC1 10.1016/j.bmcl.2003.09.068
19347356 127306 0 None -2 3 Rat 9.3 pKi = 9.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 383 2 1 3 4.7 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL354545 127306 0 None -2 3 Rat 9.3 pKi = 9.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 383 2 1 3 4.7 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
9824565 94526 0 None 501 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 440 5 2 3 5.5 NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233750 94526 0 None 501 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 440 5 2 3 5.5 NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
9866158 94705 0 None 74 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 408 5 2 3 4.5 NCc1ccccc1C1(O)CCN(C(c2ccccc2F)c2ccccc2F)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233955 94705 0 None 74 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 408 5 2 3 4.5 NCc1ccccc1C1(O)CCN(C(c2ccccc2F)c2ccccc2F)CC1 10.1016/j.bmcl.2007.03.062
44430042 161179 0 None 144 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 406 5 2 3 4.9 NCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL398794 161179 0 None 144 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 406 5 2 3 4.9 NCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
44430044 161528 0 None 380 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 400 5 2 3 4.8 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL400035 161528 0 None 380 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 400 5 2 3 4.8 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
23383564 176129 0 None 3 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 366 8 2 3 4.8 CCCCCC(c1ccccc1)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL441914 176129 0 None 3 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 366 8 2 3 4.8 CCCCCC(c1ccccc1)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
25190602 186003 0 None 50 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 8 1 4 4.6 O=C1N(CCNCC2CC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL472669 186003 0 None 50 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 8 1 4 4.6 O=C1N(CCNCC2CC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
25190619 186085 0 None 123 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 7 1 4 5.2 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL473279 186085 0 None 123 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 7 1 4 5.2 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190622 186265 0 None 131 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 8 1 4 5.3 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL474096 186265 0 None 131 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 8 1 4 5.3 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190605 187271 0 None 15 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 8 1 4 4.9 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475310 187271 0 None 15 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 8 1 4 4.9 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190603 196595 0 None 57 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 7 1 4 4.8 O=C1N(CCNC2CCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL516389 196595 0 None 57 4 Human 9.3 pKi = 9.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 7 1 4 4.8 O=C1N(CCNC2CCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
44437610 152297 0 None 42 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391487 152297 0 None 42 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
118722882 127332 0 None 43 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 336 7 1 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325879 127332 0 None 43 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 336 7 1 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545617 127332 0 None 43 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 336 7 1 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCCc2ccccc2)CC1 10.1021/ml500116x
118711485 127335 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 342 6 1 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)CCC2CCCC2)CC1 10.1021/ml500116x
CHEMBL3326220 127335 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 342 6 1 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)CCC2CCCC2)CC1 10.1021/ml500116x
CHEMBL3545621 127335 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 342 6 1 2 4.5 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)CCC2CCCC2)CC1 10.1021/ml500116x
11329662 102977 0 None 107 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CC[C@H](Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
CHEMBL260767 102977 0 None 107 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CC[C@H](Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
10022859 105946 1 None 10 4 Human 9.3 pKi = 9.3 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1021/jm991129q
CHEMBL281274 105946 1 None 10 4 Human 9.3 pKi = 9.3 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1021/jm991129q
15512228 74530 0 None 8 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-orphanin FQ from human nociceptin opioid receptor expressed in HEK293 cell membranesDisplacement of [3H]-orphanin FQ from human nociceptin opioid receptor expressed in HEK293 cell membranes
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1Cc3cccc4cccc1c34)CC2 10.1021/acs.jmedchem.5b01499
CHEMBL1907858 74530 0 None 8 3 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]-orphanin FQ from human nociceptin opioid receptor expressed in HEK293 cell membranesDisplacement of [3H]-orphanin FQ from human nociceptin opioid receptor expressed in HEK293 cell membranes
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1Cc3cccc4cccc1c34)CC2 10.1021/acs.jmedchem.5b01499
10927662 113903 0 None 251 4 Human 9.3 pKi = 9.3 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 407 2 0 3 4.9 CN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN([C@H]2CC[C@@H]3CCCC[C@@H]3C2)CC1 10.1021/jm0209174
CHEMBL316086 113903 0 None 251 4 Human 9.3 pKi = 9.3 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 407 2 0 3 4.9 CN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN([C@H]2CC[C@@H]3CCCC[C@@H]3C2)CC1 10.1021/jm0209174
25208249 190744 0 None 194 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 441 3 0 4 7.6 CC1(N2CCC(n3c(-c4cc5ccccc5o4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481707 190744 0 None 194 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 441 3 0 4 7.6 CC1(N2CCC(n3c(-c4cc5ccccc5o4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL3809510 219054 0 None 616 4 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL None None None CC[C@H](C)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
68632142 160395 0 None 2 2 Human 9.3 pKi = 9.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 480 5 0 2 6.7 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL3980782 160395 0 None 2 2 Human 9.3 pKi = 9.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 480 5 0 2 6.7 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL507269 221065 0 None - 1 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
10430819 85412 0 None 363 4 Human 9.3 pKi = 9.3 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 395 3 0 3 4.7 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(C)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112345 85412 0 None 363 4 Human 9.3 pKi = 9.3 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 395 3 0 3 4.7 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(C)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
118711490 127345 0 None -2 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 373 2 1 2 4.9 CN(C)[C@]1(c2ccccc2)CC[C@@]2(CC1)c1[nH]c3ccccc3c1CCN2C 10.1021/ml500117c
CHEMBL3326229 127345 0 None -2 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 373 2 1 2 4.9 CN(C)[C@]1(c2ccccc2)CC[C@@]2(CC1)c1[nH]c3ccccc3c1CCN2C 10.1021/ml500117c
CHEMBL3545631 127345 0 None -2 2 Human 9.3 pKi = 9.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 373 2 1 2 4.9 CN(C)[C@]1(c2ccccc2)CC[C@@]2(CC1)c1[nH]c3ccccc3c1CCN2C 10.1021/ml500117c
16131448 9624 28 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
1681 9624 28 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
1688 9624 28 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
44361543 9624 28 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
56947112 9624 28 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
CHEMBL396460 9624 28 None 1 6 Human 9.3 pKi = 9.3 Binding
Displacement of radiolabeled nociceptin from human ORL1 receptorDisplacement of radiolabeled nociceptin from human ORL1 receptor
ChEMBL None None None None 10.1021/jm8007618
44426832 92480 0 None 14 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 5 1 2 5.3 CCc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228848 92480 0 None 14 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 5 1 2 5.3 CCc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44430087 93648 0 None 309 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 615 8 1 5 5.9 CC(C)S(=O)(=O)N1CCN(Cc2ccccc2C2(O)CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232286 93648 0 None 309 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 615 8 1 5 5.9 CC(C)S(=O)(=O)N1CCN(Cc2ccccc2C2(O)CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.03.062
25190629 185894 0 None 41 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 522 8 1 4 6.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)ccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL471880 185894 0 None 41 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 522 8 1 4 6.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)ccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190604 196369 0 None 21 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 8 1 4 4.6 CCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL514662 196369 0 None 21 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 8 1 4 4.6 CCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
46879580 12640 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 476 4 1 4 3.7 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079400 12640 0 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 476 4 1 4 3.7 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL427791 220161 0 None - 1 Mouse 9.2 pKi = 9.2 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(C#N)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
1682 9627 18 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm800394v
6324645 9627 18 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm800394v
CHEMBL384755 9627 18 None 3 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm800394v
25207946 198077 0 None 91 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 469 3 0 3 7.9 CC1(N2CCC(n3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL519100 198077 0 None 91 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 469 3 0 3 7.9 CC1(N2CCC(n3c(-c4cccc(C(F)(F)F)c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
10022859 105946 1 None 10 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL281274 105946 1 None 10 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
11014751 119419 0 None 87 4 Human 9.2 pKi = 9.2 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 395 2 0 3 5.0 CN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN(C2CCCCCCCC2)CC1 10.1021/jm0209174
CHEMBL330291 119419 0 None 87 4 Human 9.2 pKi = 9.2 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 395 2 0 3 5.0 CN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN(C2CCCCCCCC2)CC1 10.1021/jm0209174
44253418 158849 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 442 6 0 3 5.7 COc1ccc(C(=O)N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
CHEMBL3967435 158849 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 442 6 0 3 5.7 COc1ccc(C(=O)N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
11761926 85409 0 None 380 4 Human 9.2 pKi = 9.2 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 437 6 0 3 5.9 CCCCN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN([C@H]2CC[C@@H](C(C)C)CC2)CC1 10.1021/jm0209174
CHEMBL2112342 85409 0 None 380 4 Human 9.2 pKi = 9.2 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 437 6 0 3 5.9 CCCCN1C[C@@H]2[C@H](C1)CN(c1ccccc1)C21CCN([C@H]2CC[C@@H](C(C)C)CC2)CC1 10.1021/jm0209174
9997843 106441 0 None 8 4 Human 9.2 pKi = 9.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 347 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL284414 106441 0 None 8 4 Human 9.2 pKi = 9.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 347 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc31)CC2 10.1021/jm991129q
9863568 148867 0 None 45 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 148867 0 None 45 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 148867 0 None 45 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 148867 0 None 45 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44430050 93791 0 None 234 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 454 6 2 3 5.8 CNCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232477 93791 0 None 234 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 454 6 2 3 5.8 CNCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
44430040 94143 0 None 39 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 386 5 2 3 4.5 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233327 94143 0 None 39 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 386 5 2 3 4.5 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2CN)CC1 10.1016/j.bmcl.2007.03.062
25190625 185896 0 None 37 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 528 7 1 4 6.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CCCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL471882 185896 0 None 37 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 528 7 1 4 6.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CCCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
25190601 187619 0 None 56 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 7 1 4 4.6 CC(C)NCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475707 187619 0 None 56 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 7 1 4 4.6 CC(C)NCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190600 196434 0 None 75 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 460 7 1 4 4.2 CCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL515142 196434 0 None 75 4 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 460 7 1 4 4.2 CCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
118662189 181379 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 379 4 0 3 4.3 CN(C)C1(c2ccccc2)CCC2(CCN(C(=O)CC3(C#N)CCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
CHEMBL4557245 181379 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 379 4 0 3 4.3 CN(C)C1(c2ccccc2)CCC2(CCN(C(=O)CC3(C#N)CCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
45102745 12815 0 None 97 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080485 12815 0 None 97 4 Human 9.2 pKi = 9.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44252989 153214 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 375 5 1 2 5.6 CN(CC1(C)CCC(c2ccccc2)(N(C)C)CC1)c1c[nH]c2ccccc12 nan
CHEMBL3921976 153214 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 375 5 1 2 5.6 CN(CC1(C)CCC(c2ccccc2)(N(C)C)CC1)c1c[nH]c2ccccc12 nan
25001412 69425 0 None 33 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL1783826 69425 0 None 33 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
53324890 64080 0 None 416 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 469 4 1 4 6.6 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650842 64080 0 None 416 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 469 4 1 4 6.6 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
10928037 85415 0 None 169 4 Human 9.1 pKi = 9.1 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 425 5 1 4 4.1 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(CCO)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112348 85415 0 None 169 4 Human 9.1 pKi = 9.1 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 425 5 1 4 4.1 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(CCO)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
1682 9627 18 None -3 2 Mouse 9.1 pKi = 9.1 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None None 10.1021/jm990075h
6324645 9627 18 None -3 2 Mouse 9.1 pKi = 9.1 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None None 10.1021/jm990075h
CHEMBL384755 9627 18 None -3 2 Mouse 9.1 pKi = 9.1 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None None 10.1021/jm990075h
CHEMBL389521 219206 0 None - 1 Mouse 9.1 pKi = 9.1 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm990075h
CHEMBL405648 219351 0 None - 1 Mouse 9.1 pKi = 9.1 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
25190618 186084 0 None 218 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 7 1 4 4.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL473278 186084 0 None 218 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 7 1 4 4.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
25190599 196802 0 None 85 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 446 6 1 4 3.9 CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL517167 196802 0 None 85 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 446 6 1 4 3.9 CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
44438988 97985 0 None 17 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 379 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3c(F)cccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240005 97985 0 None 17 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 379 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3c(F)cccc31)CC2 10.1016/j.bmcl.2007.01.069
118662074 177648 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 346 4 0 3 5.0 CN(C)C1(c2cccs2)CCC2(CCN(CC3CCCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
CHEMBL4454146 177648 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 346 4 0 3 5.0 CN(C)C1(c2cccs2)CCC2(CCN(CC3CCCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
44253136 154099 0 None 6 2 Human 9.1 pKi = 9.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 399 6 0 3 5.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccnc2)CC1 nan
CHEMBL3929120 154099 0 None 6 2 Human 9.1 pKi = 9.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 399 6 0 3 5.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccnc2)CC1 nan
CHEMBL269029 217554 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human NOP receptorBinding affinity to human NOP receptor
ChEMBL None None None C[C@H](NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
44451649 102933 0 None 57 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 1 8 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL260556 102933 0 None 57 4 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 1 8 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL412537 219781 0 None - 1 Mouse 9.1 pKi = 9.1 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1cccc(F)c1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44430085 93637 0 None 162 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 601 8 1 5 5.5 CCS(=O)(=O)N1CCN(Cc2ccccc2C2(O)CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232285 93637 0 None 162 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 601 8 1 5 5.5 CCS(=O)(=O)N1CCN(Cc2ccccc2C2(O)CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.03.062
25190616 187079 0 None 223 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 472 7 1 4 4.7 C=CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475094 187079 0 None 223 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 472 7 1 4 4.7 C=CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190614 196345 0 None 37 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 514 6 1 4 5.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL514463 196345 0 None 37 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 514 6 1 4 5.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
25190613 196426 0 None 54 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 500 6 1 4 5.5 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL515091 196426 0 None 54 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 500 6 1 4 5.5 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
18782352 97907 0 None 38 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 379 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccc(F)cc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL239824 97907 0 None 38 4 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 379 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccc(F)cc31)CC2 10.1016/j.bmcl.2007.01.069
11848225 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
8866 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL2364605 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3545616 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3962932 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
11848225 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
8866 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL2364605 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL3545616 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
CHEMBL3962932 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Displacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting methodDisplacement of [leucyl-3H]nociceptin from human nociceptin opioid receptor expressed in HEK293 cell membranes after 90 mins by scintillation counting method
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/acs.jmedchem.5b01499
1682 9627 18 None -3 2 Mouse 9.0 pKi = 9.0 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None None 10.1021/jm010221v
6324645 9627 18 None -3 2 Mouse 9.0 pKi = 9.0 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None None 10.1021/jm010221v
CHEMBL384755 9627 18 None -3 2 Mouse 9.0 pKi = 9.0 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None None 10.1021/jm010221v
10000890 127409 0 None -3 3 Rat 9.0 pKi = 9.0 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 397 2 1 3 5.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL354652 127409 0 None -3 3 Rat 9.0 pKi = 9.0 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 397 2 1 3 5.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
53322245 64086 0 None 288 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 439 4 2 6 3.9 CC1CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
CHEMBL1650848 64086 0 None 288 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 439 4 2 6 3.9 CC1CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
70690760 83440 0 None 85 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 433 5 0 3 3.9 Cc1cccc(C)c1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064160 83440 0 None 85 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 433 5 0 3 3.9 Cc1cccc(C)c1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL406905 219408 0 None - 1 Mouse 9.0 pKi = 9 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)CC1CCCCC1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
44248674 110177 0 None 602 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 442 4 0 2 6.8 CN1CCCCC1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL3084677 110177 0 None 602 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 442 4 0 2 6.8 CN1CCCCC1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
10109899 92485 0 None 28 4 Human 9.0 pKi = 9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 373 5 1 3 4.8 COc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228857 92485 0 None 28 4 Human 9.0 pKi = 9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 373 5 1 3 4.8 COc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
25190615 186080 0 None 42 4 Human 9.0 pKi = 9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 7 1 4 4.9 CCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL473272 186080 0 None 42 4 Human 9.0 pKi = 9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 7 1 4 4.9 CCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190606 186137 0 None 56 4 Human 9.0 pKi = 9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 8 0 4 5.0 CCN(CC)CCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL473701 186137 0 None 56 4 Human 9.0 pKi = 9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 488 8 0 4 5.0 CCN(CC)CCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
44437619 98003 0 None 22 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 497 10 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL240074 98003 0 None 22 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 497 10 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437610 152297 0 None 42 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437610 152297 0 None 42 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
CHEMBL391487 152297 0 None 42 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391487 152297 0 None 42 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
10301207 155434 0 None 26 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 511 11 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL393960 155434 0 None 26 4 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 511 11 0 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCSC)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
11956680 127336 0 None -2 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3325961 127336 0 None -2 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3545622 127336 0 None -2 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 376 2 2 3 4.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(O)ccc3[nH]c12 10.1021/ml500117c
CHEMBL265544 217432 0 None - 1 Mouse 9.0 pKi = 9 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(C(F)(F)F)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
CHEMBL436732 220466 0 None - 1 Human 9.0 pKi = 9.0 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N(C)[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
44430043 94323 0 None 66 4 Human 9.0 pKi = 9.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 450 5 2 3 5.0 NCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233536 94323 0 None 66 4 Human 9.0 pKi = 9.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 450 5 2 3 5.0 NCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.062
24894428 193106 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 370 3 1 3 4.6 O[C@H]1C[C@H](CN2CCC(c3ccccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
CHEMBL487485 193106 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 370 3 1 3 4.6 O[C@H]1C[C@H](CN2CCC(c3ccccc3Cl)CC2)CCc2cccnc21 10.1021/jm701590h
44438961 151762 0 None 11 4 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 377 6 1 3 4.3 CCCCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL391082 151762 0 None 11 4 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 377 6 1 3 4.3 CCCCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
118662342 178434 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 390 6 0 4 4.3 COC1(CCN2CC3(CCC(c4cccs4)(N(C)C)CC3)CC2=O)CCC1 10.1021/acsmedchemlett.6b00277
CHEMBL4466096 178434 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 390 6 0 4 4.3 COC1(CCN2CC3(CCC(c4cccs4)(N(C)C)CC3)CC2=O)CCC1 10.1021/acsmedchemlett.6b00277
9925137 127340 0 None 8 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3326222 127340 0 None 8 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3545626 127340 0 None 8 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 361 6 2 2 4.7 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
24798599 127349 0 None -3 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 346 2 2 2 4.6 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3326232 127349 0 None -3 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 346 2 2 2 4.6 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3545637 127349 0 None -3 2 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 346 2 2 2 4.6 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3ccccc3[nH]c12 10.1021/ml500117c
58358709 132579 0 None 56 4 Human 9.0 pKi = 9.0 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 449 3 1 5 4.9 C[C@H]1C[C@H]2C[C@@H](C1)C[C@H](N1[C@H]3CCC[C@@H]1C[C@H](n1c(=O)c(C(=O)O)nc4ccccc41)C3)C2 nan
CHEMBL3647962 132579 0 None 56 4 Human 9.0 pKi = 9.0 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 449 3 1 5 4.9 C[C@H]1C[C@H]2C[C@@H](C1)C[C@H](N1[C@H]3CCC[C@@H]1C[C@H](n1c(=O)c(C(=O)O)nc4ccccc41)C3)C2 nan
1684 10135 21 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
9844019 10135 21 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
CHEMBL2088034 10135 21 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10.1021/jm201629q
9997843 106441 0 None 8 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 347 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL284414 106441 0 None 8 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 347 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
44451621 102688 0 None 35 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 10 0 8 5.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cscn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259263 102688 0 None 35 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 10 0 8 5.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cscn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
10430819 85412 0 None 363 4 Human 8.9 pKi = 8.9 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 395 3 0 3 4.7 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(C)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112345 85412 0 None 363 4 Human 8.9 pKi = 8.9 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 395 3 0 3 4.7 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(C)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
15512234 112224 0 None 15 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 417 2 1 3 4.5 O=C1NCN(c2cccc(Cl)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL312021 112224 0 None 15 4 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 417 2 1 3 4.5 O=C1NCN(c2cccc(Cl)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
68917692 120768 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 358 2 1 1 5.8 CN(C)[C@]1(c2ccccc2)CC[C@@]2(CCCc3c4ccccc4[nH]c32)CC1 10.1021/ml500117c
CHEMBL3326231 120768 0 None 1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 358 2 1 1 5.8 CN(C)[C@]1(c2ccccc2)CC[C@@]2(CCCc3c4ccccc4[nH]c32)CC1 10.1021/ml500117c
44224242 154763 0 None 6 2 Human 8.9 pKi = 8.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 398 6 0 2 6.0 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2ccccc2)CC1 nan
CHEMBL3934183 154763 0 None 6 2 Human 8.9 pKi = 8.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 398 6 0 2 6.0 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2ccccc2)CC1 nan
25190624 97906 0 None 37 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 389 2 1 3 4.2 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL239822 97906 0 None 37 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 389 2 1 3 4.2 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
25190624 97906 0 None 37 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 389 2 1 3 4.2 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2007.01.069
CHEMBL239822 97906 0 None 37 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 389 2 1 3 4.2 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2007.01.069
46880033 14396 0 None 26 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 438 4 1 5 4.1 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCC4(CCCCC4)C3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1088171 14396 0 None 26 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 438 4 1 5 4.1 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCC4(CCCCC4)C3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
9905428 11181 16 None 21 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
CHEMBL101454 11181 16 None 21 3 Human 8.9 pKi = 8.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/jm034249d
9905428 11181 16 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL101454 11181 16 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
10714523 105883 1 None 22 4 Human 8.9 pKi = 8.9 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 375 2 1 3 3.8 Cc1cccc2c1CCCC2N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm991129q
CHEMBL280827 105883 1 None 22 4 Human 8.9 pKi = 8.9 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 375 2 1 3 3.8 Cc1cccc2c1CCCC2N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm991129q
25190621 186158 0 None 48 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 5 0 4 5.0 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCN2CCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL473898 186158 0 None 48 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 5 0 4 5.0 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCN2CCCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
25190612 196350 0 None 47 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 6 1 4 4.9 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL514489 196350 0 None 47 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 474 6 1 4 4.9 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
9947044 105047 0 None 15 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL27460 105047 0 None 15 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
44439000 155249 0 None 34 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 423 2 1 3 4.9 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2007.01.069
CHEMBL393807 155249 0 None 34 4 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 423 2 1 3 4.9 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccc(Cl)cc21 10.1016/j.bmcl.2007.01.069
9905428 11181 16 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b00982
CHEMBL101454 11181 16 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b00982
9905428 11181 16 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranesDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b01499
CHEMBL101454 11181 16 None 21 3 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranesDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranes
ChEMBL 326 2 0 2 4.2 O=C1Cc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b01499
44451918 102868 0 None 31 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 7 6.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cccs4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL260169 102868 0 None 31 2 Human 8.9 pKi = 8.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 7 6.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cccs4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
68633222 156914 0 None 27 2 Human 8.9 pKi = 8.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 416 6 0 2 6.2 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccc(F)c2)CC1 nan
CHEMBL3951319 156914 0 None 27 2 Human 8.9 pKi = 8.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 416 6 0 2 6.2 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccc(F)c2)CC1 nan
49843555 64082 0 None 138 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 451 4 2 6 3.8 OCC1(N2CCC(n3c(N4CC5CNCC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650844 64082 0 None 138 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 451 4 2 6 3.8 OCC1(N2CCC(n3c(N4CC5CNCC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
134578457 180734 0 None 309 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 407 5 0 3 6.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCCC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4541337 180734 0 None 309 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 407 5 0 3 6.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCCC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
25190617 186260 0 None 29 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 6 1 4 5.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL474092 186260 0 None 29 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 6 1 4 5.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCC2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
44438962 173376 0 None 16 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 391 6 1 3 4.6 CC(C)CCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL428033 173376 0 None 16 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 391 6 1 3 4.6 CC(C)CCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
19347398 127240 0 None -1 3 Rat 8.8 pKi = 8.8 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 395 3 1 3 4.6 O=C1NCN(c2ccccc2)C12CCN([C@H]1CC[C@@H](C3CCCCC3)CC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL354065 127240 0 None -1 3 Rat 8.8 pKi = 8.8 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 395 3 1 3 4.6 O=C1NCN(c2ccccc2)C12CCN([C@H]1CC[C@@H](C3CCCCC3)CC1)CC2 10.1016/s0960-894x(00)00111-6
44451595 102745 0 None 25 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 7 6.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ccsc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259511 102745 0 None 25 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 7 6.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ccsc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44252684 150186 0 None 5 2 Human 8.8 pKi = 8.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 364 7 0 2 5.6 CCCCN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3898034 150186 0 None 5 2 Human 8.8 pKi = 8.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 364 7 0 2 5.6 CCCCN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
15512243 109699 0 None 15 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 401 2 1 3 4.0 O=C1NCN(c2ccc(F)cc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL306150 109699 0 None 15 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 401 2 1 3 4.0 O=C1NCN(c2ccc(F)cc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
15512240 211851 0 None 19 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 417 2 1 3 4.5 O=C1NCN(c2ccc(Cl)cc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL77324 211851 0 None 19 3 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 417 2 1 3 4.5 O=C1NCN(c2ccc(Cl)cc2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
44252536 160072 0 None -6 2 Human 8.8 pKi = 8.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 441 6 1 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)NCc2ccccc2)CC1 nan
CHEMBL3977883 160072 0 None -6 2 Human 8.8 pKi = 8.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 441 6 1 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)NCc2ccccc2)CC1 nan
44430023 94298 0 None 79 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 372 5 2 3 4.2 NCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233503 94298 0 None 79 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 372 5 2 3 4.2 NCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
25190611 186756 0 None 23 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 460 6 1 4 4.6 CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL474687 186756 0 None 23 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 460 6 1 4 4.6 CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
118662159 180495 0 None -1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 379 5 0 3 4.3 CN(C)C1(c2ccccc2)CCC2(CC1)CC(=O)N(CCC1(C#N)CCC1)C2 10.1021/acsmedchemlett.6b00277
CHEMBL4536065 180495 0 None -1 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 379 5 0 3 4.3 CN(C)C1(c2ccccc2)CCC2(CC1)CC(=O)N(CCC1(C#N)CCC1)C2 10.1021/acsmedchemlett.6b00277
11315651 84371 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 403 5 0 5 3.1 CN(C)C(=O)C(Cc1cscn1)CN1CCC2(CC1)OCc1ccc(F)cc12 10.1021/jm201629q
CHEMBL2088037 84371 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 403 5 0 5 3.1 CN(C)C(=O)C(Cc1cscn1)CN1CCC2(CC1)OCc1ccc(F)cc12 10.1021/jm201629q
10961428 85413 0 None 102 4 Human 8.8 pKi = 8.8 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 453 5 0 3 5.7 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(CC4CC4)C[C@@H]2CN3c2ccc(F)cc2)CC1 10.1021/jm0209174
CHEMBL2112346 85413 0 None 102 4 Human 8.8 pKi = 8.8 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 453 5 0 3 5.7 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(CC4CC4)C[C@@H]2CN3c2ccc(F)cc2)CC1 10.1021/jm0209174
10950562 85414 0 None 81 4 Human 8.8 pKi = 8.8 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 457 4 0 3 6.3 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(c4ccccc4)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112347 85414 0 None 81 4 Human 8.8 pKi = 8.8 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 457 4 0 3 6.3 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(c4ccccc4)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
44451569 103173 0 None 58 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 535 10 0 9 5.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncsn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL261839 103173 0 None 58 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 535 10 0 9 5.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncsn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
11848793 196103 0 None 22 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 464 5 1 2 6.1 NC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL512414 196103 0 None 22 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 464 5 1 2 6.1 NC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
25190609 186405 0 None 34 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 433 4 1 4 3.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCO)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL474283 186405 0 None 34 4 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 433 4 1 4 3.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCO)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
25208247 190724 0 None 89 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 440 3 1 3 7.3 CC1(N2CCC(n3c(-c4ccc5cc[nH]c5c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL481548 190724 0 None 89 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 440 3 1 3 7.3 CC1(N2CCC(n3c(-c4ccc5cc[nH]c5c4)nc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
45102745 14330 0 None 117 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087657 14330 0 None 117 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44451649 102933 0 None 57 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 1 8 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL260556 102933 0 None 57 4 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 1 8 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
11626062 145727 0 None 79 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 426 2 2 3 4.1 Oc1ccc(Br)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3785095 145727 0 None 79 2 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 426 2 2 3 4.1 Oc1ccc(Br)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL507653 221223 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells
ChEMBL None None None C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC(=O)O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm800394v
10766007 37670 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 451 5 2 4 6.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(C(F)(F)F)cc3)ccc2n1 10.1021/jm0002073
CHEMBL139776 37670 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 451 5 2 4 6.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(C(F)(F)F)cc3)ccc2n1 10.1021/jm0002073
10789513 38580 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 445 7 2 4 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
CHEMBL140640 38580 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 445 7 2 4 6.3 CCCc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
10765154 175074 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 431 6 2 4 5.9 CCc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
CHEMBL434060 175074 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 431 6 2 4 5.9 CCc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
9958643 94706 0 None 151 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 528 5 2 3 5.7 NCc1ccccc1C1(O)CCN(C(c2ccccc2Br)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233956 94706 0 None 151 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 528 5 2 3 5.7 NCc1ccccc1C1(O)CCN(C(c2ccccc2Br)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.062
25190628 195950 0 None 7 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4c(Cl)cccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL511161 195950 0 None 7 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4c(Cl)cccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL406097 219374 0 None - 1 Mouse 8.7 pKi = 8.7 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(Br)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
60154191 84374 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088041 84374 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088042 84374 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
44451748 167811 0 None 20 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 0 9 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4cncn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL411643 167811 0 None 20 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 0 9 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4cncn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44430083 93543 0 None 75 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 509 6 2 4 5.5 OC1(c2ccccc2CN2CCNCC2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232075 93543 0 None 75 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 509 6 2 4 5.5 OC1(c2ccccc2CN2CCNCC2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
44574588 185215 0 None 54 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 443 4 1 2 6.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCC2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL466067 185215 0 None 54 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 443 4 1 2 6.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCC2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
12986253 127330 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 379 7 2 2 4.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325881 127330 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 379 7 2 2 4.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545610 127330 0 None -2 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 379 7 2 2 4.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](NC(=O)NCCCc2ccccc2)CC1 10.1021/ml500116x
19347402 127233 0 None 4 3 Rat 8.7 pKi = 8.7 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 341 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL353990 127233 0 None 4 3 Rat 8.7 pKi = 8.7 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 341 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL265801 217442 0 None - 1 Mouse 8.7 pKi = 8.7 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(N)=O 10.1021/jm010221v
15512228 74530 0 None 8 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL1907858 74530 0 None 8 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 383 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN([C@H]1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
44451650 102978 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CC[C@H](Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
CHEMBL260768 102978 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CC[C@H](Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
CHEMBL410396 219597 17 None -1 2 Mouse 8.0 pKi = 8 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
44252685 158072 0 None 1 2 Human 8.0 pKi = 8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 502 7 0 2 7.2 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)C(c2ccccc2)c2ccccc2)CC1 nan
CHEMBL3960588 158072 0 None 1 2 Human 8.0 pKi = 8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 502 7 0 2 7.2 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)C(c2ccccc2)c2ccccc2)CC1 nan
44248920 110170 0 None 27 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1cccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1021/jm9008218
CHEMBL3084667 110170 0 None 27 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1cccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1021/jm9008218
44413442 86718 0 None 26 4 Human 8.0 pKi = 8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 400 2 1 1 6.8 Cc1[nH]c2ccc(Cl)cc2c1C1CCN(C2Cc3cccc4cccc2c34)CC1 10.1016/j.bmcl.2006.03.094
CHEMBL212575 86718 0 None 26 4 Human 8.0 pKi = 8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 400 2 1 1 6.8 Cc1[nH]c2ccc(Cl)cc2c1C1CCN(C2Cc3cccc4cccc2c34)CC1 10.1016/j.bmcl.2006.03.094
118718290 122106 0 None 56 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 464 6 1 2 6.9 CNC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349274 122106 0 None 56 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 464 6 1 2 6.9 CNC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
11462727 196159 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 366 3 2 4 3.2 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
CHEMBL512896 196159 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 366 3 2 4 3.2 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
44574892 185441 0 None 33 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 506 6 1 2 7.2 CC(C)NC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467699 185441 0 None 33 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 506 6 1 2 7.2 CC(C)NC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
22725091 196190 0 None 2 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 439 4 1 4 5.4 OC1(c2cccnn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL513171 196190 0 None 2 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 439 4 1 4 5.4 OC1(c2cccnn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76335142 110107 0 None 34 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084540 110107 0 None 34 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76335143 110113 0 None 34 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 437 4 1 3 6.0 N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084547 110113 0 None 34 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 437 4 1 3 6.0 N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76313424 110116 0 None 60 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 497 5 1 3 6.3 CC(=O)N[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084550 110116 0 None 60 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 497 5 1 3 6.3 CC(=O)N[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76335144 110117 0 None 74 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 495 5 1 4 6.4 COC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084551 110117 0 None 74 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 495 5 1 4 6.4 COC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76313425 110120 0 None 28 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 512 6 1 2 7.1 NC(=O)[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084554 110120 0 None 28 2 Human 8.0 pKi = 8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 512 6 1 2 7.1 NC(=O)[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
15512239 211901 0 None -1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 451 2 1 3 4.9 O=C1NCN(c2cccc(C(F)(F)F)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL77877 211901 0 None -1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 451 2 1 3 4.9 O=C1NCN(c2cccc(C(F)(F)F)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
44315305 211939 0 None 1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 411 2 1 3 4.5 Cc1cc(C)cc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)c1 10.1016/s0960-894x(99)00385-6
CHEMBL78163 211939 0 None 1 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 411 2 1 3 4.5 Cc1cc(C)cc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)c1 10.1016/s0960-894x(99)00385-6
44437630 152340 0 None 6 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 1 7 4.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391518 152340 0 None 6 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 1 7 4.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
9922658 127348 0 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 308 5 1 2 4.2 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325751 127348 0 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 308 5 1 2 4.2 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545636 127348 0 None -3 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 308 5 1 2 4.2 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCc2ccccc2)CC1 10.1021/ml500116x
10713623 103751 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL26638 103751 0 None 1 3 Human 8.0 pKi = 8.0 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCCc3ccccc31)CC2 10.1021/jm991129q
11552010 145795 0 None 38 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)NC2 10.1016/j.ejmech.2016.02.014
CHEMBL3785728 145795 0 None 38 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)NC2 10.1016/j.ejmech.2016.02.014
52951941 90369 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2204346 90369 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 462 6 0 4 4.6 CC(C)N(C)C(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
129188459 181947 3 None 54 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 326 3 0 2 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(N3CCc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4570328 181947 3 None 54 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 326 3 0 2 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(N3CCc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
134563466 178071 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 412 5 2 3 4.8 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4460695 178071 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 412 5 2 3 4.8 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44391062 129402 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL360326 129402 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
18782376 98550 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 395 2 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccc(Cl)cc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL241085 98550 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 395 2 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccc(Cl)cc31)CC2 10.1016/j.bmcl.2007.01.069
44438964 154168 0 None 75 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 415 4 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1F)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL392969 154168 0 None 75 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 415 4 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1F)CC2 10.1016/j.bmcl.2007.01.069
10654047 219409 18 None -2 2 Mouse 7.0 pKi = 7 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
CHEMBL406946 219409 18 None -2 2 Mouse 7.0 pKi = 7 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
CHEMBL407461 219442 0 None - 1 Mouse 7.0 pKi = 7 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
24799509 104557 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 360 3 1 2 4.3 CC(C)(C)C1CCC(N2CCC(C(N)=O)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
CHEMBL271779 104557 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 360 3 1 2 4.3 CC(C)(C)C1CCC(N2CCC(C(N)=O)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
44574707 185567 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 446 4 0 2 7.2 N#CC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL468953 185567 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 446 4 0 2 7.2 N#CC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
15512242 109658 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 413 3 1 4 3.9 COc1ccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)cc1 10.1016/s0960-894x(99)00385-6
CHEMBL305861 109658 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 413 3 1 4 3.9 COc1ccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)cc1 10.1016/s0960-894x(99)00385-6
134134392 150473 0 None -331 3 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 309 3 1 2 4.2 Cc1ccc(C2(N(C)C)CCC(O)(c3ccccc3)CC2)cc1 nan
CHEMBL3900292 150473 0 None -331 3 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 309 3 1 2 4.2 Cc1ccc(C2(N(C)C)CCC(O)(c3ccccc3)CC2)cc1 nan
44426819 148779 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 292 3 1 3 3.2 N#CC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL387493 148779 0 None - 1 Human 5.0 pKi = 5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 292 3 1 3 3.2 N#CC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
70692893 83430 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 400 7 0 4 2.2 CCC(CC)N1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064137 83430 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 400 7 0 4 2.2 CCC(CC)N1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
44437610 152297 0 None 42 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391487 152297 0 None 42 4 Human 7.0 pKi = 7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 10 1 7 4.0 CNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44252534 159094 0 None -3 2 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 350 4 0 2 4.4 CC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3969636 159094 0 None -3 2 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 350 4 0 2 4.4 CC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44337550 116462 0 None 1 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 370 9 1 2 6.1 CCCCCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL322717 116462 0 None 1 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 370 9 1 2 6.1 CCCCCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
44252391 159703 0 None 23 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 5 0 2 4.5 CN(C)CC1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3974883 159703 0 None 23 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 5 0 2 4.5 CN(C)CC1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL143939 215551 19 None -3388 2 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None CC1(C)SSC(C)(C)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H]1C(=O)O 10.1016/j.bmcl.2006.05.060
24799325 104478 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 432 5 1 2 5.9 CC(C)(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3)CC2)CC1 10.1021/jm7009606
CHEMBL271342 104478 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 432 5 1 2 5.9 CC(C)(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3)CC2)CC1 10.1021/jm7009606
118718273 122089 0 None 38 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 497 6 0 3 6.7 CN(C)C[C@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349257 122089 0 None 38 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 497 6 0 3 6.7 CN(C)C[C@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44224242 154763 0 None 6 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 398 6 0 2 6.0 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2ccccc2)CC1 nan
CHEMBL3934183 154763 0 None 6 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 398 6 0 2 6.0 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2ccccc2)CC1 nan
10286996 170130 0 None 38 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 364 5 1 2 4.8 N[C@@H](c1cc(F)cc(F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL419179 170130 0 None 38 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 364 5 1 2 4.8 N[C@@H](c1cc(F)cc(F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
90656666 117728 0 None -186 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 481 5 2 5 4.8 CC[C@](O)([C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5)C(C)(C)C 10.1021/jm401964y
CHEMBL3262088 117728 0 None -186 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 481 5 2 5 4.8 CC[C@](O)([C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5)C(C)(C)C 10.1021/jm401964y
46880240 12825 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 429 5 1 6 2.9 CNC(=O)Cn1c(=O)n(C2CCN(Cc3nccc4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080521 12825 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 429 5 1 6 2.9 CNC(=O)Cn1c(=O)n(C2CCN(Cc3nccc4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
9836463 103608 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 313 3 1 2 3.0 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL26521 103608 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 313 3 1 2 3.0 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2003.11.083
68631642 155397 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 415 4 1 2 6.2 Cc1c(C2(N3CCCCC3)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccccc12 nan
CHEMBL3939293 155397 0 None -2 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 415 4 1 2 6.2 Cc1c(C2(N3CCCCC3)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccccc12 nan
46879478 12259 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 413 4 1 4 3.9 CNC(=O)CN1C(=O)OC2(CCN(C3CCC(C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1076208 12259 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 413 4 1 4 3.9 CNC(=O)CN1C(=O)OC2(CCN(C3CCC(C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44337230 13647 0 None 3 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 300 4 1 2 4.2 CC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL108417 13647 0 None 3 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 300 4 1 2 4.2 CC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
54581495 69423 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 434 7 0 5 4.1 O=C(OCCCN1CCC2(CC1)OCc1ccccc12)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL1783822 69423 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 434 7 0 5 4.1 O=C(OCCCN1CCC2(CC1)OCc1ccccc12)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
44253136 154099 0 None 6 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 399 6 0 3 5.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccnc2)CC1 nan
CHEMBL3929120 154099 0 None 6 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 399 6 0 3 5.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccnc2)CC1 nan
134144744 157399 0 None 2 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 436 6 1 3 6.2 CCCC(=O)OC1(c2[nH]c3ccccc3c2C)CCC(c2cccc(F)c2)(N(C)C)CC1 nan
CHEMBL3955335 157399 0 None 2 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 436 6 1 3 6.2 CCCC(=O)OC1(c2[nH]c3ccccc3c2C)CCC(c2cccc(F)c2)(N(C)C)CC1 nan
44391156 71644 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 457 7 2 6 4.8 Cc1ccc(Cl)c(OC(C(C)C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182144 71644 0 None -1 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 457 7 2 6 4.8 Cc1ccc(Cl)c(OC(C(C)C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44593575 185259 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 361 3 1 2 5.1 OC1CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466438 185259 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 361 3 1 2 5.1 OC1CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
105104 10675 40 None -794 11 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 356 4 0 3 3.3 O=C(N([C@H]1CC[C@]2(C[C@@H]1N1CCCC1)CCCO2)C)Cc1ccccc1 10.1016/j.bmcl.2006.05.060
1655 10675 40 None -794 11 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 356 4 0 3 3.3 O=C(N([C@H]1CC[C@]2(C[C@@H]1N1CCCC1)CCCO2)C)Cc1ccccc1 10.1016/j.bmcl.2006.05.060
1656 10675 40 None -794 11 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 356 4 0 3 3.3 O=C(N([C@H]1CC[C@]2(C[C@@H]1N1CCCC1)CCCO2)C)Cc1ccccc1 10.1016/j.bmcl.2006.05.060
CHEMBL440765 10675 40 None -794 11 Guinea pig 6.0 pKi = 6.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 356 4 0 3 3.3 O=C(N([C@H]1CC[C@]2(C[C@@H]1N1CCCC1)CCCO2)C)Cc1ccccc1 10.1016/j.bmcl.2006.05.060
68632581 155130 0 None -2 2 Human 8.0 pKi = 8.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 365 8 1 2 5.4 CN(C)C1(c2ccccc2)CCC(CO)(CCCCc2ccccc2)CC1 nan
CHEMBL3937167 155130 0 None -2 2 Human 8.0 pKi = 8.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 365 8 1 2 5.4 CN(C)C1(c2ccccc2)CCC(CO)(CCCCc2ccccc2)CC1 nan
10134077 108495 0 None 40 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 375 4 0 2 4.9 CCN1C(=O)N(C2CCN(CC3CCCCCCC3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL29953 108495 0 None 40 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 375 4 0 2 4.9 CCN1C(=O)N(C2CCN(CC3CCCCCCC3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
10159203 72384 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 421 7 1 5 5.5 Cc1ccc(C)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL183355 72384 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 421 7 1 5 5.5 Cc1ccc(C)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44391062 129402 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL360326 129402 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 441 7 1 5 5.8 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44426836 148894 0 None 15 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 421 4 1 2 5.5 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388314 148894 0 None 15 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 421 4 1 2 5.5 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.061
20481138 93628 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232273 93628 0 None 6 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
118718288 122104 0 None 11 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 481 6 1 4 6.0 COc1cccc([C@@]2(CN)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1016/j.bmcl.2008.10.088
CHEMBL3349272 122104 0 None 11 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 481 6 1 4 6.0 COc1cccc([C@@]2(CN)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1016/j.bmcl.2008.10.088
118718301 122118 0 None 123 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 464 6 1 2 6.9 NC[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349286 122118 0 None 123 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 464 6 1 2 6.9 NC[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
24894531 185909 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 336 3 1 3 3.9 Cc1ccccc1C1CCN(C[C@@H]2Cc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL471982 185909 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 336 3 1 3 3.9 Cc1ccccc1C1CCN(C[C@@H]2Cc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
11326750 193088 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 390 3 2 4 3.3 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)Cc2cccnc21 10.1021/jm701590h
CHEMBL487458 193088 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 390 3 2 4 3.3 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)Cc2cccnc21 10.1021/jm701590h
44574963 185293 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 522 7 2 3 6.1 CC(O)CNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466694 185293 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 522 7 2 3 6.1 CC(O)CNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44574789 185327 0 None 91 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 504 6 1 2 7.1 O=C(NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl)C1CC1 10.1016/j.bmcl.2009.03.031
CHEMBL466919 185327 0 None 91 2 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 504 6 1 2 7.1 O=C(NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl)C1CC1 10.1016/j.bmcl.2009.03.031
70419 81785 48 None 17 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 321 3 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL203356 81785 48 None 17 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 321 3 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccc1)CC2 10.1016/j.bmcl.2007.01.069
155569552 182993 0 None 61 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 509 10 5 5 3.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(=O)[C@@H](N)CCCNC(=N)N)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4594096 182993 0 None 61 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 509 10 5 5 3.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(=O)[C@@H](N)CCCNC(=N)N)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
46879537 12956 0 None -2 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 424 5 1 4 3.3 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1081191 12956 0 None -2 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 424 5 1 4 3.3 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
24798598 119362 11 None -5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3301613 119362 11 None -5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
CHEMBL3325959 119362 11 None -5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 364 2 2 2 4.8 CN[C@]1(c2ccccc2)CC[C@]2(CC1)OCCc1c3cc(F)ccc3[nH]c12 10.1021/ml500117c
155544763 180135 0 None 7 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranesDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranes
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@H]3CCCc4cccc2c43)CC1 10.1021/acs.jmedchem.5b01499
CHEMBL4527189 180135 0 None 7 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranesDisplacement of [3H]nociceptin/orphanin FQ from recombinant human nociceptin opioid receptor expressed in CHO cell membranes
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@H]3CCCc4cccc2c43)CC1 10.1021/acs.jmedchem.5b01499
90655975 117785 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 373 4 1 2 4.7 CCC1C(=O)N(C2CCN(Cc3cccc4[nH]ccc34)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262548 117785 0 None -1 3 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 373 4 1 2 4.7 CCC1C(=O)N(C2CCN(Cc3cccc4[nH]ccc34)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
21345766 86889 0 None 1 3 Guinea pig 8.0 pKi = 8.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 449 3 1 7 2.3 CN1CC[C@]23c4c5ccc(OC(=O)C(C)(C)C)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44414864 86889 0 None 1 3 Guinea pig 8.0 pKi = 8.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 449 3 1 7 2.3 CN1CC[C@]23c4c5ccc(OC(=O)C(C)(C)C)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
CHEMBL213228 86889 0 None 1 3 Guinea pig 8.0 pKi = 8.0 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 449 3 1 7 2.3 CN1CC[C@]23c4c5ccc(OC(=O)C(C)(C)C)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
73350483 97238 0 None 6 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN(C2CC[C@H]3CCCc4cccc2c43)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387193 97238 0 None 6 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN(C2CC[C@H]3CCCc4cccc2c43)CC1 10.1016/j.bmcl.2013.03.101
44438966 98546 0 None 50 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 411 4 1 3 4.5 Cc1ccccc1C(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL241079 98546 0 None 50 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 411 4 1 3 4.5 Cc1ccccc1C(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
25134075 134955 0 None 218 2 Human 7.9 pKi = 7.9 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 373 2 1 4 3.6 O=c1[nH]c2ccc(F)cc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL3665421 134955 0 None 218 2 Human 7.9 pKi = 7.9 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 373 2 1 4 3.6 O=c1[nH]c2ccc(F)cc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
70684433 83435 0 None 27 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 420 5 0 4 2.6 Cc1ccccc1N1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064145 83435 0 None 27 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 420 5 0 4 2.6 Cc1ccccc1N1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
11371415 11131 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 346 2 0 2 4.1 O=C1Cc2ccccc2N1C1CCN(C2CCCc3ccccc32)CC1 10.1021/jm034249d
CHEMBL101118 11131 0 None 1 3 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 346 2 0 2 4.1 O=C1Cc2ccccc2N1C1CCN(C2CCCc3ccccc32)CC1 10.1021/jm034249d
44451648 102932 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 0 9 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncnn4C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL260555 102932 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 0 9 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncnn4C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
9889948 38449 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 413 6 2 5 5.0 COc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1021/jm0002073
CHEMBL140519 38449 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 413 6 2 5 5.0 COc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1021/jm0002073
44430045 94524 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 400 5 2 3 4.8 Cc1ccc(C(c2ccc(C)cc2)N2CCC(O)(c3ccccc3CN)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL233748 94524 0 None 4 4 Human 7.0 pKi = 7.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 400 5 2 3 4.8 Cc1ccc(C(c2ccc(C)cc2)N2CCC(O)(c3ccccc3CN)CC2)cc1 10.1016/j.bmcl.2007.03.062
10338496 127331 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 286 3 0 2 3.9 CN(C)[C@]1(c2ccccc2)CC[C@H](N2CCCCC2)CC1 10.1021/ml500116x
CHEMBL3325883 127331 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 286 3 0 2 3.9 CN(C)[C@]1(c2ccccc2)CC[C@H](N2CCCCC2)CC1 10.1021/ml500116x
CHEMBL3545612 127331 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 286 3 0 2 3.9 CN(C)[C@]1(c2ccccc2)CC[C@H](N2CCCCC2)CC1 10.1021/ml500116x
44339530 115306 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 326 3 0 2 4.9 N#CC1(c2ccccc2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL320058 115306 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 326 3 0 2 4.9 N#CC1(c2ccccc2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
10292091 103541 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 361 3 0 2 4.6 CCN1C(=O)N(C2CCN(C3CCCCCCC3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL26464 103541 0 None 8 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 361 3 0 2 4.6 CCN1C(=O)N(C2CCN(C3CCCCCCC3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
46879629 12645 0 None 28 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 420 4 1 4 2.5 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079417 12645 0 None 28 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 420 4 1 4 2.5 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
44391012 175090 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 467 6 1 5 6.5 Cc1ccc(Cl)c(OC2(CCN3CCC(n4c(O)nc5ccccc54)CC3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL434150 175090 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 467 6 1 5 6.5 Cc1ccc(Cl)c(OC2(CCN3CCC(n4c(O)nc5ccccc54)CC3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
46880153 12284 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 358 6 1 5 2.2 CNC(=O)Cn1c(=O)n(C2CCN(CCC(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1076499 12284 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 358 6 1 5 2.2 CNC(=O)Cn1c(=O)n(C2CCN(CCC(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44391119 138817 0 None -5 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 435 8 1 5 6.0 CC(C)c1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL369540 138817 0 None -5 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 435 8 1 5 6.0 CC(C)c1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
44337231 15935 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 390 5 1 2 5.8 Cc1ccc(C(c2ccc(C)cc2)N2CC[C@H]2[C@H](N)c2cccc(Cl)c2)cc1 10.1016/s0960-894x(02)00652-2
CHEMBL110138 15935 0 None -1 4 Human 6.0 pKi = 6.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 390 5 1 2 5.8 Cc1ccc(C(c2ccc(C)cc2)N2CC[C@H]2[C@H](N)c2cccc(Cl)c2)cc1 10.1016/s0960-894x(02)00652-2
44413409 85066 0 None -5 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 324 3 1 1 5.2 Clc1ccc2[nH]cc(C3CCN(Cc4ccccc4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL210770 85066 0 None -5 3 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 324 3 1 1 5.2 Clc1ccc2[nH]cc(C3CCN(Cc4ccccc4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
44430026 95002 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 351 8 1 2 5.6 CCCCCCC1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL234773 95002 0 None 7 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 351 8 1 2 5.6 CCCCCCC1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
54584440 69421 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 447 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL1783820 69421 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 447 7 0 4 4.0 CN(CCCN1CCC2(CC1)OCc1ccccc12)C(=O)[C@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
44252987 151302 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 390 4 0 2 5.5 CN(C)C1(c2ccccc2)CCC(c2ccc(C(F)(F)F)cc2)(N(C)C)CC1 nan
CHEMBL3907138 151302 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 390 4 0 2 5.5 CN(C)C1(c2ccccc2)CCC(c2ccc(C(F)(F)F)cc2)(N(C)C)CC1 nan
11743914 116442 0 None -114 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 439 6 1 2 6.2 OC1(c2cccc(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
CHEMBL322515 116442 0 None -114 3 Human 6.9 pKi = 6.9 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 439 6 1 2 6.2 OC1(c2cccc(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
118718264 122079 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 518 7 0 2 8.0 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@](Cc1ccccc1)(CN1CCCC1)C2 10.1016/j.bmcl.2008.10.088
CHEMBL3349247 122079 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 518 7 0 2 8.0 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@](Cc1ccccc1)(CN1CCCC1)C2 10.1016/j.bmcl.2008.10.088
44402713 141958 0 None 1 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 325 3 0 4 4.0 COc1ccc2c(c1)[C@H]1O[C@@H](CN(C)C)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
CHEMBL371984 141958 0 None 1 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 325 3 0 4 4.0 COc1ccc2c(c1)[C@H]1O[C@@H](CN(C)C)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
44253564 152221 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 466 6 0 2 7.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL3914240 152221 0 None 3 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 466 6 0 2 7.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccc(C(F)(F)F)c2)CC1 nan
44252247 156218 0 None -8 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 288 4 1 2 3.2 CC(=O)NCC1(C)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3945941 156218 0 None -8 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 288 4 1 2 3.2 CC(=O)NCC1(C)CCC(c2ccccc2)(N(C)C)CC1 nan
44451573 176205 0 None -2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 575 10 0 9 6.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4noc(C(C)(C)C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL442469 176205 0 None -2 2 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 575 10 0 9 6.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4noc(C(C)(C)C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
118718297 122114 0 None 20 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 522 7 1 3 6.8 COc1ccc([C@@]2(CNC(C)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2008.10.088
CHEMBL3349282 122114 0 None 20 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 522 7 1 3 6.8 COc1ccc([C@@]2(CNC(C)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2008.10.088
24735827 98493 0 None 2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 322 3 1 4 2.0 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccn1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240895 98493 0 None 2 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 322 3 1 4 2.0 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccn1)CC2 10.1016/j.bmcl.2007.01.069
44339525 15401 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 437 3 1 2 5.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL109509 15401 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 437 3 1 2 5.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(03)00665-6
44339525 15401 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 437 3 1 2 5.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2004.08.032
CHEMBL109509 15401 0 None -11 2 Human 5.9 pKi = 5.9 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 437 3 1 2 5.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2004.08.032
44390989 172670 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 483 6 2 6 5.5 Cc1ccc(Cl)c(OC2(C(O)CN3CCC(n4c(O)nc5ccccc54)CC3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL424971 172670 0 None 4 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 483 6 2 6 5.5 Cc1ccc(Cl)c(OC2(C(O)CN3CCC(n4c(O)nc5ccccc54)CC3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
24776402 104357 0 None 10 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 448 4 0 2 5.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cccc(F)c23)CC1 10.1021/jm7009606
CHEMBL270756 104357 0 None 10 3 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 448 4 0 2 5.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cccc(F)c23)CC1 10.1021/jm7009606
44426829 92473 0 None 10 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 5.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2C(F)(F)F)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228794 92473 0 None 10 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 5.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2C(F)(F)F)CC1 10.1016/j.bmcl.2007.03.061
44430080 93542 0 None 25 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 511 7 3 3 5.9 CCNC(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232074 93542 0 None 25 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 511 7 3 3 5.9 CCNC(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
118718302 122119 0 None 38 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 506 7 1 2 7.1 CC(=O)NC[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349287 122119 0 None 38 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 506 7 1 2 7.1 CC(=O)NC[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
11256620 185914 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL471994 185914 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
76335145 110118 0 None 79 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 529 5 1 4 7.0 COC(=O)N[C@@]1(c2ccc(Cl)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084552 110118 0 None 79 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 529 5 1 4 7.0 COC(=O)N[C@@]1(c2ccc(Cl)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44574958 195961 0 None 74 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 513 5 1 4 6.5 COC(=O)NC1(c2ccc(F)cn2)C[C@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL511232 195961 0 None 74 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 513 5 1 4 6.5 COC(=O)NC1(c2ccc(F)cn2)C[C@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
22558157 117784 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 374 3 0 2 4.5 CCC1C(=O)N(C2CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262547 117784 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 374 3 0 2 4.5 CCC1C(=O)N(C2CCN(C3CCc4ccccc4C3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
44437646 97119 0 None 16 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 12 1 7 4.6 C=CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238602 97119 0 None 16 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 12 1 7 4.6 C=CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437648 154411 0 None 8 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 548 12 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL393138 154411 0 None 8 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 548 12 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437628 177444 0 None 10 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 11 1 7 4.4 CNC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL445154 177444 0 None 10 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 11 1 7 4.4 CNC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44402486 131113 0 None -2 3 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1C[C@H]2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL363619 131113 0 None -2 3 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 329 2 0 3 4.6 CN(C)C[C@@H]1C[C@H]2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
15411840 127249 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 369 2 1 3 4.0 CC(C)(C)[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL354163 127249 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 369 2 1 3 4.0 CC(C)(C)[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
25190592 194992 0 None 56 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 592 9 0 4 7.3 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O)C(C)C 10.1016/j.bmcl.2008.12.092
CHEMBL499169 194992 0 None 56 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 592 9 0 4 7.3 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O)C(C)C 10.1016/j.bmcl.2008.12.092
25190630 185924 0 None 12 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 556 8 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)c(Cl)cc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL472086 185924 0 None 12 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 556 8 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)c(Cl)cc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
71624387 97240 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 2 0 2 4.7 CC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387195 97240 0 None -1 3 Human 7.9 pKi = 7.9 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 2 0 2 4.7 CC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
9803475 84370 32 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
CHEMBL2088036 84370 32 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 443 5 0 5 3.7 COC(=O)CN1CN(c2ccccc2)C2(CCN(Cc3cccc4ccccc34)CC2)C1=O 10.1021/jm201629q
12986256 120716 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 218 2 1 2 2.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](N)CC1 10.1021/ml500116x
CHEMBL3325882 120716 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 218 2 1 2 2.3 CN(C)[C@]1(c2ccccc2)CC[C@@H](N)CC1 10.1021/ml500116x
10715726 39136 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 395 6 2 3 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3CCCc3ccccc3)ccc2n1 10.1021/jm0002073
CHEMBL141078 39136 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 395 6 2 3 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3CCCc3ccccc3)ccc2n1 10.1021/jm0002073
76335141 110105 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 533 5 1 3 6.5 NC(=O)[C@@]1(c2ccc(C(F)(F)F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084537 110105 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 533 5 1 3 6.5 NC(=O)[C@@]1(c2ccc(C(F)(F)F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
10156336 106125 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 375 5 0 2 4.9 CCCC1CCC(N2CCC(N3C(=O)N(CC)[C@@H]4CCCC[C@H]43)CC2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL282376 106125 0 None 1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 375 5 0 2 4.9 CCCC1CCC(N2CCC(N3C(=O)N(CC)[C@@H]4CCCC[C@H]43)CC2)CC1 10.1016/j.bmcl.2003.11.083
9923726 106413 0 None 11 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 333 2 1 2 3.9 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL284217 106413 0 None 11 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 333 2 1 2 3.9 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2003.11.083
44391104 71788 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 491 7 2 6 5.5 Cc1ccc(Cl)c(OC(c2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182328 71788 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 491 7 2 6 5.5 Cc1ccc(Cl)c(OC(c2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44426837 92484 0 None 19 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 421 4 1 2 5.5 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccc(Br)cc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228856 92484 0 None 19 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 421 4 1 2 5.5 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccc(Br)cc2)CC1 10.1016/j.bmcl.2007.03.061
44402487 76583 0 None -1 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL193614 76583 0 None -1 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 373 2 0 3 4.7 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL411621 219731 0 None -301 2 Mouse 6.9 pKi = 6.9 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm990075h
44252684 150186 0 None 5 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 364 7 0 2 5.6 CCCCN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3898034 150186 0 None 5 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 364 7 0 2 5.6 CCCCN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
10133332 107971 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 363 3 1 2 4.1 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL29571 107971 0 None -1 2 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 363 3 1 2 4.1 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2003.11.083
44391138 72237 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 445 7 1 5 5.7 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1cc(F)ccc1Cl 10.1016/j.bmcl.2004.11.049
CHEMBL182995 72237 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 445 7 1 5 5.7 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1cc(F)ccc1Cl 10.1016/j.bmcl.2004.11.049
44339505 16186 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 344 3 0 2 5.1 N#CC1(c2ccccc2)CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL111628 16186 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 344 3 0 2 5.1 N#CC1(c2ccccc2)CCN(Cc2ccc(Cl)c(Cl)c2)CC1 10.1016/s0960-894x(03)00665-6
122179051 128084 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3580675 128084 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
44431782 94599 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 350 4 1 4 4.2 OC1(c2nccs2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233820 94599 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 350 4 1 4 4.2 OC1(c2nccs2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
70690756 83427 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 450 7 0 5 2.6 CCOc1ccccc1N1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064132 83427 0 None -4 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 450 7 0 5 2.6 CCOc1ccccc1N1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
44430012 94832 0 None 2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 371 5 1 2 5.3 CCc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL234543 94832 0 None 2 4 Human 5.9 pKi = 5.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 371 5 1 2 5.3 CCc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
134563695 178942 0 None 3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 4 1 3 4.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(C(N)=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4473383 178942 0 None 3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 4 1 3 4.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(C(N)=O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
10269001 92462 0 None 17 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 343 4 1 2 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228690 92462 0 None 17 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 343 4 1 2 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
10269001 92462 0 None 17 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 343 4 1 2 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL228690 92462 0 None 17 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 343 4 1 2 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
10269001 92462 0 None 17 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 343 4 1 2 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2009.03.031
CHEMBL228690 92462 0 None 17 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 343 4 1 2 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2009.03.031
44574587 185214 0 None 29 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 496 6 1 4 6.4 COc1ccc(CC2(O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccc(C)cc2Cl)nc1 10.1016/j.bmcl.2009.03.031
CHEMBL466066 185214 0 None 29 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 496 6 1 4 6.4 COc1ccc(CC2(O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccc(C)cc2Cl)nc1 10.1016/j.bmcl.2009.03.031
76313427 110127 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 543 5 1 3 6.3 NC(=O)[C@@]1(c2ccc(Br)nc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084561 110127 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 543 5 1 3 6.3 NC(=O)[C@@]1(c2ccc(Br)nc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
24970041 134975 0 None 13 4 Human 7.9 pKi = 7.9 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 395 2 1 4 4.4 O=c1[nH]c2ccccc2n([C@H]2C[C@@H]3CCC[C@H](C2)N3C2CCCCCCC2)c1=O nan
CHEMBL3665440 134975 0 None 13 4 Human 7.9 pKi = 7.9 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 395 2 1 4 4.4 O=c1[nH]c2ccccc2n([C@H]2C[C@@H]3CCC[C@H](C2)N3C2CCCCCCC2)c1=O nan
10669670 41428 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccccc3Cl)ccc2n1 10.1021/jm0002073
CHEMBL142999 41428 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccccc3Cl)ccc2n1 10.1021/jm0002073
70684436 83437 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064157 83437 0 None 6 2 Human 7.9 pKi = 7.9 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
44253564 152221 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 466 6 0 2 7.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL3914240 152221 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 466 6 0 2 7.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2cccc(C(F)(F)F)c2)CC1 nan
1627 9372 20 None -5 13 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2006.05.060
1845 9372 20 None -5 13 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2006.05.060
5288826 9372 20 None -5 13 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2006.05.060
CHEMBL70 9372 20 None -5 13 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2006.05.060
DB00295 9372 20 None -5 13 Guinea pig 7.9 pKi = 7.9 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O 10.1016/j.bmcl.2006.05.060
24776411 104473 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 342 4 1 2 4.0 CNC(=O)C1(c2ccccc2)CCN(C2CCC(C(C)C)CC2)CC1 10.1021/jm7009606
CHEMBL271322 104473 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 342 4 1 2 4.0 CNC(=O)C1(c2ccccc2)CCN(C2CCC(C(C)C)CC2)CC1 10.1021/jm7009606
118705898 119643 0 None -8511 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 484 4 2 5 3.6 O=C1CCC2=C([C@@H]3Oc4c(O)ccc5c4[C@@]34CCN(CC3CC3)[C@H](C5)[C@]4(O)C2)N1Cc1ccccc1 10.1016/j.bmc.2014.05.065
CHEMBL3309515 119643 0 None -8511 4 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 484 4 2 5 3.6 O=C1CCC2=C([C@@H]3Oc4c(O)ccc5c4[C@@]34CCN(CC3CC3)[C@H](C5)[C@]4(O)C2)N1Cc1ccccc1 10.1016/j.bmc.2014.05.065
44252242 156902 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 5 0 2 4.6 CN(C)C1(Cc2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3951213 156902 0 None -6 3 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 5 0 2 4.6 CN(C)C1(Cc2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44426834 92482 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 377 4 1 2 5.4 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228850 92482 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 377 4 1 2 5.4 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.03.061
9797246 98494 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 322 3 1 4 2.0 O=C1NCN(c2ccccc2)C12CCN(Cc1cccnc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240896 98494 0 None 1 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 322 3 1 4 2.0 O=C1NCN(c2ccccc2)C12CCN(Cc1cccnc1)CC2 10.1016/j.bmcl.2007.01.069
56681954 72479 0 None -43 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 543 5 2 5 5.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)c1ccc(C(C)(C)C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834412 72479 0 None -43 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 543 5 2 5 5.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)c1ccc(C(C)(C)C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
44426817 92461 0 None 3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 325 6 1 3 3.7 CCOCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228687 92461 0 None 3 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 325 6 1 3 3.7 CCOCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44337252 12025 0 None 3 4 Human 5.9 pKi = 5.9 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 322 9 1 2 5.2 CCCCC(CCCC)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL106359 12025 0 None 3 4 Human 5.9 pKi = 5.9 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 322 9 1 2 5.2 CCCCC(CCCC)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
11165726 118392 0 None -6 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 408 3 0 2 5.4 CC(c1ccc2c(c1)Cc1ccccc1-2)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1021/jm034249d
CHEMBL328411 118392 0 None -6 3 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 408 3 0 2 5.4 CC(c1ccc2c(c1)Cc1ccccc1-2)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1021/jm034249d
44426806 175038 0 None 10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 295 4 1 2 4.1 CCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL433814 175038 0 None 10 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 295 4 1 2 4.1 CCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
24776406 102781 0 None 8 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 462 3 0 2 6.3 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cc(F)ccc23)CC1 10.1021/jm7009606
CHEMBL259681 102781 0 None 8 3 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 462 3 0 2 6.3 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cc(F)ccc23)CC1 10.1021/jm7009606
10336926 93502 0 None 33 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 333 4 1 3 4.4 OC1(c2ccco2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL231874 93502 0 None 33 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 333 4 1 3 4.4 OC1(c2ccco2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
134578518 179785 0 None 7 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 397 7 2 4 4.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNCCO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4518220 179785 0 None 7 3 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 397 7 2 4 4.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNCCO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44252681 149261 0 None -758 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 394 6 1 2 5.0 CN(C)C1(c2cccc(F)c2)CCC(C)(CNC(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3890424 149261 0 None -758 2 Human 5.9 pKi = 5.9 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 394 6 1 2 5.0 CN(C)C1(c2cccc(F)c2)CCC(C)(CNC(=O)/C=C/c2ccccc2)CC1 nan
44337131 114104 0 None 36 4 Human 7.9 pKi = 7.9 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 396 5 1 2 5.6 N[C@H](c1cccc(C(F)(F)F)c1)[C@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL317479 114104 0 None 36 4 Human 7.9 pKi = 7.9 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 396 5 1 2 5.6 N[C@H](c1cccc(C(F)(F)F)c1)[C@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
44391094 71249 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 422 7 2 6 4.8 Cc1ccc(N)cc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL181389 71249 0 None 3 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 422 7 2 6 4.8 Cc1ccc(N)cc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
44248791 110158 0 None 46 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
CHEMBL3084648 110158 0 None 46 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
44426810 92742 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 337 7 1 2 5.3 CCCCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL230253 92742 0 None 2 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 337 7 1 2 5.3 CCCCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
10089987 93540 0 None 53 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 361 4 1 2 4.9 OC1(c2ccc(F)cc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232066 93540 0 None 53 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 361 4 1 2 4.9 OC1(c2ccc(F)cc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
44574630 196202 0 None 109 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 534 6 1 3 7.4 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCN2Cc2ccccc2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL513303 196202 0 None 109 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 534 6 1 3 7.4 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCCN2Cc2ccccc2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
44438916 97995 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 327 3 1 4 2.7 O=C1NCN(c2ccccc2)C12CCN(Cc1ccsc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240033 97995 0 None 1 4 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 327 3 1 4 2.7 O=C1NCN(c2ccccc2)C12CCN(Cc1ccsc1)CC2 10.1016/j.bmcl.2007.01.069
18782384 176156 0 None 14 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 375 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1CCCCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL442090 176156 0 None 14 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 375 2 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(C1CCCCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
44438967 98547 0 None 25 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 431 4 1 3 4.9 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL241080 98547 0 None 25 4 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 431 4 1 3 4.9 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccc(Cl)cc1)CC2 10.1016/j.bmcl.2007.01.069
44575092 185461 0 None 5 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 357 4 1 2 5.0 C[C@@H]1CN(C(c2ccccc2)c2ccccc2)CC[C@@]1(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL467933 185461 0 None 5 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 357 4 1 2 5.0 C[C@@H]1CN(C(c2ccccc2)c2ccccc2)CC[C@@]1(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
44402413 131114 0 None 1 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 460 2 0 5 6.3 N#Cc1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
CHEMBL363622 131114 0 None 1 3 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 460 2 0 5 6.3 N#Cc1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
44430021 94296 0 None 5 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 368 4 1 3 4.6 N#Cc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL233501 94296 0 None 5 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 368 4 1 3 4.6 N#Cc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
122179064 128187 0 None -13182 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 477 5 2 6 4.3 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccoc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581762 128187 0 None -13182 3 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 477 5 2 6 4.3 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccoc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
24776400 163731 0 None 7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 386 1 0 2 4.7 CN1Cc2cc(F)ccc2C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1021/jm7009606
CHEMBL407275 163731 0 None 7 3 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 386 1 0 2 4.7 CN1Cc2cc(F)ccc2C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1021/jm7009606
44253419 154041 0 None 5 2 Human 5.8 pKi = 5.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 428 7 0 3 6.1 COc1ccc(CN(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
CHEMBL3928651 154041 0 None 5 2 Human 5.8 pKi = 5.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 428 7 0 3 6.1 COc1ccc(CN(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
44395286 73779 0 None -489 2 Human 6.8 pKi = 6.8 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 531 7 1 4 6.2 COC(=O)C(CCN1CCC(O)(c2ccc(Cl)c(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
CHEMBL186938 73779 0 None -489 2 Human 6.8 pKi = 6.8 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 531 7 1 4 6.2 COC(=O)C(CCN1CCC(O)(c2ccc(Cl)c(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
CHEMBL427617 220135 0 None - 1 Human 7.8 pKi = 7.8 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
69016300 160617 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 416 5 0 4 4.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2ccn(C)n2)CC1 nan
CHEMBL3982651 160617 0 None -3 2 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 416 5 0 4 4.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2ccn(C)n2)CC1 nan
10601891 103565 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 513 5 0 4 5.2 O=C(CN1CN(c2ccccc2)C2(CCN(C3CCc4cccc(Cl)c4C3)CC2)C1=O)c1ccccc1 10.1021/jm991129q
CHEMBL26483 103565 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 513 5 0 4 5.2 O=C(CN1CN(c2ccccc2)C2(CCN(C3CCc4cccc(Cl)c4C3)CC2)C1=O)c1ccccc1 10.1021/jm991129q
11757207 93792 0 None 8 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 546 9 2 4 5.9 CCCS(=O)(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232478 93792 0 None 8 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 546 9 2 4 5.9 CCCS(=O)(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
44430033 154689 0 None 50 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 363 4 1 3 5.1 Cc1ccsc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL393356 154689 0 None 50 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 363 4 1 3 5.1 Cc1ccsc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
118718277 122093 0 None 51 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 524 7 1 2 7.2 CC(=O)NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349261 122093 0 None 51 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 524 7 1 2 7.2 CC(=O)NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
76316935 110098 0 None 9 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 499 5 1 3 6.2 NC(=O)[C@@]1(c2ccc(Cl)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084530 110098 0 None 9 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 499 5 1 3 6.2 NC(=O)[C@@]1(c2ccc(Cl)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76327872 110108 0 None 30 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2cc(F)cc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084541 110108 0 None 30 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2cc(F)cc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
46880031 14221 0 None 39 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 398 4 1 5 3.3 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1086749 14221 0 None 39 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 398 4 1 5 3.3 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44437644 98572 0 None 5 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 538 12 2 8 3.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL241155 98572 0 None 5 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 538 12 2 8 3.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCCO)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
16739256 155454 0 None 61 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 457 2 1 3 5.5 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2007.01.069
CHEMBL393980 155454 0 None 61 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 457 2 1 3 5.5 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2cc(Cl)c(Cl)cc21 10.1016/j.bmcl.2007.01.069
71624266 97234 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 368 4 0 2 5.0 CCC(C)(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387189 97234 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 368 4 0 2 5.0 CCC(C)(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
10697286 106579 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 519 4 0 3 6.2 O=C1N(Cc2ccccc2)CN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL285377 106579 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 519 4 0 3 6.2 O=C1N(Cc2ccccc2)CN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
11233481 11103 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 3 0 2 4.1 CC1(C)C2CCC(CN3CCC(N4C(=O)Cc5ccccc54)CC3)C1C2 10.1021/jm034249d
CHEMBL100938 11103 0 None 1 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 3 0 2 4.1 CC1(C)C2CCC(CN3CCC(N4C(=O)Cc5ccccc54)CC3)C1C2 10.1021/jm034249d
155537352 179074 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 348 4 0 3 4.4 CCCC(=O)N1CCC2(CCC(c3sccc3C)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
CHEMBL4474989 179074 0 None -2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 348 4 0 3 4.4 CCCC(=O)N1CCC2(CCC(c3sccc3C)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
11164004 115328 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCCC3CCCCC32)CC1 10.1021/jm034249d
CHEMBL320182 115328 0 None 2 3 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCCC3CCCCC32)CC1 10.1021/jm034249d
CHEMBL414792 219936 0 None - 1 Mouse 7.8 pKi = 7.8 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None CC(C)C[C@H](N)CNCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O 10.1021/jm990075h
15512236 111665 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 413 3 1 4 3.9 COc1cccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)c1 10.1016/s0960-894x(99)00385-6
CHEMBL311185 111665 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 413 3 1 4 3.9 COc1cccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)c1 10.1016/s0960-894x(99)00385-6
25190627 196569 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4ccc(Cl)cc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL516187 196569 0 None -1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4ccc(Cl)cc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
134578342 179840 0 None 16 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 438 8 2 4 4.7 CCNCC(=O)NCc1cn(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc12 10.1021/acs.jmedchem.9b02134
CHEMBL4519453 179840 0 None 16 3 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 438 8 2 4 4.7 CCNCC(=O)NCc1cn(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc12 10.1021/acs.jmedchem.9b02134
118705899 119644 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 498 5 2 5 3.7 O=C1CCC2=C([C@@H]3Oc4c(O)ccc5c4[C@@]34CCN(CC3CC3)[C@H](C5)[C@]4(O)C2)N1CCc1ccccc1 10.1016/j.bmc.2014.05.065
CHEMBL3309516 119644 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 498 5 2 5 3.7 O=C1CCC2=C([C@@H]3Oc4c(O)ccc5c4[C@@]34CCN(CC3CC3)[C@H](C5)[C@]4(O)C2)N1CCc1ccccc1 10.1016/j.bmc.2014.05.065
118662129 182327 0 None -6 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 342 6 0 2 4.1 CCCCN1CCC2(CCC(Cc3ccccc3)(N(C)C)CC2)C1=O 10.1021/acsmedchemlett.6b00277
CHEMBL4578716 182327 0 None -6 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 342 6 0 2 4.1 CCCCN1CCC2(CCC(Cc3ccccc3)(N(C)C)CC2)C1=O 10.1021/acsmedchemlett.6b00277
44337357 14517 0 None 3 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 362 5 1 2 5.2 N[C@@H](c1ccc(Cl)cc1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL108904 14517 0 None 3 4 Human 6.8 pKi = 6.8 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 362 5 1 2 5.2 N[C@@H](c1ccc(Cl)cc1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
57502889 134968 0 None - 1 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 383 2 0 3 4.0 CN1C(=O)CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 nan
CHEMBL3665434 134968 0 None - 1 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 383 2 0 3 4.0 CN1C(=O)CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 nan
44339393 117469 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 351 3 1 2 5.0 OC1(c2ccc(Cl)cc2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL326030 117469 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 351 3 1 2 5.0 OC1(c2ccc(Cl)cc2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
44437601 97403 0 None 7 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238833 97403 0 None 7 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437643 161414 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 550 10 1 7 5.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC(C)(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL399393 161414 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 550 10 1 7 5.2 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC(C)(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
57502894 134964 0 None 3 2 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 439 5 1 3 5.5 CCC1(CC)C(=O)Nc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)C1=O nan
CHEMBL3665430 134964 0 None 3 2 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 439 5 1 3 5.5 CCC1(CC)C(=O)Nc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)C1=O nan
44574393 185435 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 357 4 1 2 5.0 C[C@H]1CN(C(c2ccccc2)c2ccccc2)CC[C@@]1(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL467676 185435 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 357 4 1 2 5.0 C[C@H]1CN(C(c2ccccc2)c2ccccc2)CC[C@@]1(O)c1ccccc1 10.1016/j.bmcl.2009.03.031
54585396 69424 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 420 8 0 4 4.6 c1ccc(CN2CCC[C@@H]2COCCCN2CCC3(CC2)OCc2ccccc23)cc1 10.1016/j.bmc.2009.05.068
CHEMBL1783823 69424 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 420 8 0 4 4.6 c1ccc(CN2CCC[C@@H]2COCCCN2CCC3(CC2)OCc2ccccc23)cc1 10.1016/j.bmc.2009.05.068
56681955 72483 0 None -18 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 545 4 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4cc(Br)c(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834416 72483 0 None -18 4 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 545 4 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4cc(Br)c(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
44437629 97399 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 10 1 7 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238796 97399 0 None 1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 10 1 7 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
10291377 105875 0 None 67 4 Human 7.8 pKi = 7.8 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 347 3 1 2 4.1 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL280778 105875 0 None 67 4 Human 7.8 pKi = 7.8 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 347 3 1 2 4.1 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2003.11.083
44426814 160237 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 5 1 2 5.0 OC1(c2ccccc2)CCN(C(Cc2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL397945 160237 0 None 1 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 5 1 2 5.0 OC1(c2ccccc2)CCN(C(Cc2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44430022 94297 0 None 11 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 2 3 4.3 OCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233502 94297 0 None 11 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 2 3 4.3 OCc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
42629117 185328 0 None 7 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 482 5 1 2 6.3 NC(=O)C1(c2ccc(F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466921 185328 0 None 7 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 482 5 1 2 6.3 NC(=O)C1(c2ccc(F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76313423 110109 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2nc(F)ccc2F)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084542 110109 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2nc(F)ccc2F)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
56658044 72480 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 519 6 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CC4CCC1C4)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834413 72480 0 None -2 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 519 6 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC1CC4CCC1C4)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
46879477 12671 0 None -4 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 454 6 1 5 4.1 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccccc3-c3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1079562 12671 0 None -4 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 454 6 1 5 4.1 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccccc3-c3ccccc3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44413408 84661 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 368 2 1 1 5.8 Fc1ccc2c(C3=CCN(C4Cc5cccc6cccc4c56)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL209399 84661 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 368 2 1 1 5.8 Fc1ccc2c(C3=CCN(C4Cc5cccc6cccc4c56)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.03.094
118711156 127342 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 4 1 2 4.0 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(Cc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325746 127342 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 4 1 2 4.0 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(Cc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545628 127342 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 4 1 2 4.0 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(Cc2ccccc2)CC1 10.1021/ml500116x
44252683 151907 0 None -2 2 Human 5.8 pKi = 5.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 288 6 1 2 4.2 CCCCC1(N(C)C)CCC(NC)(c2ccccc2)CC1 nan
CHEMBL3911970 151907 0 None -2 2 Human 5.8 pKi = 5.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 288 6 1 2 4.2 CCCCC1(N(C)C)CCC(NC)(c2ccccc2)CC1 nan
10388166 92514 0 None 22 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 433 7 0 2 7.0 c1ccc(COC2(c3ccccc3)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.061
CHEMBL229018 92514 0 None 22 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 433 7 0 2 7.0 c1ccc(COC2(c3ccccc3)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.061
44252987 151302 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 390 4 0 2 5.5 CN(C)C1(c2ccccc2)CCC(c2ccc(C(F)(F)F)cc2)(N(C)C)CC1 nan
CHEMBL3907138 151302 0 None 1 2 Human 6.8 pKi = 6.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 390 4 0 2 5.5 CN(C)C1(c2ccccc2)CCC(c2ccc(C(F)(F)F)cc2)(N(C)C)CC1 nan
44413396 145720 0 None 2 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 448 5 2 5 4.4 N#Cc1ccc2c(c1)c(C1=CCN(C3Cc4cccc5cccc3c45)CC1)cn2C[C@H](O)CN 10.1016/j.bmcl.2006.03.094
CHEMBL378453 145720 0 None 2 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 448 5 2 5 4.4 N#Cc1ccc2c(c1)c(C1=CCN(C3Cc4cccc5cccc3c45)CC1)cn2C[C@H](O)CN 10.1016/j.bmcl.2006.03.094
59159346 135818 0 None - 1 Human 4.8 pKi = 4.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 398 3 1 5 3.1 COc1ccc2c(n1)NC(=O)CC(=O)N2C1CCN(C2/C=C\CCCCC2)CC1 nan
CHEMBL3670295 135818 0 None - 1 Human 4.8 pKi = 4.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 398 3 1 5 3.1 COc1ccc2c(n1)NC(=O)CC(=O)N2C1CCN(C2/C=C\CCCCC2)CC1 nan
44430029 93457 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 385 7 1 2 5.6 OC1(CCCc2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL231664 93457 0 None 1 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 385 7 1 2 5.6 OC1(CCCc2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
18666969 39654 3 None - 1 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 0.7 CN1CC[C@]23c4c5ccc(OS(=O)(=O)O)c4O[C@H]2[C@@H](O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44414680 39654 3 None - 1 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 0.7 CN1CC[C@]23c4c5ccc(OS(=O)(=O)O)c4O[C@H]2[C@@H](O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
CHEMBL1415 39654 3 None - 1 Guinea pig 5.8 pKi = 5.8 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 0.7 CN1CC[C@]23c4c5ccc(OS(=O)(=O)O)c4O[C@H]2[C@@H](O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44252386 158791 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 462 9 1 3 5.8 CCCCC1(CNS(=O)(=O)c2ccc(Cl)cc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3966922 158791 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 462 9 1 3 5.8 CCCCC1(CNS(=O)(=O)c2ccc(Cl)cc2)CCC(c2ccccc2)(N(C)C)CC1 nan
10043439 156371 0 None 22 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 349 4 1 2 5.2 OC1(C2CCCCC2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL394695 156371 0 None 22 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 349 4 1 2 5.2 OC1(C2CCCCC2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
118718269 122085 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 457 5 2 3 5.8 NC[C@]1(C2CCCCN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349253 122085 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 457 5 2 3 5.8 NC[C@]1(C2CCCCN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718291 122107 0 None 87 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 478 6 0 2 7.2 CN(C)C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349275 122107 0 None 87 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 478 6 0 2 7.2 CN(C)C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
24894425 185908 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 364 3 1 3 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C(C)(O)C2)CC1 10.1021/jm701590h
CHEMBL471981 185908 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 364 3 1 3 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C(C)(O)C2)CC1 10.1021/jm701590h
76316937 110122 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 508 7 2 3 6.5 NC(=O)C[C@@]1(Cc2ccc(O)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084556 110122 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 508 7 2 3 6.5 NC(=O)C[C@@]1(Cc2ccc(O)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44575043 196165 0 None 28 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 471 5 2 3 5.3 NC(=O)C1(C2CCCCN2)C[C@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL512962 196165 0 None 28 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 471 5 2 3 5.3 NC(=O)C1(C2CCCCN2)C[C@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44438921 98072 0 None 3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 349 4 1 3 3.6 CCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL240216 98072 0 None 3 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 349 4 1 3 3.6 CCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
52951939 90374 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 422 5 1 4 3.7 NC(=O)[C@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2204354 90374 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 422 5 1 4 3.7 NC(=O)[C@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
44451593 163422 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 548 10 0 8 6.1 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4csc(C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL406926 163422 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 548 10 0 8 6.1 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4csc(C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL410167 219582 0 None - 1 Mouse 7.8 pKi = 7.8 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(I)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44252101 157991 0 None 36 3 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 308 4 1 2 4.1 CNC1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3959941 157991 0 None 36 3 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 308 4 1 2 4.1 CNC1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
118662042 181168 0 None -38 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 328 6 0 2 4.6 CCCCN1CCC2(CCC(Cc3ccccc3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
CHEMBL4552146 181168 0 None -38 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 328 6 0 2 4.6 CCCCN1CCC2(CCC(Cc3ccccc3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
CHEMBL2371034 216782 0 None -6 4 Human 5.8 pKi = 5.8 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL None None None CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N1[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(N)=O)CC[C@@H]1C(C)(C)C 10.1021/jm020078l
118718282 122098 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 507 6 1 3 6.5 CC(=O)NC[C@]1(c2ncccc2C)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349266 122098 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 507 6 1 3 6.5 CC(=O)NC[C@]1(c2ncccc2C)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
25129302 135817 0 None 69 2 Human 6.8 pKi = 6.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 409 2 1 3 4.9 O=C1CC(=O)N([C@@H]2C[C@@H]3CCC[C@H](C2)N3C2CCCCCCC2)c2ccccc2N1 nan
CHEMBL3670294 135817 0 None 69 2 Human 6.8 pKi = 6.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 409 2 1 3 4.9 O=C1CC(=O)N([C@@H]2C[C@@H]3CCC[C@H](C2)N3C2CCCCCCC2)c2ccccc2N1 nan
44430013 155071 0 None 6 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 385 6 1 2 5.7 CCCc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL393675 155071 0 None 6 4 Human 5.8 pKi = 5.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 385 6 1 2 5.7 CCCc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
44252835 160968 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 302 6 0 2 4.5 CCCCC1(N(C)C)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3985824 160968 0 None -4 2 Human 6.8 pKi = 6.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 302 6 0 2 4.5 CCCCC1(N(C)C)CCC(c2ccccc2)(N(C)C)CC1 nan
57502946 134971 0 None - 1 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 464 3 1 5 3.7 O=C(C1=C(n2c(=O)c(=O)[nH]c3ccccc32)CCN(C2CCCCCCC2)C1)N1CCCCC1 nan
CHEMBL3665437 134971 0 None - 1 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 464 3 1 5 3.7 O=C(C1=C(n2c(=O)c(=O)[nH]c3ccccc32)CCN(C2CCCCCCC2)C1)N1CCCCC1 nan
57502948 135821 0 None - 1 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 486 5 2 5 4.0 O=C(NCc1ccccc1)C1=C(n2c(=O)c(=O)[nH]c3ccccc32)CCN(C2CCCCCCC2)C1 nan
CHEMBL3670298 135821 0 None - 1 Human 5.8 pKi = 5.8 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 486 5 2 5 4.0 O=C(NCc1ccccc1)C1=C(n2c(=O)c(=O)[nH]c3ccccc32)CCN(C2CCCCCCC2)C1 nan
CHEMBL262928 217332 0 None - 1 Mouse 5.8 pKi = 5.8 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(N)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
58358756 132578 0 None 11 4 Human 6.8 pKi = 6.8 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 435 3 1 5 4.8 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CCC[C@H](C2)N3C23CCCC(CCC2)C3)c1=O nan
CHEMBL3647961 132578 0 None 11 4 Human 6.8 pKi = 6.8 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 435 3 1 5 4.8 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CCC[C@H](C2)N3C23CCCC(CCC2)C3)c1=O nan
44253700 159415 0 None 23 2 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 380 8 1 3 4.6 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)CCCCO)CC1 nan
CHEMBL3972320 159415 0 None 23 2 Human 7.8 pKi = 7.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 380 8 1 3 4.6 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)CCCCO)CC1 nan
44248918 110151 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1ccnc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)c1 10.1021/jm9008218
CHEMBL3084635 110151 0 None 50 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1ccnc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)c1 10.1021/jm9008218
16665918 86524 0 None 28 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 370 2 1 1 5.9 Fc1ccc2[nH]cc(C3CCN(C4Cc5cccc6cccc4c56)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL211722 86524 0 None 28 3 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 370 2 1 1 5.9 Fc1ccc2[nH]cc(C3CCN(C4Cc5cccc6cccc4c56)CC3)c2c1 10.1016/j.bmcl.2006.03.094
44426812 93377 0 None 8 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 351 8 1 2 5.7 CCCCCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL231607 93377 0 None 8 4 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 351 8 1 2 5.7 CCCCCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
11256620 185914 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL471994 185914 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
46880239 12824 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 458 6 1 6 3.5 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc(OC)c4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080520 12824 0 None 6 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 458 6 1 6 3.5 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc(OC)c4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
10160920 73747 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 447 6 0 3 5.0 CCCCN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
CHEMBL186773 73747 0 None 2 2 Human 7.8 pKi = 7.8 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 447 6 0 3 5.0 CCCCN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
127034554 145800 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 375 2 1 2 3.5 NC(=O)N1Cc2ccccc2CC1CN1CCC2(CCc3ccccc32)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3785839 145800 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 375 2 1 2 3.5 NC(=O)N1Cc2ccccc2CC1CN1CCC2(CCc3ccccc32)CC1 10.1016/j.ejmech.2016.02.014
25190583 186154 0 None 25 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 509 6 1 4 5.2 O=C1N(CCO)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL473884 186154 0 None 25 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 509 6 1 4 5.2 O=C1N(CCO)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
54756989 72477 0 None -14 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 481 5 2 5 4.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834410 72477 0 None -14 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 481 5 2 5 4.8 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
9927928 97244 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 2 0 2 4.5 O=C1CCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387199 97244 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 2 0 2 4.5 O=C1CCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2013.03.101
11581029 145844 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 346 2 0 2 4.0 CN1Cc2ccccc2CC1CN1CCC2(CCc3ccccc32)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3786338 145844 0 None 3 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 346 2 0 2 4.0 CN1Cc2ccccc2CC1CN1CCC2(CCc3ccccc32)CC1 10.1016/j.ejmech.2016.02.014
87655565 158010 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 428 5 1 4 5.4 CN(C)C1(c2ccccc2)CCC(C(=N)c2cc3ccccc3n2C)(N2CCCC2)CC1 nan
CHEMBL3960085 158010 0 None -3 2 Human 6.8 pKi = 6.8 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 428 5 1 4 5.4 CN(C)C1(c2ccccc2)CCC(C(=N)c2cc3ccccc3n2C)(N2CCCC2)CC1 nan
24799146 104508 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 436 6 1 2 5.7 CC(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
CHEMBL271542 104508 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 436 6 1 2 5.7 CC(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
44430018 94290 0 None 16 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 1 3 4.8 COc1cccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)c1 10.1016/j.bmcl.2007.03.062
CHEMBL233494 94290 0 None 16 4 Human 6.8 pKi = 6.8 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 1 3 4.8 COc1cccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)c1 10.1016/j.bmcl.2007.03.062
10178311 85886 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 387 3 0 2 4.9 CCN1C(=O)N(C2CCN(C3CCC4CCCCC4C3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL2113273 85886 0 None 1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 387 3 0 2 4.9 CCN1C(=O)N(C2CCN(C3CCC4CCCCC4C3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
44337437 11980 0 None 7 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 370 9 1 2 6.1 CCCCCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL106155 11980 0 None 7 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 370 9 1 2 6.1 CCCCCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
118662342 178434 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 390 6 0 4 4.3 COC1(CCN2CC3(CCC(c4cccs4)(N(C)C)CC3)CC2=O)CCC1 10.1021/acsmedchemlett.6b00277
CHEMBL4466096 178434 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 390 6 0 4 4.3 COC1(CCN2CC3(CCC(c4cccs4)(N(C)C)CC3)CC2=O)CCC1 10.1021/acsmedchemlett.6b00277
24776396 104232 0 None 2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 372 2 0 2 4.3 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(C)Cc2cccc(F)c23)CC1 10.1021/jm7009606
CHEMBL270133 104232 0 None 2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 372 2 0 2 4.3 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(C)Cc2cccc(F)c23)CC1 10.1021/jm7009606
24800188 163269 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 346 4 1 2 3.9 CC(C)C1CCC(N2CCC(C(N)=O)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
CHEMBL406758 163269 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 346 4 1 2 3.9 CC(C)C1CCC(N2CCC(C(N)=O)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
46880155 14444 0 None 14 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 372 5 1 5 2.6 CNC(=O)Cn1c(=O)n(C2CCN(CCC(C)(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1088569 14444 0 None 14 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 372 5 1 5 2.6 CNC(=O)Cn1c(=O)n(C2CCN(CCC(C)(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
90656667 117739 0 None -245 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 479 5 2 5 4.6 CC[C@](O)([C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5)C(C)(C)C 10.1021/jm401964y
CHEMBL3262362 117739 0 None -245 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 479 5 2 5 4.6 CC[C@](O)([C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5)C(C)(C)C 10.1021/jm401964y
44394419 72985 0 None 7 2 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 377 2 1 3 3.4 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184451 72985 0 None 7 2 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 377 2 1 3 3.4 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
44394320 130419 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 463 6 1 4 4.1 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc(OCc3ccccc3)cc2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL361926 130419 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 463 6 1 4 4.1 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc(OCc3ccccc3)cc2)CC1 10.1016/j.bmcl.2004.08.001
90655978 117788 0 None -18 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 362 6 0 2 4.6 CCC1C(=O)N(C2CCN(CCCc3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262551 117788 0 None -18 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 362 6 0 2 4.6 CCC1C(=O)N(C2CCN(CCCc3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
44426818 92466 0 None 3 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 325 4 1 4 2.9 COC(=O)C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228736 92466 0 None 3 3 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 325 4 1 4 2.9 COC(=O)C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44297727 201754 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 353 2 1 4 4.9 Oc1nc2ccccc2n1[C@H]1CCN2[C@H](C3CCCCC3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
CHEMBL54603 201754 0 None -1 3 Human 6.7 pKi = 6.7 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 353 2 1 4 4.9 Oc1nc2ccccc2n1[C@H]1CCN2[C@H](C3CCCCC3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
44252387 154498 0 None -8 2 Human 5.7 pKi = 5.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 350 6 0 2 4.8 CN(C)CC1(Cc2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3932117 154498 0 None -8 2 Human 5.7 pKi = 5.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 350 6 0 2 4.8 CN(C)CC1(Cc2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44426807 92733 0 None 12 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 309 5 1 2 4.5 CCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL230145 92733 0 None 12 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 309 5 1 2 4.5 CCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44593576 195984 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 444 4 1 4 6.1 OC1(c2cncs2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL511373 195984 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 444 4 1 4 6.1 OC1(c2cncs2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76327875 110112 0 None 19 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 515 6 1 3 6.1 NC(=O)[C@@]1(c2cc(CF)c(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084545 110112 0 None 19 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 515 6 1 3 6.1 NC(=O)[C@@]1(c2cc(CF)c(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44437640 98007 0 None 14 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 536 12 1 7 4.8 CCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240086 98007 0 None 14 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 536 12 1 7 4.8 CCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
25190582 196555 0 None 34 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 537 6 0 5 5.4 COC(=O)CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL516077 196555 0 None 34 4 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 537 6 0 5 5.4 COC(=O)CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
10407144 200200 0 None -7 4 Human 7.7 pKi = 7.7 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 375 3 0 4 4.8 CCn1c(=O)n([C@@H]2CCN3[C@H](c4ccccc4)CCC[C@@H]3C2)c2ccccc21 10.1016/j.bmcl.2003.09.068
CHEMBL52604 200200 0 None -7 4 Human 7.7 pKi = 7.7 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 375 3 0 4 4.8 CCn1c(=O)n([C@@H]2CCN3[C@H](c4ccccc4)CCC[C@@H]3C2)c2ccccc21 10.1016/j.bmcl.2003.09.068
10432317 148375 0 None 1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 421 4 1 7 1.6 CCC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44414843 148375 0 None 1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 421 4 1 7 1.6 CCC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL385048 148375 0 None 1 3 Guinea pig 7.7 pKi = 7.7 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 421 4 1 7 1.6 CCC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL414767 219933 0 None -154 2 Mouse 7.7 pKi = 7.7 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm990075h
44253569 155981 0 None 8 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 419 4 1 2 5.9 Cc1c(C2(N3CCCC3)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccc(F)cc12 nan
CHEMBL3943962 155981 0 None 8 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 419 4 1 2 5.9 Cc1c(C2(N3CCCC3)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccc(F)cc12 nan
44252534 159094 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 350 4 0 2 4.4 CC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3969636 159094 0 None -3 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 350 4 0 2 4.4 CC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44336905 174706 0 None 5 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 346 5 1 2 4.7 N[C@@H](c1cccc(F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL431445 174706 0 None 5 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 346 5 1 2 4.7 N[C@@H](c1cccc(F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
44391075 129848 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 415 6 2 6 3.8 Cc1ccc(Cl)c(OC[C@H](O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL360972 129848 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 415 6 2 6 3.8 Cc1ccc(Cl)c(OC[C@H](O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
57502947 134972 0 None - 1 Human 5.7 pKi = 5.7 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 466 3 1 6 2.6 O=C(C1=C(n2c(=O)c(=O)[nH]c3ccccc32)CCN(C2CCCCCCC2)C1)N1CCOCC1 nan
CHEMBL3665438 134972 0 None - 1 Human 5.7 pKi = 5.7 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 466 3 1 6 2.6 O=C(C1=C(n2c(=O)c(=O)[nH]c3ccccc32)CCN(C2CCCCCCC2)C1)N1CCOCC1 nan
90656664 117738 0 None -204 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 499 6 2 5 4.7 CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm401964y
CHEMBL3262361 117738 0 None -204 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 499 6 2 5 4.7 CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23C=C[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm401964y
44337362 179241 0 None 4 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 358 6 1 3 4.6 COc1ccc([C@H](N)[C@@H]2CCN2C(c2ccccc2)c2ccccc2)cc1 10.1016/s0960-894x(02)00652-2
CHEMBL448155 179241 0 None 4 4 Human 6.7 pKi = 6.7 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 358 6 1 3 4.6 COc1ccc([C@H](N)[C@@H]2CCN2C(c2ccccc2)c2ccccc2)cc1 10.1016/s0960-894x(02)00652-2
44593575 185259 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 361 3 1 2 5.1 OC1CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466438 185259 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 361 3 1 2 5.1 OC1CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
97333 92732 78 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 267 3 1 2 3.2 OC1(c2ccccc2)CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL230141 92732 78 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 267 3 1 2 3.2 OC1(c2ccccc2)CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL413178 219832 0 None - 1 Mouse 6.7 pKi = 6.7 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None Cc1ccc(C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)cc1 10.1021/jm990075h
45271534 202035 0 None 162 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 472 6 1 3 6.2 OCCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL551111 202035 0 None 162 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 472 6 1 3 6.2 OCCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
45269032 202963 0 None 208 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 428 4 1 2 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@H]1CC(C1CCCCN1)C2 10.1021/jm9008218
CHEMBL561373 202963 0 None 208 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 428 4 1 2 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@H]1CC(C1CCCCN1)C2 10.1021/jm9008218
44413330 86707 0 None 85 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 383 2 1 4 4.2 Cn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2O)c2cccnc21 10.1016/j.bmcl.2006.03.094
CHEMBL212525 86707 0 None 85 3 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 383 2 1 4 4.2 Cn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2O)c2cccnc21 10.1016/j.bmcl.2006.03.094
9844540 92494 0 None 128 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 6.1 OC1(c2ccccc2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228911 92494 0 None 128 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 6.1 OC1(c2ccccc2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
9863568 148867 0 None 45 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 148867 0 None 45 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 148867 0 None 45 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 148867 0 None 45 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44430079 93500 0 None 99 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 497 6 3 3 5.5 CNC(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL231866 93500 0 None 99 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 497 6 3 3 5.5 CNC(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
44574745 185381 0 None 13 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 493 5 2 2 6.5 CNC(=O)NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467314 185381 0 None 13 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 493 5 2 2 6.5 CNC(=O)NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
18782378 98551 0 None 46 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 395 2 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3c(Cl)cccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL241086 98551 0 None 46 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 395 2 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3c(Cl)cccc31)CC2 10.1016/j.bmcl.2007.01.069
9848110 177425 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-nociceptin from human nociceptin receptor expressed in cell membranes after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-nociceptin from human nociceptin receptor expressed in cell membranes after 60 mins by liquid scintillation counting analysis
ChEMBL 373 4 2 5 4.4 Cc1ccc2nc(/C=C/c3ccccn3)nc(N[C@H]3CC[C@@H](N)C[C@H]3C)c2c1 10.1016/j.ejmech.2018.12.012
CHEMBL4451306 177425 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-nociceptin from human nociceptin receptor expressed in cell membranes after 60 mins by liquid scintillation counting analysisDisplacement of [3H]-nociceptin from human nociceptin receptor expressed in cell membranes after 60 mins by liquid scintillation counting analysis
ChEMBL 373 4 2 5 4.4 Cc1ccc2nc(/C=C/c3ccccn3)nc(N[C@H]3CC[C@@H](N)C[C@H]3C)c2c1 10.1016/j.ejmech.2018.12.012
44437602 97429 0 None 14 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239043 97429 0 None 14 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437638 98005 0 None 22 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 494 11 1 7 4.5 CNCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240084 98005 0 None 22 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 494 11 1 7 4.5 CNCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437656 152493 0 None 7 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 10 1 6 3.7 CNC(=O)CN1CN(c2ccccc2)C2(CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)C1=O 10.1016/j.bmc.2006.11.030
CHEMBL391631 152493 0 None 7 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 10 1 6 3.7 CNC(=O)CN1CN(c2ccccc2)C2(CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)C1=O 10.1016/j.bmc.2006.11.030
44437654 152513 0 None 16 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 451 8 1 5 4.2 COc1ccc(C)c(OC(CCN2CCC3(CC2)C(=O)NCN3c2ccccc2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391650 152513 0 None 16 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 451 8 1 5 4.2 COc1ccc(C)c(OC(CCN2CCC3(CC2)C(=O)NCN3c2ccccc2)C(C)C)c1 10.1016/j.bmc.2006.11.030
10225083 173175 0 None 8 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL427683 173175 0 None 8 4 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
118711486 120767 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells at 1 uM after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells at 1 uM after 90 mins
ChEMBL 362 6 1 2 5.1 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3326225 120767 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells at 1 uM after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells at 1 uM after 90 mins
ChEMBL 362 6 1 2 5.1 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
155533462 178612 0 None 15 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 385 4 1 5 3.8 CCn1c(=O)n([C@@H]2CCN(C3CCCCCCC3)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.5b01499
CHEMBL4468676 178612 0 None 15 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from recombinant human nociceptin opioid receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 385 4 1 5 3.8 CCn1c(=O)n([C@@H]2CCN(C3CCCCCCC3)C[C@H]2CO)c2ccccc21 10.1021/acs.jmedchem.5b01499
12985907 64333 0 None 3 3 Rat 8.7 pKi = 8.7 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 4 1 3 3.8 CCC[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL166445 64333 0 None 3 3 Rat 8.7 pKi = 8.7 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 4 1 3 3.8 CCC[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
60154189 84372 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088038 84372 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088039 84372 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
11123873 85408 0 None 70 4 Human 8.7 pKi = 8.7 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 494 6 0 5 4.4 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(CCN4CCOCC4)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112341 85408 0 None 70 4 Human 8.7 pKi = 8.7 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 494 6 0 5 4.4 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(CCN4CCOCC4)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
9947044 105047 0 None 15 4 Human 8.7 pKi = 8.7 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL27460 105047 0 None 15 4 Human 8.7 pKi = 8.7 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3ccccc31)CC2 10.1021/jm991129q
25190610 186580 0 None 16 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 446 5 1 4 4.2 CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL474485 186580 0 None 16 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 446 5 1 4 4.2 CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
25190586 187082 0 None 239 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 536 8 1 4 5.8 CCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475096 187082 0 None 239 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 536 8 1 4 5.8 CCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
24800107 198640 0 None 7 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 437 3 1 5 5.4 CC1CN(c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)CC(C)N1 10.1021/jm7012979
CHEMBL519925 198640 0 None 7 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 437 3 1 5 5.4 CC1CN(c2nc3ccccc3n2C2CCN(C3(C)CCCCCCC3)CC2)CC(C)N1 10.1021/jm7012979
90655971 117779 0 None 19 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
CHEMBL3262542 117779 0 None 19 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
11826819 85410 1 None 72 4 Human 8.7 pKi = 8.7 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 471 5 0 3 6.3 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(Cc4ccccc4)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112343 85410 1 None 72 4 Human 8.7 pKi = 8.7 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 471 5 0 3 6.3 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CN(Cc4ccccc4)C[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
25190593 196517 0 None 77 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 564 10 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL515829 196517 0 None 77 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 564 10 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
129188454 176612 0 None 25 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 4 1 4 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(/C=N/O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4439811 176612 0 None 25 3 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 4 1 4 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(/C=N/O)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
10937810 85411 0 None 117 4 Human 8.7 pKi = 8.7 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 381 3 1 3 4.4 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CNC[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
CHEMBL2112344 85411 0 None 117 4 Human 8.7 pKi = 8.7 Binding
Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)Inhibition of N/OFQ binding to human Orphanin FQ receptor (Nociceptin/Orphanin)
ChEMBL 381 3 1 3 4.4 CC(C)[C@H]1CC[C@@H](N2CCC3(CC2)[C@@H]2CNC[C@@H]2CN3c2ccccc2)CC1 10.1021/jm0209174
9846747 125781 1 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
CHEMBL342580 125781 1 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
CHEMBL405212 219329 0 None - 1 Human 8.7 pKi = 8.7 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
10363496 169954 0 None 15 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against delta-opioid receptor in guinea pig brain membranesBinding affinity against delta-opioid receptor in guinea pig brain membranes
ChEMBL 398 2 2 3 4.3 Oc1ccc2c3c1O[C@H]1Cc4c([nH]c5ccccc45)[C@H]4[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/jm00038a019
CHEMBL418105 169954 0 None 15 2 Human 8.7 pKi = 8.7 Binding
Binding affinity against delta-opioid receptor in guinea pig brain membranesBinding affinity against delta-opioid receptor in guinea pig brain membranes
ChEMBL 398 2 2 3 4.3 Oc1ccc2c3c1O[C@H]1Cc4c([nH]c5ccccc45)[C@H]4[C@@H](C2)N(CC2CC2)CC[C@]314 10.1021/jm00038a019
44430084 93544 0 None 63 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 523 6 1 4 5.8 CN1CCN(Cc2ccccc2C2(O)CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232076 93544 0 None 63 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 523 6 1 4 5.8 CN1CCN(Cc2ccccc2C2(O)CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)CC1 10.1016/j.bmcl.2007.03.062
11516508 145777 0 None 31 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 382 2 2 3 4.0 Oc1ccc(Cl)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3785560 145777 0 None 31 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 382 2 2 3 4.0 Oc1ccc(Cl)c2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
9937777 182136 0 None 114 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 562 7 0 4 6.3 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL457451 182136 0 None 114 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 562 7 0 4 6.3 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
129188462 183185 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4465668 183185 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4596017 183185 0 None 190 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 367 5 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
9825723 123456 1 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 428 6 2 6 4.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc([N+](=O)[O-])cc3)ccc2n1 10.1021/jm0002073
CHEMBL337128 123456 1 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 428 6 2 6 4.9 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc([N+](=O)[O-])cc3)ccc2n1 10.1021/jm0002073
1691 8888 23 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1016/j.bmcl.2003.11.083
5311194 8888 23 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1016/j.bmcl.2003.11.083
CHEMBL357076 8888 23 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10.1016/j.bmcl.2003.11.083
10155966 196056 0 None 40 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 369 4 1 2 5.3 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL511920 196056 0 None 40 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 369 4 1 2 5.3 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
25190598 98064 0 None 12 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 389 3 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL240215 98064 0 None 12 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 389 3 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
10323169 186161 0 None 6 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 6 0 4 4.7 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL473904 186161 0 None 6 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 486 6 0 4 4.7 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
25190598 98064 0 None 12 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 389 3 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240215 98064 0 None 12 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 389 3 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
118662456 179750 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 365 5 0 3 4.8 CN(C)C1(c2ccccc2)CCC2(CCN(CCC3(C#N)CCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
CHEMBL4517646 179750 0 None 1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 365 5 0 3 4.8 CN(C)C1(c2ccccc2)CCC2(CCN(CCC3(C#N)CCC3)C2)CC1 10.1021/acsmedchemlett.6b00277
46879579 12810 0 None -2 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 438 4 1 4 4.0 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCCCCCCCC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1080464 12810 0 None -2 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 438 4 1 4 4.0 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCCCCCCCC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
44451619 102636 0 None 32 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 519 10 0 9 4.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncon4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259048 102636 0 None 32 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 519 10 0 9 4.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncon4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44438922 98566 0 None 9 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 363 5 1 3 4.0 CCCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL241112 98566 0 None 9 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 363 5 1 3 4.0 CCCC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
11544795 145794 0 None 120 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1cccc2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3785718 145794 0 None 120 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 348 2 2 3 3.4 Oc1cccc2c1CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
46178991 132574 0 None 1071 4 Human 8.6 pKi = 8.6 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 435 3 1 5 4.6 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CCC[C@H](C2)N3C2CC3CCCC(C3)C2)c1=O nan
CHEMBL3647958 132574 0 None 1071 4 Human 8.6 pKi = 8.6 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 435 3 1 5 4.6 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CCC[C@H](C2)N3C2CC3CCCC(C3)C2)c1=O nan
44253417 159466 0 None 199 2 Human 8.6 pKi = 8.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 402 6 0 4 4.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2ccn(C)n2)CC1 nan
CHEMBL3972755 159466 0 None 199 2 Human 8.6 pKi = 8.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 402 6 0 4 4.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)Cc2ccn(C)n2)CC1 nan
10618605 105411 0 None 4 4 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCc3ccccc31)CC2 10.1021/jm991129q
CHEMBL27716 105411 0 None 4 4 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 361 2 1 3 3.5 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCCc3ccccc31)CC2 10.1021/jm991129q
10593778 106018 0 None 10 4 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 347 2 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(C1Cc3ccccc3C1)CC2 10.1021/jm991129q
CHEMBL28172 106018 0 None 10 4 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 347 2 1 3 2.6 O=C1NCN(c2ccccc2)C12CCN(C1Cc3ccccc3C1)CC2 10.1021/jm991129q
44570675 190609 0 None 4 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 325 2 0 3 5.2 CC1(N2CCC(n3cnc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
CHEMBL480619 190609 0 None 4 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cellsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells
ChEMBL 325 2 0 3 5.2 CC1(N2CCC(n3cnc4ccccc43)CC2)CCCCCCC1 10.1021/jm7012979
46879581 12672 0 None 42 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 462 4 1 4 3.7 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079571 12672 0 None 42 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 462 4 1 4 3.7 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCCCCCCCC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL412479 219774 0 None - 1 Mouse 8.6 pKi = 8.6 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None CC(C)C[C@H](N)C(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O 10.1021/jm990075h
44451543 103206 0 None 41 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 0 8 5.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cocn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL262064 103206 0 None 41 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 0 8 5.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cocn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
25190587 197548 0 None 181 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 550 8 1 4 6.2 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL518325 197548 0 None 181 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 550 8 1 4 6.2 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
10718869 40774 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 461 5 2 4 5.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Br)cc3)ccc2n1 10.1021/jm0002073
CHEMBL142454 40774 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 461 5 2 4 5.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(Br)cc3)ccc2n1 10.1021/jm0002073
44438993 155210 0 None 4 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 395 2 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3cccc(Cl)c31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL393781 155210 0 None 4 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 395 2 1 3 4.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCc3cccc(Cl)c31)CC2 10.1016/j.bmcl.2007.01.069
10385808 72916 0 None 33 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 72916 0 None 33 2 Human 8.6 pKi = 8.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
44252249 155810 0 None -2 2 Human 8.6 pKi = 8.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 420 6 1 3 4.7 CN(C)C1(c2ccccc2)CCC(C)(CNS(=O)(=O)c2ccc(Cl)cc2)CC1 nan
CHEMBL3942616 155810 0 None -2 2 Human 8.6 pKi = 8.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 420 6 1 3 4.7 CN(C)C1(c2ccccc2)CCC(C)(CNS(=O)(=O)c2ccc(Cl)cc2)CC1 nan
44574585 185407 0 None 21 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 469 4 1 2 7.0 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2cccc(F)c2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL467488 185407 0 None 21 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 469 4 1 2 7.0 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2cccc(F)c2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
46880238 12821 0 None 51 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 442 5 1 5 3.8 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc(C)c4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080508 12821 0 None 51 2 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 442 5 1 5 3.8 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc(C)c4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
25190594 182040 0 None 87 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 564 9 1 4 6.5 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL457244 182040 0 None 87 4 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 564 9 1 4 6.5 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
10574643 106366 0 None 2 4 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL283910 106366 0 None 2 4 Human 8.6 pKi = 8.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN([C@H]1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
11795019 105390 0 None 3 4 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)cccc3C1)CC2 10.1021/jm991129q
CHEMBL27699 105390 0 None 3 4 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)cccc3C1)CC2 10.1021/jm991129q
118662291 179174 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 320 5 0 3 4.6 CCCCN1CCC2(CCC(c3cccs3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
CHEMBL4476510 179174 0 None -1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 320 5 0 3 4.6 CCCCN1CCC2(CCC(c3cccs3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
46879538 12957 0 None 4 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 462 5 1 4 3.0 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1081192 12957 0 None 4 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 462 5 1 4 3.0 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
90655973 117782 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262545 117782 0 None -2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL414541 219916 0 None - 1 Human 7.7 pKi = 7.7 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)O 10.1021/jm0202021
44253419 154041 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 428 7 0 3 6.1 COc1ccc(CN(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
CHEMBL3928651 154041 0 None 5 2 Human 7.7 pKi = 7.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 428 7 0 3 6.1 COc1ccc(CN(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
44391133 71899 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 457 8 2 6 4.9 CCCC(Oc1cc(C)ccc1Cl)C(O)CN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/j.bmcl.2004.11.049
CHEMBL182410 71899 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 457 8 2 6 4.9 CCCC(Oc1cc(C)ccc1Cl)C(O)CN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/j.bmcl.2004.11.049
118718280 122096 0 None 21 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 509 8 1 4 6.7 CCNC[C@]1(c2cccc(OC)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349264 122096 0 None 21 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 509 8 1 4 6.7 CCNC[C@]1(c2cccc(OC)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
25235412 122108 0 None 38 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349276 122108 0 None 38 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718292 122109 0 None 45 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 508 6 1 3 7.0 COC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349277 122109 0 None 45 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 508 6 1 3 7.0 COC(=O)NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
24894647 193348 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 351 3 1 4 3.2 Cc1ccccc1N1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL487826 193348 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 351 3 1 4 3.2 Cc1ccccc1N1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
44574791 185356 0 None 30 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 464 5 1 3 7.1 O/N=C/C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467119 185356 0 None 30 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 464 5 1 3 7.1 O/N=C/C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
25235412 110095 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084527 110095 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 492 6 1 2 6.8 CC(=O)NC[C@@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44437642 98528 0 None 12 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 536 11 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL240941 98528 0 None 12 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 536 11 1 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437645 98573 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 552 13 1 8 4.0 COCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL241157 98573 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 552 13 1 8 4.0 COCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
118711486 120767 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 362 6 1 2 5.1 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3326225 120767 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 362 6 1 2 5.1 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
10669669 42040 0 None - 1 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3cccc(Cl)c3)ccc2n1 10.1021/jm0002073
CHEMBL143605 42040 0 None - 1 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3cccc(Cl)c3)ccc2n1 10.1021/jm0002073
22562137 97243 0 None -2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 3 0 2 4.6 CC(C)C1CCC(N2CCC(N3C(=O)CCc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387198 97243 0 None -2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 3 0 2 4.6 CC(C)C1CCC(N2CCC(N3C(=O)CCc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
10836379 169945 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL418020 169945 0 None -2 4 Human 7.7 pKi = 7.7 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN([C@@H]1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
134563704 183413 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4451073 183413 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4597933 183413 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 381 6 1 3 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
3655995 115522 6 None -2 3 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/jm034249d
CHEMBL320874 115522 6 None -2 3 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/jm034249d
3655995 115522 6 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.5b00982
CHEMBL320874 115522 6 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1021/acs.jmedchem.5b00982
3655995 115522 6 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL320874 115522 6 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 306 3 0 2 3.2 O=C1Cc2ccccc2N1C1CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2013.03.101
46179069 132575 0 None 117 3 Human 6.7 pKi = 6.7 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 421 3 1 5 4.2 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CC3CCCC(C3)C2)c1=O nan
CHEMBL3647959 132575 0 None 117 3 Human 6.7 pKi = 6.7 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 421 3 1 5 4.2 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CC3CCCC(C3)C2)c1=O nan
25190579 196412 0 None 3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 437 6 0 3 5.1 C=CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL514965 196412 0 None 3 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 437 6 0 3 5.1 C=CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
66911347 120667 0 None -4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 295 3 1 2 3.9 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(c2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325745 120667 0 None -4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 295 3 1 2 3.9 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(c2ccccc2)CC1 10.1021/ml500116x
44253421 158135 0 None -7 2 Human 5.7 pKi = 5.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 393 4 1 2 5.4 Cc1c(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccc(F)cc12 nan
CHEMBL3961206 158135 0 None -7 2 Human 5.7 pKi = 5.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 393 4 1 2 5.4 Cc1c(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccc(F)cc12 nan
44252839 153757 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 338 5 1 3 4.1 CNC1(c2ccccc2)CCC(c2ccc(OC)cc2)(N(C)C)CC1 nan
CHEMBL3926333 153757 0 None 3 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 338 5 1 3 4.1 CNC1(c2ccccc2)CCC(c2ccc(OC)cc2)(N(C)C)CC1 nan
44253565 149190 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 5 0 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2cccc(F)c2)CC1 nan
CHEMBL3889835 149190 0 None 1 2 Human 7.7 pKi = 7.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 5 0 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2cccc(F)c2)CC1 nan
24776398 104671 0 None 8 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 368 1 0 2 4.6 CN1Cc2ccccc2C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1021/jm7009606
CHEMBL272390 104671 0 None 8 3 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 368 1 0 2 4.6 CN1Cc2ccccc2C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1021/jm7009606
44426842 150034 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 499 4 1 2 6.3 OC1(c2ccccc2)CCN(C(c2ccccc2Br)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL389666 150034 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 499 4 1 2 6.3 OC1(c2ccccc2)CCN(C(c2ccccc2Br)c2ccccc2Br)CC1 10.1016/j.bmcl.2007.03.061
24894533 193087 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 370 3 2 4 3.0 Cc1cc(F)ccc1[C@H]1CCN(C[C@@H]2Cc3cccnc3[C@@H](O)C2)C[C@@H]1O 10.1021/jm701590h
CHEMBL487457 193087 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 370 3 2 4 3.0 Cc1cc(F)ccc1[C@H]1CCN(C[C@@H]2Cc3cccnc3[C@@H](O)C2)C[C@@H]1O 10.1021/jm701590h
46879536 13129 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 5 1 3 3.9 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1082092 13129 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 5 1 3 3.9 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
44451518 166692 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 0 8 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cc(C)on4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL410706 166692 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 0 8 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cc(C)on4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44253416 155887 0 None 11 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 631 11 0 9 7.8 COc1ccc(Oc2nc(Oc3ccc(OC)cc3)nc(N(C)C3(c4ccccc4)CCC(c4ccccc4)(N(C)C)CC3)n2)cc1 nan
CHEMBL3943194 155887 0 None 11 2 Human 6.7 pKi = 6.7 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 631 11 0 9 7.8 COc1ccc(Oc2nc(Oc3ccc(OC)cc3)nc(N(C)C3(c4ccccc4)CCC(c4ccccc4)(N(C)C)CC3)n2)cc1 nan
118718293 122110 0 None 12 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 506 6 0 2 7.1 CC(=O)N(C)C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349278 122110 0 None 12 2 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 506 6 0 2 7.1 CC(=O)N(C)C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
9848990 195944 1 None -812 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
CHEMBL2368861 195944 1 None -812 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
CHEMBL511142 195944 1 None -812 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
9848990 195944 1 None -812 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL2368861 195944 1 None -812 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL511142 195944 1 None -812 6 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
71624267 97235 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 312 3 0 2 3.6 O=C1Cc2ccccc2N1C1CCN(CC2CCCCC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387190 97235 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 312 3 0 2 3.6 O=C1Cc2ccccc2N1C1CCN(CC2CCCCC2)CC1 10.1016/j.bmcl.2013.03.101
44366689 127754 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 903 22 10 10 -0.7 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)NC1S[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
CHEMBL356210 127754 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 903 22 10 10 -0.7 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)NC1S[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
44426822 143778 0 None 27 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 344 4 1 3 4.2 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccn2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL374602 143778 0 None 27 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 344 4 1 3 4.2 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccn2)CC1 10.1016/j.bmcl.2007.03.061
131534 171434 23 None -19498 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 544 7 1 3 6.1 CN(C)C(=O)C(CCN1CCC(O)(c2ccc(Cl)c(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
CHEMBL421665 171434 23 None -19498 2 Human 5.7 pKi = 5.7 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 544 7 1 3 6.1 CN(C)C(=O)C(CCN1CCC(O)(c2ccc(Cl)c(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
46879627 13059 0 None -4 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 385 3 1 4 3.4 CNC(=O)CN1C(=O)OC2(CCN(C3CCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1081741 13059 0 None -4 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 385 3 1 4 3.4 CNC(=O)CN1C(=O)OC2(CCN(C3CCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
134563500 182843 0 None 6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 436 5 1 4 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCC(N)CC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4590786 182843 0 None 6 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 436 5 1 4 5.4 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCC(N)CC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
118662169 180650 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 314 3 0 2 3.3 CC(=O)N1CCC2(CCC(Cc3ccccc3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
CHEMBL4539568 180650 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 314 3 0 2 3.3 CC(=O)N1CCC2(CCC(Cc3ccccc3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
44430028 93456 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 5 1 2 4.8 OC1(Cc2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL231661 93456 0 None -1 4 Human 5.7 pKi = 5.7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 5 1 2 4.8 OC1(Cc2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
44391069 70675 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 452 8 1 7 5.1 Cc1ccc([N+](=O)[O-])cc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL180499 70675 0 None -1 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 452 8 1 7 5.1 Cc1ccc([N+](=O)[O-])cc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
10500922 104389 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3cc(Cl)ccc3C1)CC2 10.1021/jm991129q
CHEMBL27093 104389 0 None -2 4 Human 6.7 pKi = 6.7 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3cc(Cl)ccc3C1)CC2 10.1021/jm991129q
60154191 84374 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088041 84374 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088042 84374 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 432 5 0 4 4.2 CN(C)C(=O)C(Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
71454460 85451 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 324 3 0 2 3.5 O=C1Cc2ccccc2N1C1CCN(C[C@H]2CC3CCC2C3)CC1 10.1021/jm034249d
CHEMBL2112407 85451 0 None 5 3 Human 7.7 pKi = 7.7 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 324 3 0 2 3.5 O=C1Cc2ccccc2N1C1CCN(C[C@H]2CC3CCC2C3)CC1 10.1021/jm034249d
44248790 110163 0 None 40 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 500 4 0 2 7.7 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccc(Br)cn1)C2 10.1021/jm9008218
CHEMBL3084656 110163 0 None 40 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 500 4 0 2 7.7 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccc(Br)cn1)C2 10.1021/jm9008218
44574850 196130 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 494 6 1 3 6.1 COc1ccc(C2(C(N)=O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2009.03.031
CHEMBL512612 196130 0 None 2 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 494 6 1 3 6.1 COc1ccc(C2(C(N)=O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2009.03.031
76316936 110101 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 495 6 1 4 5.5 COc1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
CHEMBL3084533 110101 0 None 6 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 495 6 1 4 5.5 COc1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
54756990 72478 0 None -10 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 543 7 2 5 5.7 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834411 72478 0 None -10 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 543 7 2 5 5.7 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)CC(C)(C)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
46879668 12740 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 456 5 1 3 4.3 CNC(=O)CN1Cc2ccccc2N(C2CCN(Cc3ccc(C)c4ccccc34)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079941 12740 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 456 5 1 3 4.3 CNC(=O)CN1Cc2ccccc2N(C2CCN(Cc3ccc(C)c4ccccc34)CC2)C1=O 10.1016/j.bmcl.2009.09.028
44437613 153669 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 10 0 7 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)N(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL392548 153669 0 None 8 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 10 0 7 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)N(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
25134076 134956 0 None 36 4 Human 7.6 pKi = 7.6 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 369 3 1 4 3.5 CC(C)C1CCC(N2CCC(n3c(=O)c(=O)[nH]c4ccccc43)CC2)CC1 nan
CHEMBL3665422 134956 0 None 36 4 Human 7.6 pKi = 7.6 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 369 3 1 4 3.5 CC(C)C1CCC(N2CCC(n3c(=O)c(=O)[nH]c4ccccc43)CC2)CC1 nan
44339374 117374 0 None -56 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 473 6 1 2 6.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
CHEMBL325536 117374 0 None -56 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 473 6 1 2 6.9 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
44426831 92474 0 None 5 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 5.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228795 92474 0 None 5 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 5.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccc(C(F)(F)F)cc2)CC1 10.1016/j.bmcl.2007.03.061
10137134 98481 0 None 7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 423 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1c3ccccc3CCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240870 98481 0 None 7 4 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 423 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1c3ccccc3CCc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
10110916 73036 0 None 24 2 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 389 2 1 3 4.0 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184646 73036 0 None 24 2 Human 6.7 pKi = 6.7 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 389 2 1 3 4.0 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
44402566 173060 0 None -23 3 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 478 3 0 5 6.5 CN(C)c1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
CHEMBL427007 173060 0 None -23 3 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 478 3 0 5 6.5 CN(C)c1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
46879628 12644 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 396 4 1 4 2.8 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCCCCC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079416 12644 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 396 4 1 4 2.8 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCCCCC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
46879993 12993 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 370 4 1 5 2.5 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1081375 12993 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 370 4 1 5 2.5 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
57502905 134960 0 None - 1 Human 6.6 pKi = 6.6 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 387 2 1 3 4.1 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2cccc(F)c2N1 nan
CHEMBL3665426 134960 0 None - 1 Human 6.6 pKi = 6.6 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 387 2 1 3 4.1 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2cccc(F)c2N1 nan
9947155 73081 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 363 2 1 3 3.7 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184864 73081 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 363 2 1 3 3.7 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCCCCCC2)CC1 10.1016/j.bmcl.2004.08.001
44248915 110169 0 None 25 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 468 5 0 3 7.6 CSc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
CHEMBL3084666 110169 0 None 25 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 468 5 0 3 7.6 CSc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
24776408 164182 0 None 173 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 358 2 1 2 4.0 CC(C)C1CCC(N2CCC3(CC2)C(=O)NCc2cc(F)ccc23)CC1 10.1021/jm7009606
CHEMBL407846 164182 0 None 173 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 358 2 1 2 4.0 CC(C)C1CCC(N2CCC3(CC2)C(=O)NCc2cc(F)ccc23)CC1 10.1021/jm7009606
9863568 148867 0 None 45 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL388123 148867 0 None 45 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL535844 148867 0 None 45 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL541636 148867 0 None 45 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44430008 157776 0 None 30 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 361 4 1 2 4.9 OC1(c2cccc(F)c2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL395838 157776 0 None 30 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 361 4 1 2 4.9 OC1(c2cccc(F)c2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
22970051 160040 0 None 11 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 323 6 1 2 4.8 CCCCC1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL397761 160040 0 None 11 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 323 6 1 2 4.8 CCCCC1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
15541261 98351 0 None 6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 397 4 1 3 4.2 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL240657 98351 0 None 6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 397 4 1 3 4.2 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
15541261 98351 0 None 6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 397 4 1 3 4.2 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240657 98351 0 None 6 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 397 4 1 3 4.2 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2007.01.069
44437652 97402 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 548 11 1 7 4.9 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CCC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238819 97402 0 None 4 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 548 11 1 7 4.9 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CCC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
155542684 179928 0 None 41 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 466 10 2 4 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(=O)CCCCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4521436 179928 0 None 41 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 466 10 2 4 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CNC(=O)CCCCCN)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
134563496 181332 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 409 5 1 4 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC(O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4556227 181332 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 409 5 1 4 4.7 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC(O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
68632578 155212 0 None 8 2 Human 6.6 pKi = 6.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 393 6 0 3 3.9 CN(C)C(=O)CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3937815 155212 0 None 8 2 Human 6.6 pKi = 6.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 393 6 0 3 3.9 CN(C)C(=O)CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44394283 72937 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 4 1 3 3.7 CCCC1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184260 72937 0 None -1 2 Human 6.6 pKi = 6.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 4 1 3 3.7 CCCC1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
44339500 14239 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 387 3 1 2 5.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL108695 14239 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 387 3 1 2 5.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(03)00665-6
25190578 186783 0 None 5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 435 5 0 3 4.6 C#CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL474708 186783 0 None 5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 435 5 0 3 4.6 C#CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
69016300 160617 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 416 5 0 4 4.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2ccn(C)n2)CC1 nan
CHEMBL3982651 160617 0 None -3 2 Human 6.6 pKi = 6.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 416 5 0 4 4.4 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)c2ccn(C)n2)CC1 nan
10194236 114042 0 None 28 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 396 5 1 2 5.6 N[C@@H](c1cccc(C(F)(F)F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL316961 114042 0 None 28 4 Human 6.6 pKi = 6.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 396 5 1 2 5.6 N[C@@H](c1cccc(C(F)(F)F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
56668405 72481 0 None -35 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 545 4 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4c(Br)cc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834414 72481 0 None -35 4 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 545 4 2 5 5.2 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4c(Br)cc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
44391103 72345 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 461 7 1 5 5.9 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.11.049
CHEMBL183135 72345 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 461 7 1 5 5.9 CC(C)C(CCN1CCC(n2c(O)nc3ccccc32)CC1)Oc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.11.049
10070040 106066 4 None -169 3 Human 7.6 pKi = 7.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 408 7 0 4 3.9 CCC(=O)N(c1ccccc1)[C@@]1(C(=O)OC)CCN(CCc2ccccc2)C[C@H]1C 10.1021/jm991129q
CHEMBL28198 106066 4 None -169 3 Human 7.6 pKi = 7.6 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 408 7 0 4 3.9 CCC(=O)N(c1ccccc1)[C@@]1(C(=O)OC)CCN(CCc2ccccc2)C[C@H]1C 10.1021/jm991129q
44248792 110162 0 None 9 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 438 4 1 3 6.6 Oc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
CHEMBL3084655 110162 0 None 9 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 438 4 1 3 6.6 Oc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
10091033 153903 0 None 38 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 377 4 1 2 5.4 OC1(c2ccc(Cl)cc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL392753 153903 0 None 38 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 377 4 1 2 5.4 OC1(c2ccc(Cl)cc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
118718272 122088 0 None 53 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 511 6 1 3 6.3 CC(=O)NC[C@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349256 122088 0 None 53 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 511 6 1 3 6.3 CC(=O)NC[C@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
24894425 185908 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 364 3 1 3 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C(C)(O)C2)CC1 10.1021/jm701590h
CHEMBL471981 185908 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 364 3 1 3 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C(C)(O)C2)CC1 10.1021/jm701590h
134563698 178510 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 426 6 2 3 4.9 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4467156 178510 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 426 6 2 3 4.9 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
122179056 128179 0 None -2454 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581752 128179 0 None -2454 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
118718283 122099 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 548 7 1 4 7.0 NC[C@]1(c2ncccc2CN2CCCCC2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349267 122099 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 548 7 1 4 7.0 NC[C@]1(c2ncccc2CN2CCCCC2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44402627 78613 0 None -7 3 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 504 3 0 5 6.2 O=C1CCN1c1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
CHEMBL196932 78613 0 None -7 3 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 504 3 0 5 6.2 O=C1CCN1c1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
44438971 97902 0 None 6 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1cccc(Cl)c1)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL239819 97902 0 None 6 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1cccc(Cl)c1)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2007.01.069
44391134 130091 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 425 7 1 5 5.3 Cc1ccc(F)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL361576 130091 0 None 2 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 425 7 1 5 5.3 Cc1ccc(F)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
44248919 110166 0 None 213 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 440 4 0 2 7.0 Fc1cccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1021/jm9008218
CHEMBL3084661 110166 0 None 213 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 440 4 0 2 7.0 Fc1cccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1021/jm9008218
24894653 196120 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 392 3 0 4 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C3(C2)OCCO3)CC1 10.1021/jm701590h
CHEMBL512530 196120 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 392 3 0 4 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C3(C2)OCCO3)CC1 10.1021/jm701590h
11781971 103416 0 None 3 3 Rat 7.6 pKi = 7.6 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 313 2 1 3 2.7 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL263575 103416 0 None 3 3 Rat 7.6 pKi = 7.6 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 313 2 1 3 2.7 O=C1NCN(c2ccccc2)C12CCN(C1CCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL413516 219853 0 None - 1 Mouse 7.6 pKi = 7.6 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm990075h
44252539 160644 0 None 52 2 Human 7.6 pKi = 7.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 328 4 0 3 4.5 CN(C)C1(c2ccccc2)CCC(c2cccs2)(N(C)C)CC1 nan
CHEMBL3982887 160644 0 None 52 2 Human 7.6 pKi = 7.6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 328 4 0 3 4.5 CN(C)C1(c2ccccc2)CCC(c2cccs2)(N(C)C)CC1 nan
44438975 97905 0 None 5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 433 4 1 3 4.5 O=C1NCN(c2ccccc2)C12CCN(C(c1cccc(F)c1)c1cccc(F)c1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL239821 97905 0 None 5 4 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 433 4 1 3 4.5 O=C1NCN(c2ccccc2)C12CCN(C(c1cccc(F)c1)c1cccc(F)c1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL411168 219645 0 None - 1 Mouse 5.6 pKi = 5.6 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None Cc1ccc(CNCC(=O)NCC(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)cc1 10.1021/jm990075h
CHEMBL425456 220113 0 None - 1 Mouse 5.6 pKi = 5.6 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None CC(C)CNCC(=O)NCC(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O 10.1021/jm990075h
CHEMBL438234 220537 0 None - 1 Mouse 5.6 pKi = 5.6 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCC1CCCCC1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
11327115 214900 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 402 4 0 2 5.8 CC(c1ccc(C2CCCCC2)cc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1021/jm034249d
CHEMBL97979 214900 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 402 4 0 2 5.8 CC(c1ccc(C2CCCCC2)cc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1021/jm034249d
46880115 14290 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 446 5 1 5 3.9 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(c4ccccc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087277 14290 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 446 5 1 5 3.9 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(c4ccccc4)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44337232 115395 0 None -1 4 Human 5.6 pKi = 5.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 518 5 1 2 6.7 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccc(Br)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(02)00652-2
CHEMBL320582 115395 0 None -1 4 Human 5.6 pKi = 5.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 518 5 1 2 6.7 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccc(Br)cc1)c1ccc(Br)cc1 10.1016/s0960-894x(02)00652-2
46880151 14301 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 356 5 1 5 2.0 CNC(=O)Cn1c(=O)n(C2CCN(CC3CCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087369 14301 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 356 5 1 5 2.0 CNC(=O)Cn1c(=O)n(C2CCN(CC3CCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
46880152 14302 0 None 7 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 384 5 1 5 2.8 CNC(=O)Cn1c(=O)n(C2CCN(CC3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087370 14302 0 None 7 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 384 5 1 5 2.8 CNC(=O)Cn1c(=O)n(C2CCN(CC3CCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44337461 115308 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 498 5 1 2 7.2 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1cccc(C(F)(F)F)c1)c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(02)00652-2
CHEMBL320061 115308 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 498 5 1 2 7.2 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1cccc(C(F)(F)F)c1)c1cccc(C(F)(F)F)c1 10.1016/s0960-894x(02)00652-2
44337229 15970 0 None 60 4 Human 7.6 pKi = 7.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 360 7 1 2 5.5 CCCCC(c1cccc(F)c1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL110379 15970 0 None 60 4 Human 7.6 pKi = 7.6 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 360 7 1 2 5.5 CCCCC(c1cccc(F)c1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
24776403 168083 0 None 70 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 448 4 0 2 5.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cc(F)ccc23)CC1 10.1021/jm7009606
CHEMBL412290 168083 0 None 70 3 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 448 4 0 2 5.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cc(F)ccc23)CC1 10.1021/jm7009606
44426833 151055 0 None 7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 377 4 1 2 5.4 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL390498 151055 0 None 7 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 377 4 1 2 5.4 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccc(Cl)c2)CC1 10.1016/j.bmcl.2007.03.061
25190584 196545 0 None 27 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 523 7 0 4 5.9 COCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL516024 196545 0 None 27 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 523 7 0 4 5.9 COCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
122179059 128182 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 517 6 2 6 4.7 COc1ccc([C@@H](O)[C@@]2(C)C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(O)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)cc1 10.1021/acs.jmedchem.5b00130
CHEMBL3581755 128182 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 517 6 2 6 4.7 COc1ccc([C@@H](O)[C@@]2(C)C[C@@]34CC[C@]2(OC)[C@@H]2Oc5c(O)ccc6c5[C@@]23CCN(CC2CC2)[C@@H]4C6)cc1 10.1021/acs.jmedchem.5b00130
70690757 83431 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064139 83431 0 None 19 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 405 5 0 3 3.3 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2)CC1 10.1016/j.ejmech.2012.07.021
70690758 83432 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 423 5 0 3 3.4 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2F)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064140 83432 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 423 5 0 3 3.4 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2F)CC1 10.1016/j.ejmech.2012.07.021
71624269 97237 0 None -11 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 320 3 0 2 3.8 CC(c1ccccc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387192 97237 0 None -11 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 320 3 0 2 3.8 CC(c1ccccc1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
1647 8095 45 None -28 9 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
5462471 8095 45 None -28 9 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
CHEMBL113995 8095 45 None -28 9 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
CHEMBL38874 8095 45 None -28 9 Guinea pig 7.6 pKi = 7.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
24800015 104445 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 450 5 1 2 6.1 CC(C)(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
CHEMBL271187 104445 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 450 5 1 2 6.1 CC(C)(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3F)CC2)CC1 10.1021/jm7009606
44394345 134071 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 397 2 1 3 2.9 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL365870 134071 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 397 2 1 3 2.9 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
21345764 86497 0 None 2 3 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 435 4 1 7 1.9 CC(C)C(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44414863 86497 0 None 2 3 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 435 4 1 7 1.9 CC(C)C(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL211576 86497 0 None 2 3 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 435 4 1 7 1.9 CC(C)C(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
10395965 113542 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 899 22 10 9 -0.6 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
CHEMBL3144469 113542 0 None 3 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 899 22 10 9 -0.6 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
44430009 175549 0 None 10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 4 1 2 5.1 Cc1cccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)c1 10.1016/j.bmcl.2007.03.062
CHEMBL437380 175549 0 None 10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 4 1 2 5.1 Cc1cccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)c1 10.1016/j.bmcl.2007.03.062
118718275 122091 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 499 6 2 3 6.0 CC(=O)NC[C@]1(C2CCCCN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349259 122091 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 499 6 2 3 6.0 CC(=O)NC[C@]1(C2CCCCN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718286 122102 0 None 28 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 571 6 1 3 6.9 CC(=O)NC[C@]1(c2ccc(Br)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349270 122102 0 None 28 2 Human 7.6 pKi = 7.6 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 571 6 1 3 6.9 CC(=O)NC[C@]1(c2ccc(Br)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
155536757 179004 0 None -5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 362 4 0 3 4.7 Cc1ccsc1C1(N(C)C)CCC2(CCN(C(=O)CC(C)C)C2)CC1 10.1021/acsmedchemlett.6b00277
CHEMBL4474067 179004 0 None -5 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 362 4 0 3 4.7 Cc1ccsc1C1(N(C)C)CCC2(CCN(C(=O)CC(C)C)C2)CC1 10.1021/acsmedchemlett.6b00277
127043001 147144 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1577 43 25 17 -1.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL3808398 147144 0 None -10 4 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1577 43 25 17 -1.7 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(F)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
71461579 85222 0 None 4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 324 3 0 2 3.5 O=C1Cc2ccccc2N1C1CCN(C[C@@H]2CC3CCC2C3)CC1 10.1021/jm034249d
CHEMBL2111608 85222 0 None 4 3 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 324 3 0 2 3.5 O=C1Cc2ccccc2N1C1CCN(C[C@@H]2CC3CCC2C3)CC1 10.1021/jm034249d
44248788 110164 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 412 4 0 3 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1cnco1)C2 10.1021/jm9008218
CHEMBL3084657 110164 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 412 4 0 3 6.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1cnco1)C2 10.1021/jm9008218
1614 9273 45 None -186 6 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
443363 9273 45 None -186 6 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
CHEMBL13786 9273 45 None -186 6 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
DB12668 9273 45 None -186 6 Guinea pig 6.6 pKi = 6.6 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL None None None None 10.1016/j.bmcl.2006.05.060
44391081 69380 0 None 5 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 471 8 2 6 5.2 Cc1ccc(Cl)c(OC(CC(C)C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL178318 69380 0 None 5 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 471 8 2 6 5.2 Cc1ccc(Cl)c(OC(CC(C)C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
46879578 12809 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 427 3 1 4 4.6 CNC(=O)CN1C(=O)OC2(CCN(C3CCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080463 12809 0 None -1 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 427 3 1 4 4.6 CNC(=O)CN1C(=O)OC2(CCN(C3CCCCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44297435 201772 0 None -12 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 353 2 1 4 4.9 Oc1nc2ccccc2n1[C@@H]1CCN2[C@H](C3CCCCC3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
CHEMBL54735 201772 0 None -12 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 353 2 1 4 4.9 Oc1nc2ccccc2n1[C@@H]1CCN2[C@H](C3CCCCC3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
44394324 72929 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 403 2 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184234 72929 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 403 2 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2004.08.001
44451572 165512 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 528 10 0 7 5.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ccncc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL409351 165512 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 528 10 0 7 5.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ccncc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
11187225 185944 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL472168 185944 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
44391023 70655 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 399 6 1 5 4.8 Cc1ccc(Cl)c(OCCCN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL180402 70655 0 None 1 2 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 399 6 1 5 4.8 Cc1ccc(Cl)c(OCCCN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44574851 185265 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 548 6 1 3 7.0 NC(=O)C1(c2ccc(OC(F)(F)F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466469 185265 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 548 6 1 3 7.0 NC(=O)C1(c2ccc(OC(F)(F)F)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
70692895 83434 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 411 5 0 3 3.7 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(C2CCCCC2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064143 83434 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 411 5 0 3 3.7 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(C2CCCCC2)CC1 10.1016/j.ejmech.2012.07.021
44248916 110174 0 None 58 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1cccnc1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL3084672 110174 0 None 58 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 436 4 0 2 7.2 Cc1cccnc1[C@@H]1C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
118718271 122087 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 469 5 1 3 6.1 NC[C@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349255 122087 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 469 5 1 3 6.1 NC[C@]1(c2cccc(F)n2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
76324309 110099 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 543 5 1 3 6.3 NC(=O)[C@@]1(c2ccc(Br)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084531 110099 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 543 5 1 3 6.3 NC(=O)[C@@]1(c2ccc(Br)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
46880237 12820 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 428 5 1 5 3.5 CNC(=O)Cn1c(=O)n(C2CCN(Cc3cccc4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080507 12820 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 428 5 1 5 3.5 CNC(=O)Cn1c(=O)n(C2CCN(Cc3cccc4ccccc34)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44437647 97118 0 None 14 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 584 12 1 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCc4ccccc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238600 97118 0 None 14 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 584 12 1 7 5.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NCc4ccccc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437641 98191 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 550 13 1 7 5.2 CCCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240298 98191 0 None 5 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 550 13 1 7 5.2 CCCCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
11393860 11222 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 346 2 0 2 3.6 O=C1Cc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1021/jm034249d
CHEMBL101676 11222 0 None 1 3 Human 7.5 pKi = 7.5 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 346 2 0 2 3.6 O=C1Cc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1021/jm034249d
118662117 178077 0 None -7 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 332 4 0 2 4.1 CN(C)C1(C2CCCC2)CCC2(CCN(C(=O)CC3CC3)C2)CC1 10.1021/acsmedchemlett.6b00277
CHEMBL4460776 178077 0 None -7 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 332 4 0 2 4.1 CN(C)C1(C2CCCC2)CCC2(CCN(C(=O)CC3CC3)C2)CC1 10.1021/acsmedchemlett.6b00277
44451696 102666 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 9 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4nc(C)no4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259157 102666 0 None 3 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 9 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4nc(C)no4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
11624970 145919 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 374 2 0 2 3.9 CC(=O)N1Cc2ccccc2CC1CN1CCC2(CCc3ccccc32)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3787051 145919 0 None 2 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 374 2 0 2 3.9 CC(=O)N1Cc2ccccc2CC1CN1CCC2(CCc3ccccc32)CC1 10.1016/j.ejmech.2016.02.014
16665917 86549 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 342 3 1 1 5.8 Fc1ccc2[nH]cc(C3CCN(CC4CCCCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL211846 86549 0 None -1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 342 3 1 1 5.8 Fc1ccc2[nH]cc(C3CCN(CC4CCCCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
10171862 127341 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 5 0 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@H](OCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325749 127341 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 5 0 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@H](OCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545627 127341 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 5 0 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@H](OCc2ccccc2)CC1 10.1021/ml500116x
57502908 134966 0 None - 1 Human 6.5 pKi = 6.5 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 383 3 0 5 3.9 CCn1c(=O)c(=O)n(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 nan
CHEMBL3665432 134966 0 None - 1 Human 6.5 pKi = 6.5 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 383 3 0 5 3.9 CCn1c(=O)c(=O)n(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 nan
66911347 153596 0 None -1 3 Human 5.5 pKi = 5.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 295 3 1 2 3.9 CN(C)C1(c2ccccc2)CCC(O)(c2ccccc2)CC1 nan
CHEMBL3924824 153596 0 None -1 3 Human 5.5 pKi = 5.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 295 3 1 2 3.9 CN(C)C1(c2ccccc2)CCC(O)(c2ccccc2)CC1 nan
44252989 153214 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 375 5 1 2 5.6 CN(CC1(C)CCC(c2ccccc2)(N(C)C)CC1)c1c[nH]c2ccccc12 nan
CHEMBL3921976 153214 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 375 5 1 2 5.6 CN(CC1(C)CCC(c2ccccc2)(N(C)C)CC1)c1c[nH]c2ccccc12 nan
44426816 92460 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 311 5 1 3 3.4 COCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228686 92460 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 311 5 1 3 3.4 COCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
46879630 12646 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 427 3 1 4 4.3 CNC(=O)CN1C(=O)OC2(CCN(C3CCC(C(C)(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1079418 12646 0 None -2 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 427 3 1 4 4.3 CNC(=O)CN1C(=O)OC2(CCN(C3CCC(C(C)(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44252988 152916 0 None 1 2 Human 5.5 pKi = 5.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 352 5 0 3 4.5 COc1ccc(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
CHEMBL3919659 152916 0 None 1 2 Human 5.5 pKi = 5.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 352 5 0 3 4.5 COc1ccc(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
44593576 195984 0 None 6 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 444 4 1 4 6.1 OC1(c2cncs2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL511373 195984 0 None 6 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 444 4 1 4 6.1 OC1(c2cncs2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44391124 103213 0 None 19 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 457 8 1 6 5.5 COc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL262104 103213 0 None 19 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 457 8 1 6 5.5 COc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
45268153 202913 0 None 102 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 467 5 0 3 6.7 N#CCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL561115 202913 0 None 102 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 467 5 0 3 6.7 N#CCN1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
44426843 92502 0 None 102 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 403 6 1 4 4.8 COc1ccccc1C(c1ccccc1OC)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228964 92502 0 None 102 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 403 6 1 4 4.8 COc1ccccc1C(c1ccccc1OC)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44426827 150767 0 None 48 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1cccc(C(c2ccccc2)N2CCC(O)(c3ccccc3)CC2)c1 10.1016/j.bmcl.2007.03.061
CHEMBL390279 150767 0 None 48 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1cccc(C(c2ccccc2)N2CCC(O)(c3ccccc3)CC2)c1 10.1016/j.bmcl.2007.03.061
44574631 185288 0 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 457 4 2 4 5.1 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2=NCCCN2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL466679 185288 0 None 204 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 457 4 2 4 5.1 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2=NCCCN2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
44574538 195985 0 None 13 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 438 4 1 3 6.0 OC1(c2cccnc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL511374 195985 0 None 13 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 438 4 1 3 6.0 OC1(c2cccnc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44574708 196223 0 None 40 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 465 5 1 2 6.7 O=C(O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL513471 196223 0 None 40 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 465 5 1 2 6.7 O=C(O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76324308 110094 0 None 28 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 496 6 1 2 6.6 NC(=O)[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084526 110094 0 None 28 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 496 6 1 2 6.6 NC(=O)[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76320666 110121 0 None 63 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 510 7 1 2 7.0 NC(=O)C[C@@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084555 110121 0 None 63 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 510 7 1 2 7.0 NC(=O)C[C@@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76309740 110125 0 None 23 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 1 3 5.5 NC(=O)[C@@]1(c2cccnc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084559 110125 0 None 23 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 1 3 5.5 NC(=O)[C@@]1(c2cccnc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44437649 97401 0 None 39 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 11 1 7 4.5 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238818 97401 0 None 39 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 11 1 7 4.5 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(=O)NC4CC4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437601 97403 0 None 7 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238833 97403 0 None 7 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437605 97663 0 None 37 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 507 11 0 7 5.2 CCC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239260 97663 0 None 37 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 507 11 0 7 5.2 CCC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437637 98672 0 None 22 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 529 10 0 8 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CS(C)(=O)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL241357 98672 0 None 22 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 529 10 0 8 4.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CS(C)(=O)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437606 152296 0 None 45 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 494 10 1 7 3.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(N)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391486 152296 0 None 45 4 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 494 10 1 7 3.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CC(N)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
70696991 83436 0 None 22 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064156 83436 0 None 22 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
24776395 104776 0 None 154 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 354 2 0 2 4.2 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(C)Cc2ccccc23)CC1 10.1021/jm7009606
CHEMBL272852 104776 0 None 154 3 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 354 2 0 2 4.2 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(C)Cc2ccccc23)CC1 10.1021/jm7009606
127033703 145812 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 388 3 2 3 4.4 Cc1cc(F)ccc1C1CCN(CC2Cc3c(Cl)ccc(O)c3CN2)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3785952 145812 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 388 3 2 3 4.4 Cc1cc(F)ccc1C1CCN(CC2Cc3c(Cl)ccc(O)c3CN2)CC1 10.1016/j.ejmech.2016.02.014
86279209 117781 0 None 2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262544 117781 0 None 2 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 414 3 0 2 5.9 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H]4CCCc5cccc3c54)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
25190596 184468 0 None 19 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 576 8 0 4 6.7 O=C1N(CCCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL464191 184468 0 None 19 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 576 8 0 4 6.7 O=C1N(CCCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
44438917 161788 0 None 5 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 355 3 1 3 3.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL401451 161788 0 None 5 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 355 3 1 3 3.3 O=C1NCN(c2ccccc2)C12CCN(Cc1ccccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
10837001 105427 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 443 2 0 3 4.6 CN1CN(c2ccccc2)C2(CCN(C3CCc4c(Cl)ccc(Cl)c4C3)CC2)C1=O 10.1021/jm991129q
CHEMBL27729 105427 0 None -1 4 Human 8.5 pKi = 8.5 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 443 2 0 3 4.6 CN1CN(c2ccccc2)C2(CCN(C3CCc4c(Cl)ccc(Cl)c4C3)CC2)C1=O 10.1021/jm991129q
15411840 175418 0 None 2 3 Rat 8.5 pKi = 8.5 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 369 2 1 3 4.0 CC(C)(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL436243 175418 0 None 2 3 Rat 8.5 pKi = 8.5 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 369 2 1 3 4.0 CC(C)(C)[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
44451779 173480 0 None 67 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 517 10 0 8 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4cccn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL428253 173480 0 None 67 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 517 10 0 8 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4cccn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
9932834 185319 0 None 6 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 437 4 1 2 6.6 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466847 185319 0 None 6 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 437 4 1 2 6.6 OC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
90655972 117780 0 None 8 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
CHEMBL3262543 117780 0 None 8 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 386 2 0 2 5.0 O=C1Cc2ccccc2N1C1CCN([C@@H]2CC[C@@H]3CCCc4cccc2c43)CC1 10.1016/j.bmc.2014.02.047
11152739 196024 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 364 3 1 3 4.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1C 10.1021/jm701590h
CHEMBL511658 196024 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 364 3 1 3 4.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1C 10.1021/jm701590h
25190590 183574 0 None 91 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 536 7 0 4 5.8 CN(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL460636 183574 0 None 91 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 536 7 0 4 5.8 CN(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
44438920 154077 1 None 14 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 335 3 1 3 3.2 CC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL392893 154077 1 None 14 4 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 335 3 1 3 3.2 CC(c1ccccc1)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
46880116 14291 0 None 36 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 424 4 1 5 3.5 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC4CCCCC4C3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087278 14291 0 None 36 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 424 4 1 5 3.5 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC4CCCCC4C3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44451517 102657 0 None 15 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 546 10 0 8 5.9 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4c(C)noc4C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259120 102657 0 None 15 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 546 10 0 8 5.9 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4c(C)noc4C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
127034292 145857 0 None 95 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 338 3 1 2 4.0 Cc1cc(F)ccc1C1CCN(CC2Cc3ccccc3CN2)CC1 10.1016/j.ejmech.2016.02.014
CHEMBL3786469 145857 0 None 95 2 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 338 3 1 2 4.0 Cc1cc(F)ccc1C1CCN(CC2Cc3ccccc3CN2)CC1 10.1016/j.ejmech.2016.02.014
44574629 195619 0 None 213 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 458 4 2 3 4.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCNC2=O)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL506634 195619 0 None 213 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 458 4 2 3 4.9 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(C2CCNC2=O)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
25190626 195951 0 None 38 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 522 7 1 4 5.7 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCc2ccccc2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL511162 195951 0 None 38 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 522 7 1 4 5.7 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCc2ccccc2)CN3c2ccccc2)c2ccccc21 10.1016/j.bmcl.2008.12.092
CHEMBL428668 220244 0 None - 1 Mouse 8.4 pKi = 8.4 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1F)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
44561020 185964 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 384 3 2 4 3.4 Cc1cc(F)ccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
CHEMBL472304 185964 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 384 3 2 4 3.4 Cc1cc(F)ccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1O 10.1021/jm701590h
25190591 196858 0 None 263 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 548 8 1 4 6.0 O=C1N(CCNC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL517265 196858 0 None 263 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 548 8 1 4 6.0 O=C1N(CCNC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
11956573 127347 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 376 2 1 2 5.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)SCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3326230 127347 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 376 2 1 2 5.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)SCCc1c3ccccc3[nH]c12 10.1021/ml500117c
CHEMBL3545633 127347 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 376 2 1 2 5.7 CN(C)[C@]1(c2ccccc2)CC[C@]2(CC1)SCCc1c3ccccc3[nH]c12 10.1021/ml500117c
10385808 72916 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 72916 0 None 33 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
44451837 166330 0 None 57 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 517 10 1 7 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4c[nH]cn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL410257 166330 0 None 57 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 517 10 1 7 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4c[nH]cn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
70688697 83439 0 None 36 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 437 5 0 3 3.8 Cc1cc(F)ccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064159 83439 0 None 36 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 437 5 0 3 3.8 Cc1cc(F)ccc1C1CCN(CCC(=O)N2c3ccccc3C[C@H]2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
25190595 195133 0 None 70 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 604 9 1 4 7.4 O=C1N(CCNCC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL501088 195133 0 None 70 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 604 9 1 4 7.4 O=C1N(CCNCC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
44451542 103205 0 None 21 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 0 8 5.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncco4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL262062 103205 0 None 21 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 0 8 5.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncco4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44394381 73754 0 None 23 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 448 5 1 4 2.7 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(N)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL186822 73754 0 None 23 2 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 448 5 1 4 2.7 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(N)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
10042904 170101 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL418980 170101 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
10042904 97232 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 3 0 2 4.3 CC(C)C1CCC(N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387187 97232 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 3 0 2 4.3 CC(C)C1CCC(N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL429363 220305 0 None - 1 Mouse 8.4 pKi = 8.4 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
15512235 110300 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 397 2 1 3 4.2 Cc1cccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)c1 10.1016/s0960-894x(99)00385-6
CHEMBL308522 110300 0 None 2 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 397 2 1 3 4.2 Cc1cccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)c1 10.1016/s0960-894x(99)00385-6
15512238 170143 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 461 2 1 3 4.6 O=C1NCN(c2cccc(Br)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL419272 170143 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 461 2 1 3 4.6 O=C1NCN(c2cccc(Br)c2)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
44337379 14502 0 None 60 4 Human 7.5 pKi = 7.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 342 7 1 2 5.3 CCCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL108893 14502 0 None 60 4 Human 7.5 pKi = 7.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 342 7 1 2 5.3 CCCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
24894430 193350 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 336 3 1 3 3.9 O[C@H]1C[C@H](CN2CCC(c3ccccc3)CC2)CCc2cccnc21 10.1021/jm701590h
CHEMBL487827 193350 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 336 3 1 3 3.9 O[C@H]1C[C@H](CN2CCC(c3ccccc3)CC2)CCc2cccnc21 10.1021/jm701590h
44402603 140359 0 None -2 3 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL371207 140359 0 None -2 3 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 329 2 0 3 4.6 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccc(Cl)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
44339540 15720 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 369 3 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL109803 15720 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 369 3 1 2 4.8 OC1(c2ccc(Cl)cc2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(03)00665-6
10194236 114042 0 None 28 4 Human 7.5 pKi = 7.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 396 5 1 2 5.6 N[C@@H](c1cccc(C(F)(F)F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL316961 114042 0 None 28 4 Human 7.5 pKi = 7.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 396 5 1 2 5.6 N[C@@H](c1cccc(C(F)(F)F)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
118718296 122113 0 None 67 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 510 6 1 2 6.9 CC(=O)NC[C@]1(c2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349281 122113 0 None 67 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 510 6 1 2 6.9 CC(=O)NC[C@]1(c2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44574848 185357 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 498 5 1 2 6.8 NC(=O)C1(c2ccc(Cl)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467131 185357 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 498 5 1 2 6.8 NC(=O)C1(c2ccc(Cl)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76313421 110102 0 None 6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 480 5 2 4 5.1 NC(=O)[C@@]1(c2ccc(N)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084534 110102 0 None 6 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 480 5 2 4 5.1 NC(=O)[C@@]1(c2ccc(N)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
10158555 195884 0 None 4 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 411 4 0 3 4.5 CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL510201 195884 0 None 4 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 411 4 0 3 4.5 CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
45102745 12814 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080484 12814 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 412 5 1 5 3.4 CNC(=O)Cn1c(=O)n(C2CCN([C@H]3CC[C@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
70692894 83433 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 473 5 0 3 4.3 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2C(F)(F)F)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064141 83433 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 473 5 0 3 4.3 CN(C)C(=O)C1Cc2ccccc2N1C(=O)CCN1CCC(c2ccccc2C(F)(F)F)CC1 10.1016/j.ejmech.2012.07.021
134563699 182855 0 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 440 7 2 3 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4591048 182855 0 None 12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 440 7 2 3 5.3 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CCCNC(N)=S)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44402482 147280 0 None -16 3 Rat 5.5 pKi = 5.5 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 534 4 0 6 6.2 Brc1ccc2c(c1)[C@H]1O[C@H](Cn3oc4ccc(CN5CCOCC5)cc43)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
CHEMBL381000 147280 0 None -16 3 Rat 5.5 pKi = 5.5 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 534 4 0 6 6.2 Brc1ccc2c(c1)[C@H]1O[C@H](Cn3oc4ccc(CN5CCOCC5)cc43)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
10427620 155442 0 None 36 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 344 4 1 3 4.2 OC1(c2ccccn2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL393971 155442 0 None 36 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 344 4 1 3 4.2 OC1(c2ccccn2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
44574706 195633 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 453 5 0 1 7.6 FCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL506803 195633 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 453 5 0 1 7.6 FCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL407671 219455 0 None - 1 Mouse 6.5 pKi = 6.5 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)CC1CCCCC1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
CHEMBL412606 219788 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccc(O)cc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm990075h
CHEMBL428167 220201 0 None - 1 Mouse 5.5 pKi = 5.5 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)CNCc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm990075h
44391052 136447 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 425 7 1 5 5.3 Cc1cc(F)ccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL367367 136447 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 425 7 1 5 5.3 Cc1cc(F)ccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
25129300 134961 0 None 117 2 Human 7.5 pKi = 7.5 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 387 2 1 3 4.1 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2cc(F)ccc2N1 nan
CHEMBL3665427 134961 0 None 117 2 Human 7.5 pKi = 7.5 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 387 2 1 3 4.1 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2cc(F)ccc2N1 nan
19347398 65496 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 395 3 1 3 4.6 O=C1NCN(c2ccccc2)C12CCN([C@H]1CC[C@H](C3CCCCC3)CC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL168513 65496 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 395 3 1 3 4.6 O=C1NCN(c2ccccc2)C12CCN([C@H]1CC[C@H](C3CCCCC3)CC1)CC2 10.1016/s0960-894x(00)00111-6
44337459 12097 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 430 5 1 2 6.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(02)00652-2
CHEMBL106785 12097 0 None -1 4 Human 5.5 pKi = 5.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 430 5 1 2 6.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccc(Cl)cc1)c1ccc(Cl)cc1 10.1016/s0960-894x(02)00652-2
9925737 92741 0 None 12 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 281 3 1 2 3.7 CC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL230249 92741 0 None 12 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 281 3 1 2 3.7 CC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44426823 143780 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 344 4 1 3 4.2 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccnc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL374603 143780 0 None 2 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 344 4 1 3 4.2 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccnc2)CC1 10.1016/j.bmcl.2007.03.061
44253418 158849 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 442 6 0 3 5.7 COc1ccc(C(=O)N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
CHEMBL3967435 158849 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 442 6 0 3 5.7 COc1ccc(C(=O)N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
10274330 73447 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 430 4 0 4 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC#N)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL185415 73447 0 None -1 2 Human 7.5 pKi = 7.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 430 4 0 4 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC#N)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
118718270 122086 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 532 7 0 2 7.6 O=C1CCCN1C[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349254 122086 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 532 7 0 2 7.6 O=C1CCCN1C[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
90663953 113544 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 903 22 10 10 -1.0 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@@H]2SC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
CHEMBL3144471 113544 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 903 22 10 10 -1.0 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@@H]2SC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
44337551 14653 0 None 57 4 Human 7.5 pKi = 7.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 356 8 1 2 5.7 CCCCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL108995 14653 0 None 57 4 Human 7.5 pKi = 7.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 356 8 1 2 5.7 CCCCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
44366822 128291 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 903 22 10 10 -1.0 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@@H]2SC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
CHEMBL358403 128291 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 903 22 10 10 -1.0 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@@H]2SC[C@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
44248789 110175 0 None 33 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 440 4 0 2 7.0 Fc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
CHEMBL3084673 110175 0 None 33 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 440 4 0 2 7.0 Fc1ccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1021/jm9008218
44430007 93790 0 None 17 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 361 4 1 2 4.9 OC1(c2ccccc2F)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232476 93790 0 None 17 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 361 4 1 2 4.9 OC1(c2ccccc2F)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
118718276 122092 0 None 41 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 482 6 1 2 7.0 NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349260 122092 0 None 41 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 482 6 1 2 7.0 NC[C@]1(Cc2ccc(F)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
25190573 187268 0 None 39 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 439 6 0 3 5.3 CCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475308 187268 0 None 39 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 439 6 0 3 5.3 CCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
122179053 128175 0 None -676 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581743 128175 0 None -676 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
134154039 159644 0 None -676 3 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 503 5 2 5 4.7 CO[C@@]12C=C[C@]3(C[C@@]1(C)[C@@H](O)c1ccc(F)cc1)[C@@H]1Cc4ccc(O)c5c4[C@]3(CCN1CC1CC1)[C@@H]2O5 nan
CHEMBL3974294 159644 0 None -676 3 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 503 5 2 5 4.7 CO[C@@]12C=C[C@]3(C[C@@]1(C)[C@@H](O)c1ccc(F)cc1)[C@@H]1Cc4ccc(O)c5c4[C@]3(CCN1CC1CC1)[C@@H]2O5 nan
122179053 128175 0 None -676 3 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3581743 128175 0 None -676 3 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 503 5 2 5 4.7 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
44252838 158616 0 None -5 2 Human 7.5 pKi = 7.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 444 7 0 2 6.5 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3965425 158616 0 None -5 2 Human 7.5 pKi = 7.5 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 444 7 0 2 6.5 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
90306885 117742 0 None -85 3 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 493 5 2 6 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3262372 117742 0 None -85 3 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 493 5 2 6 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
90306885 117742 0 None -85 3 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 493 5 2 6 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3262372 117742 0 None -85 3 Human 7.5 pKi = 7.5 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 493 5 2 6 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
10199984 73007 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 383 2 1 3 3.2 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184547 73007 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 383 2 1 3 3.2 O=S1(=O)Nc2ccccc2N1C1CCN(C2CCc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
10193971 117275 0 None 15 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 378 7 1 2 5.6 CCCCC(c1cc(F)cc(F)c1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL324895 117275 0 None 15 4 Human 6.5 pKi = 6.5 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 378 7 1 2 5.6 CCCCC(c1cc(F)cc(F)c1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
44366690 127668 0 None 12 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 899 22 10 9 -0.6 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)NC1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
CHEMBL355931 127668 0 None 12 4 Human 7.5 pKi = 7.5 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 899 22 10 9 -0.6 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)NC1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
44426824 92468 0 None 11 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 349 4 1 3 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccs2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228740 92468 0 None 11 4 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 349 4 1 3 4.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccs2)CC1 10.1016/j.bmcl.2007.03.061
118718268 122084 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 493 6 1 3 6.2 CC(=O)NC[C@]1(c2cccnc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349252 122084 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 493 6 1 3 6.2 CC(=O)NC[C@]1(c2cccnc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
46880030 14205 0 None 51 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 384 4 1 5 2.9 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1086622 14205 0 None 51 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 384 4 1 5 2.9 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
25129299 134959 0 None 10 4 Human 7.5 pKi = 7.5 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 369 2 1 3 3.9 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc2N1 nan
CHEMBL3665425 134959 0 None 10 4 Human 7.5 pKi = 7.5 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 369 2 1 3 3.9 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc2N1 nan
44413401 85323 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 297 3 1 2 4.3 c1cnc2[nH]cc(C3CCN(CC4CCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL211210 85323 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 297 3 1 2 4.3 c1cnc2[nH]cc(C3CCN(CC4CCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
44426830 150770 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 5.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL390280 150770 0 None 1 4 Human 6.5 pKi = 6.5 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 411 4 1 2 5.8 OC1(c2ccccc2)CCN(C(c2ccccc2)c2cccc(C(F)(F)F)c2)CC1 10.1016/j.bmcl.2007.03.061
10134217 73050 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 377 3 1 3 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184698 73050 0 None 2 2 Human 6.5 pKi = 6.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 377 3 1 3 3.8 CC(C)C1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
22562135 71638 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 351 5 1 3 3.5 CC(C)CCC(C)N1CCC(N2c3ccccc3NS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL182131 71638 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 351 5 1 3 3.5 CC(C)CCC(C)N1CCC(N2c3ccccc3NS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
76313426 110123 0 None 12 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 484 5 1 2 7.3 N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084557 110123 0 None 12 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 484 5 1 2 7.3 N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44438963 98543 0 None 13 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 421 2 1 3 4.7 O=C1NCN(c2ccccc2)C12CCN(C1c3ccccc3C=Cc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL241067 98543 0 None 13 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 421 2 1 3 4.7 O=C1NCN(c2ccccc2)C12CCN(C1c3ccccc3C=Cc3ccccc31)CC2 10.1016/j.bmcl.2007.01.069
44252986 156244 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 376 4 1 2 5.2 CNC1(c2ccccc2)CCC(c2ccc(C(F)(F)F)cc2)(N(C)C)CC1 nan
CHEMBL3946074 156244 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 376 4 1 2 5.2 CNC1(c2ccccc2)CCC(c2ccc(C(F)(F)F)cc2)(N(C)C)CC1 nan
44252242 156902 0 None -6 3 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 5 0 2 4.6 CN(C)C1(Cc2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3951213 156902 0 None -6 3 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 5 0 2 4.6 CN(C)C1(Cc2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44337473 16065 0 None 7 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 328 6 1 2 5.0 CCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL110933 16065 0 None 7 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 328 6 1 2 5.0 CCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
10831914 37704 0 None - 1 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 353 3 2 3 5.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3-c3ccccc3)ccc2n1 10.1021/jm0002073
CHEMBL139816 37704 0 None - 1 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 353 3 2 3 5.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3-c3ccccc3)ccc2n1 10.1021/jm0002073
10150260 117222 0 None 33 4 Human 7.4 pKi = 7.4 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 362 5 1 2 5.2 N[C@@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL324635 117222 0 None 33 4 Human 7.4 pKi = 7.4 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 362 5 1 2 5.2 N[C@@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
44391092 71442 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 421 8 1 5 5.4 CCc1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL181830 71442 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 421 8 1 5 5.4 CCc1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
44451673 175735 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 9 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4noc(C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL438919 175735 0 None 5 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 533 10 0 9 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4noc(C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
10669671 38513 1 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc2ccc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)cc2c(N)n1 10.1021/jm0002073
CHEMBL140580 38513 1 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 417 5 2 4 5.6 Cc1cc2ccc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)cc2c(N)n1 10.1021/jm0002073
44395410 73666 1 None -10 2 Human 6.4 pKi = 6.4 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 405 6 1 2 5.8 OC1(c2ccc(Cl)cc2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
CHEMBL186426 73666 1 None -10 2 Human 6.4 pKi = 6.4 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 405 6 1 2 5.8 OC1(c2ccc(Cl)cc2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.032
68629836 160050 0 None -7 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 314 5 1 2 4.6 CNC1(c2ccccc2)CCC(CC2CCCC2)(N(C)C)CC1 nan
CHEMBL3977691 160050 0 None -7 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 314 5 1 2 4.6 CNC1(c2ccccc2)CCC(CC2CCCC2)(N(C)C)CC1 nan
44437602 97429 0 None 14 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239043 97429 0 None 14 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
22725091 196190 0 None 2 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 439 4 1 4 5.4 OC1(c2cccnn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL513171 196190 0 None 2 2 Human 5.4 pKi = 5.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 439 4 1 4 5.4 OC1(c2cccnn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44430024 160353 0 None 47 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 307 4 1 2 4.0 OC1(C2CC2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL398039 160353 0 None 47 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 307 4 1 2 4.0 OC1(C2CC2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
127043559 147288 0 None -9 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1603 43 26 18 -1.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL3810104 147288 0 None -9 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1603 43 26 18 -1.5 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c(C)cc(O)cc2C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
44391104 71788 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 491 7 2 6 5.5 Cc1ccc(Cl)c(OC(c2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182328 71788 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 491 7 2 6 5.5 Cc1ccc(Cl)c(OC(c2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44574671 185216 0 None 9 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 452 4 1 3 6.0 Cc1ccnc(C2(O)C3CCC2CN(C(c2ccccc2Cl)c2ccccc2Cl)C3)c1 10.1016/j.bmcl.2009.03.031
CHEMBL466082 185216 0 None 9 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 452 4 1 3 6.0 Cc1ccnc(C2(O)C3CCC2CN(C(c2ccccc2Cl)c2ccccc2Cl)C3)c1 10.1016/j.bmcl.2009.03.031
9902874 106730 0 None 24 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 347 3 1 2 4.0 CC(C)C1CCC(N2CCC(N3C(=O)N[C@@H]4CCCC[C@H]43)CC2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL286411 106730 0 None 24 3 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 347 3 1 2 4.0 CC(C)C1CCC(N2CCC(N3C(=O)N[C@@H]4CCCC[C@H]43)CC2)CC1 10.1016/j.bmcl.2003.11.083
44391157 71660 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 452 8 1 7 5.1 Cc1ccc([N+](=O)[O-])c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182202 71660 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 452 8 1 7 5.1 Cc1ccc([N+](=O)[O-])c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
118718262 122077 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 492 8 1 2 7.5 CCNC[C@@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349245 122077 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 492 8 1 2 7.5 CCNC[C@@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718299 122116 0 None 43 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 466 3 1 2 7.2 Fc1ccc2c(c1)[C@@]1(CN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349284 122116 0 None 43 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 466 3 1 2 7.2 Fc1ccc2c(c1)[C@@]1(CN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3810101 219055 0 None 48 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
15512233 174638 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 401 2 1 3 4.0 O=C1NCN(c2ccccc2F)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
CHEMBL431002 174638 0 None 3 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 401 2 1 3 4.0 O=C1NCN(c2ccccc2F)C12CCN(C1Cc3cccc4cccc1c34)CC2 10.1016/s0960-894x(99)00385-6
24776399 104725 0 None 9 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 386 1 0 2 4.7 CN1Cc2cccc(F)c2C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1021/jm7009606
CHEMBL272600 104725 0 None 9 3 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 386 1 0 2 4.7 CN1Cc2cccc(F)c2C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1021/jm7009606
68632271 149685 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 6 1 2 4.5 CNC1(c2ccccc2)CCC(Cc2ccccc2)(CN(C)C)CC1 nan
CHEMBL3893777 149685 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 336 6 1 2 4.5 CNC1(c2ccccc2)CCC(Cc2ccccc2)(CN(C)C)CC1 nan
90656668 117731 0 None -1096 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 501 6 2 5 4.9 CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm401964y
CHEMBL3262091 117731 0 None -1096 4 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 501 6 2 5 4.9 CC[C@@](O)(c1ccccc1)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm401964y
CHEMBL263859 217374 0 None - 1 Mouse 6.4 pKi = 6.4 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(N)=O 10.1021/jm990075h
59159347 134965 0 None - 1 Human 4.4 pKi = 4.4 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 427 3 1 5 3.7 COC(=O)c1ccc2c(c1)N(C1CCN(C3CCCCCCC3)CC1)C(=O)CC(=O)N2 nan
CHEMBL3665431 134965 0 None - 1 Human 4.4 pKi = 4.4 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 427 3 1 5 3.7 COC(=O)c1ccc2c(c1)N(C1CCN(C3CCCCCCC3)CC1)C(=O)CC(=O)N2 nan
10225083 173175 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
CHEMBL427683 173175 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmcl.2004.11.049
16007142 146131 0 None 97 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 353 2 1 2 5.2 c1cc2c3c(cccc3c1)C(N1CCC(c3c[nH]c4ncccc34)CC1)C2 10.1016/j.bmcl.2006.03.094
CHEMBL379297 146131 0 None 97 3 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 353 2 1 2 5.2 c1cc2c3c(cccc3c1)C(N1CCC(c3c[nH]c4ncccc34)CC1)C2 10.1016/j.bmcl.2006.03.094
9951673 92481 0 None 154 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 377 4 1 2 5.4 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228849 92481 0 None 154 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 377 4 1 2 5.4 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.061
9820782 150031 0 None 426 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 4 1 2 5.4 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL389665 150031 0 None 426 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 4 1 2 5.4 Cc1ccccc1C(c1ccccc1C)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
118718274 122090 0 None 63 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.2 COc1cccc([C@@]2(CNC(C)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1016/j.bmcl.2008.10.088
CHEMBL3349258 122090 0 None 63 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.2 COc1cccc([C@@]2(CNC(C)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1016/j.bmcl.2008.10.088
44574744 196086 0 None 114 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 436 4 1 2 6.6 NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL512258 196086 0 None 114 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 436 4 1 2 6.6 NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76309739 110096 0 None 13 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 1 3 5.5 NC(=O)[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084528 110096 0 None 13 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 1 3 5.5 NC(=O)[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44437615 97152 0 None 67 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 509 10 0 8 4.4 COC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238637 97152 0 None 67 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 509 10 0 8 4.4 COC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437626 97398 0 None 26 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 11 0 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCN(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL238795 97398 0 None 26 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 508 11 0 7 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCN(C)C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44437601 97403 0 None 7 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL238833 97403 0 None 7 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 481 10 0 7 4.9 COCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437602 97429 0 None 14 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239043 97429 0 None 14 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437636 152217 0 None 31 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 513 10 0 7 4.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(C[S+](C)[O-])c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL391422 152217 0 None 31 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 513 10 0 7 4.6 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(C[S+](C)[O-])c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
10225083 173175 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL427683 173175 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
24970041 134973 0 None 131 3 Human 8.4 pKi = 8.4 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 395 2 1 4 4.4 O=c1[nH]c2ccccc2n([C@@H]2C[C@@H]3CCC[C@H](C2)N3C2CCCCCCC2)c1=O nan
CHEMBL3665439 134973 0 None 131 3 Human 8.4 pKi = 8.4 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 395 2 1 4 4.4 O=c1[nH]c2ccccc2n([C@@H]2C[C@@H]3CCC[C@H](C2)N3C2CCCCCCC2)c1=O nan
9806799 186053 0 None 141 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 522 7 1 4 5.4 CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL473068 186053 0 None 141 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 522 7 1 4 5.4 CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
44437602 97429 0 None 14 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
CHEMBL239043 97429 0 None 14 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 4.9 COCCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2008.01.005
16747695 175531 0 None 39 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 546 8 2 4 5.9 CC(C)S(=O)(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL437177 175531 0 None 39 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 546 8 2 4 5.9 CC(C)S(=O)(=O)NCc1ccccc1C1(O)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
44451805 102980 0 None 28 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 517 10 0 8 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4ccnc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL260784 102980 0 None 28 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 517 10 0 8 5.0 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4ccnc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
53325608 64085 0 None 53 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 439 4 1 6 3.9 CN1CCN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CC1 10.1016/j.bmc.2010.07.034
CHEMBL1650847 64085 0 None 53 4 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 439 4 1 6 3.9 CN1CCN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CC1 10.1016/j.bmc.2010.07.034
53319617 64087 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 441 4 1 4 5.8 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650849 64087 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 441 4 1 4 5.8 OCC1(N2CCC(n3c(-c4ccc(F)c(Cl)c4)nc4ccccc43)CC2)CCCCC1 10.1016/j.bmc.2010.07.034
53316969 64088 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 357 3 2 4 3.4 O=c1[nH]c2ccccc2n1C1CCN(C2(CO)CCCCCCC2)CC1 10.1016/j.bmc.2010.07.034
CHEMBL1650851 64088 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 357 3 2 4 3.4 O=c1[nH]c2ccccc2n1C1CCN(C2(CO)CCCCCCC2)CC1 10.1016/j.bmc.2010.07.034
11372427 185934 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 380 4 2 4 3.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1CO 10.1021/jm701590h
CHEMBL472125 185934 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 380 4 2 4 3.5 Cc1ccccc1[C@@H]1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)C[C@H]1CO 10.1021/jm701590h
11188910 196222 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 404 3 2 4 3.7 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)CCc2cccnc21 10.1021/jm701590h
CHEMBL513423 196222 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 404 3 2 4 3.7 O[C@H]1C[C@H](CN2CC[C@H](c3ccc(F)cc3Cl)[C@@H](O)C2)CCc2cccnc21 10.1021/jm701590h
10109140 127344 4 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 323 5 1 2 4.4 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(CCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325747 127344 4 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 323 5 1 2 4.4 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(CCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545630 127344 4 None -2 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 323 5 1 2 4.4 CN(C)[C@]1(c2ccccc2)CC[C@@](O)(CCc2ccccc2)CC1 10.1021/ml500116x
11187225 185944 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL472168 185944 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.3 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
25190608 196021 0 None 3 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 445 4 0 4 4.5 CC(=O)CN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL511649 196021 0 None 3 4 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 445 4 0 4 4.5 CC(=O)CN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
57720736 127339 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 374 2 1 2 5.3 Cc1ccc2[nH]c3c(c2c1)CCO[C@]31CC[C@](c2ccccc2)(N(C)C)CC1 10.1021/ml500117c
CHEMBL3325960 127339 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 374 2 1 2 5.3 Cc1ccc2[nH]c3c(c2c1)CCO[C@]31CC[C@](c2ccccc2)(N(C)C)CC1 10.1021/ml500117c
CHEMBL3545625 127339 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 374 2 1 2 5.3 Cc1ccc2[nH]c3c(c2c1)CCO[C@]31CC[C@](c2ccccc2)(N(C)C)CC1 10.1021/ml500117c
52951938 84366 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2088031 84366 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
53316968 64079 0 None 85 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 453 4 2 6 4.3 CC1(C)CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
CHEMBL1650841 64079 0 None 85 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 453 4 2 6 4.3 CC1(C)CN(c2nc3ccccc3n2C2CCN(C3(CO)CCCCCCC3)CC2)CCN1 10.1016/j.bmc.2010.07.034
52951938 84366 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088031 84366 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 448 6 1 4 4.3 CC(C)NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
44430048 94322 0 None 100 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 316 4 2 3 3.4 NCc1ccccc1C1(O)CCN(CC2CCCCCC2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233535 94322 0 None 100 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 316 4 2 3 3.4 NCc1ccccc1C1(O)CCN(CC2CCCCCC2)CC1 10.1016/j.bmcl.2007.03.062
11583008 182642 5 None 213 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 439 4 1 4 5.4 OC1(c2ncccn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
CHEMBL4585935 182642 5 None 213 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting methodDisplacement of [125I][Tyr14]nociceptin/orphanin FQ from human nociceptin opioid receptor expressed in CHO cell membranes after 1 hr by microplate scintillation counting method
ChEMBL 439 4 1 4 5.4 OC1(c2ncccn2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/acs.jmedchem.5b01499
10475466 151763 0 None 5 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 389 4 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)C1CCCC1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL391083 151763 0 None 5 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 389 4 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)C1CCCC1)CC2 10.1016/j.bmcl.2007.01.069
9885005 65516 0 None 1 3 Rat 8.3 pKi = 8.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 3 1 3 3.6 CC(C)[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL168578 65516 0 None 1 3 Rat 8.3 pKi = 8.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 3 1 3 3.6 CC(C)[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
44332117 114678 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCC[C@@H]3C2)CC1 10.1021/jm034249d
CHEMBL319307 114678 0 None 3 3 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCC[C@@H]3C2)CC1 10.1021/jm034249d
24776407 104519 1 None 812 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 340 2 1 2 3.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)NCc2ccccc23)CC1 10.1021/jm7009606
CHEMBL271590 104519 1 None 812 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 340 2 1 2 3.9 CC(C)C1CCC(N2CCC3(CC2)C(=O)NCc2ccccc23)CC1 10.1021/jm7009606
46880114 14289 0 None 10 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 4 1 5 3.8 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C)(C)CC3(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087276 14289 0 None 10 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 4 1 5 3.8 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C)(C)CC3(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
19347346 64261 0 None 2 3 Rat 8.3 pKi = 8.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 327 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL165885 64261 0 None 2 3 Rat 8.3 pKi = 8.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 327 2 1 3 3.1 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
44451777 163176 0 None 25 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 531 10 0 8 5.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4ccnc4C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL406647 163176 0 None 25 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 531 10 0 8 5.3 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cn4ccnc4C)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44451594 165085 0 None 10 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 528 10 0 7 5.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ccccn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL408909 165085 0 None 10 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 528 10 0 7 5.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ccccn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44252533 153984 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 438 6 0 2 6.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3928190 153984 0 None -1 2 Human 8.3 pKi = 8.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 438 6 0 2 6.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
44574890 185410 0 None 10 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 478 5 1 2 6.4 CNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467497 185410 0 None 10 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 478 5 1 2 6.4 CNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44574849 195959 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 542 5 1 2 6.9 NC(=O)C1(c2ccc(Br)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL511223 195959 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 542 5 1 2 6.9 NC(=O)C1(c2ccc(Br)cc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44394284 72961 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 365 5 1 3 3.1 CC(C)CCC(C)N1CCC(N2c3ccccc3CNS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184381 72961 0 None 1 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 365 5 1 3 3.1 CC(C)CCC(C)N1CCC(N2c3ccccc3CNS2(=O)=O)CC1 10.1016/j.bmcl.2004.08.001
71624389 97245 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 2 0 2 5.1 CC1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387200 97245 0 None -1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 2 0 2 5.1 CC1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
10454860 146652 0 None 2 2 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 421 3 0 7 1.0 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)[O-])C=C[C@H]4[C@@H](C2)[N+](C)(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL379928 146652 0 None 2 2 Guinea pig 6.4 pKi = 6.4 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 421 3 0 7 1.0 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)[O-])C=C[C@H]4[C@@H](C2)[N+](C)(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
76313422 110106 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 508 6 2 4 4.6 NC(=O)c1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
CHEMBL3084538 110106 0 None 3 2 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 508 6 2 4 4.6 NC(=O)c1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
68632816 153071 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 366 6 1 3 3.9 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)CC(=O)O)CC1 nan
CHEMBL3920864 153071 0 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 366 6 1 3 3.9 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)CC(=O)O)CC1 nan
60154189 84372 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088038 84372 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088039 84372 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
44426815 92716 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 297 4 2 3 2.7 OCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL230039 92716 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 297 4 2 3 2.7 OCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44402544 77093 0 None -22 3 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 511 3 0 4 8.1 Brc1ccc2c(c1)[C@H]1O[C@H](Cn3oc4ccc(-c5ccccc5)cc43)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
CHEMBL194442 77093 0 None -22 3 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 511 3 0 4 8.1 Brc1ccc2c(c1)[C@H]1O[C@H](Cn3oc4ccc(-c5ccccc5)cc43)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
46879475 12781 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 429 5 1 6 2.9 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc4ccccc4n3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1080273 12781 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 429 5 1 6 2.9 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc4ccccc4n3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44426813 93378 0 None 7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 335 4 1 2 4.9 OC1(c2ccccc2)CCN(C(c2ccccc2)C2CCCC2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL231608 93378 0 None 7 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 335 4 1 2 4.9 OC1(c2ccccc2)CCN(C(c2ccccc2)C2CCCC2)CC1 10.1016/j.bmcl.2007.03.061
44402373 130779 0 None 1 3 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 313 2 0 3 4.1 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL362950 130779 0 None 1 3 Rat 7.4 pKi = 7.4 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 313 2 0 3 4.1 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
9883872 127049 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 327 2 1 3 3.0 C[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL352490 127049 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 327 2 1 3 3.0 C[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
10139672 132666 0 None 4 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 463 5 0 5 3.4 COC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
CHEMBL364844 132666 0 None 4 2 Human 7.4 pKi = 7.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 463 5 0 5 3.4 COC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2004.08.001
44451724 102603 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 1 8 4.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4nnc(C)[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL258897 102603 0 None 2 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 1 8 4.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4nnc(C)[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
10154848 105954 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 349 6 0 2 4.3 CCN1C(=O)N(C2CCN(C(C)CCC(C)C)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL281322 105954 0 None -1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 349 6 0 2 4.3 CCN1C(=O)N(C2CCN(C(C)CCC(C)C)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
44402415 141991 0 None -13 2 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 520 3 0 6 6.3 Brc1ccc2c(c1)[C@H]1O[C@H](Cn3oc4ccc(N5CCOCC5)cc43)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
CHEMBL372244 141991 0 None -13 2 Rat 5.4 pKi = 5.4 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 520 3 0 6 6.3 Brc1ccc2c(c1)[C@H]1O[C@H](Cn3oc4ccc(N5CCOCC5)cc43)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
9880173 104075 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 321 5 1 2 3.6 CC(C)CCC(C)N1CCC(N2C(=O)N[C@@H]3CCCC[C@H]32)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL26909 104075 0 None 1 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 321 5 1 2 3.6 CC(C)CCC(C)N1CCC(N2C(=O)N[C@@H]3CCCC[C@H]32)CC1 10.1016/j.bmcl.2003.11.083
44391079 139267 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 407 7 1 5 5.2 Cc1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
CHEMBL369786 139267 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 407 7 1 5 5.2 Cc1ccccc1OC(CCN1CCC(n2c(O)nc3ccccc32)CC1)C(C)C 10.1016/j.bmcl.2004.11.049
24776409 104736 0 None 91 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 354 1 1 2 4.3 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)NCc2ccccc23)CC1 10.1021/jm7009606
CHEMBL272640 104736 0 None 91 3 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 354 1 1 2 4.3 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)NCc2ccccc23)CC1 10.1021/jm7009606
44426841 92496 0 None 2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 379 4 1 2 5.0 OC1(c2ccccc2)CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228913 92496 0 None 2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 379 4 1 2 5.0 OC1(c2ccccc2)CCN(C(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1016/j.bmcl.2007.03.061
76327877 110119 0 None 19 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 0 3 6.6 CN(C)[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084553 110119 0 None 19 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 0 3 6.6 CN(C)[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
127044528 147146 0 None -83 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1474 43 23 18 -1.9 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCN1Cc2ccccc2C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
CHEMBL3808415 147146 0 None -83 4 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1474 43 23 18 -1.9 CC[C@H](C)[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CCN1Cc2ccccc2C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc2c(C)cc(O)cc2C)C1=O)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/acs.jmedchem.5b01976
44337108 118159 0 None 6 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 430 5 1 2 6.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1cccc(Cl)c1)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL327118 118159 0 None 6 4 Human 6.4 pKi = 6.4 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 430 5 1 2 6.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1cccc(Cl)c1)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
44252835 160968 0 None -4 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 302 6 0 2 4.5 CCCCC1(N(C)C)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3985824 160968 0 None -4 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 302 6 0 2 4.5 CCCCC1(N(C)C)CCC(c2ccccc2)(N(C)C)CC1 nan
46179068 132580 0 None 27 4 Human 7.4 pKi = 7.4 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 465 3 1 5 5.9 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CCCCCCCCCCC2)c1=O nan
CHEMBL3647963 132580 0 None 27 4 Human 7.4 pKi = 7.4 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 465 3 1 5 5.9 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CCCCCCCCCCC2)c1=O nan
71229805 117729 0 None -295 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
CHEMBL3262089 117729 0 None -295 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
71229805 117729 0 None -295 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3262089 117729 0 None -295 5 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
71229805 117729 0 None -295 5 Human 7.4 pKi = 7.4 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3262089 117729 0 None -295 5 Human 7.4 pKi = 7.4 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
71229805 117729 0 None -295 5 Human 7.4 pKi = 7.4 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3262089 117729 0 None -295 5 Human 7.4 pKi = 7.4 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.5 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
134563691 177841 0 None 11 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 381 5 0 3 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN(C)C)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4457077 177841 0 None 11 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 381 5 0 3 5.6 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN(C)C)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44430025 94520 0 None 16 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 309 4 1 2 4.3 CC(C)C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233721 94520 0 None 16 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 309 4 1 2 4.3 CC(C)C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
44252838 158616 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 444 7 0 2 6.5 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3965425 158616 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 444 7 0 2 6.5 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
10275388 169975 0 None -16 2 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 445 7 0 2 5.7 CCN1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL418197 169975 0 None -16 2 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 445 7 0 2 5.7 CCN1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
10202108 105170 1 None -16 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 417 6 1 2 5.0 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL27539 105170 1 None -16 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 417 6 1 2 5.0 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2003.11.083
44426844 148866 0 None 1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 403 6 1 4 4.8 COc1ccc(C(c2ccc(OC)cc2)N2CCC(O)(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.061
CHEMBL388122 148866 0 None 1 4 Human 6.4 pKi = 6.4 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 403 6 1 4 4.8 COc1ccc(C(c2ccc(OC)cc2)N2CCC(O)(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.061
24898825 134173 0 None -13 2 Human 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: Radioligand dose-displacement binding assays for μ-opioid receptors used 0.2 nM[3H]-diprenorphine (NEN, Boston, Mass.), with 5-20 mg membrane protein/well in a final volume of 500 μl binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Reactions were carried out in the absence or presence of increasing concentrations of unlabeled naloxone. All reactions were conducted in 96-deep well polypropylene plates for 1-2 hr at room temperature. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard, Meriden, Conn.) presoaked in 0.5% polyethylemimine using a 96-well tissue harvester (Brandel, Gaithersburg, Md.) followed by performing three filtration washes with 500 μl of ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. BetaScint scintillation cocktail (Wallac, Turku, Finland) was added (50 μl/well), and plates were counted using a Packard Top-Count for 1 min/well.Radioligand Binding Assay: Radioligand dose-displacement binding assays for μ-opioid receptors used 0.2 nM[3H]-diprenorphine (NEN, Boston, Mass.), with 5-20 mg membrane protein/well in a final volume of 500 μl binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Reactions were carried out in the absence or presence of increasing concentrations of unlabeled naloxone. All reactions were conducted in 96-deep well polypropylene plates for 1-2 hr at room temperature. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard, Meriden, Conn.) presoaked in 0.5% polyethylemimine using a 96-well tissue harvester (Brandel, Gaithersburg, Md.) followed by performing three filtration washes with 500 μl of ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. BetaScint scintillation cocktail (Wallac, Turku, Finland) was added (50 μl/well), and plates were counted using a Packard Top-Count for 1 min/well.
ChEMBL 426 8 0 2 6.1 CCC(=O)N(c1ccccc1)C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 nan
CHEMBL3659471 134173 0 None -13 2 Human 5.4 pKi = 5.4 Binding
Radioligand Binding Assay: Radioligand dose-displacement binding assays for μ-opioid receptors used 0.2 nM[3H]-diprenorphine (NEN, Boston, Mass.), with 5-20 mg membrane protein/well in a final volume of 500 μl binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Reactions were carried out in the absence or presence of increasing concentrations of unlabeled naloxone. All reactions were conducted in 96-deep well polypropylene plates for 1-2 hr at room temperature. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard, Meriden, Conn.) presoaked in 0.5% polyethylemimine using a 96-well tissue harvester (Brandel, Gaithersburg, Md.) followed by performing three filtration washes with 500 μl of ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. BetaScint scintillation cocktail (Wallac, Turku, Finland) was added (50 μl/well), and plates were counted using a Packard Top-Count for 1 min/well.Radioligand Binding Assay: Radioligand dose-displacement binding assays for μ-opioid receptors used 0.2 nM[3H]-diprenorphine (NEN, Boston, Mass.), with 5-20 mg membrane protein/well in a final volume of 500 μl binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Reactions were carried out in the absence or presence of increasing concentrations of unlabeled naloxone. All reactions were conducted in 96-deep well polypropylene plates for 1-2 hr at room temperature. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard, Meriden, Conn.) presoaked in 0.5% polyethylemimine using a 96-well tissue harvester (Brandel, Gaithersburg, Md.) followed by performing three filtration washes with 500 μl of ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. BetaScint scintillation cocktail (Wallac, Turku, Finland) was added (50 μl/well), and plates were counted using a Packard Top-Count for 1 min/well.
ChEMBL 426 8 0 2 6.1 CCC(=O)N(c1ccccc1)C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 nan
44366823 103779 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 903 22 10 10 -1.0 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2SC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
CHEMBL266609 103779 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 903 22 10 10 -1.0 CC(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2SC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)NC(Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm020078l
46879667 12739 0 None -6 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 438 4 1 4 3.7 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079940 12739 0 None -6 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 438 4 1 4 3.7 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC(C(C)(C)C)CC3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
71230446 128185 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 527 5 2 6 5.5 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccc(Cl)s1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581760 128185 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 527 5 2 6 5.5 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccc(Cl)s1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
134563650 176624 0 None 16 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 354 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4439997 176624 0 None 16 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 354 4 1 3 5.0 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CO)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
10114637 73830 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 447 6 1 3 4.9 O=S1(=O)Nc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL187183 73830 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 447 6 1 3 4.9 O=S1(=O)Nc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
90663950 113539 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 843 21 10 8 0.9 N=C(N)NCCCCC(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@H](Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
CHEMBL3144465 113539 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 843 21 10 8 0.9 N=C(N)NCCCCC(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@H](Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
59159323 134958 0 None 7 4 Human 6.3 pKi = 6.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 454 4 1 6 2.7 NC(=O)Cn1c(=O)c(=O)n(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2ccccc21 nan
CHEMBL3665424 134958 0 None 7 4 Human 6.3 pKi = 6.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 454 4 1 6 2.7 NC(=O)Cn1c(=O)c(=O)n(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2ccccc21 nan
46879476 12670 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 428 5 1 5 3.5 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1079561 12670 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 428 5 1 5 3.5 CNC(=O)Cn1c(=O)n(C2CCN(Cc3ccc4ccccc4c3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
10362733 94977 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 386 5 1 3 4.8 CN(C)c1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL234761 94977 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 386 5 1 3 4.8 CN(C)c1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
44430036 94833 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 296 4 2 3 2.6 NCc1ccccc1C1(O)CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL234581 94833 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 296 4 2 3 2.6 NCc1ccccc1C1(O)CCN(Cc2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
44414813 39879 0 None -1 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 379 3 1 6 1.3 COc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44414814 39879 0 None -1 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 379 3 1 6 1.3 COc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL1417 39879 0 None -1 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 379 3 1 6 1.3 COc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44437627 175751 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 584 13 0 7 6.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCN(C)Cc4ccccc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL439035 175751 0 None 3 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 584 13 0 7 6.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCN(C)Cc4ccccc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
44394344 72953 0 None 14 2 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 383 2 1 3 2.5 O=S1(=O)NCc2ccccc2N1C1CCN(C2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184328 72953 0 None 14 2 Human 7.3 pKi = 7.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 383 2 1 3 2.5 O=S1(=O)NCc2ccccc2N1C1CCN(C2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
9824313 37529 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 399 5 3 5 4.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(O)cc3)ccc2n1 10.1021/jm0002073
CHEMBL139566 37529 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 399 5 3 5 4.7 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(O)cc3)ccc2n1 10.1021/jm0002073
44391063 103502 0 None -4 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 497 7 2 6 5.7 Cc1ccc(Cl)c(OC(C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)C2CCCCC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL264288 103502 0 None -4 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 497 7 2 6 5.7 Cc1ccc(Cl)c(OC(C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)C2CCCCC2)c1 10.1016/j.bmcl.2004.11.049
90306863 117743 0 None -29512 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 488 5 2 6 3.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)c1ccncc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
CHEMBL3262377 117743 0 None -29512 3 Human 5.3 pKi = 5.3 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 488 5 2 6 3.9 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)c1ccncc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
44253566 150418 0 None 6 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 352 6 1 3 3.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)CCO)CC1 nan
CHEMBL3899856 150418 0 None 6 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 352 6 1 3 3.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)CCO)CC1 nan
44248917 110165 0 None 17 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 500 4 0 2 7.7 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ncccc1Br)C2 10.1021/jm9008218
CHEMBL3084660 110165 0 None 17 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 500 4 0 2 7.7 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ncccc1Br)C2 10.1021/jm9008218
76327873 110110 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2ncc(F)cc2F)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084543 110110 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2ncc(F)cc2F)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
127043364 147156 0 None -22 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1575 43 26 18 -2.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
CHEMBL3808523 147156 0 None -22 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting methodDisplacement of [3H]OFQ/nociceptin from human nociceptin receptor expressed in HEK293 cell membrane incubated for 1 hr by TopCount scintillation counting method
ChEMBL 1575 43 26 18 -2.1 Cc1cc(O)cc(C)c1C[C@H](N)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H]1Cc2ccccc2CN(CCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)C1=O 10.1021/acs.jmedchem.5b01976
10225083 173175 0 None 8 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL427683 173175 0 None 8 4 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 437 8 1 5 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)[nH]c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
25190585 186029 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 508 6 1 4 5.2 NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL472867 186029 0 None -1 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 508 6 1 4 5.2 NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
122179060 128183 0 None -912 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 521 5 2 5 5.4 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(Cl)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581756 128183 0 None -912 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 521 5 2 5 5.4 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(Cl)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
46879992 12992 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 356 4 1 5 2.1 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1081374 12992 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 356 4 1 5 2.1 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
46880154 12285 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 372 7 1 5 2.6 CNC(=O)Cn1c(=O)n(C2CCN(CCCC(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1076500 12285 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 372 7 1 5 2.6 CNC(=O)Cn1c(=O)n(C2CCN(CCCC(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
10315818 94141 0 None 36 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 349 4 1 3 4.8 OC1(c2cccs2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233323 94141 0 None 36 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 349 4 1 3 4.8 OC1(c2cccs2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
44252682 150366 0 None -15 2 Human 7.3 pKi = 7.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 7 1 3 4.8 CN(C)C1(c2cccc(F)c2)CCC(C)(CNS(=O)(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3899387 150366 0 None -15 2 Human 7.3 pKi = 7.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 7 1 3 4.8 CN(C)C1(c2cccc(F)c2)CCC(C)(CNS(=O)(=O)/C=C/c2ccccc2)CC1 nan
25190580 187417 0 None 204 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 521 7 0 3 7.0 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475496 187417 0 None 204 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 521 7 0 3 7.0 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
54580479 69422 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 419 8 1 4 4.2 c1ccc(CN2CCC[C@@H]2CNCCCN2CCC3(CC2)OCc2ccccc23)cc1 10.1016/j.bmc.2009.05.068
CHEMBL1783821 69422 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 419 8 1 4 4.2 c1ccc(CN2CCC[C@@H]2CNCCCN2CCC3(CC2)OCc2ccccc23)cc1 10.1016/j.bmc.2009.05.068
46880117 12283 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 382 4 1 5 2.4 CNC(=O)Cn1c(=O)n(C2CCN(C3CC4CCC3C4)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1076484 12283 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 382 4 1 5 2.4 CNC(=O)Cn1c(=O)n(C2CCN(C3CC4CCC3C4)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
44337212 14507 0 None 81 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 378 7 1 2 5.6 CCCCC(c1cc(F)cc(F)c1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL108900 14507 0 None 81 4 Human 7.3 pKi = 7.3 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 378 7 1 2 5.6 CCCCC(c1cc(F)cc(F)c1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
24894652 185817 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 348 3 0 3 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C(=O)C2)CC1 10.1021/jm701590h
CHEMBL471301 185817 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 348 3 0 3 4.4 Cc1ccccc1C1CCN(C[C@@H]2CCc3cccnc3C(=O)C2)CC1 10.1021/jm701590h
44438978 152586 0 None 16 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 433 4 1 3 4.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccc(F)cc1)c1ccc(F)cc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL391703 152586 0 None 16 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 433 4 1 3 4.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccc(F)cc1)c1ccc(F)cc1)CC2 10.1016/j.bmcl.2007.01.069
68632581 155130 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 365 8 1 2 5.4 CN(C)C1(c2ccccc2)CCC(CO)(CCCCc2ccccc2)CC1 nan
CHEMBL3937167 155130 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 365 8 1 2 5.4 CN(C)C1(c2ccccc2)CCC(CO)(CCCCc2ccccc2)CC1 nan
118662014 179647 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 272 2 1 2 2.5 CN(C)C1(c2ccccc2)CCC2(CC1)CNC(=O)C2 10.1021/acsmedchemlett.6b00277
CHEMBL4515245 179647 0 None -2 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 272 2 1 2 2.5 CN(C)C1(c2ccccc2)CCC2(CC1)CNC(=O)C2 10.1021/acsmedchemlett.6b00277
44181744 110150 9 None 102 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
CHEMBL3084634 110150 9 None 102 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccn1)C2 10.1021/jm9008218
44249047 110153 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1cccnc1)C2 10.1021/jm9008218
CHEMBL3084637 110153 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1cccnc1)C2 10.1021/jm9008218
44426835 92476 0 None 35 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 361 4 1 2 4.9 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2F)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228802 92476 0 None 35 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 361 4 1 2 4.9 OC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2F)CC1 10.1016/j.bmcl.2007.03.061
44426808 151506 0 None 5 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 323 6 1 2 4.9 CCCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL390882 151506 0 None 5 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 323 6 1 2 4.9 CCCCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
118718265 122080 0 None 74 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 493 6 1 3 6.2 CC(=O)NC[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349248 122080 0 None 74 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 493 6 1 3 6.2 CC(=O)NC[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
25190589 195923 0 None 44 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 590 8 1 4 7.1 O=C1N(CCNC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL510745 195923 0 None 44 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 590 8 1 4 7.1 O=C1N(CCNC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
46879670 12742 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 474 4 1 4 3.1 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079943 12742 0 None 2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 474 4 1 4 3.1 CNC(=O)CN1Cc2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
44437604 97430 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 5.2 CCOCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL239045 97430 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 495 11 0 7 5.2 CCOCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437639 98006 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 11 1 7 4.4 CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL240085 98006 0 None 57 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 522 11 1 7 4.4 CCNC(=O)Cn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44437623 151958 0 None 53 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 523 11 0 8 4.8 COC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
CHEMBL391234 151958 0 None 53 4 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 523 11 0 8 4.8 COC(=O)CCn1c(=O)n(C2CCN(CCC(Oc3cc(OC)ccc3C)C(C)C)CC2)c2ccccc21 10.1016/j.bmc.2006.11.030
44394487 72220 0 None 21 2 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 512 7 1 5 2.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCNS(C)(=O)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL182967 72220 0 None 21 2 Human 8.3 pKi = 8.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 512 7 1 5 2.8 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCNS(C)(=O)=O)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
15512241 211643 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 397 2 1 3 4.2 Cc1ccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)cc1 10.1016/s0960-894x(99)00385-6
CHEMBL75676 211643 0 None 10 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptorDisplacement of [3H]-orphanin FQ from human OrphaninFQ (hOFQ) receptor
ChEMBL 397 2 1 3 4.2 Cc1ccc(N2CNC(=O)C23CCN(C2Cc4cccc5cccc2c45)CC3)cc1 10.1016/s0960-894x(99)00385-6
60154192 84375 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 416 5 0 4 3.7 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088043 84375 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 416 5 0 4 3.7 CN(C)C(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
44574586 196102 0 None 102 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 453 4 1 4 5.7 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2ccncn2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL512411 196102 0 None 102 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 453 4 1 4 5.7 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(c2ccncn2)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
46880089 14320 0 None 53 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 398 4 1 5 3.2 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C)(C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087532 14320 0 None 53 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 398 4 1 5 3.2 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C)(C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
9799433 97241 1 None -4 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 368 4 0 2 5.2 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387196 97241 1 None -4 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 368 4 0 2 5.2 CCC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
44574790 196241 0 None 19 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 488 5 1 3 6.8 Clc1ccccc1C(c1ccccc1Cl)N1C2CCC1CC(c1ccccc1)(c1nc[nH]n1)C2 10.1016/j.bmcl.2009.03.031
CHEMBL513660 196241 0 None 19 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 488 5 1 3 6.8 Clc1ccccc1C(c1ccccc1Cl)N1C2CCC1CC(c1ccccc1)(c1nc[nH]n1)C2 10.1016/j.bmcl.2009.03.031
70686907 84161 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 420 5 1 4 3.5 CNC(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2086647 84161 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 420 5 1 4 3.5 CNC(=O)C(Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
52952043 90372 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 420 5 1 4 3.5 CNC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2204349 90372 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 420 5 1 4 3.5 CNC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
44253138 149995 0 None 138 2 Human 8.3 pKi = 8.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 538 9 1 8 6.1 CNc1nc(Oc2ccc(OC)cc2)nc(N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)n1 nan
CHEMBL3896402 149995 0 None 138 2 Human 8.3 pKi = 8.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 538 9 1 8 6.1 CNc1nc(Oc2ccc(OC)cc2)nc(N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)n1 nan
25190607 185813 0 None 26 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 431 4 0 3 5.4 CCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL471262 185813 0 None 26 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 431 4 0 3 5.4 CCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O 10.1016/j.bmcl.2008.12.092
9924406 120766 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 347 5 2 2 4.7 CN(C)C1(c2ccccc2)CCC(NCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
CHEMBL3326221 120766 0 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 347 5 2 2 4.7 CN(C)C1(c2ccccc2)CCC(NCc2c[nH]c3ccccc23)CC1 10.1021/ml500116x
118711243 127333 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 336 5 1 2 3.7 CN(C)C1(c2ccccc2)CCC(NC(=O)Cc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325880 127333 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 336 5 1 2 3.7 CN(C)C1(c2ccccc2)CCC(NC(=O)Cc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545618 127333 0 None -2 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 336 5 1 2 3.7 CN(C)C1(c2ccccc2)CCC(NC(=O)Cc2ccccc2)CC1 10.1021/ml500116x
44430049 94707 0 None 33 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 364 3 2 3 4.2 CC1(C)CCC(N2CCC(O)(c3ccccc3CN)CC2)c2ccccc21 10.1016/j.bmcl.2007.03.062
CHEMBL233957 94707 0 None 33 4 Human 8.3 pKi = 8.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 364 3 2 3 4.2 CC1(C)CCC(N2CCC(O)(c3ccccc3CN)CC2)c2ccccc21 10.1016/j.bmcl.2007.03.062
46880090 14331 0 None 14 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 4 1 5 3.8 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C(C)(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087658 14331 0 None 14 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 426 4 1 5 3.8 CNC(=O)Cn1c(=O)n(C2CCN(C3CCC(C(C)(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
10024362 87069 0 None 28 3 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 407 3 1 7 1.2 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44414842 87069 0 None 28 3 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 407 3 1 7 1.2 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL214040 87069 0 None 28 3 Guinea pig 8.3 pKi = 8.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 407 3 1 7 1.2 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)C=C[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
127034023 145932 0 None 52 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 331 2 0 1 4.8 c1ccc2c(c1)CCC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3787174 145932 0 None 52 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 331 2 0 1 4.8 c1ccc2c(c1)CCC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
70690755 83426 0 None 25 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064130 83426 0 None 25 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 419 5 0 3 3.6 Cc1ccccc1C1CCN(CCC(=O)N2c3ccccc3CC2C(=O)N(C)C)CC1 10.1016/j.ejmech.2012.07.021
9954388 106315 1 None 1 4 Human 8.3 pKi = 8.3 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL283480 106315 1 None 1 4 Human 8.3 pKi = 8.3 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 429 2 1 3 4.3 O=C1NCN(c2ccccc2)C12CCN(C1CCc3c(Cl)ccc(Cl)c3C1)CC2 10.1021/jm991129q
25128942 134977 0 None 21 4 Human 8.3 pKi = 8.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 377 2 1 4 3.5 O=c1[nH]c2ccccc2n([C@H]2C[C@H]3C=C[C@@H](C2)N3C2/C=C\CCCCC2)c1=O nan
CHEMBL3665443 134977 0 None 21 4 Human 8.3 pKi = 8.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 377 2 1 4 3.5 O=c1[nH]c2ccccc2n([C@H]2C[C@H]3C=C[C@@H](C2)N3C2/C=C\CCCCC2)c1=O nan
52951940 84367 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 1 4 3.2 NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
CHEMBL2088032 84367 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 406 5 1 4 3.2 NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm201629q
52951940 84367 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 406 5 1 4 3.2 NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2088032 84367 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 406 5 1 4 3.2 NC(=O)[C@H](Cc1ccccc1F)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
11451023 113999 0 None 1 3 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1021/jm034249d
CHEMBL316699 113999 0 None 1 3 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 352 2 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1021/jm034249d
127034022 145781 0 None 8 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 333 2 0 2 4.2 c1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)CO2 10.1016/j.ejmech.2016.02.014
CHEMBL3785605 145781 0 None 8 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 333 2 0 2 4.2 c1ccc2c(c1)CC(CN1CCC3(CCc4ccccc43)CC1)CO2 10.1016/j.ejmech.2016.02.014
10066285 198508 0 None -5 4 Human 8.2 pKi = 8.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 347 2 1 4 4.7 Oc1nc2ccccc2n1[C@@H]1CCN2[C@H](c3ccccc3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
CHEMBL51972 198508 0 None -5 4 Human 8.2 pKi = 8.2 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 347 2 1 4 4.7 Oc1nc2ccccc2n1[C@@H]1CCN2[C@H](c3ccccc3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
46179069 132575 0 None 117 3 Human 8.2 pKi = 8.2 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 421 3 1 5 4.2 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CC3CCCC(C3)C2)c1=O nan
CHEMBL3647959 132575 0 None 117 3 Human 8.2 pKi = 8.2 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 421 3 1 5 4.2 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CC3CCCC(C3)C2)c1=O nan
10548749 179210 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccc(Cl)cc3C1)CC2 10.1021/jm991129q
CHEMBL447779 179210 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccc(Cl)cc3C1)CC2 10.1021/jm991129q
118662309 178269 0 None 5 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 328 4 0 2 4.0 CCCC(=O)N1CCC2(CCC(c3ccccc3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
CHEMBL4463703 178269 0 None 5 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 328 4 0 2 4.0 CCCC(=O)N1CCC2(CCC(c3ccccc3)(N(C)C)CC2)C1 10.1021/acsmedchemlett.6b00277
136036819 102696 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 10 2 8 3.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4n[nH]c(=O)[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259291 102696 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 534 10 2 8 3.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4n[nH]c(=O)[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44451872 102835 0 None 12 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 529 10 0 8 5.1 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cnccn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259964 102835 0 None 12 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 529 10 0 8 5.1 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cnccn4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44430081 155758 0 None 20 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 510 6 1 4 5.9 OC1(c2ccccc2CN2CCOCC2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL394222 155758 0 None 20 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 510 6 1 4 5.9 OC1(c2ccccc2CN2CCOCC2)CCN(C(c2ccccc2Cl)c2ccccc2Cl)CC1 10.1016/j.bmcl.2007.03.062
118718281 122097 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 465 5 1 3 6.3 Cc1cccnc1[C@@]1(CN)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349265 122097 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 465 5 1 3 6.3 Cc1cccnc1[C@@]1(CN)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718298 122115 1 None 23 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 448 3 1 2 7.1 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@]1(CNc3ccccc31)C2 10.1016/j.bmcl.2008.10.088
CHEMBL3349283 122115 1 None 23 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 448 3 1 2 7.1 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@]1(CNc3ccccc31)C2 10.1016/j.bmcl.2008.10.088
9802205 123313 0 None - 1 Human 7.3 pKi = 7.3 Binding
Compound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cellsCompound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells
ChEMBL 383 5 2 4 5.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccccc3)ccc2n1 10.1021/jm0002073
CHEMBL336238 123313 0 None - 1 Human 7.3 pKi = 7.3 Binding
Compound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cellsCompound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells
ChEMBL 383 5 2 4 5.0 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccccc3)ccc2n1 10.1021/jm0002073
1222 8445 49 None -194 32 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2008.12.092
3396 8445 49 None -194 32 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2008.12.092
85 8445 49 None -194 32 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2008.12.092
CHEMBL46516 8445 49 None -194 32 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2008.12.092
DB04842 8445 49 None -194 32 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2008.12.092
CHEMBL265392 217423 0 None - 1 Mouse 6.3 pKi = 6.3 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None C[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O 10.1021/jm010221v
10052051 73751 0 None -3162 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 510 7 1 3 5.5 CN(C)C(=O)C(CCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
CHEMBL186795 73751 0 None -3162 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 510 7 1 3 5.5 CN(C)C(=O)C(CCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
44391102 130549 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 533 7 1 7 6.6 Cc1ccc(Cl)c(OC2(C(CN3CCC(n4c(O)nc5ccccc54)CC3)n3ccnc3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL362240 130549 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 533 7 1 7 6.6 Cc1ccc(Cl)c(OC2(C(CN3CCC(n4c(O)nc5ccccc54)CC3)n3ccnc3)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
44252537 160619 0 None -2 2 Human 7.3 pKi = 7.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 5 1 2 4.6 CCNC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3982674 160619 0 None -2 2 Human 7.3 pKi = 7.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 5 1 2 4.6 CCNC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
10133108 85882 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 359 2 1 2 4.1 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL2113262 85882 0 None 4 3 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 359 2 1 2 4.1 O=C1N[C@@H]2CCCC[C@H]2N1C1CCN(C2CCC3CCCCC3C2)CC1 10.1016/j.bmcl.2003.11.083
24776404 104773 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 444 3 0 2 6.2 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2ccccc23)CC1 10.1021/jm7009606
CHEMBL272805 104773 0 None 1 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 444 3 0 2 6.2 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2ccccc23)CC1 10.1021/jm7009606
10093682 93541 2 None 20 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 421 4 1 2 5.5 OC1(c2ccc(Br)cc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL232067 93541 2 None 20 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 421 4 1 2 5.5 OC1(c2ccc(Br)cc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
24894783 193500 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 352 3 2 4 2.8 Cc1ccccc1[C@H]1CCN(C[C@@H]2Cc3cccnc3[C@@H](O)C2)C[C@@H]1O 10.1021/jm701590h
CHEMBL488655 193500 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 352 3 2 4 2.8 Cc1ccccc1[C@H]1CCN(C[C@@H]2Cc3cccnc3[C@@H](O)C2)C[C@@H]1O 10.1021/jm701590h
25129301 134976 0 None 239 3 Human 7.3 pKi = 7.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 370 2 1 4 3.3 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2cccnc2N1 nan
CHEMBL3665441 134976 0 None 239 3 Human 7.3 pKi = 7.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 370 2 1 4 3.3 O=C1CC(=O)N(C2CCN(C3CCCCCCC3)CC2)c2cccnc2N1 nan
9969865 72522 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 377 4 1 3 4.0 CCCC1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL183464 72522 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 377 4 1 3 4.0 CCCC1CCC(N2CCC(N3c4ccccc4NS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
12114744 84782 0 None 1 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 469 4 1 7 2.5 CN1CC[C@]23c4c5ccc(OC(=O)c6ccccc6)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44414877 84782 0 None 1 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 469 4 1 7 2.5 CN1CC[C@]23c4c5ccc(OC(=O)c6ccccc6)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
CHEMBL209751 84782 0 None 1 2 Guinea pig 6.3 pKi = 6.3 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 469 4 1 7 2.5 CN1CC[C@]23c4c5ccc(OC(=O)c6ccccc6)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44391067 70233 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 425 7 1 5 5.3 Cc1cc(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)ccc1F 10.1016/j.bmcl.2004.11.049
CHEMBL179797 70233 0 None 1 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 425 7 1 5 5.3 Cc1cc(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)C(C)C)ccc1F 10.1016/j.bmcl.2004.11.049
44413361 145159 0 None 16 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 370 2 1 1 5.9 Fc1ccc2c(C3CCN(C4Cc5cccc6cccc4c56)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL377237 145159 0 None 16 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 370 2 1 1 5.9 Fc1ccc2c(C3CCN(C4Cc5cccc6cccc4c56)CC3)c[nH]c2c1 10.1016/j.bmcl.2006.03.094
12985907 127184 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 4 1 3 3.8 CCC[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL353608 127184 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 355 4 1 3 3.8 CCC[C@H]1CC[C@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
25128941 134967 0 None 81 4 Human 7.3 pKi = 7.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 394 3 0 6 3.4 N#CCn1c(=O)c(=O)n(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 nan
CHEMBL3665433 134967 0 None 81 4 Human 7.3 pKi = 7.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 394 3 0 6 3.4 N#CCn1c(=O)c(=O)n(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 nan
44253137 156866 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 445 7 2 7 4.3 CNc1nc(NC)nc(N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)n1 nan
CHEMBL3950879 156866 0 None 1 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 445 7 2 7 4.3 CNc1nc(NC)nc(N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)n1 nan
44426828 92472 0 None 51 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccc(C(c2ccccc2)N2CCC(O)(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.061
CHEMBL228793 92472 0 None 51 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 4 1 2 5.1 Cc1ccc(C(c2ccccc2)N2CCC(O)(c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.061
25190576 196530 0 None 35 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 465 6 0 3 5.7 O=C1N(CC2CCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL515901 196530 0 None 35 3 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 465 6 0 3 5.7 O=C1N(CC2CCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
44252538 156166 0 None 10 2 Human 7.3 pKi = 7.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 314 4 1 3 4.2 CNC1(c2ccccc2)CCC(c2cccs2)(N(C)C)CC1 nan
CHEMBL3945501 156166 0 None 10 2 Human 7.3 pKi = 7.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 314 4 1 3 4.2 CNC1(c2ccccc2)CCC(c2cccs2)(N(C)C)CC1 nan
68629836 160050 0 None -7 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 314 5 1 2 4.6 CNC1(c2ccccc2)CCC(CC2CCCC2)(N(C)C)CC1 nan
CHEMBL3977691 160050 0 None -7 2 Human 6.3 pKi = 6.3 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 314 5 1 2 4.6 CNC1(c2ccccc2)CCC(CC2CCCC2)(N(C)C)CC1 nan
44297697 108513 0 None -30 4 Human 6.3 pKi = 6.3 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 375 3 0 4 4.8 CCn1c(=O)n([C@H]2CCN3[C@H](c4ccccc4)CCC[C@@H]3C2)c2ccccc21 10.1016/j.bmcl.2003.09.068
CHEMBL299660 108513 0 None -30 4 Human 6.3 pKi = 6.3 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 375 3 0 4 4.8 CCn1c(=O)n([C@H]2CCN3[C@H](c4ccccc4)CCC[C@@H]3C2)c2ccccc21 10.1016/j.bmcl.2003.09.068
10043898 92503 0 None 6 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 5 0 2 5.4 COC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228965 92503 0 None 6 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 357 5 0 2 5.4 COC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44402704 133167 0 None -17 3 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 373 2 0 3 4.7 CN(C)C[C@@H]1C[C@H]2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL365101 133167 0 None -17 3 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 373 2 0 3 4.7 CN(C)C[C@@H]1C[C@H]2c3ccccc3Oc3ccc(Br)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
24799848 104477 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 436 6 1 2 5.7 CC(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccc(F)cc3)CC2)CC1 10.1021/jm7009606
CHEMBL271341 104477 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 436 6 1 2 5.7 CC(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccc(F)cc3)CC2)CC1 10.1021/jm7009606
9924923 155463 0 None 16 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 4 1 2 5.1 Cc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL393985 155463 0 None 16 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 357 4 1 2 5.1 Cc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
118718263 122078 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 492 7 0 2 7.5 CN(C)C[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349246 122078 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 492 7 0 2 7.5 CN(C)C[C@]1(Cc2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44413286 145842 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 325 3 1 2 5.1 c1cnc2[nH]cc(C3CCN(CC4CCCCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL378633 145842 0 None 3 3 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 325 3 1 2 5.1 c1cnc2[nH]cc(C3CCN(CC4CCCCCCC4)CC3)c2c1 10.1016/j.bmcl.2006.03.094
76331525 110124 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 542 6 1 3 7.7 COC(=O)N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084558 110124 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 542 6 1 3 7.7 COC(=O)N[C@@]1(Cc2ccc(Cl)cc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
25190581 187420 0 None 199 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 535 7 0 3 7.3 CC(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL475497 187420 0 None 199 4 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 535 7 0 3 7.3 CC(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O 10.1016/j.bmcl.2008.12.092
122179057 128180 0 None -398 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccc(C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581753 128180 0 None -398 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccc(C)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
122179058 128181 0 None -794 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581754 128181 0 None -794 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccc(F)cc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
25128942 134978 0 None 12 4 Human 7.3 pKi = 7.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 377 2 1 4 3.5 O=c1[nH]c2ccccc2n([C@@H]2C[C@H]3C=C[C@@H](C2)N3C2/C=C\CCCCC2)c1=O nan
CHEMBL3665444 134978 0 None 12 4 Human 7.3 pKi = 7.3 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 377 2 1 4 3.5 O=c1[nH]c2ccccc2n([C@@H]2C[C@H]3C=C[C@@H](C2)N3C2/C=C\CCCCC2)c1=O nan
22562132 175241 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 369 2 1 3 2.8 O=S1(=O)Nc2ccccc2N1C1CCN(C2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL435091 175241 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 369 2 1 3 2.8 O=S1(=O)Nc2ccccc2N1C1CCN(C2Cc3ccccc3C2)CC1 10.1016/j.bmcl.2004.08.001
44252988 152916 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 352 5 0 3 4.5 COc1ccc(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
CHEMBL3919659 152916 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 352 5 0 3 4.5 COc1ccc(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)cc1 nan
44413385 84431 0 None 4 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 386 2 1 1 6.5 Clc1cccc2c(C3CCN(C4Cc5cccc6cccc4c56)CC3)c[nH]c12 10.1016/j.bmcl.2006.03.094
CHEMBL208862 84431 0 None 4 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 386 2 1 1 6.5 Clc1cccc2c(C3CCN(C4Cc5cccc6cccc4c56)CC3)c[nH]c12 10.1016/j.bmcl.2006.03.094
25190574 196364 0 None 13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 453 7 0 3 5.7 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL514606 196364 0 None 13 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 453 7 0 3 5.7 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
10286440 11999 0 None 14 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 314 5 1 2 4.6 CCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL106235 11999 0 None 14 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 314 5 1 2 4.6 CCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
122179063 128186 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 493 5 2 6 4.8 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581761 128186 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 493 5 2 6 4.8 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
10172398 14504 0 None 2 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 360 5 1 2 5.0 Cc1ccc([C@H](N)[C@@H]2CCN2C(c2ccccc2)c2ccccc2)cc1F 10.1016/s0960-894x(02)00652-2
CHEMBL108894 14504 0 None 2 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 360 5 1 2 5.0 Cc1ccc([C@H](N)[C@@H]2CCN2C(c2ccccc2)c2ccccc2)cc1F 10.1016/s0960-894x(02)00652-2
118718278 122094 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 536 7 0 2 8.2 Fc1ccc(C[C@@]2(CN3CCCC3)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2008.10.088
CHEMBL3349262 122094 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 536 7 0 2 8.2 Fc1ccc(C[C@@]2(CN3CCCC3)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2008.10.088
24894431 197970 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.1 CC1(c2ccccc2)CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL518922 197970 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 350 3 1 3 4.1 CC1(c2ccccc2)CCN(C[C@@H]2CCc3cccnc3[C@@H](O)C2)CC1 10.1021/jm701590h
54580478 69418 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 393 7 2 4 2.6 N[C@H](Cc1ccccc1)C(=O)NCCCN1CCC2(CC1)OCc1ccccc12 10.1016/j.bmc.2009.05.068
CHEMBL1783817 69418 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 393 7 2 4 2.6 N[C@H](Cc1ccccc1)C(=O)NCCCN1CCC2(CC1)OCc1ccccc12 10.1016/j.bmc.2009.05.068
54585395 69419 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 393 7 2 4 2.6 N[C@@H](Cc1ccccc1)C(=O)NCCCN1CCC2(CC1)OCc1ccccc12 10.1016/j.bmc.2009.05.068
CHEMBL1783818 69419 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 393 7 2 4 2.6 N[C@@H](Cc1ccccc1)C(=O)NCCCN1CCC2(CC1)OCc1ccccc12 10.1016/j.bmc.2009.05.068
57502917 134970 0 None -1 4 Human 6.2 pKi = 6.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 440 3 1 6 3.3 O=c1[nH]c2ccc(N3CCOCC3)cc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL3665436 134970 0 None -1 4 Human 6.2 pKi = 6.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 440 3 1 6 3.3 O=c1[nH]c2ccc(N3CCOCC3)cc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
10384734 161754 0 None 17 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 1 3 4.8 COc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL401234 161754 0 None 17 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 1 3 4.8 COc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
10022129 92512 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 6 0 2 5.8 CCOC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL229016 92512 0 None 6 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 6 0 2 5.8 CCOC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44395306 73646 0 None -2570 2 Human 6.2 pKi = 6.2 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 463 7 1 4 5.2 COC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
CHEMBL186300 73646 0 None -2570 2 Human 6.2 pKi = 6.2 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 463 7 1 4 5.2 COC(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
44252241 154987 0 None 100 3 Human 8.2 pKi = 8.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 322 4 0 2 4.5 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3935944 154987 0 None 100 3 Human 8.2 pKi = 8.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 322 4 0 2 4.5 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
16061455 110159 0 None 194 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 423 4 0 3 6.3 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ncccn1)C2 10.1021/jm9008218
CHEMBL3084649 110159 0 None 194 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 423 4 0 3 6.3 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ncccn1)C2 10.1021/jm9008218
44426840 92495 0 None 24 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 379 4 1 2 5.0 OC1(c2ccccc2)CCN(C(c2ccccc2F)c2ccccc2F)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228912 92495 0 None 24 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 379 4 1 2 5.0 OC1(c2ccccc2)CCN(C(c2ccccc2F)c2ccccc2F)CC1 10.1016/j.bmcl.2007.03.061
16733371 122081 0 None 123 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 479 7 1 3 6.7 CCNC[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349249 122081 0 None 123 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 479 7 1 3 6.7 CCNC[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718289 122105 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 450 5 1 2 6.6 NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349273 122105 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 450 5 1 2 6.6 NC[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44561518 196233 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 363 3 1 2 5.2 Cc1ccccc1C1CCN(C[C@@H]2CCc3c(C)cccc3[C@@H](O)C2)CC1 10.1021/jm701590h
CHEMBL513585 196233 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human ORL1 expressed in CHO cells
ChEMBL 363 3 1 2 5.2 Cc1ccccc1C1CCN(C[C@@H]2CCc3c(C)cccc3[C@@H](O)C2)CC1 10.1021/jm701590h
44574743 185380 0 None 95 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 494 5 1 3 7.0 COC(=O)NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL467313 185380 0 None 95 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 494 5 1 3 7.0 COC(=O)NC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44574705 185566 0 None 104 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 451 5 1 2 6.6 OCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL468952 185566 0 None 104 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 451 5 1 2 6.6 OCC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
76324310 110100 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 479 5 1 3 5.8 Cc1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
CHEMBL3084532 110100 0 None 4 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 479 5 1 3 5.8 Cc1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
76320665 110115 0 None 51 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 479 5 1 3 6.1 CC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084549 110115 0 None 51 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 479 5 1 3 6.1 CC(=O)N[C@@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
10020165 114069 1 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 340 3 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(CC2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b00982
CHEMBL317152 114069 1 None 2 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N/OFQ from human nociceptin receptorDisplacement of [3H]N/OFQ from human nociceptin receptor
ChEMBL 340 3 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(CC2CCCCCCC2)CC1 10.1021/acs.jmedchem.5b00982
44437617 161757 0 None 16 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 523 11 0 8 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCOC(C)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
CHEMBL401248 161757 0 None 16 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 523 11 0 8 4.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(CCOC(C)=O)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2006.11.030
10020165 114069 1 None 2 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 340 3 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(CC2CCCCCCC2)CC1 10.1021/jm034249d
CHEMBL317152 114069 1 None 2 3 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 340 3 0 2 4.4 O=C1Cc2ccccc2N1C1CCN(CC2CCCCCCC2)CC1 10.1021/jm034249d
10385808 72916 0 None 33 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184127 72916 0 None 33 2 Human 8.2 pKi = 8.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 391 3 1 3 3.5 CC(C)C1CCC(N2CCC(N3c4ccccc4CNS3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
10832445 104207 0 None 2 4 Human 8.2 pKi = 8.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 361 2 1 3 3.0 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc3C1)CC2 10.1021/jm991129q
CHEMBL26999 104207 0 None 2 4 Human 8.2 pKi = 8.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 361 2 1 3 3.0 O=C1NCN(c2ccccc2)C12CCN(C1CCc3ccccc3C1)CC2 10.1021/jm991129q
44438974 97904 0 None 89 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 433 4 1 3 4.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1F)c1ccccc1F)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL239820 97904 0 None 89 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 433 4 1 3 4.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1F)c1ccccc1F)CC2 10.1016/j.bmcl.2007.01.069
44414829 39999 6 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 1.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
5484063 39999 6 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 1.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
CHEMBL1418 39999 6 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 365 2 2 6 1.0 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)C=C[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
46879539 12266 0 None 53 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 448 5 1 4 3.0 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1076242 12266 0 None 53 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 448 5 1 4 3.0 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC(C(C)C)CC3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
10788833 37822 0 None - 1 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 431 5 1 4 5.6 Cc1cc(N)c2cc(N(C)C(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
CHEMBL139934 37822 0 None - 1 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 431 5 1 4 5.6 Cc1cc(N)c2cc(N(C)C(=O)c3ccccc3COc3ccc(Cl)cc3)ccc2n1 10.1021/jm0002073
71624270 97239 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 3 0 2 4.8 CC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387194 97239 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 3 0 2 4.8 CC1C(=O)N(C2CCN([C@H]3CC[C@@H](C(C)C)CC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
53326167 64083 0 None 5 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 541 6 1 6 5.7 OCC1(N2CCC(n3c(N4CC5CN(Cc6ccccc6)CC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650845 64083 0 None 5 4 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 541 6 1 6 5.7 OCC1(N2CCC(n3c(N4CC5CN(Cc6ccccc6)CC5C4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
24776401 165755 0 None 141 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 430 4 0 2 5.8 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2ccccc23)CC1 10.1021/jm7009606
CHEMBL409621 165755 0 None 141 3 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 430 4 0 2 5.8 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2ccccc23)CC1 10.1021/jm7009606
CHEMBL414543 219918 0 None - 1 Human 8.2 pKi = 8.2 Binding
Affinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cellsAffinity for human Opioid receptor like 1 (ORL-1) expressed in HEK293 cells
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)N(C)C(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/jm0202021
25190620 186086 0 None 12 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 516 7 0 4 6.1 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O)C(C)C 10.1016/j.bmcl.2008.12.092
CHEMBL473280 186086 0 None 12 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 516 7 0 4 6.1 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O)C(C)C 10.1016/j.bmcl.2008.12.092
10504545 106274 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 469 4 0 3 5.2 C=CCN1CN(c2ccccc2)C2(CCN(C3CCc4c(Cl)ccc(Cl)c4C3)CC2)C1=O 10.1021/jm991129q
CHEMBL283265 106274 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 469 4 0 3 5.2 C=CCN1CN(c2ccccc2)C2(CCN(C3CCc4c(Cl)ccc(Cl)c4C3)CC2)C1=O 10.1021/jm991129q
9934232 98583 0 None 407 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL241272 98583 0 None 407 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
9934232 98583 0 None 407 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL241272 98583 0 None 407 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
44391111 72378 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 443 7 2 6 4.6 CCC(Oc1cc(C)ccc1Cl)C(O)CN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/j.bmcl.2004.11.049
CHEMBL183323 72378 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 443 7 2 6 4.6 CCC(Oc1cc(C)ccc1Cl)C(O)CN1CCC(n2c(O)nc3ccccc32)CC1 10.1016/j.bmcl.2004.11.049
54584439 69420 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 393 8 2 4 2.8 O=C(CNCc1ccccc1)NCCCN1CCC2(CC1)OCc1ccccc12 10.1016/j.bmc.2009.05.068
CHEMBL1783819 69420 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 393 8 2 4 2.8 O=C(CNCc1ccccc1)NCCCN1CCC2(CC1)OCc1ccccc12 10.1016/j.bmc.2009.05.068
118662183 178481 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 334 5 0 3 4.1 CCCCN1CCC2(CCC(c3cccs3)(N(C)C)CC2)C1=O 10.1021/acsmedchemlett.6b00277
CHEMBL4466714 178481 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 334 5 0 3 4.1 CCCCN1CCC2(CCC(c3cccs3)(N(C)C)CC2)C1=O 10.1021/acsmedchemlett.6b00277
44380305 66111 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 439 2 1 3 6.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
CHEMBL170674 66111 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 439 2 1 3 6.3 O=C1NCN(c2ccccc2)C12CCN(C1CCCCCCCCCCCCCC1)CC2 10.1016/s0960-894x(00)00111-6
59159326 135819 0 None - 1 Human 5.2 pKi = 5.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 398 3 1 5 3.1 COc1ccc2c(n1)N(C1CCN(C3/C=C\CCCCC3)CC1)C(=O)CC(=O)N2 nan
CHEMBL3670296 135819 0 None - 1 Human 5.2 pKi = 5.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 398 3 1 5 3.1 COc1ccc2c(n1)N(C1CCN(C3/C=C\CCCCC3)CC1)C(=O)CC(=O)N2 nan
44394559 73082 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 407 3 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL184865 73082 0 None -2 2 Human 6.2 pKi = 6.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 407 3 1 3 3.7 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2004.08.001
44438912 97984 0 None 8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 327 3 1 3 3.0 O=C1NCN(c2ccccc2)C12CCN(CC1CCCCC1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240001 97984 0 None 8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 327 3 1 3 3.0 O=C1NCN(c2ccccc2)C12CCN(CC1CCCCC1)CC2 10.1016/j.bmcl.2007.01.069
57502893 134963 0 None 4 2 Human 6.2 pKi = 6.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 383 3 1 3 4.0 CC(C)C1CCC(N2CCC(N3C(=O)CC(=O)Nc4ccccc43)CC2)CC1 nan
CHEMBL3665429 134963 0 None 4 2 Human 6.2 pKi = 6.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 383 3 1 3 4.0 CC(C)C1CCC(N2CCC(N3C(=O)CC(=O)Nc4ccccc43)CC2)CC1 nan
44426803 92714 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 6 1 2 5.2 OC1(c2ccccc2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL230033 92714 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 371 6 1 2 5.2 OC1(c2ccccc2)CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44413362 146726 0 None 12 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 471 6 1 4 5.3 CN(C)C[C@@H](O)Cn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2ccc(F)cc21 10.1016/j.bmcl.2006.03.094
CHEMBL379971 146726 0 None 12 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 471 6 1 4 5.3 CN(C)C[C@@H](O)Cn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2ccc(F)cc21 10.1016/j.bmcl.2006.03.094
10314141 95001 0 None 17 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 323 3 1 2 4.6 CC(C)(C)C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL234771 95001 0 None 17 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 323 3 1 2 4.6 CC(C)(C)C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
118718285 122101 0 None 56 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.2 COc1ccc([C@@]2(CNC(C)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2008.10.088
CHEMBL3349269 122101 0 None 56 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 523 7 1 4 6.2 COc1ccc([C@@]2(CNC(C)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2008.10.088
46880088 14319 0 None 5 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 384 4 1 5 2.8 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCC3(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
CHEMBL1087531 14319 0 None 5 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 384 4 1 5 2.8 CNC(=O)Cn1c(=O)n(C2CCN(C3CCCC3(C)C)CC2)c2ccccc21 10.1016/j.bmcl.2009.09.028
122179061 128184 0 None -691 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(F)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581757 128184 0 None -691 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 505 5 2 5 4.9 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1cccc(F)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
44253568 152472 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 4 2 2 5.1 CNC1(c2[nH]c3ccccc3c2C)CCC(c2cccc(F)c2)(N(C)C)CC1 nan
CHEMBL3916201 152472 0 None -3 2 Human 6.2 pKi = 6.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 4 2 2 5.1 CNC1(c2[nH]c3ccccc3c2C)CCC(c2cccc(F)c2)(N(C)C)CC1 nan
44390999 72366 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 343 4 2 5 3.3 Oc1nc2ccccc2n1C1CCN(CC(O)C2CCCCC2)CC1 10.1016/j.bmcl.2004.11.049
CHEMBL183242 72366 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 343 4 2 5 3.3 Oc1nc2ccccc2n1C1CCN(CC(O)C2CCCCC2)CC1 10.1016/j.bmcl.2004.11.049
44402349 140218 0 None -2 3 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 450 2 1 5 6.0 Nc1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
CHEMBL370607 140218 0 None -2 3 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 450 2 1 5 6.0 Nc1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
57502892 134962 0 None 10 2 Human 6.2 pKi = 6.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 425 4 1 3 5.4 CCC1(CC)C(=O)Nc2ccccc2N(C2CCN(C3CCCCCCC3)CC2)C1=O nan
CHEMBL3665428 134962 0 None 10 2 Human 6.2 pKi = 6.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 425 4 1 3 5.4 CCC1(CC)C(=O)Nc2ccccc2N(C2CCN(C3CCCCCCC3)CC2)C1=O nan
44252533 153984 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 438 6 0 2 6.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3928190 153984 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 438 6 0 2 6.1 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)/C=C/c2ccccc2)CC1 nan
44394405 71341 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 505 5 0 5 4.6 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(=O)OC(C)(C)C)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL181545 71341 0 None 4 2 Human 7.2 pKi = 7.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 505 5 0 5 4.6 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CC(=O)OC(C)(C)C)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
25134074 134954 0 None - 1 Human 7.2 pKi = 7.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 373 2 1 4 3.6 O=c1[nH]c2c(F)cccc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL3665420 134954 0 None - 1 Human 7.2 pKi = 7.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 373 2 1 4 3.6 O=c1[nH]c2c(F)cccc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL414963 219944 0 None - 1 Mouse 6.2 pKi = 6.2 Binding
Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.Affinity to nociceptin receptors on mouse forebrain membranes by [3H]NC-NH2 displacement.
ChEMBL None None None Cc1ccc(C[C@H](N)CNCC(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)cc1 10.1021/jm990075h
10154739 103803 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 347 4 1 2 4.1 CCCC1CCC(N2CCC(N3C(=O)N[C@@H]4CCCC[C@H]43)CC2)CC1 10.1016/j.bmcl.2003.11.083
CHEMBL26681 103803 0 None -1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 347 4 1 2 4.1 CCCC1CCC(N2CCC(N3C(=O)N[C@@H]4CCCC[C@H]43)CC2)CC1 10.1016/j.bmcl.2003.11.083
44252100 155915 0 None -10 2 Human 6.2 pKi = 6.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 403 5 0 4 4.7 CN(C)C1(C(=O)c2cc3ccccc3n2C)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3943372 155915 0 None -10 2 Human 6.2 pKi = 6.2 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 403 5 0 4 4.7 CN(C)C1(C(=O)c2cc3ccccc3n2C)CCC(c2ccccc2)(N(C)C)CC1 nan
44337123 117277 0 None 54 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 398 5 1 2 5.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1cccc(F)c1)c1cccc(F)c1 10.1016/s0960-894x(02)00652-2
CHEMBL324897 117277 0 None 54 4 Human 7.2 pKi = 7.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 398 5 1 2 5.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1cccc(F)c1)c1cccc(F)c1 10.1016/s0960-894x(02)00652-2
134578506 181079 0 None 58 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 437 5 1 4 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCC(O)CC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4550088 181079 0 None 58 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 437 5 1 4 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CCC(O)CC4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
24776412 179452 0 None 40 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 418 6 1 2 5.6 CC(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3)CC2)CC1 10.1021/jm7009606
CHEMBL449966 179452 0 None 40 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 418 6 1 2 5.6 CC(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccccc3)CC2)CC1 10.1021/jm7009606
25134073 134953 0 None 2 4 Human 7.2 pKi = 7.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 355 2 1 4 3.4 O=c1[nH]c2ccccc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL3665419 134953 0 None 2 4 Human 7.2 pKi = 7.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 355 2 1 4 3.4 O=c1[nH]c2ccccc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
44339526 16097 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 403 3 1 2 5.2 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL111105 16097 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 403 3 1 2 5.2 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccc(C(F)(F)F)cc2)CC1 10.1016/s0960-894x(03)00665-6
10252647 186004 0 None 8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 439 5 0 3 5.3 CC(C)N1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL472676 186004 0 None 8 4 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 439 5 0 3 5.3 CC(C)N1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
44413384 173133 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 358 3 1 1 6.4 Clc1cccc2c(C3CCN(CC4CCCCCCC4)CC3)c[nH]c12 10.1016/j.bmcl.2006.03.094
CHEMBL427395 173133 0 None -1 3 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 358 3 1 1 6.4 Clc1cccc2c(C3CCN(CC4CCCCCCC4)CC3)c[nH]c12 10.1016/j.bmcl.2006.03.094
56661555 72482 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 501 4 2 5 5.1 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4c(Cl)cc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL1834415 72482 0 None -5 4 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 501 4 2 5 5.1 CO[C@]12CC[C@@]3(C[C@@H]1[C@@](C)(O)C(C)(C)C)[C@H]1Cc4c(Cl)cc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
118718284 122100 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 590 8 1 4 7.2 CC(=O)NC[C@]1(c2ncccc2CN2CCCCC2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349268 122100 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 590 8 1 4 7.2 CC(=O)NC[C@]1(c2ncccc2CN2CCCCC2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44430046 94525 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 440 5 2 3 5.5 NCc1ccccc1C1(O)CCN(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233749 94525 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 440 5 2 3 5.5 NCc1ccccc1C1(O)CCN(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)CC1 10.1016/j.bmcl.2007.03.062
44426839 175602 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 387 5 2 3 4.5 O=C(O)c1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL437742 175602 0 None -2 3 Human 5.2 pKi = 5.2 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 387 5 2 3 4.5 O=C(O)c1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44574889 185408 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 507 6 2 3 5.2 NC(=O)c1ccc(C2(C(N)=O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2009.03.031
CHEMBL467494 185408 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 507 6 2 3 5.2 NC(=O)c1ccc(C2(C(N)=O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccccc2Cl)cc1 10.1016/j.bmcl.2009.03.031
118718295 122112 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 518 6 0 2 7.3 O=C1CCCN1C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349280 122112 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 518 6 0 2 7.3 O=C1CCCN1C[C@]1(c2ccccc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118662014 179647 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 272 2 1 2 2.5 CN(C)C1(c2ccccc2)CCC2(CC1)CNC(=O)C2 10.1021/acsmedchemlett.6b00277
CHEMBL4515245 179647 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter methodDisplacement of [3H]-nociceptin/orphanin FQ from recombinant ORL1 receptor (unknown origin) expressed in CHO cell membranes measured after 1 hr by scintillation counter method
ChEMBL 272 2 1 2 2.5 CN(C)C1(c2ccccc2)CCC2(CC1)CNC(=O)C2 10.1021/acsmedchemlett.6b00277
59159321 135820 0 None 173 2 Human 7.2 pKi = 7.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 445 3 1 5 3.6 COC(=O)C1(N2CCC(N3C(=O)CC(=O)Nc4ccc(F)cc43)CC2)CCCCCCC1 nan
CHEMBL3670297 135820 0 None 173 2 Human 7.2 pKi = 7.2 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 445 3 1 5 3.6 COC(=O)C1(N2CCC(N3C(=O)CC(=O)Nc4ccc(F)cc43)CC2)CCCCCCC1 nan
44337249 11987 0 None 6 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 360 7 1 2 5.5 CCCCC(c1cccc(F)c1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL106190 11987 0 None 6 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 360 7 1 2 5.5 CCCCC(c1cccc(F)c1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
44337460 115956 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 398 5 1 2 5.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/s0960-894x(02)00652-2
CHEMBL321462 115956 0 None 3 4 Human 6.2 pKi = 6.2 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 398 5 1 2 5.5 N[C@H](c1cccc(Cl)c1)[C@@H]1CCN1C(c1ccc(F)cc1)c1ccc(F)cc1 10.1016/s0960-894x(02)00652-2
44249048 110157 0 None 11 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccncc1)C2 10.1021/jm9008218
CHEMBL3084642 110157 0 None 11 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 422 4 0 2 6.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccncc1)C2 10.1021/jm9008218
44402509 77397 0 None 1 3 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 295 2 0 3 4.0 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccccc3[C@@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL194994 77397 0 None 1 3 Rat 7.2 pKi = 7.2 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 295 2 0 3 4.0 CN(C)C[C@H]1C[C@H]2c3ccccc3Oc3ccccc3[C@@H]2O1 10.1016/j.bmcl.2005.03.076
44339449 15871 7 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 353 3 1 2 4.3 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL109916 15871 7 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 353 3 1 2 4.3 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccc(F)cc2)CC1 10.1016/s0960-894x(03)00665-6
9902583 104246 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 341 4 0 2 3.7 CCN1C(=O)N(C2CCN(Cc3ccccc3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL27018 104246 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 341 4 0 2 3.7 CCN1C(=O)N(C2CCN(Cc3ccccc3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
9845765 37999 0 None - 1 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 397 5 2 4 5.3 Cc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1021/jm0002073
CHEMBL140103 37999 0 None - 1 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 397 5 2 4 5.3 Cc1ccc(OCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1021/jm0002073
44248550 110172 0 None 128 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 519 6 0 3 7.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ncccc1CN1CCCCC1)C2 10.1021/jm9008218
CHEMBL3084669 110172 0 None 128 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 519 6 0 3 7.9 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ncccc1CN1CCCCC1)C2 10.1021/jm9008218
118718266 122082 0 None 109 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 479 6 0 3 6.6 CN(C)C[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349250 122082 0 None 109 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 479 6 0 3 6.6 CN(C)C[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
118718279 122095 0 None 87 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 451 5 1 3 6.0 NC[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349263 122095 0 None 87 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 451 5 1 3 6.0 NC[C@]1(c2ccccn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
44574891 196244 0 None 30 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 492 6 1 2 6.8 CCNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL513667 196244 0 None 30 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 492 6 1 2 6.8 CCNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44247589 110097 0 None 17 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084529 110097 0 None 17 4 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 483 5 1 3 5.7 NC(=O)[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
76327876 110114 0 None 29 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 455 4 1 3 6.1 N[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084548 110114 0 None 29 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 455 4 1 3 6.1 N[C@@]1(c2ccc(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44414783 148447 0 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 367 2 2 6 1.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)CC[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44414784 148447 0 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 367 2 2 6 1.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)CC[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
CHEMBL385448 148447 0 None 2 3 Guinea pig 8.2 pKi = 8.2 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 367 2 2 6 1.2 CN1CC[C@]23c4c5ccc(O)c4O[C@H]2[C@@H](OS(=O)(=O)O)CC[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
46879716 12813 0 None 38 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 460 4 1 4 3.1 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
CHEMBL1080483 12813 0 None 38 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 460 4 1 4 3.1 CNC(=O)CN1c2ccccc2N(C2CCN(C3CCC4CCCCC4C3)CC2)S1(=O)=O 10.1016/j.bmcl.2009.09.028
9883872 65934 0 None 8 3 Rat 8.2 pKi = 8.2 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 327 2 1 3 3.0 C[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
CHEMBL169947 65934 0 None 8 3 Rat 8.2 pKi = 8.2 Binding
Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1Inhibition against binding of radioligand [leucyl-3H]-OFQ to membrane of human embryonic kidney 293 cells overexpressing rat Opioid receptor like 1
ChEMBL 327 2 1 3 3.0 C[C@H]1CC[C@@H](N2CCC3(CC2)C(=O)NCN3c2ccccc2)CC1 10.1016/s0960-894x(00)00111-6
10646744 104183 0 None -2 4 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 439 4 1 4 3.3 O=C1N(CCO)CN(c2ccccc2)C12CCN(C1CCc3cccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL26987 104183 0 None -2 4 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 439 4 1 4 3.3 O=C1N(CCO)CN(c2ccccc2)C12CCN(C1CCc3cccc(Cl)c3C1)CC2 10.1021/jm991129q
10572810 106337 0 None 2 4 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3cccc(Cl)c3C1)CC2 10.1021/jm991129q
CHEMBL283617 106337 0 None 2 4 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing human Opioid receptor like 1
ChEMBL 395 2 1 3 3.6 O=C1NCN(c2ccccc2)C12CCN(C1CCc3cccc(Cl)c3C1)CC2 10.1021/jm991129q
44574539 185224 0 None 97 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 466 4 1 3 6.6 Cc1ccnc(C2(O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccc(C)cc2Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL466126 185224 0 None 97 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 466 4 1 3 6.6 Cc1ccnc(C2(O)CC3CCC(C2)N3C(c2ccccc2Cl)c2ccc(C)cc2Cl)c1 10.1016/j.bmcl.2009.03.031
60154189 84372 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088038 84372 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
CHEMBL2088039 84372 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 388 5 0 6 2.2 CN(C)C(=O)C(CN1CCC2(CC1)OCCc1ccsc12)Cn1cccn1 10.1021/jm201629q
44253567 151275 0 None 48 2 Human 8.1 pKi = 8.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 6 1 3 3.6 CNC(=O)CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3906866 151275 0 None 48 2 Human 8.1 pKi = 8.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 6 1 3 3.6 CNC(=O)CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44574632 196083 0 None 41 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 433 6 2 3 5.5 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(CCCO)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
CHEMBL512247 196083 0 None 41 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 433 6 2 3 5.5 Cc1ccc(C(c2ccccc2Cl)N2C3CCC2CC(O)(CCCO)C3)c(Cl)c1 10.1016/j.bmcl.2009.03.031
118722880 127327 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 322 6 1 2 4.2 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325878 127327 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 322 6 1 2 4.2 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545580 127327 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 322 6 1 2 4.2 CN(C)[C@]1(c2ccccc2)CC[C@@H](NCCc2ccccc2)CC1 10.1021/ml500116x
10137876 131827 0 None 11 2 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 435 5 1 4 3.2 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCO)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL364398 131827 0 None 11 2 Human 8.1 pKi = 8.1 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 435 5 1 4 3.2 CC(C)C1CCC(N2CCC(N3c4ccccc4CN(CCO)S3(=O)=O)CC2)CC1 10.1016/j.bmcl.2004.08.001
11461888 11398 3 None -2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
CHEMBL102900 11398 3 None -2 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1021/jm034249d
11461888 11398 3 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL102900 11398 3 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 338 2 0 2 4.0 O=C1Cc2ccccc2N1C1CCN(C2C3CCCC2CCC3)CC1 10.1016/j.bmcl.2013.03.101
10156821 185318 0 None 67 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 383 4 1 2 5.7 OC1(c2ccccc2)CC2CCCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
CHEMBL466846 185318 0 None 67 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 383 4 1 2 5.7 OC1(c2ccccc2)CC2CCCC(C1)N2C(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2009.03.031
71624265 97233 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 4 0 2 4.4 CCC[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387188 97233 0 None -1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 340 4 0 2 4.4 CCC[C@H]1CC[C@@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1016/j.bmcl.2013.03.101
46879669 12741 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 436 4 1 4 3.4 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC4CCCCC4C3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
CHEMBL1079942 12741 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 436 4 1 4 3.4 CNC(=O)CN1N=C(c2ccccc2)C2(CCN(C3CCC4CCCCC4C3)CC2)C1=O 10.1016/j.bmcl.2009.09.028
44451592 102697 0 None 22 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 1 8 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cnn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259292 102697 0 None 22 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 518 10 1 8 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cnn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
118718294 122111 0 None 60 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 504 6 0 2 7.7 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@@](CN1CCCC1)(c1ccccc1)C2 10.1016/j.bmcl.2008.10.088
CHEMBL3349279 122111 0 None 60 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 504 6 0 2 7.7 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@@](CN1CCCC1)(c1ccccc1)C2 10.1016/j.bmcl.2008.10.088
45270712 202083 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 470 4 0 2 6.7 CC(=O)N1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
CHEMBL551454 202083 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 470 4 0 2 6.7 CC(=O)N1CCCCC1C1C[C@@H]2CC[C@@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1021/jm9008218
10042904 215185 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
CHEMBL99738 215185 0 None -3 3 Human 7.2 pKi = 7.2 Binding
Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.Binding affinity against human Nociceptin receptor on CHO cell membranes by [3H]N/OFQ displacement.
ChEMBL 340 3 0 2 4.3 CC(C)[C@H]1CC[C@H](N2CCC(N3C(=O)Cc4ccccc43)CC2)CC1 10.1021/jm034249d
44413441 86717 0 None -2 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 372 3 1 1 6.7 Cc1[nH]c2ccc(Cl)cc2c1C1CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2006.03.094
CHEMBL212574 86717 0 None -2 4 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 372 3 1 1 6.7 Cc1[nH]c2ccc(Cl)cc2c1C1CCN(CC2CCCCCCC2)CC1 10.1016/j.bmcl.2006.03.094
10182346 131430 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 449 6 1 4 4.4 O=S1(=O)Nc2ccccc2N1C1CCN(Cc2ccc(OCc3ccccc3)cc2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL364147 131430 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 449 6 1 4 4.4 O=S1(=O)Nc2ccccc2N1C1CCN(Cc2ccc(OCc3ccccc3)cc2)CC1 10.1016/j.bmcl.2004.08.001
44339450 116990 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 385 3 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL323729 116990 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 385 3 1 2 5.3 OC1(c2cccc(C(F)(F)F)c2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
11480038 113541 0 None 35 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 900 22 10 9 -0.2 CC(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
CHEMBL3144468 113541 0 None 35 3 Human 7.1 pKi = 7.1 Binding
Binding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cellsBinding affinity against human opioid receptor like 1 (hORL) was determined using [leucyl-3H]nociceptin in vitro in CHO cells
ChEMBL 900 22 10 9 -0.2 CC(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@H]1CC[C@H]2CCC[C@@H](C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](Cc3ccc(Cl)cc3)C(N)=O)N2C1=O 10.1021/jm031034v
10317947 92513 0 None 20 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 385 7 0 2 6.2 CCCOC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL229017 92513 0 None 20 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 385 7 0 2 6.2 CCCOC1(c2ccccc2)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
76335140 110103 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 481 5 2 4 5.2 NC(=O)[C@@]1(c2ccc(O)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084535 110103 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 481 5 2 4 5.2 NC(=O)[C@@]1(c2ccc(O)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44252683 151907 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 288 6 1 2 4.2 CCCCC1(N(C)C)CCC(NC)(c2ccccc2)CC1 nan
CHEMBL3911970 151907 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 288 6 1 2 4.2 CCCCC1(N(C)C)CCC(NC)(c2ccccc2)CC1 nan
44337129 11958 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 420 7 1 3 6.3 N[C@@H](c1ccc(Oc2ccccc2)cc1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
CHEMBL106043 11958 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 420 7 1 3 6.3 N[C@@H](c1ccc(Oc2ccccc2)cc1)[C@@H]1CCN1C(c1ccccc1)c1ccccc1 10.1016/s0960-894x(02)00652-2
44252990 155181 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 389 6 1 2 5.6 CN(Cc1c[nH]c2ccccc12)CC1(C)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3937593 155181 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 389 6 1 2 5.6 CN(Cc1c[nH]c2ccccc12)CC1(C)CCC(c2ccccc2)(N(C)C)CC1 nan
118718300 122117 0 None 13 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 462 3 1 2 7.4 Cc1ccc2c(c1)[C@@]1(CN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349285 122117 0 None 13 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 462 3 1 2 7.4 Cc1ccc2c(c1)[C@@]1(CN2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
24800016 104444 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 450 5 1 2 6.1 CC(C)(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccc(F)cc3)CC2)CC1 10.1021/jm7009606
CHEMBL271185 104444 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 450 5 1 2 6.1 CC(C)(C)C1CCC(N2CCC(C(=O)NCc3ccccc3)(c3ccc(F)cc3)CC2)CC1 10.1021/jm7009606
44337163 12196 0 None 3 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 342 7 1 2 5.3 CCCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL107288 12196 0 None 3 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 342 7 1 2 5.3 CCCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
76331524 110104 0 None 6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 490 5 1 4 5.4 N#Cc1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
CHEMBL3084536 110104 0 None 6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 490 5 1 4 5.4 N#Cc1ccc([C@]2(C(N)=O)C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)nc1 10.1016/j.bmcl.2009.03.057
90306885 117742 0 None -85 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 493 5 2 6 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
CHEMBL3262372 117742 0 None -85 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cellsDisplacement of [3H]-N/OFQ from recombinant nociceptin opioid receptor (unknown origin) expressed in HEK cells
ChEMBL 493 5 2 6 4.6 CO[C@]12CC[C@@]3(C[C@@H]1[C@](C)(O)c1cccs1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
44402816 147480 0 None -3 3 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 325 3 0 4 4.0 COc1ccc2c(c1)[C@H]1O[C@H](CN(C)C)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
CHEMBL381664 147480 0 None -3 3 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 325 3 0 4 4.0 COc1ccc2c(c1)[C@H]1O[C@H](CN(C)C)C[C@H]1c1ccccc1O2 10.1016/j.bmcl.2005.03.076
134156152 157918 0 None -5 2 Human 6.1 pKi = 6.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 394 6 1 2 5.0 CC(NC(=O)/C=C/c1ccccc1)C1CCC(c2cccc(F)c2)(N(C)C)CC1 nan
CHEMBL3959501 157918 0 None -5 2 Human 6.1 pKi = 6.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 394 6 1 2 5.0 CC(NC(=O)/C=C/c1ccccc1)C1CCC(c2cccc(F)c2)(N(C)C)CC1 nan
90655976 117786 0 None -38 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 438 7 0 2 6.2 CCC1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262549 117786 0 None -38 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 438 7 0 2 6.2 CCC1C(=O)N(C2CCN(CCC(c3ccccc3)c3ccccc3)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
44414724 39763 0 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 381 3 1 6 1.6 COc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44414725 39763 0 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 381 3 1 6 1.6 COc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL1416 39763 0 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 381 3 1 6 1.6 COc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44391093 71232 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 505 8 2 6 5.4 Cc1ccc(Cl)c(OC(Cc2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL181342 71232 0 None -2 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 505 8 2 6 5.4 Cc1ccc(Cl)c(OC(Cc2ccccc2)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
9848990 195944 1 None -812 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
CHEMBL2368861 195944 1 None -812 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
CHEMBL511142 195944 1 None -812 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm401964y
9848990 195944 1 None -812 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL2368861 195944 1 None -812 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
CHEMBL511142 195944 1 None -812 6 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 467 4 2 5 4.4 CO[C@@]12CC[C@@]3(C[C@@H]1[C@](C)(O)C(C)(C)C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/jm2003238
44252682 150366 0 None -15 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 7 1 3 4.8 CN(C)C1(c2cccc(F)c2)CCC(C)(CNS(=O)(=O)/C=C/c2ccccc2)CC1 nan
CHEMBL3899387 150366 0 None -15 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 430 7 1 3 4.8 CN(C)C1(c2cccc(F)c2)CCC(C)(CNS(=O)(=O)/C=C/c2ccccc2)CC1 nan
44337513 11968 0 None 2 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 356 8 1 2 5.7 CCCCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL106084 11968 0 None 2 4 Human 6.1 pKi = 6.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 356 8 1 2 5.7 CCCCCC(c1ccccc1)N1CC[C@H]1[C@@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
10413540 132294 0 None -707 2 Human 7.1 pKi = 7.1 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 497 7 1 4 5.5 COC(=O)C(CCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
CHEMBL364625 132294 0 None -707 2 Human 7.1 pKi = 7.1 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 497 7 1 4 5.5 COC(=O)C(CCN1CCC(O)(c2cccc(C(F)(F)F)c2)CC1)(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2004.08.032
10171862 127346 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 5 0 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3325748 127346 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 5 0 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCc2ccccc2)CC1 10.1021/ml500116x
CHEMBL3545632 127346 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 309 5 0 2 4.6 CN(C)[C@]1(c2ccccc2)CC[C@@H](OCc2ccccc2)CC1 10.1021/ml500116x
44297519 107395 0 None -16 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 347 2 1 4 4.7 Oc1nc2ccccc2n1[C@H]1CCN2[C@H](c3ccccc3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
CHEMBL291901 107395 0 None -16 3 Human 6.1 pKi = 6.1 Binding
Binding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cellsBinding affinity for human nociceptin (NOP) receptor using [3H]N/OFQ as radioligand transfected into CHO cells
ChEMBL 347 2 1 4 4.7 Oc1nc2ccccc2n1[C@H]1CCN2[C@H](c3ccccc3)CCC[C@@H]2C1 10.1016/j.bmcl.2003.09.068
44337452 12027 0 None 75 4 Human 7.1 pKi = 7.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 328 6 1 2 5.0 CCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL106366 12027 0 None 75 4 Human 7.1 pKi = 7.1 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 328 6 1 2 5.0 CCCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
76324311 110126 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 1 3 5.5 NC(=O)[C@@]1(c2ccncc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084560 110126 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 465 5 1 3 5.5 NC(=O)[C@@]1(c2ccncc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
122179052 128173 0 None -1995 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581741 128173 0 None -1995 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
44328141 103743 0 None -1995 3 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 1182 31 16 15 -4.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O nan
CHEMBL266314 103743 0 None -1995 3 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 1182 31 16 15 -4.4 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O nan
122179052 128173 0 None -1995 3 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3581741 128173 0 None -1995 3 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 499 5 2 5 4.8 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1cccc(C)c1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
10596013 128280 0 None - 1 Human 7.1 pKi = 7.1 Binding
Compound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cellsCompound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells
ChEMBL 381 5 2 3 5.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3CCc3ccccc3)ccc2n1 10.1021/jm0002073
CHEMBL358306 128280 0 None - 1 Human 7.1 pKi = 7.1 Binding
Compound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cellsCompound was evaluated for its ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells
ChEMBL 381 5 2 3 5.2 Cc1cc(N)c2cc(NC(=O)c3ccccc3CCc3ccccc3)ccc2n1 10.1021/jm0002073
44574672 196163 0 None 79 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 451 5 0 2 7.3 COC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL512950 196163 0 None 79 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 451 5 0 2 7.3 COC1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
25190597 184469 0 None 35 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 576 7 0 4 6.7 O=C1N(CCN2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL464192 184469 0 None 35 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 576 7 0 4 6.7 O=C1N(CCN2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
44402586 78672 0 None 5 3 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 313 2 0 3 4.1 CN(C)C[C@@H]1C[C@H]2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
CHEMBL197135 78672 0 None 5 3 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 313 2 0 3 4.1 CN(C)C[C@@H]1C[C@H]2c3ccccc3Oc3ccc(F)cc3[C@H]2O1 10.1016/j.bmcl.2005.03.076
1692 8935 29 None 12 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm0002073
5311340 8935 29 None 12 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm0002073
CHEMBL140979 8935 29 None 12 4 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm0002073
1692 8935 29 None 12 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm020078l
5311340 8935 29 None 12 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm020078l
CHEMBL140979 8935 29 None 12 4 Human 8.1 pKi = 8.1 Binding
Binding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cellsBinding affinity for opioid receptor like type, human Opioid receptor like 1 expressed in membrane homogenates of COS-1 or CHO cells
ChEMBL 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 10.1021/jm020078l
44574962 185292 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 522 8 1 3 6.4 COCCNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
CHEMBL466693 185292 0 None 7 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 522 8 1 3 6.4 COCCNC(=O)C1(c2ccccc2)CC2CCC(C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.031
44391155 72042 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 475 7 1 5 6.6 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182819 72042 0 None 1 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 475 7 1 5 6.6 Cc1ccc(Cl)c(OC(CCN2CCC(n3c(O)nc4ccccc43)CC2)c2ccccc2)c1 10.1016/j.bmcl.2004.11.049
44439001 98552 0 None 7 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 407 2 1 3 4.4 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccc(F)cc21 10.1016/j.bmcl.2007.01.069
CHEMBL241087 98552 0 None 7 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 407 2 1 3 4.4 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccc(F)cc21 10.1016/j.bmcl.2007.01.069
56664973 72475 0 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 481 6 2 5 4.8 CCC(C)(C)[C@](C)(O)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm2003238
CHEMBL1834409 72475 0 None -5 4 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation countingDisplacement of [3H]N/OFQ from human NOP receptor expressed in CHO cells after 60 mins by scintillation counting
ChEMBL 481 6 2 5 4.8 CCC(C)(C)[C@](C)(O)[C@H]1C[C@@]23CC[C@]1(OC)[C@@H]1Oc4c(O)ccc5c4[C@@]12CCN(CC1CC1)[C@@H]3C5 10.1021/jm2003238
10646745 106306 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 439 4 0 4 3.9 COCN1CN(c2ccccc2)C2(CCN(C3CCc4cccc(Cl)c4C3)CC2)C1=O 10.1021/jm991129q
CHEMBL283432 106306 0 None -1 4 Human 8.1 pKi = 8.1 Binding
Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1Competitive binding affinity against transfected HEK293 cells expressing Opioid receptor like 1
ChEMBL 439 4 0 4 3.9 COCN1CN(c2ccccc2)C2(CCN(C3CCc4cccc(Cl)c4C3)CC2)C1=O 10.1021/jm991129q
11602409 145903 0 None 26 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 332 2 1 2 3.7 c1ccc2c(c1)CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
CHEMBL3786899 145903 0 None 26 2 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 332 2 1 2 3.7 c1ccc2c(c1)CNC(CN1CCC3(CCc4ccccc43)CC1)C2 10.1016/j.ejmech.2016.02.014
90655974 117783 0 None -8 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 374 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCc4ccccc43)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
CHEMBL3262546 117783 0 None -8 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranesDisplacement of [3H]N/OFQ from human nociceptin opioid receptor transfected in CHO cell membranes
ChEMBL 374 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCc4ccccc43)CC2)c2ccccc21 10.1016/j.bmc.2014.02.047
25190588 181581 0 None 28 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 576 8 1 4 6.8 O=C1N(CCNC2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL456225 181581 0 None 28 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 576 8 1 4 6.8 O=C1N(CCNC2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 10.1016/j.bmcl.2008.12.092
71624388 97242 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
CHEMBL2387197 97242 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 354 3 0 2 5.1 CCC1C(=O)N(C2CCN(C3CCCCCCC3)CC2)c2ccccc21 10.1016/j.bmcl.2013.03.101
24776397 104726 0 None 11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 372 2 0 2 4.3 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(C)Cc2cc(F)ccc23)CC1 10.1021/jm7009606
CHEMBL272601 104726 0 None 11 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 372 2 0 2 4.3 CC(C)C1CCC(N2CCC3(CC2)C(=O)N(C)Cc2cc(F)ccc23)CC1 10.1021/jm7009606
25134077 134957 0 None 48 4 Human 8.1 pKi = 8.1 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 397 2 1 4 3.8 O=c1[nH]c2ccccc2n(C2CCN(C3Cc4cccc5cccc3c45)CC2)c1=O nan
CHEMBL3665423 134957 0 None 48 4 Human 8.1 pKi = 8.1 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 397 2 1 4 3.8 O=c1[nH]c2ccccc2n(C2CCN(C3Cc4cccc5cccc3c45)CC2)c1=O nan
81689704 128177 0 None -1995 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581750 128177 0 None -1995 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
134134623 151287 0 None -1995 3 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.7 CO[C@@]12CC[C@]3(C[C@@]1(C)[C@@H](O)c1ccccc1)[C@@H]1Cc4ccc(O)c5c4[C@]3(CCN1CC1CC1)[C@@H]2O5 nan
CHEMBL3907014 151287 0 None -1995 3 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.7 CO[C@@]12CC[C@]3(C[C@@]1(C)[C@@H](O)c1ccccc1)[C@@H]1Cc4ccc(O)c5c4[C@]3(CCN1CC1CC1)[C@@H]2O5 nan
81689704 128177 0 None -1995 3 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3581750 128177 0 None -1995 3 Human 7.1 pKi = 7.1 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 487 5 2 5 4.7 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
53319616 64084 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 467 4 0 7 4.1 COC(=O)C1(N2CCC(n3c(N4CCN(C)CC4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
CHEMBL1650846 64084 0 None 3 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 minsDisplacement of [3H]N/OFQ from human NOP receptor expressed in HEK293 cells after 45 mins
ChEMBL 467 4 0 7 4.1 COC(=O)C1(N2CCC(n3c(N4CCN(C)CC4)nc4ccccc43)CC2)CCCCCCC1 10.1016/j.bmc.2010.07.034
16665915 145722 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 358 3 1 1 5.8 Fc1ccc2[nH]cc(C3CCN(Cc4cccc5ccccc45)CC3)c2c1 10.1016/j.bmcl.2006.03.094
CHEMBL378458 145722 0 None -1 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 358 3 1 1 5.8 Fc1ccc2[nH]cc(C3CCN(Cc4cccc5ccccc45)CC3)c2c1 10.1016/j.bmcl.2006.03.094
44413301 146330 0 None 10 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 367 2 0 3 5.2 Cn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2cccnc21 10.1016/j.bmcl.2006.03.094
CHEMBL379657 146330 0 None 10 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 367 2 0 3 5.2 Cn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2cccnc21 10.1016/j.bmcl.2006.03.094
24776405 102738 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 462 3 0 2 6.3 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cccc(F)c23)CC1 10.1021/jm7009606
CHEMBL259473 102738 0 None 2 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 462 3 0 2 6.3 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)N(Cc2ccccc2)Cc2cccc(F)c23)CC1 10.1021/jm7009606
15586319 127334 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 288 3 0 3 2.7 CN(C)[C@]1(c2ccccc2)CC[C@H](N2CCOCC2)CC1 10.1021/ml500116x
CHEMBL3326219 127334 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 288 3 0 3 2.7 CN(C)[C@]1(c2ccccc2)CC[C@H](N2CCOCC2)CC1 10.1021/ml500116x
CHEMBL3545620 127334 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 minsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells after 90 mins
ChEMBL 288 3 0 3 2.7 CN(C)[C@]1(c2ccccc2)CC[C@H](N2CCOCC2)CC1 10.1021/ml500116x
44391137 72879 0 None -7 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 510 7 1 6 6.1 Cc1ccc(Cl)c(OC2(C(CN3CCC(n4c(O)nc5ccccc54)CC3)N(C)C)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL183918 72879 0 None -7 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 510 7 1 6 6.1 Cc1ccc(Cl)c(OC2(C(CN3CCC(n4c(O)nc5ccccc54)CC3)N(C)C)CCCCC2)c1 10.1016/j.bmcl.2004.11.049
44426821 92467 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 422 5 2 3 4.6 O=C(Nc1c(F)cccc1F)C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228738 92467 0 None -2 4 Human 5.1 pKi = 5.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 422 5 2 3 4.6 O=C(Nc1c(F)cccc1F)C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
118718267 122083 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 451 5 1 3 6.0 NC[C@]1(c2cccnc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349251 122083 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 451 5 1 3 6.0 NC[C@]1(c2cccnc2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
9824268 171833 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 398 5 3 5 4.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(N)cc3)ccc2n1 10.1021/jm0002073
CHEMBL422641 171833 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 398 5 3 5 4.5 Cc1cc(N)c2cc(NC(=O)c3ccccc3COc3ccc(N)cc3)ccc2n1 10.1021/jm0002073
44413414 145199 1 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 341 3 1 2 5.1 c1ccc2c(CN3CCC(c4c[nH]c5ncccc45)CC3)cccc2c1 10.1016/j.bmcl.2006.03.094
CHEMBL377402 145199 1 None -2 3 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 341 3 1 2 5.1 c1ccc2c(CN3CCC(c4c[nH]c5ncccc45)CC3)cccc2c1 10.1016/j.bmcl.2006.03.094
122179055 128178 0 None -6760 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581751 128178 0 None -6760 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 501 5 2 5 5.0 CO[C@]12CC[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1C)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
21345767 87000 0 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 471 4 1 7 2.8 CN1CC[C@]23c4c5ccc(OC(=O)c6ccccc6)c4O[C@H]2[C@@H](OS(=O)(=O)O)CC[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
44414801 87000 0 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 471 4 1 7 2.8 CN1CC[C@]23c4c5ccc(OC(=O)c6ccccc6)c4O[C@H]2[C@@H](OS(=O)(=O)O)CC[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
CHEMBL213737 87000 0 None 1 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 471 4 1 7 2.8 CN1CC[C@]23c4c5ccc(OC(=O)c6ccccc6)c4O[C@H]2[C@@H](OS(=O)(=O)O)CC[C@H]3[C@H]1C5 10.1016/j.bmcl.2006.05.060
10178563 106281 0 None -4 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 391 4 0 2 4.9 CCN1C(=O)N(C2CCN(Cc3ccc4ccccc4c3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL283301 106281 0 None -4 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 391 4 0 2 4.9 CCN1C(=O)N(C2CCN(Cc3ccc4ccccc4c3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
44438914 98495 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 322 3 1 4 2.0 O=C1NCN(c2ccccc2)C12CCN(Cc1ccncc1)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL240897 98495 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 322 3 1 4 2.0 O=C1NCN(c2ccccc2)C12CCN(Cc1ccncc1)CC2 10.1016/j.bmcl.2007.01.069
44339707 117420 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 326 3 0 2 4.9 N#CC1(c2ccccc2)CCN(Cc2cccc3ccccc23)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL325774 117420 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 326 3 0 2 4.9 N#CC1(c2ccccc2)CCN(Cc2cccc3ccccc23)CC1 10.1016/s0960-894x(03)00665-6
25190575 186005 0 None 7 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 451 6 0 3 5.3 O=C1N(CC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL472677 186005 0 None 7 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 451 6 0 3 5.3 O=C1N(CC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
44394375 130462 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 461 6 1 3 4.5 O=S1(=O)NCc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL362160 130462 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 461 6 1 3 4.5 O=S1(=O)NCc2ccccc2N1C1CCN(CCC(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2004.08.001
54581497 69426 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
CHEMBL1783827 69426 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cellsDisplacement of [3H]N/OFQ from human recombinant NOP receptor expressed in CHO cells
ChEMBL 473 8 1 3 5.3 O=C(NCCCN1CCC(c2c(Cl)cccc2Cl)CC1)[C@@H]1CCCN1Cc1ccccc1 10.1016/j.bmc.2009.05.068
44391099 72713 0 None -7 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 429 6 2 6 4.2 Cc1ccc(Cl)c(OC(C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL183603 72713 0 None -7 2 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 429 6 2 6 4.2 Cc1ccc(Cl)c(OC(C)C(O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
12114743 175593 0 None -2 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 409 3 1 7 1.5 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
44414785 175593 0 None -2 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 409 3 1 7 1.5 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
CHEMBL437682 175593 0 None -2 2 Guinea pig 6.1 pKi = 6.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
ChEMBL 409 3 1 7 1.5 CC(=O)Oc1ccc2c3c1O[C@H]1[C@@H](OS(=O)(=O)O)CC[C@H]4[C@@H](C2)N(C)CC[C@]314 10.1016/j.bmcl.2006.05.060
25190572 186258 0 None 6 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 425 5 0 3 4.9 CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
CHEMBL474091 186258 0 None 6 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 425 5 0 3 4.9 CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O 10.1016/j.bmcl.2008.12.092
44430016 94289 0 None 11 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 1 3 4.8 COc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL233493 94289 0 None 11 4 Human 7.1 pKi = 7.1 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 373 5 1 3 4.8 COc1ccccc1C1(O)CCN(C(c2ccccc2)c2ccccc2)CC1 10.1016/j.bmcl.2007.03.062
10668903 41715 1 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 403 5 2 4 5.3 Nc1ccnc2ccc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)cc12 10.1021/jm0002073
CHEMBL143243 41715 1 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 403 5 2 4 5.3 Nc1ccnc2ccc(NC(=O)c3ccccc3COc3ccc(Cl)cc3)cc12 10.1021/jm0002073
44252837 151588 0 None -5 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 328 5 0 2 4.9 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3909426 151588 0 None -5 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 328 5 0 2 4.9 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C)CC1 nan
44339463 16117 0 None -346 2 Human 6.1 pKi = 6.1 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 419 3 1 2 6.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
CHEMBL111233 16117 0 None -346 2 Human 6.1 pKi = 6.1 Binding
Binding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cellsBinding affinity against human orphanin FQ receptor expressed in recombinant HEK 293 cells
ChEMBL 419 3 1 2 6.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/s0960-894x(03)00665-6
44339463 16117 0 None -346 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 419 3 1 2 6.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2004.08.032
CHEMBL111233 16117 0 None -346 2 Human 6.1 pKi = 6.1 Binding
Binding affinity for opioid receptor like 1 expressed in HEK293 cells Binding affinity for opioid receptor like 1 expressed in HEK293 cells
ChEMBL 419 3 1 2 6.0 OC1(c2ccc(Cl)c(C(F)(F)F)c2)CCN(Cc2ccc3ccccc3c2)CC1 10.1016/j.bmcl.2004.08.032
69616387 85788 0 None -5 3 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 295 2 0 3 4.0 CN(C)CC1CC2c3ccccc3Oc3ccccc3C2O1 10.1016/j.bmcl.2005.03.076
CHEMBL2113093 85788 0 None -5 3 Rat 7.1 pKi = 7.1 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 295 2 0 3 4.0 CN(C)CC1CC2c3ccccc3Oc3ccccc3C2O1 10.1016/j.bmcl.2005.03.076
10715725 126007 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 395 5 2 3 5.5 Cc1ccc(CCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1021/jm0002073
CHEMBL343424 126007 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.Ability to displace [3H]nociceptin ( 0.5 nM ) binding from Opioid receptor like 1 expressed in HeLa cells.
ChEMBL 395 5 2 3 5.5 Cc1ccc(CCc2ccccc2C(=O)Nc2ccc3nc(C)cc(N)c3c2)cc1 10.1021/jm0002073
118705901 119645 0 None -7943 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 490 4 2 5 4.0 O=C1CCC2=C([C@@H]3Oc4c(O)ccc5c4[C@@]34CCN(CC3CC3)[C@H](C5)[C@]4(O)C2)N1CC1CCCCC1 10.1016/j.bmc.2014.05.065
CHEMBL3309518 119645 0 None -7943 4 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting methodDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
ChEMBL 490 4 2 5 4.0 O=C1CCC2=C([C@@H]3Oc4c(O)ccc5c4[C@@]34CCN(CC3CC3)[C@H](C5)[C@]4(O)C2)N1CC1CCCCC1 10.1016/j.bmc.2014.05.065
44276782 106104 0 None 4 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 375 4 0 2 4.7 CCN1C(=O)N(C2CCN(C3CCC(C(C)C)CC3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
CHEMBL282195 106104 0 None 4 2 Human 7.1 pKi = 7.1 Binding
Binding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assayBinding affinity towards Nociceptin/orphanin FQ (N/OFQ) receptor from recombinant HEK293 cell membranes was determined using binding assay
ChEMBL 375 4 0 2 4.7 CCN1C(=O)N(C2CCN(C3CCC(C(C)C)CC3)CC2)[C@@H]2CCCC[C@H]21 10.1016/j.bmcl.2003.11.083
25190577 196490 0 None 26 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 493 6 0 3 6.5 O=C1N(CC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
CHEMBL515554 196490 0 None 26 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
ChEMBL 493 6 0 3 6.5 O=C1N(CC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 10.1016/j.bmcl.2008.12.092
25128943 134969 0 None 14 4 Human 7.1 pKi = 7.1 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 356 2 1 5 2.8 O=c1[nH]c2ncccc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL3665435 134969 0 None 14 4 Human 7.1 pKi = 7.1 Binding
ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.ORL-1 Receptor Binding Assay: ORL-1 Receptor Binding Assay Procedures: Membranes from recombinant HEK-293 cells expressing the human opioid receptor-like receptor (ORL-1) (Receptor Biology) were prepared by lysing cells in ice-cold hypotonic buffer (2.5 mM MgCl2, 50 mM HEPES, pH 7.4) (10mL/10 cm dish) followed by homogenization with a tissue grinder/Teflon pestle. Membranes were collected by centrifugation at 30,000×g for 15 min at 4° C. and pellets resuspended in hypotonic buffer to a final concentration 1-3mg/mL. Protein concentrations were determined using the BioRad protein assay reagent with bovine serum albumen as standard. Aliquots of the ORL-1 receptor membranes were stored at −80° C.
ChEMBL 356 2 1 5 2.8 O=c1[nH]c2ncccc2n(C2CCN(C3CCCCCCC3)CC2)c1=O nan
CHEMBL415583 219970 0 None - 1 Mouse 7.1 pKi = 7.1 Binding
Inhibition of [3H]NC-NH2 binding to mouse forebrain membranesInhibition of [3H]NC-NH2 binding to mouse forebrain membranes
ChEMBL None None None COc1ccc(C[C@H](NC(=O)CNC(=O)CNC(=O)[C@@H](N)Cc2ccccc2)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(N)=O)[C@@H](C)O)cc1 10.1021/jm010221v
44252837 151588 0 None -5 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 328 5 0 2 4.9 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3909426 151588 0 None -5 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 328 5 0 2 4.9 CN(C)C1(CC2CCCC2)CCC(c2ccccc2)(N(C)C)CC1 nan
44249045 110152 0 None 46 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 452 5 0 3 6.9 COc1cccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1021/jm9008218
CHEMBL3084636 110152 0 None 46 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 452 5 0 3 6.9 COc1cccc([C@@H]2C[C@@H]3CC[C@H](C2)N3C(c2ccccc2Cl)c2ccccc2Cl)n1 10.1021/jm9008218
44249046 110171 0 None 37 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 421 4 0 1 7.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccc1)C2 10.1021/jm9008218
CHEMBL3084668 110171 0 None 37 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation countingDisplacement of [125I]-Tyr14-N/OFQ from human NOP receptor expressed in CHO cells by Topcount microplate scintillation counting
ChEMBL 421 4 0 1 7.5 Clc1ccccc1C(c1ccccc1Cl)N1[C@H]2CC[C@@H]1C[C@H](c1ccccc1)C2 10.1021/jm9008218
44426838 92486 0 None 13 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 373 5 2 3 4.3 OCc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL228858 92486 0 None 13 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 373 5 2 3 4.3 OCc1ccccc1C(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
44426811 168527 0 None 14 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 337 6 1 2 5.1 CC(C)CCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
CHEMBL413791 168527 0 None 14 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranesDisplacement of [125I][14Tyr]nociceptin FQ from human cloned NOP receptor expressed in CHO cell membranes
ChEMBL 337 6 1 2 5.1 CC(C)CCC(c1ccccc1)N1CCC(O)(c2ccccc2)CC1 10.1016/j.bmcl.2007.03.061
76327874 110111 0 None 8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2cc(F)c(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
CHEMBL3084544 110111 0 None 8 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned ORL1 receptor expressed in CHO cells
ChEMBL 501 5 1 3 5.8 NC(=O)[C@@]1(c2cc(F)c(F)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2009.03.057
44438965 173641 0 None 87 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 431 4 1 3 4.9 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
CHEMBL428563 173641 0 None 87 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 431 4 1 3 4.9 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1Cl)CC2 10.1016/j.bmcl.2007.01.069
44438968 175779 0 None 38 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 425 4 1 3 4.8 Cc1ccccc1C(c1ccccc1C)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
CHEMBL439212 175779 0 None 38 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membraneDisplacement of [125I]nociceptin from human nociceptin receptor expressed in CHO cell membrane
ChEMBL 425 4 1 3 4.8 Cc1ccccc1C(c1ccccc1C)N1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1016/j.bmcl.2007.01.069
46179067 132577 0 None 177 4 Human 8.1 pKi = 8.1 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 451 3 1 5 5.5 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CCCCCCCCCC2)c1=O nan
CHEMBL3647960 132577 0 None 177 4 Human 8.1 pKi = 8.1 Binding
ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.ORL-1 Receptor Binding Assay: Radioligand binding assays (screening and dose-displacement) used 0.1 nM [3H]-nociceptin (NEN; 87.7 Ci/mmole) with 10-20 μg membrane protein in a final volume of 500 μL binding buffer (10 mM MgCl2, 1 mM EDTA, 5% DMSO, 50 mM HEPES, pH 7.4). Non-specific binding was determined in the presence of 10 nM unlabeled nociceptin (American Peptide Company). All reactions were performed in 96-deep well polypropylene plates for 1 h at about 25° C. Binding reactions were terminated by rapid filtration onto 96-well Unifilter GF/C filter plates (Packard) presoaked in 0.5% polyethylenimine (Sigma). Harvesting was performed using a 96-well tissue harvester (Packard) followed by three filtration washes with 5004 ice-cold binding buffer. Filter plates were subsequently dried at 50° C. for 2-3 hours. Fifty μL/well scintillation cocktail (BetaScint; Wallac) was added and plates were counted in a Packard Top-Count for 1 min/well.
ChEMBL 451 3 1 5 5.5 O=C(O)c1nc2ccccc2n([C@@H]2C[C@@H]3CC[C@H](C2)N3C2CCCCCCCCCC2)c1=O nan
52951942 90371 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 436 5 1 4 4.0 CNC(=O)[C@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
CHEMBL2204348 90371 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation countingDisplacement of [3H]nociceptin from human recombinant NOP receptor expressed in CHO cells after 60 mins by microbeta scintillation counting
ChEMBL 436 5 1 4 4.0 CNC(=O)[C@H](Cc1ccccc1Cl)CN1CCC2(CC1)OCCc1cc(F)sc12 10.1021/jm101487v
60154190 84373 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 398 5 0 4 3.6 CN(C)C(=O)C(Cc1ccccc1)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
CHEMBL2088040 84373 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counterDisplacement of [3H]Nociceptin from human recombinant NOP receptor expressed in CHO cells by scintillation counter
ChEMBL 398 5 0 4 3.6 CN(C)C(=O)C(Cc1ccccc1)CN1CCC2(CC1)OCCc1ccsc12 10.1021/jm201629q
11956918 127328 0 None -8 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 390 3 1 3 5.0 COc1ccc2[nH]c3c(c2c1)CCO[C@]31CC[C@](c2ccccc2)(N(C)C)CC1 10.1021/ml500117c
CHEMBL3325962 127328 0 None -8 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 390 3 1 3 5.0 COc1ccc2[nH]c3c(c2c1)CCO[C@]31CC[C@](c2ccccc2)(N(C)C)CC1 10.1021/ml500117c
CHEMBL3545583 127328 0 None -8 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 390 3 1 3 5.0 COc1ccc2[nH]c3c(c2c1)CCO[C@]31CC[C@](c2ccccc2)(N(C)C)CC1 10.1021/ml500117c
134578456 178916 0 None 32 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 423 5 1 4 5.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC[C@@H](O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4473045 178916 0 None 32 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 423 5 1 4 5.1 CC(C)[C@H]1CC[C@@H](N2CCC(n3cc(CN4CC[C@@H](O)C4)c4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
44451895 102582 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 528 10 0 7 5.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cccnc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL258781 102582 0 None 5 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 528 10 0 7 5.7 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4cccnc4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44430047 161529 0 None 64 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 408 5 2 3 4.5 NCc1ccccc1C1(O)CCN(C(c2cccc(F)c2)c2cccc(F)c2)CC1 10.1016/j.bmcl.2007.03.062
CHEMBL400036 161529 0 None 64 4 Human 8.0 pKi = 8.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 408 5 2 3 4.5 NCc1ccccc1C1(O)CCN(C(c2cccc(F)c2)c2cccc(F)c2)CC1 10.1016/j.bmcl.2007.03.062
129188443 176316 3 None 38 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
CHEMBL4435280 176316 3 None 38 4 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting methodDisplacement of [3H]N/OFQ from human NOP expressed in CHO cell membrane incubated for 60 mins by liquid scintillation counting method
ChEMBL 324 3 0 2 5.5 CC(C)[C@H]1CC[C@@H](N2CCC(n3ccc4ccccc43)CC2)CC1 10.1021/acs.jmedchem.9b02134
70682351 83438 0 None 24 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 423 5 0 3 3.4 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.021
CHEMBL2064158 83438 0 None 24 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assayDisplacement of [3H]N/OFQ from human recombinant ORL1 receptor expressed in HEK293 cells after 45 mins by scintillation proximity assay
ChEMBL 423 5 0 3 3.4 CN(C)C(=O)[C@@H]1Cc2ccccc2N1C(=O)CCN1CCC(c2ccc(F)cc2)CC1 10.1016/j.ejmech.2012.07.021
71624268 97236 0 None -2 3 Human 8.0 pKi = 8 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 326 3 0 2 4.0 CC(C1CCCCC1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
CHEMBL2387191 97236 0 None -2 3 Human 8.0 pKi = 8 Binding
Displacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cellsDisplacement of [3H] N/OFQ from human nociceptin receptor transfected in CHO cells
ChEMBL 326 3 0 2 4.0 CC(C1CCCCC1)N1CCC(N2C(=O)Cc3ccccc32)CC1 10.1016/j.bmcl.2013.03.101
44252536 160072 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 441 6 1 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)NCc2ccccc2)CC1 nan
CHEMBL3977883 160072 0 None -6 2 Human 7.1 pKi = 7.1 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 441 6 1 2 5.8 CN(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C(=O)NCc2ccccc2)CC1 nan
24776410 104722 0 None 40 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 372 1 1 2 4.4 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)NCc2cc(F)ccc23)CC1 10.1021/jm7009606
CHEMBL272592 104722 0 None 40 3 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 372 1 1 2 4.4 CC(C)(C)C1CCC(N2CCC3(CC2)C(=O)NCc2cc(F)ccc23)CC1 10.1021/jm7009606
44391031 71618 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 415 6 2 6 3.8 Cc1ccc(Cl)c(OC[C@@H](O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
CHEMBL182049 71618 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cellsBinding affinity towards human opioid receptor like 1 was determined by using [3H]nociceptin as radioligand expressed in Chinese hamster ovary (CHO) cells
ChEMBL 415 6 2 6 3.8 Cc1ccc(Cl)c(OC[C@@H](O)CN2CCC(n3c(O)nc4ccccc43)CC2)c1 10.1016/j.bmcl.2004.11.049
44575091 196168 0 None 7 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 438 4 1 3 5.7 OC1(c2cccnc2)C2CCC1CN(C(c1ccccc1Cl)c1ccccc1Cl)C2 10.1016/j.bmcl.2009.03.031
CHEMBL512982 196168 0 None 7 2 Human 6.0 pKi = 6.0 Binding
Displacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin from human cloned NOP receptor expressed in CHO cells
ChEMBL 438 4 1 3 5.7 OC1(c2cccnc2)C2CCC1CN(C(c1ccccc1Cl)c1ccccc1Cl)C2 10.1016/j.bmcl.2009.03.031
44451620 102687 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 519 10 1 9 3.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4nnn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL259262 102687 0 None 1 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 519 10 1 9 3.8 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4nnn[nH]4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44430014 94123 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 399 7 1 2 6.1 CCCCc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
CHEMBL233287 94123 0 None - 1 Human 5.0 pKi = 5.0 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membraneDisplacement of [125I][Tyr14]nociceptin FQ from human NOP receptor expressed in CHO cell membrane
ChEMBL 399 7 1 2 6.1 CCCCc1ccc(C2(O)CCN(C(c3ccccc3)c3ccccc3)CC2)cc1 10.1016/j.bmcl.2007.03.062
24776413 104786 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 328 4 1 2 3.7 CC(C)C1CCC(N2CCC(C(N)=O)(c3ccccc3)CC2)CC1 10.1021/jm7009606
CHEMBL272896 104786 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in HEK293 cells
ChEMBL 328 4 1 2 3.7 CC(C)C1CCC(N2CCC(C(N)=O)(c3ccccc3)CC2)CC1 10.1021/jm7009606
44253698 156249 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 473 7 0 7 4.4 CN(C)c1nc(N(C)C)nc(N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)n1 nan
CHEMBL3946171 156249 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 473 7 0 7 4.4 CN(C)c1nc(N(C)C)nc(N(C)C2(c3ccccc3)CCC(c3ccccc3)(N(C)C)CC2)n1 nan
10150001 15934 0 None 5 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 342 5 1 2 4.9 Cc1ccc([C@H](N)[C@@H]2CCN2C(c2ccccc2)c2ccccc2)cc1 10.1016/s0960-894x(02)00652-2
CHEMBL110126 15934 0 None 5 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 342 5 1 2 4.9 Cc1ccc([C@H](N)[C@@H]2CCN2C(c2ccccc2)c2ccccc2)cc1 10.1016/s0960-894x(02)00652-2
44337351 115471 0 None 77 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 314 5 1 2 4.6 CCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
CHEMBL320804 115471 0 None 77 4 Human 7.0 pKi = 7.0 Binding
Binding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pMBinding affinity at human ORL1 receptor was determined by using [125I]nociceptin radioligand in Chinese hamster ovary (CHO) cell membranes at a concentration of 23 pM
ChEMBL 314 5 1 2 4.6 CCC(c1ccccc1)N1CC[C@H]1[C@H](N)c1cccc(Cl)c1 10.1016/s0960-894x(02)00652-2
44413314 86729 0 None 5 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 397 4 1 4 4.7 OCCn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2cccnc21 10.1016/j.bmcl.2006.03.094
CHEMBL212630 86729 0 None 5 2 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 397 4 1 4 4.7 OCCn1cc(C2CCN(C3Cc4cccc5cccc3c45)CC2)c2cccnc21 10.1016/j.bmcl.2006.03.094
44252100 155915 0 None -10 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 403 5 0 4 4.7 CN(C)C1(C(=O)c2cc3ccccc3n2C)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3943372 155915 0 None -10 2 Human 6.0 pKi = 6.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 403 5 0 4 4.7 CN(C)C1(C(=O)c2cc3ccccc3n2C)CCC(c2ccccc2)(N(C)C)CC1 nan
44252537 160619 0 None -2 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 5 1 2 4.6 CCNC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
CHEMBL3982674 160619 0 None -2 2 Human 7.0 pKi = 7.0 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 379 5 1 2 4.6 CCNC(=O)N(C)C1(c2ccccc2)CCC(c2ccccc2)(N(C)C)CC1 nan
44451647 162969 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 0 9 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncn(C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
CHEMBL406409 162969 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO cellsDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO cells
ChEMBL 532 10 0 9 4.4 COc1ccc(C)c(OC(CCN2CCC(n3c(=O)n(Cc4ncn(C)n4)c4ccccc43)CC2)C(C)C)c1 10.1016/j.bmc.2008.01.005
44394529 73996 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 433 4 1 3 4.2 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc(-c3ccccc3)cc2)CC1 10.1016/j.bmcl.2004.08.001
CHEMBL187907 73996 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibition of [3H]nociceptin binding to human Opioid receptor like 1Inhibition of [3H]nociceptin binding to human Opioid receptor like 1
ChEMBL 433 4 1 3 4.2 O=S1(=O)NCc2ccccc2N1C1CCN(Cc2ccc(-c3ccccc3)cc2)CC1 10.1016/j.bmcl.2004.08.001
44402676 142793 0 None -2 3 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 449 2 0 4 6.7 Cc1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
CHEMBL373174 142793 0 None -2 3 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligandIn vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
ChEMBL 449 2 0 4 6.7 Cc1ccc2on(C[C@@H]3C[C@H]4c5ccccc5Oc5ccc(Br)cc5[C@H]4O3)c2c1 10.1016/j.bmcl.2005.03.076
122179050 128172 0 None -1230 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 485 5 2 5 4.5 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
CHEMBL3581740 128172 0 None -1230 3 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting methodDisplacement of [3H]nociceptin from human NOP receptor expressed in HEK293 cell membranes incubated for 1 hr by beta counting method
ChEMBL 485 5 2 5 4.5 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 10.1021/acs.jmedchem.5b00130
44328202 214436 0 None -1230 3 Human 7.0 pKi = 7.0 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 385 5 4 9 1.3 CC(C)c1ccccc1Nc1ncnc2c1ncn2[C@H]1OC(CO)C(O)C1O nan
CHEMBL95302 214436 0 None -1230 3 Human 7.0 pKi = 7.0 Binding
Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assay: As Alt et al., 2002. Membranes (20 μg) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 μM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 385 5 4 9 1.3 CC(C)c1ccccc1Nc1ncnc2c1ncn2[C@H]1OC(CO)C(O)C1O nan
122179050 128172 0 None -1230 3 Human 7.0 pKi = 7.0 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 485 5 2 5 4.5 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
CHEMBL3581740 128172 0 None -1230 3 Human 7.0 pKi = 7.0 Binding
Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.Ligand Binding Assays: As Alt et al., 2002. Membranes (20 ug) are incubated in 50 mM Tris-HCl, pH 7.4 with [3H]diprenorphine or [3H]nociceptin in the absence or presence of varying concentrations of test compounds for 60 min in a shaking water bath at 25° C. Nonspecific binding is measured using 10 uM naloxone (MOR, DOR, KOR) or N/OFQ (NOP). Samples are filtered through GF/C glass-fiber filtermats mounted on a Brandel cell harvester and rinsed four times with 4° C. 50 mM Tris-HCl, pH 7.4 buffer. Filtermats are dried and 0.1 ml EcoLume scintillation cocktail added to each sample area to soak the filter. Each filtermat in a heat-sealed bag, is counted in a Wallac 1450 MicroBeta Liquid Scintillation and Luminescence Counter.
ChEMBL 485 5 2 5 4.5 CO[C@]12C=C[C@@]3(C[C@]1(C)[C@H](O)c1ccccc1)[C@H]1Cc4ccc(O)c5c4[C@@]3(CCN1CC1CC1)[C@H]2O5 nan
11848225 7664 52 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
8866 7664 52 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL2364605 7664 52 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3545616 7664 52 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
CHEMBL3962932 7664 52 None -4 7 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assayDisplacement of [3H]nociceptin from human NOP receptor expressed in CHO-K1 cells by scintillation proximity assay
ChEMBL 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 10.1021/ml500117c
44413232 148313 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 443 7 1 4 5.2 CN(C)C[C@@H](O)Cn1cc(C2CCN(CC3CCCCCCC3)CC2)c2cc(F)ccc21 10.1016/j.bmcl.2006.03.094
CHEMBL384681 148313 0 None 1 3 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cellsDisplacement of [125I]Tyr14-nociceptin from ORL1 receptor expressed in HEK293 cells
ChEMBL 443 7 1 4 5.2 CN(C)C[C@@H](O)Cn1cc(C2CCN(CC3CCCCCCC3)CC2)c2cc(F)ccc21 10.1016/j.bmcl.2006.03.094
118718287 122103 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 576 7 1 4 7.2 CC(=O)NC[C@]1(c2ccc(N3CCCCC3)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
CHEMBL3349271 122103 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cellsDisplacement of [125I][Tyr14]nociceptin FQ from human cloned nociceptin receptor expressed in CHO cells
ChEMBL 576 7 1 4 7.2 CC(=O)NC[C@]1(c2ccc(N3CCCCC3)cn2)C[C@@H]2CC[C@H](C1)N2C(c1ccccc1Cl)c1ccccc1Cl 10.1016/j.bmcl.2008.10.088
46917150 159818 0 None 1 2 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 429 5 0 4 5.2 CN(C)C1(c2ccccc2)CCC(C(=O)c2cc3ccccc3n2C)(N2CCCC2)CC1 nan
CHEMBL3975775 159818 0 None 1 2 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 429 5 0 4 5.2 CN(C)C1(c2ccccc2)CCC(C(=O)c2cc3ccccc3n2C)(N2CCCC2)CC1 nan
44252388 157943 0 None -2 2 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 375 4 1 2 5.3 Cc1c(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccccc12 nan
CHEMBL3959625 157943 0 None -2 2 Human 6.0 pKi = 6 Binding
Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).Binding Assay: The compounds were examined with membranes of recombinant CHO-ORL 1 cells in a receptor binding assay with 3H-nociceptin/orphanin FQ. This test system was conducted in accordance with the method outlined by Ardati et al. (Mol. Pharmacol., 51, 1997, pp. 816-824). The concentration of 3H-nociceptin/orphanin FQ amounted to 0.5 nM in these tests. The binding assays were conducted in each case on 20 ug of membrane protein per 200ul of preparation in 50 mM of HEPES, pH 7.4, 10 nM of MgCl2 and 1 mM of EDTA. The binding to the ORL 1-receptor was determined using 1 mg of WGA-SPA beads (Amersham-Pharmacia, Freiburg) in each case by incubating the preparation for one hour at RT and then conducting measurements in the Trilux scintillation counter (Wallac, Finland).
ChEMBL 375 4 1 2 5.3 Cc1c(C2(N(C)C)CCC(c3ccccc3)(N(C)C)CC2)[nH]c2ccccc12 nan
16131448 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
16131448 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
1681 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
1688 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
44361543 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
56947112 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8849681
CHEMBL396460 9624 28 None 1 6 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1685 10701 0 None - 1 Human 10.7 pKd None 10.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15509719
23383556 186136 0 UNDEFINED 25 4 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 488 9 1 4 5.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL473700 186136 0 UNDEFINED 25 4 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 488 9 1 4 5.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190623 196492 0 UNDEFINED 204 4 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 502 8 1 4 5.6 CC(C)CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL515575 196492 0 UNDEFINED 204 4 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 502 8 1 4 5.6 CC(C)CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190602 186003 0 UNDEFINED 50 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 486 8 1 4 4.6 O=C1N(CCNCC2CC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
CHEMBL472669 186003 0 UNDEFINED 50 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 486 8 1 4 4.6 O=C1N(CCNCC2CC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
25190619 186085 0 UNDEFINED 123 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 488 7 1 4 5.2 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL473279 186085 0 UNDEFINED 123 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 488 7 1 4 5.2 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190622 186265 0 UNDEFINED 131 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 488 8 1 4 5.3 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL474096 186265 0 UNDEFINED 131 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 488 8 1 4 5.3 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190605 187271 0 UNDEFINED 15 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 488 8 1 4 4.9 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL475310 187271 0 UNDEFINED 15 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 488 8 1 4 4.9 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190603 196595 0 UNDEFINED 57 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 486 7 1 4 4.8 O=C1N(CCNC2CCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
CHEMBL516389 196595 0 UNDEFINED 57 4 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 486 7 1 4 4.8 O=C1N(CCNC2CCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
25190629 185894 0 UNDEFINED 41 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 522 8 1 4 6.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)ccc43)CC2)C1=O None
CHEMBL471880 185894 0 UNDEFINED 41 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 522 8 1 4 6.0 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)ccc43)CC2)C1=O None
25190604 196369 0 UNDEFINED 21 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 474 8 1 4 4.6 CCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL514662 196369 0 UNDEFINED 21 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 474 8 1 4 4.6 CCCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190625 185896 0 UNDEFINED 37 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 528 7 1 4 6.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CCCCC2)CN3c2ccccc2)c2ccccc21 None
CHEMBL471882 185896 0 UNDEFINED 37 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 528 7 1 4 6.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CCCCC2)CN3c2ccccc2)c2ccccc21 None
25190601 187619 0 UNDEFINED 56 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 474 7 1 4 4.6 CC(C)NCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL475707 187619 0 UNDEFINED 56 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 474 7 1 4 4.6 CC(C)NCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190600 196434 0 UNDEFINED 75 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 460 7 1 4 4.2 CCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL515142 196434 0 UNDEFINED 75 4 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 460 7 1 4 4.2 CCNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190618 186084 0 UNDEFINED 218 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 486 7 1 4 4.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CC2)CN3c2ccccc2)c2ccccc21 None
CHEMBL473278 186084 0 UNDEFINED 218 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 486 7 1 4 4.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCC2CC2)CN3c2ccccc2)c2ccccc21 None
25190599 196802 0 UNDEFINED 85 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 446 6 1 4 3.9 CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL517167 196802 0 UNDEFINED 85 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 446 6 1 4 3.9 CNCCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190616 187079 0 UNDEFINED 223 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 472 7 1 4 4.7 C=CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL475094 187079 0 UNDEFINED 223 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 472 7 1 4 4.7 C=CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190614 196345 0 UNDEFINED 37 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 514 6 1 4 5.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCCC2)CN3c2ccccc2)c2ccccc21 None
CHEMBL514463 196345 0 UNDEFINED 37 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 514 6 1 4 5.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCCC2)CN3c2ccccc2)c2ccccc21 None
25190613 196426 0 UNDEFINED 54 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 500 6 1 4 5.5 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCC2)CN3c2ccccc2)c2ccccc21 None
CHEMBL515091 196426 0 UNDEFINED 54 4 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 500 6 1 4 5.5 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCCC2)CN3c2ccccc2)c2ccccc21 None
25190615 186080 0 UNDEFINED 42 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 474 7 1 4 4.9 CCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL473272 186080 0 UNDEFINED 42 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 474 7 1 4 4.9 CCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190606 186137 0 UNDEFINED 56 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 488 8 0 4 5.0 CCN(CC)CCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
CHEMBL473701 186137 0 UNDEFINED 56 4 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 488 8 0 4 5.0 CCN(CC)CCN1CN(c2ccccc2)C2(CCN(Cc3c(Cl)cccc3Cl)CC2)C1=O None
25190624 97906 0 UNDEFINED 37 4 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 389 2 1 3 4.2 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccccc21 None
CHEMBL239822 97906 0 UNDEFINED 37 4 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 389 2 1 3 4.2 CC1(C)CCC(N2CCC3(CC2)C(=O)NCN3c2ccccc2)c2ccccc21 None
25190621 186158 0 UNDEFINED 48 4 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 486 5 0 4 5.0 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCN2CCCC2)CN3c2ccccc2)c2ccccc21 None
CHEMBL473898 186158 0 UNDEFINED 48 4 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 486 5 0 4 5.0 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCN2CCCC2)CN3c2ccccc2)c2ccccc21 None
25190612 196350 0 UNDEFINED 47 4 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 474 6 1 4 4.9 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL514489 196350 0 UNDEFINED 47 4 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 474 6 1 4 4.9 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190617 186260 0 UNDEFINED 29 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 486 6 1 4 5.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCC2)CN3c2ccccc2)c2ccccc21 None
CHEMBL474092 186260 0 UNDEFINED 29 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 486 6 1 4 5.1 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNC2CCC2)CN3c2ccccc2)c2ccccc21 None
25190611 186756 0 UNDEFINED 23 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 460 6 1 4 4.6 CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL474687 186756 0 UNDEFINED 23 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 460 6 1 4 4.6 CCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190609 186405 0 UNDEFINED 34 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 433 4 1 4 3.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCO)CN3c2ccccc2)c2ccccc21 None
CHEMBL474283 186405 0 UNDEFINED 34 4 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 433 4 1 4 3.9 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCO)CN3c2ccccc2)c2ccccc21 None
25190628 195950 0 UNDEFINED 7 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4c(Cl)cccc43)CC2)C1=O None
CHEMBL511161 195950 0 UNDEFINED 7 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4c(Cl)cccc43)CC2)C1=O None
None 223084 0 UNDEFINED -48977 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 341 2 2 5 1.5 C1CC1CN2CCC34C5C(=O)CCC3(C2CC6=C4C(=C(C=C6)O)O5)O None
None 224251 0 UNDEFINED -245470 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 550 4 5 7 2.2 CC1=CC=C(C=C1)C(=O)NC2CCC3(C4CC5=C6C3(C2OC6=C(C=C5)O)CCN4CC7CC7)O.C(=O)(C(=O)O)O None
None 224253 0 UNDEFINED -1071519 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 614 4 5 7 2.7 C1CC1CN2CCC34C5C(CCC3(C2CC6=C4C(=C(C=C6)O)O5)O)NC(=O)C7=CC=C(C=C7)Br.C(=O)(C(=O)O)O None
None 224254 0 UNDEFINED -2691 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 662 4 5 7 2.5 C1CC1CN2CCC34C5C(CCC3(C2CC6=C4C(=C(C=C6)O)O5)O)NC(=O)C7=CC=C(C=C7)I.C(=O)(C(=O)O)O None
None 224255 0 UNDEFINED -2691 4 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 592 4 5 7 3.2 CC(C)(C)C1=CC=C(C=C1)C(=O)NC2CCC3(C4CC5=C6C3(C2OC6=C(C=C5)O)CCN4CC7CC7)O.C(=O)(C(=O)O)O None
25190592 194992 0 UNDEFINED 56 4 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 592 9 0 4 7.3 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O)C(C)C None
CHEMBL499169 194992 0 UNDEFINED 56 4 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 592 9 0 4 7.3 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O)C(C)C None
25190630 185924 0 UNDEFINED 12 4 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 556 8 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)c(Cl)cc43)CC2)C1=O None
CHEMBL472086 185924 0 UNDEFINED 12 4 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 556 8 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4cc(Cl)c(Cl)cc43)CC2)C1=O None
25190627 196569 0 UNDEFINED -1 4 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4ccc(Cl)cc43)CC2)C1=O None
CHEMBL516187 196569 0 UNDEFINED -1 4 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 494 8 1 4 5.2 CCCCNCCN1CN(c2ccccc2)C2(CCN(C3CCCc4ccc(Cl)cc43)CC2)C1=O None
25190583 186154 0 UNDEFINED 25 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 509 6 1 4 5.2 O=C1N(CCO)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL473884 186154 0 UNDEFINED 25 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 509 6 1 4 5.2 O=C1N(CCO)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190582 196555 0 UNDEFINED 34 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 537 6 0 5 5.4 COC(=O)CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL516077 196555 0 UNDEFINED 34 4 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 537 6 0 5 5.4 COC(=O)CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190610 186580 0 UNDEFINED 16 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 446 5 1 4 4.2 CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL474485 186580 0 UNDEFINED 16 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 446 5 1 4 4.2 CNCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190586 187082 0 UNDEFINED 239 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 536 8 1 4 5.8 CCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL475096 187082 0 UNDEFINED 239 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 536 8 1 4 5.8 CCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190593 196517 0 UNDEFINED 77 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 564 10 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL515829 196517 0 UNDEFINED 77 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 564 10 1 4 6.6 CCCCNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
9937777 182136 0 UNDEFINED 114 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 562 7 0 4 6.3 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL457451 182136 0 UNDEFINED 114 4 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 562 7 0 4 6.3 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190598 98064 0 UNDEFINED 12 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 389 3 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
CHEMBL240215 98064 0 UNDEFINED 12 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 389 3 1 3 3.9 O=C1NCN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
10323169 186161 0 UNDEFINED 6 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 486 6 0 4 4.7 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
CHEMBL473904 186161 0 UNDEFINED 6 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 486 6 0 4 4.7 O=C1N(CCN2CCCC2)CN(c2ccccc2)C12CCN(Cc1c(Cl)cccc1Cl)CC2 None
25190587 197548 0 UNDEFINED 181 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 550 8 1 4 6.2 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL518325 197548 0 UNDEFINED 181 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 550 8 1 4 6.2 CC(C)NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190594 182040 0 UNDEFINED 87 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 564 9 1 4 6.5 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL457244 182040 0 UNDEFINED 87 4 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 564 9 1 4 6.5 CC(C)CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190579 196412 0 UNDEFINED 3 4 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 0 3 5.1 C=CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL514965 196412 0 UNDEFINED 3 4 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 437 6 0 3 5.1 C=CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
15541261 98351 0 UNDEFINED 6 4 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 397 4 1 3 4.2 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
CHEMBL240657 98351 0 UNDEFINED 6 4 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 397 4 1 3 4.2 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
25190578 186783 0 UNDEFINED 5 4 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 435 5 0 3 4.6 C#CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL474708 186783 0 UNDEFINED 5 4 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 435 5 0 3 4.6 C#CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
25190584 196545 0 UNDEFINED 27 4 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 523 7 0 4 5.9 COCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL516024 196545 0 UNDEFINED 27 4 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 523 7 0 4 5.9 COCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190596 184468 0 UNDEFINED 19 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 576 8 0 4 6.7 O=C1N(CCCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL464191 184468 0 UNDEFINED 19 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 576 8 0 4 6.7 O=C1N(CCCN2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190590 183574 0 UNDEFINED 91 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 536 7 0 4 5.8 CN(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL460636 183574 0 UNDEFINED 91 4 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 536 7 0 4 5.8 CN(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190626 195951 0 UNDEFINED 38 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 522 7 1 4 5.7 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCc2ccccc2)CN3c2ccccc2)c2ccccc21 None
CHEMBL511162 195951 0 UNDEFINED 38 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 522 7 1 4 5.7 CC1(C)CCC(N2CCC3(CC2)C(=O)N(CCNCc2ccccc2)CN3c2ccccc2)c2ccccc21 None
25190591 196858 0 UNDEFINED 263 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 548 8 1 4 6.0 O=C1N(CCNC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL517265 196858 0 UNDEFINED 263 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 548 8 1 4 6.0 O=C1N(CCNC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190595 195133 0 UNDEFINED 70 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 604 9 1 4 7.4 O=C1N(CCNCC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL501088 195133 0 UNDEFINED 70 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 604 9 1 4 7.4 O=C1N(CCNCC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
10158555 195884 0 UNDEFINED 4 4 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 411 4 0 3 4.5 CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL510201 195884 0 UNDEFINED 4 4 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 411 4 0 3 4.5 CN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
25190573 187268 0 UNDEFINED 39 4 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 439 6 0 3 5.3 CCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL475308 187268 0 UNDEFINED 39 4 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 439 6 0 3 5.3 CCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
9806799 186053 0 UNDEFINED 141 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 522 7 1 4 5.4 CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL473068 186053 0 UNDEFINED 141 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 522 7 1 4 5.4 CNCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
None 224252 0 UNDEFINED -9 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 604 4 5 7 2.9 C1CC1CN2CCC34C5C(CCC3(C2CC6=C4C(=C(C=C6)O)O5)O)NC(=O)C7=CC=C(C=C7)C(F)(F)F.C(=O)(C(=O)O)O None
25190608 196021 0 UNDEFINED 3 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 445 4 0 4 4.5 CC(=O)CN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL511649 196021 0 UNDEFINED 3 4 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 445 4 0 4 4.5 CC(=O)CN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
25190585 186029 0 UNDEFINED -1 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 508 6 1 4 5.2 NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL472867 186029 0 UNDEFINED -1 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 508 6 1 4 5.2 NCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190580 187417 0 UNDEFINED 204 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 521 7 0 3 7.0 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL475496 187417 0 UNDEFINED 204 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 521 7 0 3 7.0 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190589 195923 0 UNDEFINED 44 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 590 8 1 4 7.1 O=C1N(CCNC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL510745 195923 0 UNDEFINED 44 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 590 8 1 4 7.1 O=C1N(CCNC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190607 185813 0 UNDEFINED 26 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 431 4 0 3 5.4 CCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
CHEMBL471262 185813 0 UNDEFINED 26 4 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 431 4 0 3 5.4 CCCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O None
1222 8445 49 UNDEFINED -194 32 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 8445 49 UNDEFINED -194 32 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 8445 49 UNDEFINED -194 32 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 8445 49 UNDEFINED -194 32 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 8445 49 UNDEFINED -194 32 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
25190576 196530 0 UNDEFINED 35 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 465 6 0 3 5.7 O=C1N(CC2CCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
CHEMBL515901 196530 0 UNDEFINED 35 3 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 465 6 0 3 5.7 O=C1N(CC2CCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
25190581 187420 0 UNDEFINED 199 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 535 7 0 3 7.3 CC(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
CHEMBL475497 187420 0 UNDEFINED 199 4 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 535 7 0 3 7.3 CC(C)CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3Cl)c3ccccc3Cl)CC2)C1=O None
25190574 196364 0 UNDEFINED 13 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 453 7 0 3 5.7 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL514606 196364 0 UNDEFINED 13 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 453 7 0 3 5.7 CCCCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
1222 8445 49 None -194 32 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 8445 49 None -194 32 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 8445 49 None -194 32 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 8445 49 None -194 32 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 8445 49 None -194 32 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]nociceptin from human NOP expressed in CHO cellsDisplacement of [125I]nociceptin from human NOP expressed in CHO cells
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
25190620 186086 0 UNDEFINED 12 4 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 516 7 0 4 6.1 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O)C(C)C None
CHEMBL473280 186086 0 UNDEFINED 12 4 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 516 7 0 4 6.1 CC(C)N(CCN1CN(c2ccccc2)C2(CCN(C3CCC(C)(C)c4ccccc43)CC2)C1=O)C(C)C None
9934232 98583 0 UNDEFINED 407 4 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL241272 98583 0 UNDEFINED 407 4 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 465 4 1 3 5.5 O=C1NCN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
10252647 186004 0 UNDEFINED 8 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 439 5 0 3 5.3 CC(C)N1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL472676 186004 0 UNDEFINED 8 4 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 439 5 0 3 5.3 CC(C)N1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
3033050 222781 0 None -5 9 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysisDisplacement of [3H]-N/OFQ from human nociceptin opioid receptor transfected in CHO cells after 60 mins by beta-plate liquid scintillation counting analysis
Drug Central 467 4 2 5 4.4 CC(C)(C)C(C)(C1CC23CCC1(C4C25CCN(C3CC6=C5C(=C(C=C6)O)O4)CC7CC7)OC)O None
1627 9372 20 None -5 13 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
Drug Central 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O None
1845 9372 20 None -5 13 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
Drug Central 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O None
5288826 9372 20 None -5 13 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
Drug Central 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O None
CHEMBL70 9372 20 None -5 13 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
Drug Central 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O None
DB00295 9372 20 None -5 13 Guinea pig 8.1 pKi = 8.1 Binding
Displacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brainDisplacement of radiolabeled NalBzOH from kappa3 opioid receptor in Hartley guinea pig brain
Drug Central 285 0 2 4 1.2 O[C@H]1C=C[C@@H]2[C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)C)ccc1O None
25190597 184469 0 UNDEFINED 35 4 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 576 7 0 4 6.7 O=C1N(CCN2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL464192 184469 0 UNDEFINED 35 4 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 576 7 0 4 6.7 O=C1N(CCN2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190588 181581 0 UNDEFINED 28 4 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 576 8 1 4 6.8 O=C1N(CCNC2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
CHEMBL456225 181581 0 UNDEFINED 28 4 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 576 8 1 4 6.8 O=C1N(CCNC2CCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1Cl)c1ccccc1Cl)CC2 None
25190575 186005 0 UNDEFINED 7 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 451 6 0 3 5.3 O=C1N(CC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
CHEMBL472677 186005 0 UNDEFINED 7 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 451 6 0 3 5.3 O=C1N(CC2CC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
25190572 186258 0 UNDEFINED 6 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 425 5 0 3 4.9 CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
CHEMBL474091 186258 0 UNDEFINED 6 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 425 5 0 3 4.9 CCN1CN(c2ccccc2)C2(CCN(C(c3ccccc3)c3ccccc3)CC2)C1=O None
25190577 196490 0 UNDEFINED 26 3 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 493 6 0 3 6.5 O=C1N(CC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
CHEMBL515554 196490 0 UNDEFINED 26 3 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 493 6 0 3 6.5 O=C1N(CC2CCCCC2)CN(c2ccccc2)C12CCN(C(c1ccccc1)c1ccccc1)CC2 None
12419 9252 29 None 12 3 Human 10.1 pKi = 10.1 Binding
Binding affinity for hNOPBinding affinity for hNOP
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
24800108 9252 29 None 12 3 Human 10.1 pKi = 10.1 Binding
Binding affinity for hNOPBinding affinity for hNOP
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
CHEMBL481512 9252 29 None 12 3 Human 10.1 pKi = 10.1 Binding
Binding affinity for hNOPBinding affinity for hNOP
Guide to Pharmacology 408 3 1 4 5.6 CC1(CCCCCCC1)N2CCC(CC2)N3C(=NC4=C3C=CC=C4)[C@H]5CNCCC5 19125610
49843739 10440 0 None 6 3 Human 7.9 pKi = 7.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 386 2 0 2 5.0 O=C1Cc2c(N1C1CCN(CC1)C1CCC3c4c1cccc4CCC3)cccc2 19773529
8867 10440 0 None 6 3 Human 7.9 pKi = 7.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 386 2 0 2 5.0 O=C1Cc2c(N1C1CCN(CC1)C1CCC3c4c1cccc4CCC3)cccc2 19773529
CHEMBL3262554 10440 0 None 6 3 Human 7.9 pKi = 7.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 386 2 0 2 5.0 O=C1Cc2c(N1C1CCN(CC1)C1CCC3c4c1cccc4CCC3)cccc2 19773529
11597355 10327 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 439 4 1 4 5.4 Clc1ccccc1C(c1ccccc1Cl)N1[C@@H]2CC[C@H]1CC(C2)(O)c1ncccn1 20006596
8869 10327 0 None - 1 Human 8.3 pKi = 8.3 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 439 4 1 4 5.4 Clc1ccccc1C(c1ccccc1Cl)N1[C@@H]2CC[C@H]1CC(C2)(O)c1ncccn1 20006596
8870 7296 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 437 6 4 5 3.1 Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CCC(CC1)c1cccc(c1)O 25635572
91938095 7296 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 437 6 4 5 3.1 Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CCC(CC1)c1cccc(c1)O 25635572
CHEMBL3613442 7296 0 None -1 4 Human 8.8 pKi = 8.8 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 437 6 4 5 3.1 Oc1ccc2c(c1)CN[C@H](C2)C(=O)N[C@@H](C(C)C)CN1CCC(CC1)c1cccc(c1)O 25635572
8868 10320 31 None -3 6 Mouse 8.9 pKi = 8.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
9887077 10320 31 None -3 6 Mouse 8.9 pKi = 8.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
CHEMBL513136 10320 31 None -3 6 Mouse 8.9 pKi = 8.9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
11848225 7664 52 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8866 7664 52 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL2364605 7664 52 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3545616 7664 52 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3962932 7664 52 None 2 7 Rat 9.0 pKi = 9 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
11848225 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8866 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL2364605 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3545616 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
CHEMBL3962932 7664 52 None -4 7 Human 9.1 pKi = 9.1 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 378 2 1 2 5.1 Fc1ccc2c(c1)c1CCOC3(c1[nH]2)CCC(CC3)(N(C)C)c1ccccc1 24713140
8868 10320 31 None -1 6 Rat 9.4 pKi = 9.4 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
9887077 10320 31 None -1 6 Rat 9.4 pKi = 9.4 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
CHEMBL513136 10320 31 None -1 6 Rat 9.4 pKi = 9.4 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
8868 10320 31 None 1 6 Human 9.5 pKi = 9.5 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
9887077 10320 31 None 1 6 Human 9.5 pKi = 9.5 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
CHEMBL513136 10320 31 None 1 6 Human 9.5 pKi = 9.5 Binding
Radioligand binding assayRadioligand binding assay
Guide to Pharmacology 397 4 1 2 5.9 Cc1ccccc1C(c1ccccc1C)N1C2CCC1CC(C2)(O)c1ccccc1 18492950
52914971 9186 37 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 24678969
52914971 9186 37 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 31937563
9462 9186 37 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 24678969
9462 9186 37 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 31937563
CHEMBL3304244 9186 37 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 24678969
CHEMBL3304244 9186 37 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 31937563
DB16048 9186 37 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 24678969
DB16048 9186 37 None - 1 Human 10.0 pKi = 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 480 4 1 7 4.4 OCc1cccnc1n1nc(c(c1)CN1CCC2(CC1)OCC(c1c2sc(c1)Cl)(F)F)C 31937563
16131448 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
16131448 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
16131448 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1681 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1681 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1681 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1688 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1688 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1688 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
44361543 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
44361543 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
44361543 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
56947112 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
56947112 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
56947112 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
CHEMBL396460 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
CHEMBL396460 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
CHEMBL396460 9624 28 None 1 6 Human 10.1 pKi = 10.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9413015
1694 10700 0 None - 1 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
25081457 10700 0 None - 1 Human 10.2 pKi = 10.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
1682 9627 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
1682 9627 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1682 9627 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1682 9627 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
6324645 9627 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
6324645 9627 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
6324645 9627 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
6324645 9627 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
CHEMBL384755 9627 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10369464
CHEMBL384755 9627 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
CHEMBL384755 9627 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
CHEMBL384755 9627 18 None 3 2 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9191955
8865 10012 0 None - 1 Human 10.3 pKi = 10.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 24903280
1686 9847 0 None - 1 Human 11.1 pKi = 11.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12070757
1686 9847 0 None - 1 Human 11.1 pKi = 11.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15743186
50922685 7521 0 None -5 4 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 481 6 2 5 4.8 CO[C@]12CC[C@]3(C[C@@H]1[C@@](C(CC)(C)C)(O)C)[C@@]14[C@H]2Oc2c4c(C[C@H]3N(CC1)CC1CC1)ccc2O 21177476
9294 7521 0 None -5 4 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 481 6 2 5 4.8 CO[C@]12CC[C@]3(C[C@@H]1[C@@](C(CC)(C)C)(O)C)[C@@]14[C@H]2Oc2c4c(C[C@H]3N(CC1)CC1CC1)ccc2O 21177476
1691 8888 23 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10940356
5311194 8888 23 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10940356
CHEMBL357076 8888 23 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 399 5 1 5 4.0 OC[C@@H]1CN(CC[C@H]1n1c(=O)n(c2c1cccc2)CC)CC1CCCCCCC1 10940356
1679 7056 24 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1679 7056 24 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
9963005 7056 24 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
9963005 7056 24 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL437723 7056 24 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
CHEMBL437723 7056 24 None 1 2 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
132427684 7297 0 None - 1 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 5 1 3 3.9 CNC(=O)CC1C(=O)N(c2c1cccc2)C1CCN(CC1)[C@@H]1CC[C@@H](CC1)C(C)C 29232769
9747 7297 0 None - 1 Human 9.0 pKi = 9.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 5 1 3 3.9 CNC(=O)CC1C(=O)N(c2c1cccc2)C1CCN(CC1)[C@@H]1CC[C@@H](CC1)C(C)C 29232769
10047612 10302 15 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
10047612 10302 15 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
1693 10302 15 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
1693 10302 15 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
CHEMBL559569 10302 15 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 14593080
CHEMBL559569 10302 15 None 173 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 417 3 1 2 6.2 O[C@H]1C[C@H](CCc2c1cccc2C)CN1CCC(CC1)c1c(Cl)cccc1Cl 17329552
1684 10135 21 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10758169
1684 10135 21 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
9844019 10135 21 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10758169
9844019 10135 21 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
CHEMBL2088034 10135 21 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 10758169
CHEMBL2088034 10135 21 None - 1 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 401 2 1 3 4.4 O=C1NCN(C21CCN(CC2)[C@H]1CC[C@H]2c3c1cccc3CCC2)c1ccccc1 11006485
1680 7057 0 None 2 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1680 7057 0 None 2 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
15512229 10158 0 None 1 7 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10476866
8864 10158 0 None 1 7 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10476866
CHEMBL355202 10158 0 None 1 7 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 383 2 1 3 3.9 O=C1NCN(C21CCN(CC2)[C@@H]1Cc2c3c1cccc3ccc2)c1ccccc1 10476866
10296561 7829 26 None 23 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
7361 7829 26 None 23 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
CHEMBL201945 7829 26 None 23 2 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 433 7 1 4 3.7 O=C([C@H]1CCCN1Cc1ccccc1)NCCCN1CCC2(CC1)OCc1c2cccc1 19445927
1651 9496 26 None -19 10 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 None
4673 9496 26 None -19 10 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 None
6445230 9496 26 None -19 10 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 None
CHEMBL267495 9496 26 None -19 10 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 None
DB13471 9496 26 None -19 10 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 476 5 2 6 3.1 CN([C@@H]1CC[C@@]2([C@@]34[C@H]1Oc1c4c(C[C@H]2N(CC3)CC2CC2)ccc1O)O)C(=O)/C=C/c1ccoc1 None
1683 9628 0 None - 1 Human 10.4 pKi None 10.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
1696 9825 0 None - 1 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10488086
5311338 9825 0 None - 1 Human 7.6 pKi None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 10488086
1692 8935 29 None 12 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 11101358
5311340 8935 29 None 12 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 11101358
CHEMBL140979 8935 29 None 12 4 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 6 2 4 5.5 CCc1ccc(cc1)OCc1ccccc1C(=O)Nc1ccc2c(c1)c(N)cc(n2)C 11101358
1695 9650 0 None - 1 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12010780
1679 7056 24 None -1 2 Mouse 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
9963005 7056 24 None -1 2 Mouse 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL437723 7056 24 None -1 2 Mouse 8.8 pKi None 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1680 7057 0 None -2 2 Mouse 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1690 8417 0 None - 1 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12967935
16131448 9624 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1681 9624 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
1688 9624 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
44361543 9624 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
56947112 9624 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
CHEMBL396460 9624 28 None -2 6 Mouse 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9353393
16143911 7255 16 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863
1689 7255 16 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863
CHEMBL505874 7255 16 None - 1 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11097863