Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
CHEMBL2165920 207588 23 None -21 2 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm300535s
CHEMBL5085013 213170 0 None -1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
CHEMBL5085013 213170 0 None -1 4 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
44542330 196295 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 days
ChEMBL 312 3 3 3 3.3 N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)s1 10.1021/jm9011998
CHEMBL573518 196295 0 None 1 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 days
ChEMBL 312 3 3 3 3.3 N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)s1 10.1021/jm9011998
44542328 196440 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assay
ChEMBL 296 3 3 3 2.8 N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 10.1021/acs.jmedchem.0c00643
CHEMBL4785076 196440 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assay
ChEMBL 296 3 3 3 2.8 N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 10.1021/acs.jmedchem.0c00643
CHEMBL574565 196440 0 None 2 2 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assay
ChEMBL 296 3 3 3 2.8 N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 10.1021/acs.jmedchem.0c00643
123797 2751 23 None -5 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL None None None None 10.1016/j.bmc.2019.01.003
1479 2751 23 None -5 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL None None None None 10.1016/j.bmc.2019.01.003
CHEMBL429731 2751 23 None -5 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 minsAgonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL None None None None 10.1016/j.bmc.2019.01.003
44542326 196221 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 days
ChEMBL 270 4 3 3 2.9 CC(C)c1ccccc1-c1ccc(/C=N/NC(=N)N)o1 10.1021/jm9011998
CHEMBL572825 196221 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 days
ChEMBL 270 4 3 3 2.9 CC(C)c1ccccc1-c1ccc(/C=N/NC(=N)N)o1 10.1021/jm9011998
44542176 196271 1 None -1 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assay
ChEMBL 318 2 3 2 2.0 N=C(N)N/N=C/c1ccc(Br)c(Br)c1 10.1021/acs.jmedchem.0c00643
CHEMBL4784123 196271 1 None -1 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assay
ChEMBL 318 2 3 2 2.0 N=C(N)N/N=C/c1ccc(Br)c(Br)c1 10.1021/acs.jmedchem.0c00643
CHEMBL573297 196271 1 None -1 2 Human 4.8 pEC50 = 4.8 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assay
ChEMBL 318 2 3 2 2.0 N=C(N)N/N=C/c1ccc(Br)c(Br)c1 10.1021/acs.jmedchem.0c00643
CHEMBL2165920 207588 23 None -21 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human NPFF1 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm300535s
162670510 182396 0 None 12 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4793250 182396 0 None 12 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162670510 182396 0 None 12 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4793250 182396 0 None 12 5 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL5091560 213540 0 None -4 5 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
CHEMBL5091560 213540 0 None -4 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
162644880 178868 0 None -2 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4740521 178868 0 None -2 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162644880 178868 0 None -2 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4740521 178868 0 None -2 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
118724977 115997 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Antagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to controlAntagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to control
ChEMBL 394 8 5 4 1.7 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361416 115997 0 None - 1 Human 4.7 pEC50 = 4.7 Functional
Antagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to controlAntagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to control
ChEMBL 394 8 5 4 1.7 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL5090298 213482 0 None -3 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
118735685 118382 0 None -141 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human NPFF1R expressed in CHO cells assessed as effect on forskolin-induced cAMP accumulation after 15 mins by luminescence based assayAgonist activity at human NPFF1R expressed in CHO cells assessed as effect on forskolin-induced cAMP accumulation after 15 mins by luminescence based assay
ChEMBL 1765 61 21 21 3.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1)C(=O)O 10.1021/jm5019675
CHEMBL3422516 118382 0 None -141 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human NPFF1R expressed in CHO cells assessed as effect on forskolin-induced cAMP accumulation after 15 mins by luminescence based assayAgonist activity at human NPFF1R expressed in CHO cells assessed as effect on forskolin-induced cAMP accumulation after 15 mins by luminescence based assay
ChEMBL 1765 61 21 21 3.0 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCc1cn([C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)nn1)C(=O)O 10.1021/jm5019675
CHEMBL5090298 213482 0 None -3 5 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
44542178 197083 4 None -2 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 264 2 3 2 2.2 N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 10.1021/jm300535s
CHEMBL4794542 197083 4 None -2 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 264 2 3 2 2.2 N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 10.1021/jm300535s
CHEMBL583068 197083 4 None -2 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 264 2 3 2 2.2 N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 10.1021/jm300535s
162649206 179403 0 None 7 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4746919 179403 0 None 7 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162649206 179403 0 None 7 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4746919 179403 0 None 7 5 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
101882820 116014 0 None -4 2 Human 5.6 pEC50 = 5.6 Functional
Antagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to controlAntagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to control
ChEMBL 443 8 4 3 3.3 N=C(N)NCC(=O)NCC1(Cc2cccc3ccccc23)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361433 116014 0 None -4 2 Human 5.6 pEC50 = 5.6 Functional
Antagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to controlAntagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to control
ChEMBL 443 8 4 3 3.3 N=C(N)NCC(=O)NCC1(Cc2cccc3ccccc23)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
123797 2751 23 None -5 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
1479 2751 23 None -5 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
CHEMBL429731 2751 23 None -5 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
123797 2751 23 None -5 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
1479 2751 23 None -5 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
CHEMBL429731 2751 23 None -5 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.1c00694
CHEMBL5086601 213266 0 None -1 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
CHEMBL5086601 213266 0 None -1 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
162643991 181216 0 None -14 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1126 32 14 14 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4777999 181216 0 None -14 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1126 32 14 14 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
162643991 181216 0 None -14 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1126 32 14 14 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4777999 181216 0 None -14 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1126 32 14 14 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL2165920 207588 23 None -21 2 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at human NPFF1R expressed in HEK293 cells by dynamic mass redistribution assayAgonist activity at human NPFF1R expressed in HEK293 cells by dynamic mass redistribution assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
162643968 181201 0 None -7 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1115 32 14 14 -2.5 CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4777803 181201 0 None -7 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1115 32 14 14 -2.5 CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
162643968 181201 0 None -7 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1115 32 14 14 -2.5 CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4777803 181201 0 None -7 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1115 32 14 14 -2.5 CSCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL2165920 207588 23 None -21 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NPFF1 receptor Y5.38A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor Y5.38A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm300535s
44542332 196296 0 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 days
ChEMBL 309 3 3 3 2.5 Cn1c(/C=N/NC(=N)N)ccc1-c1ccccc1C(F)(F)F 10.1021/jm9011998
CHEMBL573519 196296 0 None -2 2 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 days
ChEMBL 309 3 3 3 2.5 Cn1c(/C=N/NC(=N)N)ccc1-c1ccccc1C(F)(F)F 10.1021/jm9011998
162666603 181804 0 None -26 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1128 33 16 15 -5.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4785222 181804 0 None -26 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1128 33 16 15 -5.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
44542178 197083 4 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assay
ChEMBL 264 2 3 2 2.2 N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 10.1021/acs.jmedchem.0c00643
CHEMBL4794542 197083 4 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assay
ChEMBL 264 2 3 2 2.2 N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 10.1021/acs.jmedchem.0c00643
CHEMBL583068 197083 4 None -2 2 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293T cells harboring EP2 incubated for 15 mins by cAMP assay
ChEMBL 264 2 3 2 2.2 N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 10.1021/acs.jmedchem.0c00643
162666603 181804 0 None -26 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1128 33 16 15 -5.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4785222 181804 0 None -26 5 Human 5.5 pEC50 = 5.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1128 33 16 15 -5.0 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
162648597 179179 0 None 3 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4744365 179179 0 None 3 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162648597 179179 0 None 3 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4744365 179179 0 None 3 5 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
101882819 1082 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to controlAntagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to control
ChEMBL 394 8 5 4 1.7 NC(=N)NCCNC(=O)C1(CCN(CC1)Cc1ccccc1)Nc1ccccc1 10.1021/jm500989n
11235 1082 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to controlAntagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to control
ChEMBL 394 8 5 4 1.7 NC(=N)NCCNC(=O)C1(CCN(CC1)Cc1ccccc1)Nc1ccccc1 10.1021/jm500989n
CHEMBL3361425 1082 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
Antagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to controlAntagonist activity at human NPFF1 receptor expressed in CHO cells assessed as reversal of NPVF-induced inhibition of intracellular cAMP accumulation after 10 mins by liquid scintillation counting analysis relative to control
ChEMBL 394 8 5 4 1.7 NC(=N)NCCNC(=O)C1(CCN(CC1)Cc1ccccc1)Nc1ccccc1 10.1021/jm500989n
162668843 182007 0 None -2 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4788060 182007 0 None -2 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162668843 182007 0 None -2 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4788060 182007 0 None -2 5 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162651091 179652 0 None -1 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4750006 179652 0 None -1 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162651091 179652 0 None -1 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4750006 179652 0 None -1 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
44542328 196440 0 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 days
ChEMBL 296 3 3 3 2.8 N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 10.1021/jm9011998
CHEMBL4785076 196440 0 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 days
ChEMBL 296 3 3 3 2.8 N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 10.1021/jm9011998
CHEMBL574565 196440 0 None 2 2 Human 7.4 pEC50 = 7.4 Functional
Agonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 days
ChEMBL 296 3 3 3 2.8 N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 10.1021/jm9011998
CHEMBL2165920 207588 23 None -21 2 Human 8.3 pEC50 = 8.3 Functional
Agonist activity at human NPFF1 receptor Y7.33A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor Y7.33A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm300535s
CHEMBL5094675 213733 0 None -3 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
CHEMBL5094675 213733 0 None -3 5 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
60168134 81697 0 None -3 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human NPFF1 receptor Y7.33A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor Y7.33A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 374 3 3 3 3.5 N=C(N)N/N=C/c1ccc(-c2ccc(Br)cc2C(F)(F)F)o1 10.1021/jm300535s
CHEMBL2165921 81697 0 None -3 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human NPFF1 receptor Y7.33A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor Y7.33A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 374 3 3 3 3.5 N=C(N)N/N=C/c1ccc(-c2ccc(Br)cc2C(F)(F)F)o1 10.1021/jm300535s
1486 3271 23 None -1 5 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NPFF1 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/jm300535s
53320361 3271 23 None -1 5 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NPFF1 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/jm300535s
CHEMBL1672380 3271 23 None -1 5 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NPFF1 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor F/Y7.35A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/jm300535s
118724536 115940 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Antagonist activity at human NPFF1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation relative to controlAntagonist activity at human NPFF1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation relative to control
ChEMBL 481 11 5 4 2.3 CC(=N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm500989n
CHEMBL3360829 115940 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
Antagonist activity at human NPFF1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation relative to controlAntagonist activity at human NPFF1 receptor expressed in CHO cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation relative to control
ChEMBL 481 11 5 4 2.3 CC(=N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm500989n
1486 3271 23 None -1 5 Human 5.3 pEC50 = 5.3 Functional
Antagonist activity at human NPFFR1 expressed in CHO cells assessed as reversal of NPVF-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 10 mins by liquid scintillation counting methodAntagonist activity at human NPFFR1 expressed in CHO cells assessed as reversal of NPVF-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 10 mins by liquid scintillation counting method
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/acs.jmedchem.0c00643
53320361 3271 23 None -1 5 Human 5.3 pEC50 = 5.3 Functional
Antagonist activity at human NPFFR1 expressed in CHO cells assessed as reversal of NPVF-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 10 mins by liquid scintillation counting methodAntagonist activity at human NPFFR1 expressed in CHO cells assessed as reversal of NPVF-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 10 mins by liquid scintillation counting method
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/acs.jmedchem.0c00643
CHEMBL1672380 3271 23 None -1 5 Human 5.3 pEC50 = 5.3 Functional
Antagonist activity at human NPFFR1 expressed in CHO cells assessed as reversal of NPVF-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 10 mins by liquid scintillation counting methodAntagonist activity at human NPFFR1 expressed in CHO cells assessed as reversal of NPVF-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 10 mins by liquid scintillation counting method
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/acs.jmedchem.0c00643
CHEMBL2165920 207588 23 None -21 2 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at human NPFF1 receptor expressed in HEK293 cells assessed as reduction in forskolin- stimulated cAMP levelAgonist activity at human NPFF1 receptor expressed in HEK293 cells assessed as reduction in forskolin- stimulated cAMP level
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
CHEMBL5086463 213257 0 None -2 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
44542176 196271 1 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 318 2 3 2 2.0 N=C(N)N/N=C/c1ccc(Br)c(Br)c1 10.1021/jm300535s
CHEMBL4784123 196271 1 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 318 2 3 2 2.0 N=C(N)N/N=C/c1ccc(Br)c(Br)c1 10.1021/jm300535s
CHEMBL573297 196271 1 None -1 2 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 318 2 3 2 2.0 N=C(N)N/N=C/c1ccc(Br)c(Br)c1 10.1021/jm300535s
CHEMBL5086463 213257 0 None -2 4 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
162668623 182035 0 None -1 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1097 31 14 13 -2.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4788431 182035 0 None -1 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1097 31 14 13 -2.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
162668623 182035 0 None -1 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1097 31 14 13 -2.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4788431 182035 0 None -1 5 Human 7.3 pEC50 = 7.3 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1097 31 14 13 -2.2 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](C)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
60168134 81697 0 None -3 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 374 3 3 3 3.5 N=C(N)N/N=C/c1ccc(-c2ccc(Br)cc2C(F)(F)F)o1 10.1021/jm300535s
CHEMBL2165921 81697 0 None -3 2 Human 5.3 pEC50 = 5.3 Functional
Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 374 3 3 3 3.5 N=C(N)N/N=C/c1ccc(-c2ccc(Br)cc2C(F)(F)F)o1 10.1021/jm300535s
CHEMBL5085455 213195 0 None -14 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
CHEMBL5085455 213195 0 None -14 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CCCCNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
162647830 179261 0 None -3 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1112 32 15 14 -3.9 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4745148 179261 0 None -3 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1112 32 15 14 -3.9 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162647830 179261 0 None -3 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1112 32 15 14 -3.9 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4745148 179261 0 None -3 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1112 32 15 14 -3.9 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
162647830 179261 0 None -3 5 Human 6.2 pEC50 = 6.2 Functional
Partial agonist activity at NPFFR1 (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsPartial agonist activity at NPFFR1 (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 1112 32 15 14 -3.9 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00643
CHEMBL4745148 179261 0 None -3 5 Human 6.2 pEC50 = 6.2 Functional
Partial agonist activity at NPFFR1 (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 minsPartial agonist activity at NPFFR1 (unknown origin) expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins
ChEMBL 1112 32 15 14 -3.9 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00643
162647830 179261 0 None -3 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1112 32 15 14 -3.9 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4745148 179261 0 None -3 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1112 32 15 14 -3.9 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162647830 179261 0 None -3 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1112 32 15 14 -3.9 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4745148 179261 0 None -3 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1112 32 15 14 -3.9 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
162666625 181663 0 None -134 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK-293A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by [3H] cAMP addition measured after 2 hrs by scintillation counting methodAgonist activity at NPFFR1 (unknown origin) expressed in HEK-293A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by [3H] cAMP addition measured after 2 hrs by scintillation counting method
ChEMBL 1228 33 14 14 -1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00643
CHEMBL4783555 181663 0 None -134 3 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK-293A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by [3H] cAMP addition measured after 2 hrs by scintillation counting methodAgonist activity at NPFFR1 (unknown origin) expressed in HEK-293A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by [3H] cAMP addition measured after 2 hrs by scintillation counting method
ChEMBL 1228 33 14 14 -1.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00643
162658841 180430 0 None -15 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1172 35 15 15 -3.2 CSCC[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4759079 180430 0 None -15 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1172 35 15 15 -3.2 CSCC[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
162658841 180430 0 None -15 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1172 35 15 15 -3.2 CSCC[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4759079 180430 0 None -15 5 Human 6.2 pEC50 = 6.2 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1172 35 15 15 -3.2 CSCC[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
162677056 182972 0 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4800237 182972 0 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
162677056 182972 0 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4800237 182972 0 None 2 5 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1116 23 14 15 -2.8 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSC[C@@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)C(=O)NCC(=O)N[C@@H](Cc2ccccc2)C(=O)N1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL2165920 207588 23 None -21 2 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human NPFF1 receptor H/Q6.69A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor H/Q6.69A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm300535s
1486 3271 23 None -1 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/jm300535s
53320361 3271 23 None -1 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/jm300535s
CHEMBL1672380 3271 23 None -1 5 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor expressed in COS1 cells assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/jm300535s
CHEMBL2165920 207588 23 None -21 2 Human 5.1 pEC50 = 5.1 Functional
Agonist activity at human NPFF1 receptor E5.27A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor E5.27A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm300535s
162659824 180628 0 None -4 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4761246 180628 0 None -4 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
44542324 196323 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 days
ChEMBL 242 3 3 3 2.1 Cc1ccccc1-c1ccc(/C=N/NC(=N)N)o1 10.1021/jm9011998
CHEMBL573738 196323 0 None 1 2 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 days
ChEMBL 242 3 3 3 2.1 Cc1ccccc1-c1ccc(/C=N/NC(=N)N)o1 10.1021/jm9011998
162659824 180628 0 None -4 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
CHEMBL4761246 180628 0 None -4 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1118 31 16 15 -3.4 N=C(N)NCCC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](CS)NC(=O)[C@H](Cc1ccccc1)NC(=O)CNC(=O)[C@@H](CS)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c01367
44542320 196515 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 days
ChEMBL 306 3 3 2 3.2 N=C(N)N/N=C(\c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1021/jm9011998
CHEMBL575058 196515 0 None 1 2 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 daysAgonist activity at human NPFF1 receptor expressed in cells assessed as beta-galactosidase levels after 5 days
ChEMBL 306 3 3 2 3.2 N=C(N)N/N=C(\c1ccccc1)c1ccc(Cl)c(Cl)c1 10.1021/jm9011998
162670764 182369 0 None -31 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1041 29 14 13 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4792870 182369 0 None -31 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1041 29 14 13 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
162670764 182369 0 None -31 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1041 29 14 13 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4792870 182369 0 None -31 5 Human 6.1 pEC50 = 6.1 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1041 29 14 13 -3.6 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL5082892 213058 0 None 1 5 Human 7.1 pEC50 = 7.1 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
CHEMBL2165920 207588 23 None -21 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human NPFF1 receptor F5.34A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor F5.34A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm300535s
CHEMBL5082892 213058 0 None 1 5 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assayAgonist activity at NPFF1R (unknown origin) expressed in HEK293-A cells assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins in presence of 3-isobutyl-1-methylxanthine followed by forskolin and compound addition by competitive PKA binding assay
ChEMBL None None None CN1C(=O)CNC(=O)[C@H](NC(=O)[C@@H](N)Cc2ccc(O)cc2)CNC(=O)C[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)NC(=O)[C@@H]1Cc1ccccc1 10.1021/acs.jmedchem.1c00694
162654268 180093 0 None -7 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1126 33 15 14 -3.7 CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4755334 180093 0 None -7 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1126 33 15 14 -3.7 CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
162654268 180093 0 None -7 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1126 33 15 14 -3.7 CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4755334 180093 0 None -7 4 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1126 33 15 14 -3.7 CN[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)NCC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
132941097 182686 0 None -25 5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1055 29 13 13 -3.2 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4796596 182686 0 None -25 5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1055 29 13 13 -3.2 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
132941097 182686 0 None -25 5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1055 29 13 13 -3.2 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL4796596 182686 0 None -25 5 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assayAgonist activity at NPFFR1 (unknown origin) expressed in HEK293-A cells assessed as reduction in forskolin-induced cAMP accumulation incubated for 30 mins by competition PKA binding assay
ChEMBL 1055 29 13 13 -3.2 C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.6b01181
CHEMBL2165920 207588 23 None -21 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human NPFF1 receptor D6.59A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingAgonist activity at human NPFF1 receptor D6.59A mutant assessed as [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm300535s
155515973 169452 0 None 1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 minsAntagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 1165 30 12 11 2.7 N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmc.2019.01.003
CHEMBL4442534 169452 0 None 1 3 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 minsAntagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 1165 30 12 11 2.7 N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmc.2019.01.003
102509168 181079 0 None 18 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human NPFFR1 expressed in CHO-K1 cells assessed as reversal of agonist-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by LANCE ultra cAMP assayAntagonist activity at human NPFFR1 expressed in CHO-K1 cells assessed as reversal of agonist-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by LANCE ultra cAMP assay
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1021/acs.jmedchem.0c00643
CHEMBL4776204 181079 0 None 18 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human NPFFR1 expressed in CHO-K1 cells assessed as reversal of agonist-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by LANCE ultra cAMP assayAntagonist activity at human NPFFR1 expressed in CHO-K1 cells assessed as reversal of agonist-induced inhibition of forskolin-stimulated cAMP accumulation incubated for 30 mins by LANCE ultra cAMP assay
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1021/acs.jmedchem.0c00643
1486 3271 23 None -1 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 minsAntagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1016/j.bmc.2019.01.003
53320361 3271 23 None -1 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 minsAntagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1016/j.bmc.2019.01.003
CHEMBL1672380 3271 23 None -1 5 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 minsAntagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1016/j.bmc.2019.01.003
155520785 169941 0 None -2 4 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 minsAntagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 1165 30 12 11 2.7 N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmc.2019.01.003
CHEMBL4449491 169941 0 None -2 4 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 minsAntagonist activity at NPFF1 receptor (unknown origin) expressed in HEK293A cells assessed as reversal of NPPF induced inhibition of forskolin-stimulated cAMP accumulation measured after 30 mins
ChEMBL 1165 30 12 11 2.7 N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmc.2019.01.003
CHEMBL5085324 213190 0 None - 0 Human 7.8 pKd = 7.8 Functional
Antagonist activity at human NPFF1 receptor expressed in HEK293 cells assessed as rightward shift of the dose dependent curve of (S)-N1-((S)-1-((S)-1-amino-1-oxo-3-phenylpropan-2-ylamino)-5-guanidino-1-oxopentan-2-yl)-2-((S)-1-((S)-2-((S)-4-amino-2-((S)-1-((S)-2-amino-3-methylbutanoyl)pyrrolidine-2-carboxamido)-4-oxobutanamido)-4-methylpentanoyl)pyrrolidine-2-carboxamido)pentanediamideAntagonist activity at human NPFF1 receptor expressed in HEK293 cells assessed as rightward shift of the dose dependent curve of (S)-N1-((S)-1-((S)-1-amino-1-oxo-3-phenylpropan-2-ylamino)-5-guanidino-1-oxopentan-2-yl)-2-((S)-1-((S)-2-((S)-4-amino-2-((S)-1-((S)-2-amino-3-methylbutanoyl)pyrrolidine-2-carboxamido)-4-oxobutanamido)-4-methylpentanoyl)pyrrolidine-2-carboxamido)pentanediamide
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)C=C(c1ccccc1)c1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
CHEMBL5091013 213516 0 None - 0 Human 7.7 pKd = 7.7 Functional
Antagonist activity at human NPFF1 receptor expressed in HEK293 cells assessed as rightward shift of the dose dependent curve of (S)-N1-((S)-1-((S)-1-amino-1-oxo-3-phenylpropan-2-ylamino)-5-guanidino-1-oxopentan-2-yl)-2-((S)-1-((S)-2-((S)-4-amino-2-((S)-1-((S)-2-amino-3-methylbutanoyl)pyrrolidine-2-carboxamido)-4-oxobutanamido)-4-methylpentanoyl)pyrrolidine-2-carboxamido)pentanediamideAntagonist activity at human NPFF1 receptor expressed in HEK293 cells assessed as rightward shift of the dose dependent curve of (S)-N1-((S)-1-((S)-1-amino-1-oxo-3-phenylpropan-2-ylamino)-5-guanidino-1-oxopentan-2-yl)-2-((S)-1-((S)-2-((S)-4-amino-2-((S)-1-((S)-2-amino-3-methylbutanoyl)pyrrolidine-2-carboxamido)-4-oxobutanamido)-4-methylpentanoyl)pyrrolidine-2-carboxamido)pentanediamide
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)C=C(c1ccccc1)c1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c00256
1485 624 27 None - 2 Human 7.7 pKd = 7.7 Functional
Competitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingCompetitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm300535s
3474 624 27 None - 2 Human 7.7 pKd = 7.7 Functional
Competitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingCompetitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm300535s
5311023 624 27 None - 2 Human 7.7 pKd = 7.7 Functional
Competitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingCompetitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm300535s
CHEMBL332347 624 27 None - 2 Human 7.7 pKd = 7.7 Functional
Competitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingCompetitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/jm300535s
CHEMBL5085324 213190 0 None - 0 Human 7.5 pKd = 7.5 Functional
Antagonist activity at human NPFF1R expressed in CHO cells by GTPgammaS assayAntagonist activity at human NPFF1R expressed in CHO cells by GTPgammaS assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)C=C(c1ccccc1)c1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
60168135 81698 0 None - 1 Human 7.4 pKd = 7.4 Functional
Competitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingCompetitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 220 2 3 2 1.7 N=C(N)N/N=C/C12CC3CC(CC(C3)C1)C2 10.1021/jm300535s
CHEMBL2165922 81698 0 None - 1 Human 7.4 pKd = 7.4 Functional
Competitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation countingCompetitive antagonist activity at human NPFF1 receptor expressed in COS1 cells assessed as inhibition of NPVF-induced [3H]inositol phosphate accumulation after 2 hrs by liquid scintillation counting
ChEMBL 220 2 3 2 1.7 N=C(N)N/N=C/C12CC3CC(CC(C3)C1)C2 10.1021/jm300535s


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
155461914 182239 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human NPFFR1 expressed in CHO cells by [35S]-GTP S binding assayAgonist activity at human NPFFR1 expressed in CHO cells by [35S]-GTP S binding assay
ChEMBL 1014 25 10 10 2.5 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](CCCN2CCC(Cc3ccccc3)CC2)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1=O 10.1021/acs.jmedchem.0c00643
CHEMBL4790994 182239 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human NPFFR1 expressed in CHO cells by [35S]-GTP S binding assayAgonist activity at human NPFFR1 expressed in CHO cells by [35S]-GTP S binding assay
ChEMBL 1014 25 10 10 2.5 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](CCCN2CCC(Cc3ccccc3)CC2)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1=O 10.1021/acs.jmedchem.0c00643
44542328 196440 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at NPFFR1 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR1 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay
ChEMBL 296 3 3 3 2.8 N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 10.1021/acs.jmedchem.0c00643
CHEMBL4785076 196440 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at NPFFR1 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR1 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay
ChEMBL 296 3 3 3 2.8 N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 10.1021/acs.jmedchem.0c00643
CHEMBL574565 196440 0 None - 0 Human 6.6 pEC50 = 6.6 Binding
Agonist activity at NPFFR1 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR1 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay
ChEMBL 296 3 3 3 2.8 N=C(N)N/N=C/c1ccc(-c2ccccc2C(F)(F)F)o1 10.1021/acs.jmedchem.0c00643
44542178 197083 4 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at NPFFR1 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR1 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay
ChEMBL 264 2 3 2 2.2 N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 10.1021/acs.jmedchem.0c00643
CHEMBL4794542 197083 4 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at NPFFR1 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR1 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay
ChEMBL 264 2 3 2 2.2 N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 10.1021/acs.jmedchem.0c00643
CHEMBL583068 197083 4 None - 0 Human 5.5 pEC50 = 5.5 Binding
Agonist activity at NPFFR1 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assayAgonist activity at NPFFR1 (unknown origin) expressed in mouse NIH3T3 cells by receptor selection and amplification technology assay
ChEMBL 264 2 3 2 2.2 N=C(N)N/N=C/c1ccc(Cl)c(C(F)(F)F)c1 10.1021/acs.jmedchem.0c00643
CHEMBL3360830 209830 0 None -6 2 Human 7.2 pEC50 = 7.2 Binding
Agonist activity at human NPFF1 receptorAgonist activity at human NPFF1 receptor
ChEMBL None None None CC(C)C[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](N)Cc1ccc(O)cc1 10.1021/jm500989n
162676940 182746 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human NPFFR1 expressed in CHO cells by [35S]-GTP S binding assayAgonist activity at human NPFFR1 expressed in CHO cells by [35S]-GTP S binding assay
ChEMBL 897 23 13 10 -1.0 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](Cc2ccccc2)C(N)=O)C1=O 10.1021/acs.jmedchem.0c00643
CHEMBL4797394 182746 0 None - 0 Human 7.1 pEC50 = 7.1 Binding
Agonist activity at human NPFFR1 expressed in CHO cells by [35S]-GTP S binding assayAgonist activity at human NPFFR1 expressed in CHO cells by [35S]-GTP S binding assay
ChEMBL 897 23 13 10 -1.0 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](Cc2ccccc2)C(N)=O)C1=O 10.1021/acs.jmedchem.0c00643
102270377 181622 0 None - 1 Rat 10.0 pIC50 = 10 Binding
Displacement of [125I](Tyr)NPF from rat NPFFR1 expressed in rat PC12 cells incubated for 1 hrDisplacement of [125I](Tyr)NPF from rat NPFFR1 expressed in rat PC12 cells incubated for 1 hr
ChEMBL 576 12 7 6 -0.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.0c00643
CHEMBL4782986 181622 0 None - 1 Rat 10.0 pIC50 = 10 Binding
Displacement of [125I](Tyr)NPF from rat NPFFR1 expressed in rat PC12 cells incubated for 1 hrDisplacement of [125I](Tyr)NPF from rat NPFFR1 expressed in rat PC12 cells incubated for 1 hr
ChEMBL 576 12 7 6 -0.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.0c00643
CHEMBL1672379 207087 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrs
ChEMBL None None None None 10.1021/ml1002053
16735569 141802 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrs
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml1002053
CHEMBL388586 141802 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrs
ChEMBL 798 21 10 7 1.3 CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml1002053
1281 2157 27 None - 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrs
ChEMBL None None None None 10.1021/ml1002053
1283 2157 27 None - 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrs
ChEMBL None None None None 10.1021/ml1002053
25240297 2157 27 None - 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrs
ChEMBL None None None None 10.1021/ml1002053
CHEMBL376756 2157 27 None - 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrs
ChEMBL None None None None 10.1021/ml1002053
25138123 178668 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrs
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml1002053
CHEMBL472833 178668 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrsDisplacement of (D-[125I]Tyr1, MePhe3)-NPFF from NPFFR1 after 2 hrs
ChEMBL 781 21 9 6 2.9 CC(C)C[C@H](/C=C/CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccc(F)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/ml1002053
123797 2751 23 None -1 4 Human 9.0 pKd = 9.0 Binding
Binding affinity to human NPFFR1 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assayBinding affinity to human NPFFR1 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c00643
1479 2751 23 None -1 4 Human 9.0 pKd = 9.0 Binding
Binding affinity to human NPFFR1 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assayBinding affinity to human NPFFR1 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c00643
CHEMBL429731 2751 23 None -1 4 Human 9.0 pKd = 9.0 Binding
Binding affinity to human NPFFR1 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assayBinding affinity to human NPFFR1 expressed in green monkey COS-7 cell membranes by [125I]-1DMeNPFF radioligand based saturation binding assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c00643
CHEMBL2165920 207588 23 None 10 2 Human 11.0 pKi = 11 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
123797 2751 23 None -1 4 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
1479 2751 23 None -1 4 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
CHEMBL429731 2751 23 None -1 4 Human 10.2 pKi = 10.2 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None None 10.1021/acs.jmedchem.1c00256
71463277 83749 0 None 1819 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208337 83749 0 None 1819 2 Human 9.5 pKi = 9.5 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2165920 207588 23 None 10 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]YVP from human NPFFR1 expressed in CHO cells by gamma-counter methodDisplacement of [125I]YVP from human NPFFR1 expressed in CHO cells by gamma-counter method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00643
CHEMBL5093771 213669 0 None 4 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)C=C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1Br)C(N)=O 10.1021/acs.jmedchem.1c00256
71456101 83733 0 None 60 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 450 12 6 4 0.7 N=C(N)NCCC[C@@H](NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208303 83733 0 None 60 2 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 450 12 6 4 0.7 N=C(N)NCCC[C@@H](NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
71463272 83732 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 573 13 6 6 2.6 N=C(N)NCCC[C@H](NC(=O)CCN1c2ccccc2Sc2ccccc21)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208301 83732 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 573 13 6 6 2.6 N=C(N)NCCC[C@H](NC(=O)CCN1c2ccccc2Sc2ccccc21)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
162673140 182441 0 None 37 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]-FFRF-NH2 from human NPFFR1 expressed in CHO cell membrane by Topcount scintillation counting methodDisplacement of [3H]-FFRF-NH2 from human NPFFR1 expressed in CHO cell membrane by Topcount scintillation counting method
ChEMBL 241 1 2 3 2.3 NC1=NC=C(c2ccc(Cl)c(Cl)c2)CN1 10.1021/acs.jmedchem.0c00643
CHEMBL4793841 182441 0 None 37 2 Human 9.0 pKi = 9 Binding
Displacement of [3H]-FFRF-NH2 from human NPFFR1 expressed in CHO cell membrane by Topcount scintillation counting methodDisplacement of [3H]-FFRF-NH2 from human NPFFR1 expressed in CHO cell membrane by Topcount scintillation counting method
ChEMBL 241 1 2 3 2.3 NC1=NC=C(c2ccc(Cl)c(Cl)c2)CN1 10.1021/acs.jmedchem.0c00643
CHEMBL2165920 207588 23 None 10 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]YVP from human NPFFR1 expressed in HEK293 cells by radioligand binding assayDisplacement of [125I]YVP from human NPFFR1 expressed in HEK293 cells by radioligand binding assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00643
CHEMBL414263 211370 3 None -2 4 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I]-1DMeNPFF from rat NPFFR1 expressed in HEK293 cells incubated for 2 hrs by scintillation counting methodDisplacement of [125I]-1DMeNPFF from rat NPFFR1 expressed in HEK293 cells incubated for 2 hrs by scintillation counting method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N(C)[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00643
CHEMBL5082175 213019 0 None 8 2 Human 8.0 pKi = 8 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)C=C(c1ccccc1)c1ccccc1)C(=O)N[C@H](Cc1ccccc1Br)C(N)=O 10.1021/acs.jmedchem.1c00256
71457909 83741 0 None -2 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 514 13 6 4 1.8 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208319 83741 0 None -2 2 Human 8.0 pKi = 8 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 514 13 6 4 1.8 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
44542176 196271 1 None 1 2 Human 7.0 pKi = 7 Binding
Displacement of 125I-NPFF from human NPFFR1 incubated for 2 hrs by TopCount scintillation counting methodDisplacement of 125I-NPFF from human NPFFR1 incubated for 2 hrs by TopCount scintillation counting method
ChEMBL 318 2 3 2 2.0 N=C(N)N/N=C/c1ccc(Br)c(Br)c1 10.1021/acs.jmedchem.0c00643
CHEMBL4784123 196271 1 None 1 2 Human 7.0 pKi = 7 Binding
Displacement of 125I-NPFF from human NPFFR1 incubated for 2 hrs by TopCount scintillation counting methodDisplacement of 125I-NPFF from human NPFFR1 incubated for 2 hrs by TopCount scintillation counting method
ChEMBL 318 2 3 2 2.0 N=C(N)N/N=C/c1ccc(Br)c(Br)c1 10.1021/acs.jmedchem.0c00643
CHEMBL573297 196271 1 None 1 2 Human 7.0 pKi = 7 Binding
Displacement of 125I-NPFF from human NPFFR1 incubated for 2 hrs by TopCount scintillation counting methodDisplacement of 125I-NPFF from human NPFFR1 incubated for 2 hrs by TopCount scintillation counting method
ChEMBL 318 2 3 2 2.0 N=C(N)N/N=C/c1ccc(Br)c(Br)c1 10.1021/acs.jmedchem.0c00643
127041619 136609 0 None -12302 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assayDisplacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3746386 136609 0 None -12302 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assayDisplacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747715 136609 0 None -12302 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assayDisplacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL3747822 136609 0 None -12302 2 Human 6.0 pKi = 6 Binding
Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assayDisplacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay
ChEMBL 615 15 7 5 2.2 CCC(=O)NCCNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
102270377 181622 0 None - 1 Rat 7.0 pKi = 7 Binding
Displacement of [125I](Tyr)NPF from rat NPFFR1 expressed in rat PC12 cells incubated for 1 hrDisplacement of [125I](Tyr)NPF from rat NPFFR1 expressed in rat PC12 cells incubated for 1 hr
ChEMBL 576 12 7 6 -0.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.0c00643
CHEMBL4782986 181622 0 None - 1 Rat 7.0 pKi = 7 Binding
Displacement of [125I](Tyr)NPF from rat NPFFR1 expressed in rat PC12 cells incubated for 1 hrDisplacement of [125I](Tyr)NPF from rat NPFFR1 expressed in rat PC12 cells incubated for 1 hr
ChEMBL 576 12 7 6 -0.3 N=C(N)NCCC[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1)C(=O)N1Cc2ccccc2C[C@H]1C(N)=O 10.1021/acs.jmedchem.0c00643
118724988 116008 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 408 9 5 4 1.8 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(CCc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361428 116008 0 None -3 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 408 9 5 4 1.8 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(CCc2ccccc2)CC1 10.1021/jm500989n
71463276 83748 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 454 12 6 5 0.3 COc1cccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1016/j.bmcl.2012.10.049
CHEMBL2208334 83748 0 None 1 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 454 12 6 5 0.3 COc1cccc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 10.1016/j.bmcl.2012.10.049
71463279 83752 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 424 11 6 4 0.3 N=C(N)NCCC[C@@H](NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208340 83752 0 None 1 2 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 424 11 6 4 0.3 N=C(N)NCCC[C@@H](NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL5091013 213516 0 None 114 3 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)C=C(c1ccccc1)c1ccccc1)C(=O)NCC(N)=O 10.1021/acs.jmedchem.1c00256
71454357 83744 0 None 6 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)c1cccc(-c2ccccc2)c1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208323 83744 0 None 6 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)c1cccc(-c2ccccc2)c1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
10008757 188426 0 None -7585 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assayDisplacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
CHEMBL508974 188426 0 None -7585 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assayDisplacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay
ChEMBL 602 14 6 6 2.3 CCOC(=O)CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.5b00925
118724991 116012 0 None 4 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 472 8 5 4 2.5 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccc(Br)cc2)CC1 10.1021/jm500989n
CHEMBL3361431 116012 0 None 4 2 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 472 8 5 4 2.5 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccc(Br)cc2)CC1 10.1021/jm500989n
101882820 116014 0 None -3 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 443 8 4 3 3.3 N=C(N)NCC(=O)NCC1(Cc2cccc3ccccc23)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361433 116014 0 None -3 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 443 8 4 3 3.3 N=C(N)NCC(=O)NCC1(Cc2cccc3ccccc23)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
71454353 83736 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 482 11 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208306 83736 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 482 11 6 4 1.2 N=C(N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
118724980 116000 0 None 6 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 454 10 5 6 1.8 COc1cc(NC2(CNC(=O)CNC(=N)N)CCN(Cc3ccccc3)CC2)cc(OC)c1 10.1021/jm500989n
CHEMBL3361419 116000 0 None 6 4 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 454 10 5 6 1.8 COc1cc(NC2(CNC(=O)CNC(=N)N)CCN(Cc3ccccc3)CC2)cc(OC)c1 10.1021/jm500989n
1485 624 27 None -4 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human NPFF1 receptor expressed in CHO cellsBinding affinity to human NPFF1 receptor expressed in CHO cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
3474 624 27 None -4 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human NPFF1 receptor expressed in CHO cellsBinding affinity to human NPFF1 receptor expressed in CHO cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
5311023 624 27 None -4 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human NPFF1 receptor expressed in CHO cellsBinding affinity to human NPFF1 receptor expressed in CHO cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
CHEMBL332347 624 27 None -4 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human NPFF1 receptor expressed in CHO cellsBinding affinity to human NPFF1 receptor expressed in CHO cells
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
9869458 92516 4 None 38 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]YVP from human NPFFR1 expressed in CHO cellsDisplacement of [125I]YVP from human NPFFR1 expressed in CHO cells
ChEMBL 473 11 6 4 2.6 N=C(N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.0c00643
CHEMBL2440929 92516 4 None 38 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]YVP from human NPFFR1 expressed in CHO cellsDisplacement of [125I]YVP from human NPFFR1 expressed in CHO cells
ChEMBL 473 11 6 4 2.6 N=C(N)NCCC[C@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)NCc1ccc(O)cc1 10.1021/acs.jmedchem.0c00643
71456103 83738 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 475 11 6 5 0.8 N=C(N)NCCC[C@H](NC(=O)c1ccc2ccccc2n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208312 83738 0 None -2 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 475 11 6 5 0.8 N=C(N)NCCC[C@H](NC(=O)c1ccc2ccccc2n1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
9920663 181175 7 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human NPFFR1 by radioligand binding assayBinding affinity to human NPFFR1 by radioligand binding assay
ChEMBL 200 1 3 2 1.8 Cc1cc(NC(=N)N)nc2ccccc12 10.1021/acs.jmedchem.0c00643
CHEMBL4777535 181175 7 None -1 4 Human 7.9 pKi = 7.9 Binding
Binding affinity to human NPFFR1 by radioligand binding assayBinding affinity to human NPFFR1 by radioligand binding assay
ChEMBL 200 1 3 2 1.8 Cc1cc(NC(=N)N)nc2ccccc12 10.1021/acs.jmedchem.0c00643
CHEMBL5091693 213548 0 None 36 2 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)C=C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CC(N)=O)C(N)=O 10.1021/acs.jmedchem.1c00256
1486 3271 23 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/acs.jmedchem.1c00256
53320361 3271 23 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/acs.jmedchem.1c00256
CHEMBL1672380 3271 23 None 1 2 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/acs.jmedchem.1c00256
118724990 116011 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 444 8 5 4 2.9 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccc3ccccc3c2)CC1 10.1021/jm500989n
CHEMBL3361430 116011 0 None 3 2 Human 6.9 pKi = 6.9 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 444 8 5 4 2.9 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccc3ccccc3c2)CC1 10.1021/jm500989n
71450762 83731 0 None 15 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 514 13 6 4 1.8 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208299 83731 0 None 15 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 514 13 6 4 1.8 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
118724986 116006 0 None -5 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 304 6 6 4 -0.2 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCNCC1 10.1021/jm500989n
CHEMBL3361426 116006 0 None -5 2 Human 4.8 pKi = 4.8 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 304 6 6 4 -0.2 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCNCC1 10.1021/jm500989n
118724985 116005 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 407 9 4 3 2.5 N=C(N)NCC(=O)NCC1(CCc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361424 116005 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 407 9 4 3 2.5 N=C(N)NCC(=O)NCC1(CCc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL5088703 213396 0 None 35 2 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None C[C@@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)C=C(c1ccccc1)c1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
136998789 115994 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 656 8 4 7 6.8 CC(C)(C)OC(=O)/N=C(\NC(=O)OC(C)(C)C)Nc1cccc(C(=O)NCC2(Nc3ccccc3)CCN(Cc3ccccc3)CC2)c1 10.1021/jm500989n
CHEMBL3361413 115994 0 None -1 2 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 656 8 4 7 6.8 CC(C)(C)OC(=O)/N=C(\NC(=O)OC(C)(C)C)Nc1cccc(C(=O)NCC2(Nc3ccccc3)CCN(Cc3ccccc3)CC2)c1 10.1021/jm500989n
118724987 116007 0 None -5 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 400 8 5 4 2.1 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(CC2CCCCC2)CC1 10.1021/jm500989n
CHEMBL3361427 116007 0 None -5 2 Human 5.8 pKi = 5.8 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 400 8 5 4 2.1 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(CC2CCCCC2)CC1 10.1021/jm500989n
71454359 83746 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208326 83746 0 None 2 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
72194631 181281 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-FFRF-NH2 from human FLAG-tagged NPFFR1 expressed in CHO cell membrane incubated for 30 mins by Topcount scintillation counting methodDisplacement of [3H]-FFRF-NH2 from human FLAG-tagged NPFFR1 expressed in CHO cell membrane incubated for 30 mins by Topcount scintillation counting method
ChEMBL 483 11 2 3 5.1 O=C(N[C@@H](CCCN1CCCCC1)C(=O)NCCc1ccccc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.0c00643
CHEMBL4778746 181281 0 None 3 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-FFRF-NH2 from human FLAG-tagged NPFFR1 expressed in CHO cell membrane incubated for 30 mins by Topcount scintillation counting methodDisplacement of [3H]-FFRF-NH2 from human FLAG-tagged NPFFR1 expressed in CHO cell membrane incubated for 30 mins by Topcount scintillation counting method
ChEMBL 483 11 2 3 5.1 O=C(N[C@@H](CCCN1CCCCC1)C(=O)NCCc1ccccc1)c1ccccc1-c1ccccc1 10.1021/acs.jmedchem.0c00643
1485 624 27 None -4 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assayDisplacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
3474 624 27 None -4 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assayDisplacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
5311023 624 27 None -4 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assayDisplacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
CHEMBL332347 624 27 None -4 4 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assayDisplacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay
ChEMBL 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 10.1021/acs.jmedchem.5b00925
118724542 115944 0 None 3 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 337 6 4 3 2.6 N=C(N)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3360836 115944 0 None 3 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 337 6 4 3 2.6 N=C(N)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
118724982 116002 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 462 8 5 4 3.0 N=C(N)NCC(=O)NCC1(Nc2ccc(Cl)c(Cl)c2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361421 116002 0 None 2 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 462 8 5 4 3.0 N=C(N)NCC(=O)NCC1(Nc2ccc(Cl)c(Cl)c2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
136948074 115995 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 656 8 4 7 6.8 CC(C)(C)OC(=O)/N=C(\NC(=O)OC(C)(C)C)Nc1ccc(C(=O)NCC2(Nc3ccccc3)CCN(Cc3ccccc3)CC2)cc1 10.1021/jm500989n
CHEMBL3361414 115995 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 656 8 4 7 6.8 CC(C)(C)OC(=O)/N=C(\NC(=O)OC(C)(C)C)Nc1ccc(C(=O)NCC2(Nc3ccccc3)CCN(Cc3ccccc3)CC2)cc1 10.1021/jm500989n
71461185 83129 0 None 10 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 424 11 6 4 0.3 N=C(N)NCCC[C@@H](NC(=O)c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2204019 83129 0 None 10 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 424 11 6 4 0.3 N=C(N)NCCC[C@@H](NC(=O)c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL414263 211370 3 None -7 4 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]YVP from human NPFFR1 expressed in HEK293 cells by radioligand binding assayDisplacement of [125I]YVP from human NPFFR1 expressed in HEK293 cells by radioligand binding assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N(C)[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00643
71454358 83745 0 None 46 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208325 83745 0 None 46 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2ccccc2)cc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
71463278 83750 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208338 83750 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
102080626 170729 0 None -107 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]YVP from human NPFFR1 expressed in CHO cells by gamma-counter methodDisplacement of [125I]YVP from human NPFFR1 expressed in CHO cells by gamma-counter method
ChEMBL 1377 39 15 16 -3.5 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N(C)C(=O)[C@@H]1CCCN1C(=O)[C@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00643
CHEMBL4460742 170729 0 None -107 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]YVP from human NPFFR1 expressed in CHO cells by gamma-counter methodDisplacement of [125I]YVP from human NPFFR1 expressed in CHO cells by gamma-counter method
ChEMBL 1377 39 15 16 -3.5 CC(C)C[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)N(C)C(=O)[C@@H]1CCCN1C(=O)[C@H](N)CC(N)=O)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00643
118724981 116001 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 424 9 5 5 1.7 COc1cccc(NC2(CNC(=O)CNC(=N)N)CCN(Cc3ccccc3)CC2)c1 10.1021/jm500989n
CHEMBL3361420 116001 0 None 4 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 424 9 5 5 1.7 COc1cccc(NC2(CNC(=O)CNC(=N)N)CCN(Cc3ccccc3)CC2)c1 10.1021/jm500989n
CHEMBL5084208 213129 0 None 7 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)C=C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.1c00256
1486 3271 23 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1016/j.bmcl.2012.10.049
53320361 3271 23 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1016/j.bmcl.2012.10.049
CHEMBL1672380 3271 23 None 1 2 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1016/j.bmcl.2012.10.049
9955930 83751 0 None 3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 424 11 6 4 0.3 N=C(N)NCCC[C@H](NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208339 83751 0 None 3 2 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 424 11 6 4 0.3 N=C(N)NCCC[C@H](NC(=O)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
136998790 115996 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 670 9 4 7 6.7 CC(C)(C)OC(=O)/N=C(\NC(=O)OC(C)(C)C)Nc1ccc(CC(=O)NCC2(Nc3ccccc3)CCN(Cc3ccccc3)CC2)cc1 10.1021/jm500989n
CHEMBL3361415 115996 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 670 9 4 7 6.7 CC(C)(C)OC(=O)/N=C(\NC(=O)OC(C)(C)C)Nc1ccc(CC(=O)NCC2(Nc3ccccc3)CCN(Cc3ccccc3)CC2)cc1 10.1021/jm500989n
9942758 182906 2 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human NPFFR1 by radioligand binding assayBinding affinity to human NPFFR1 by radioligand binding assay
ChEMBL 234 1 3 2 2.5 Cc1cc(NC(=N)N)nc2ccc(Cl)cc12 10.1021/acs.jmedchem.0c00643
CHEMBL4799458 182906 2 None 1 4 Human 7.6 pKi = 7.6 Binding
Binding affinity to human NPFFR1 by radioligand binding assayBinding affinity to human NPFFR1 by radioligand binding assay
ChEMBL 234 1 3 2 2.5 Cc1cc(NC(=N)N)nc2ccc(Cl)cc12 10.1021/acs.jmedchem.0c00643
118724973 115993 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 636 11 4 7 5.8 CC(C)(C)OC(=O)/N=C(\NCCCCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1)NC(=O)OC(C)(C)C 10.1021/jm500989n
CHEMBL3361412 115993 0 None -1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 636 11 4 7 5.8 CC(C)(C)OC(=O)/N=C(\NCCCCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1)NC(=O)OC(C)(C)C 10.1021/jm500989n
9942758 182906 2 None -1 4 Rat 7.6 pKi = 7.6 Binding
Binding affinity to rat NPFFR1 by radioligand binding assayBinding affinity to rat NPFFR1 by radioligand binding assay
ChEMBL 234 1 3 2 2.5 Cc1cc(NC(=N)N)nc2ccc(Cl)cc12 10.1021/acs.jmedchem.0c00643
CHEMBL4799458 182906 2 None -1 4 Rat 7.6 pKi = 7.6 Binding
Binding affinity to rat NPFFR1 by radioligand binding assayBinding affinity to rat NPFFR1 by radioligand binding assay
ChEMBL 234 1 3 2 2.5 Cc1cc(NC(=N)N)nc2ccc(Cl)cc12 10.1021/acs.jmedchem.0c00643
CHEMBL326770 209543 5 None -1 4 Rat 7.6 pKi = 7.6 Binding
Displacement of [125I]-1DMeNPFF from rat NPFFR1 expressed in HEK293 cells incubated for 2 hrs by scintillation counting methodDisplacement of [125I]-1DMeNPFF from rat NPFFR1 expressed in HEK293 cells incubated for 2 hrs by scintillation counting method
ChEMBL None None None NC(=O)CC[C@H](NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00643
118724972 115021 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 622 10 4 7 5.4 CC(C)(C)OC(=O)/N=C(/NCCCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1)NC(=O)OC(C)(C)C 10.1021/jm500989n
CHEMBL3352907 115021 0 None 1 2 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 622 10 4 7 5.4 CC(C)(C)OC(=O)/N=C(/NCCCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1)NC(=O)OC(C)(C)C 10.1021/jm500989n
71463275 83740 0 None 11 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 438 12 6 4 0.2 N=C(N)NCCC[C@@H](NC(=O)Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208317 83740 0 None 11 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 438 12 6 4 0.2 N=C(N)NCCC[C@@H](NC(=O)Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
71454352 83735 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 482 11 6 4 1.2 N=C(N)NCCC[C@@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208305 83735 0 None 4 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 482 11 6 4 1.2 N=C(N)NCCC[C@@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
118724539 115942 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 465 12 6 5 1.9 N=C(N)NCCC[C@H](N)C(=O)NCC1(Nc2ccccc2)CCN(CCc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3360833 115942 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 465 12 6 5 1.9 N=C(N)NCCC[C@H](N)C(=O)NCC1(Nc2ccccc2)CCN(CCc2ccccc2)CC1 10.1021/jm500989n
118724995 116017 0 None 3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 469 9 4 3 3.8 N=C(N)NCC(=O)NCC1(Cc2ccc(-c3ccccc3)cc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361436 116017 0 None 3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 469 9 4 3 3.8 N=C(N)NCC(=O)NCC1(Cc2ccc(-c3ccccc3)cc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
118724543 115945 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 351 7 4 3 2.7 N=C(N)NCC1(Nc2ccccc2)CCN(CCc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3360837 115945 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 351 7 4 3 2.7 N=C(N)NCC1(Nc2ccccc2)CCN(CCc2ccccc2)CC1 10.1021/jm500989n
CHEMBL2165920 207588 23 None 10 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm500989n
CHEMBL3360830 209830 0 None -6 2 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL None None None CC(C)C[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](N)Cc1ccc(O)cc1 10.1021/jm500989n
118724994 116016 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 443 8 4 3 3.3 N=C(N)NCC(=O)NCC1(Cc2ccc3ccccc3c2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361435 116016 0 None -1 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 443 8 4 3 3.3 N=C(N)NCC(=O)NCC1(Cc2ccc3ccccc3c2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
118724977 115997 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 394 8 5 4 1.7 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361416 115997 0 None 1 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 394 8 5 4 1.7 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL5087609 213336 0 None 16 2 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)C=C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/acs.jmedchem.1c00256
118724992 116013 0 None 4 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 452 9 5 6 1.5 COC(=O)c1ccc(CN2CCC(CNC(=O)CNC(=N)N)(Nc3ccccc3)CC2)cc1 10.1021/jm500989n
CHEMBL3361432 116013 0 None 4 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 452 9 5 6 1.5 COC(=O)c1ccc(CN2CCC(CNC(=O)CNC(=N)N)(Nc3ccccc3)CC2)cc1 10.1021/jm500989n
118724971 115992 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 452 8 3 5 3.8 CC(C)(C)OC(=O)NCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361411 115992 0 None -1 2 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 452 8 3 5 3.8 CC(C)(C)OC(=O)NCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
71452593 83739 0 None 12 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 438 12 6 4 0.2 N=C(N)NCCC[C@@H](NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208316 83739 0 None 12 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 438 12 6 4 0.2 N=C(N)NCCC[C@@H](NC(=O)Cc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
71457908 83730 0 None -2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 463 11 7 4 0.7 N=C(N)NCCC[C@H](NC(=O)c1ccc2cc[nH]c2c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208296 83730 0 None -2 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 463 11 7 4 0.7 N=C(N)NCCC[C@H](NC(=O)c1ccc2cc[nH]c2c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL5093184 213640 0 None 38 2 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells 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=C(c1ccccc1)c1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
CHEMBL3360830 209830 0 None -6 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL None None None CC(C)C[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](N)Cc1ccc(O)cc1 10.1021/jm500989n
CHEMBL5090293 213481 0 None 47 2 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)C=C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
CHEMBL5085324 213190 0 None 165 3 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)C=C(c1ccccc1)c1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
CHEMBL326770 209543 5 None -2 4 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-1DMeNPFF from human NPFFR1 expressed in HEK293 cells incubated for 2 hrs by scintillation counting methodDisplacement of [125I]-1DMeNPFF from human NPFFR1 expressed in HEK293 cells incubated for 2 hrs by scintillation counting method
ChEMBL None None None NC(=O)CC[C@H](NC(=O)[C@@H]1CCCN1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00643
118724984 116004 0 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 393 8 4 3 2.1 N=C(N)NCC(=O)NCC1(Cc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361423 116004 0 None -5 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 393 8 4 3 2.1 N=C(N)NCC(=O)NCC1(Cc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
118724993 116015 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 461 8 4 3 3.4 N=C(N)NCC(=O)NCC1(Cc2ccc(Cl)c(Cl)c2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361434 116015 0 None -5 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 461 8 4 3 3.4 N=C(N)NCC(=O)NCC1(Cc2ccc(Cl)c(Cl)c2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
118724970 115991 0 None 6 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 408 9 5 4 2.1 N=C(N)NCCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361410 115991 0 None 6 2 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 408 9 5 4 2.1 N=C(N)NCCC(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
118724540 115943 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 501 11 6 5 3.0 N=C(N)NCCC[C@H](N)C(=O)NCC1(Nc2ccccc2)CCN(Cc2ccc3ccccc3c2)CC1 10.1021/jm500989n
CHEMBL3360834 115943 0 None -1 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 501 11 6 5 3.0 N=C(N)NCCC[C@H](N)C(=O)NCC1(Nc2ccccc2)CCN(Cc2ccc3ccccc3c2)CC1 10.1021/jm500989n
101882818 115941 0 None -144 5 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 451 11 6 5 1.8 N=C(N)NCCC[C@H](N)C(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3360832 115941 0 None -144 5 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [125I]YVP from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 451 11 6 5 1.8 N=C(N)NCCC[C@H](N)C(=O)NCC1(Nc2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
71457910 83742 0 None 30 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208320 83742 0 None 30 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)c1ccccc1-c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
71463273 83737 0 None 4 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 482 11 6 4 1.2 N=C(N)NCCC[C@@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208307 83737 0 None 4 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 482 11 6 4 1.2 N=C(N)NCCC[C@@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
118724983 116003 0 None 6 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 379 7 4 3 1.8 N=C(N)NCC(=O)NCC1(c2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361422 116003 0 None 6 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 379 7 4 3 1.8 N=C(N)NCC(=O)NCC1(c2ccccc2)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL5076959 212700 0 None 5 2 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None CC(C)C[C@@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)C=C(c1ccccc1)c1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
118724989 116009 0 None -4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 444 8 5 4 2.9 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(Cc2cccc3ccccc23)CC1 10.1021/jm500989n
CHEMBL3361429 116009 0 None -4 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 444 8 5 4 2.9 N=C(N)NCC(=O)NCC1(Nc2ccccc2)CCN(Cc2cccc3ccccc23)CC1 10.1021/jm500989n
118724536 115940 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human NPFF1 receptor expressed in CHO cellsAntagonist activity at human NPFF1 receptor expressed in CHO cells
ChEMBL 481 11 5 4 2.3 CC(=N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm500989n
CHEMBL3360829 115940 0 None 1 2 Human 7.2 pKi = 7.2 Binding
Antagonist activity at human NPFF1 receptor expressed in CHO cellsAntagonist activity at human NPFF1 receptor expressed in CHO cells
ChEMBL 481 11 5 4 2.3 CC(=N)NCCC[C@H](NC(=O)C12CC3CC(CC(C3)C1)C2)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/jm500989n
102509168 181079 0 None 4 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1021/acs.jmedchem.1c00256
CHEMBL4776204 181079 0 None 4 3 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](C(N)=O)c1ccccc1 10.1021/acs.jmedchem.1c00256
CHEMBL5082273 213026 0 None 30 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)C=C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(N)=O 10.1021/acs.jmedchem.1c00256
1486 3271 23 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]YVP from human NPFFR1 expressed in CHO cellsDisplacement of [125I]YVP from human NPFFR1 expressed in CHO cells
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/acs.jmedchem.0c00643
53320361 3271 23 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]YVP from human NPFFR1 expressed in CHO cellsDisplacement of [125I]YVP from human NPFFR1 expressed in CHO cells
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/acs.jmedchem.0c00643
CHEMBL1672380 3271 23 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]YVP from human NPFFR1 expressed in CHO cellsDisplacement of [125I]YVP from human NPFFR1 expressed in CHO cells
ChEMBL None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 10.1021/acs.jmedchem.0c00643
CHEMBL5085023 213172 0 None 1 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)C=C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1021/acs.jmedchem.1c00256
71456104 83743 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)c1cccc(-c2ccccc2)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208322 83743 0 None 1 2 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 500 12 6 4 1.9 N=C(N)NCCC[C@@H](NC(=O)c1cccc(-c2ccccc2)c1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL5071745 212495 0 None 42 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)C=C(c1ccccc1)c1ccccc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(N)=O 10.1021/acs.jmedchem.1c00256
CHEMBL5075638 212617 0 None 85 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)C=C(c1ccccc1)c1ccccc1)C(=O)N[C@@H](CCc1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
162663612 181421 0 None 2 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NPFF from human NPFFR1 expressed in CHO cell membranes incubated for 120 mins by scintillation/luminescence counting methodDisplacement of [125I]NPFF from human NPFFR1 expressed in CHO cell membranes incubated for 120 mins by scintillation/luminescence counting method
ChEMBL 523 11 1 7 4.8 COc1ccc(CN[C@H]2C[C@@H](C(=O)OCCc3ccc([N+](=O)[O-])cc3)N(Cc3ccccc3Cl)C2)cc1 10.1021/acs.jmedchem.0c00643
CHEMBL4780551 181421 0 None 2 2 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]NPFF from human NPFFR1 expressed in CHO cell membranes incubated for 120 mins by scintillation/luminescence counting methodDisplacement of [125I]NPFF from human NPFFR1 expressed in CHO cell membranes incubated for 120 mins by scintillation/luminescence counting method
ChEMBL 523 11 1 7 4.8 COc1ccc(CN[C@H]2C[C@@H](C(=O)OCCc3ccc([N+](=O)[O-])cc3)N(Cc3ccccc3Cl)C2)cc1 10.1021/acs.jmedchem.0c00643
127041327 136607 0 None -1445 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assayDisplacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
CHEMBL3746851 136607 0 None -1445 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assayDisplacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
CHEMBL3747820 136607 0 None -1445 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assayDisplacement of [3H]NPVF from human NPFF1 expressed in CHO cells by radioligand binding assay
ChEMBL 611 13 6 7 2.0 Cn1cc(CNC(=O)/N=C(/N)NCCC[C@@H](NC(=O)C(c2ccccc2)c2ccccc2)C(=O)NCc2ccc(O)cc2)nn1 10.1021/acs.jmedchem.5b00925
CHEMBL5088429 213385 0 None 70 2 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None CC(C)[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)C=C(c1ccccc1)c1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
9920663 181175 7 None 1 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity to rat NPFFR1 by radioligand binding assayBinding affinity to rat NPFFR1 by radioligand binding assay
ChEMBL 200 1 3 2 1.8 Cc1cc(NC(=N)N)nc2ccccc12 10.1021/acs.jmedchem.0c00643
CHEMBL4777535 181175 7 None 1 4 Rat 8.2 pKi = 8.2 Binding
Binding affinity to rat NPFFR1 by radioligand binding assayBinding affinity to rat NPFFR1 by radioligand binding assay
ChEMBL 200 1 3 2 1.8 Cc1cc(NC(=N)N)nc2ccccc12 10.1021/acs.jmedchem.0c00643
71456101 83733 0 None 60 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL 450 12 6 4 0.7 N=C(N)NCCC[C@@H](NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
CHEMBL2208303 83733 0 None 60 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL 450 12 6 4 0.7 N=C(N)NCCC[C@@H](NC(=O)/C=C/c1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
CHEMBL5074999 212581 0 None 100 3 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None N=C(N)NCCC[C@@H](NC(=O)C=C(c1ccccc1)c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
CHEMBL414263 211370 3 None -7 4 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-1DMeNPFF from human NPFFR1 expressed in HEK293 cells incubated for 2 hrs by scintillation counting methodDisplacement of [125I]-1DMeNPFF from human NPFFR1 expressed in HEK293 cells incubated for 2 hrs by scintillation counting method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](N)Cc1ccc(O)cc1)C(=O)N(C)[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.0c00643
71456102 83734 0 None 23 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL 450 12 6 4 0.7 N=C(N)NCCC[C@@H](NC(=O)/C=C/c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
CHEMBL2208304 83734 0 None 23 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL 450 12 6 4 0.7 N=C(N)NCCC[C@@H](NC(=O)/C=C/c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
CHEMBL5082270 213024 0 None 75 2 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting methodDisplacement of [125I]-1DMeNPFF from recombinant human NPFF1 receptor expressed in CHO cells by TopCount scintillation counting method
ChEMBL None None None C[C@H](NC(=O)[C@@H](CCCNC(=N)N)NC(=O)C=C(c1ccccc1)c1ccccc1)C(N)=O 10.1021/acs.jmedchem.1c00256
101882819 1082 0 None 2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 394 8 5 4 1.7 NC(=N)NCCNC(=O)C1(CCN(CC1)Cc1ccccc1)Nc1ccccc1 10.1021/jm500989n
11235 1082 0 None 2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 394 8 5 4 1.7 NC(=N)NCCNC(=O)C1(CCN(CC1)Cc1ccccc1)Nc1ccccc1 10.1021/jm500989n
CHEMBL3361425 1082 0 None 2 5 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 394 8 5 4 1.7 NC(=N)NCCNC(=O)C1(CCN(CC1)Cc1ccccc1)Nc1ccccc1 10.1021/jm500989n
71456102 83734 0 None 23 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 450 12 6 4 0.7 N=C(N)NCCC[C@@H](NC(=O)/C=C/c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208304 83734 0 None 23 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 450 12 6 4 0.7 N=C(N)NCCC[C@@H](NC(=O)/C=C/c1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
71463271 83729 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 474 11 6 4 1.4 N=C(N)NCCC[C@H](NC(=O)c1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
CHEMBL2208294 83729 0 None 1 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation countingDisplacement of [3H]FFRF-NH2 from human flag-tagged NPFF1 receptor expressed in CHO cells by scintillation counting
ChEMBL 474 11 6 4 1.4 N=C(N)NCCC[C@H](NC(=O)c1cccc2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(N)=O 10.1016/j.bmcl.2012.10.049
162676733 183002 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NPFF from human NPFFR1 expressed in CHO cell membranes incubated for 120 mins by scintillation/luminescence counting methodDisplacement of [125I]NPFF from human NPFFR1 expressed in CHO cell membranes incubated for 120 mins by scintillation/luminescence counting method
ChEMBL 444 11 1 5 4.8 CCCCCOC(=O)[C@@H]1C[C@H](NCc2ccc(OC)cc2)CN1Cc1ccccc1Cl 10.1021/acs.jmedchem.0c00643
CHEMBL4800557 183002 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]NPFF from human NPFFR1 expressed in CHO cell membranes incubated for 120 mins by scintillation/luminescence counting methodDisplacement of [125I]NPFF from human NPFFR1 expressed in CHO cell membranes incubated for 120 mins by scintillation/luminescence counting method
ChEMBL 444 11 1 5 4.8 CCCCCOC(=O)[C@@H]1C[C@H](NCc2ccc(OC)cc2)CN1Cc1ccccc1Cl 10.1021/acs.jmedchem.0c00643
118724978 115998 0 None 2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 408 9 5 4 1.4 N=C(N)NCC(=O)NCC1(NCc2ccccc2)CCCN(Cc2ccccc2)C1 10.1021/jm500989n
CHEMBL3361417 115998 0 None 2 2 Human 6.0 pKi = 6.0 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 408 9 5 4 1.4 N=C(N)NCC(=O)NCC1(NCc2ccccc2)CCCN(Cc2ccccc2)C1 10.1021/jm500989n
118724979 115999 0 None 3 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 444 8 5 4 2.9 N=C(N)NCC(=O)NCC1(Nc2cccc3ccccc23)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
CHEMBL3361418 115999 0 None 3 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysisDisplacement of [3H]NPVF from human NPFF1 receptor expressed in CHO cells after 1 hr by liquid scintillation counting analysis
ChEMBL 444 8 5 4 2.9 N=C(N)NCC(=O)NCC1(Nc2cccc3ccccc23)CCN(Cc2ccccc2)CC1 10.1021/jm500989n
101882819 1082 0 None 2 5 Human 7.1 pKi = 7.1 Binding
Binding affinity.Binding affinity.
Guide to Pharmacology 394 8 5 4 1.7 NC(=N)NCCNC(=O)C1(CCN(CC1)Cc1ccccc1)Nc1ccccc1 25268943
11235 1082 0 None 2 5 Human 7.1 pKi = 7.1 Binding
Binding affinity.Binding affinity.
Guide to Pharmacology 394 8 5 4 1.7 NC(=N)NCCNC(=O)C1(CCN(CC1)Cc1ccccc1)Nc1ccccc1 25268943
CHEMBL3361425 1082 0 None 2 5 Human 7.1 pKi = 7.1 Binding
Binding affinity.Binding affinity.
Guide to Pharmacology 394 8 5 4 1.7 NC(=N)NCCNC(=O)C1(CCN(CC1)Cc1ccccc1)Nc1ccccc1 25268943
1486 3271 23 None 1 2 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 16407169
53320361 3271 23 None 1 2 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 16407169
CHEMBL1672380 3271 23 None 1 2 Human 7.2 pKi = 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None NC(=N)NCCC[C@@H](C(=O)N[C@H](C(=O)N)Cc1ccccc1)NC(=O)C12CC3CC(C2)CC(C1)C3 16407169
1478 1504 0 None -199 2 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12242085
1478 1504 0 None -199 2 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12421602
4018 236 0 None - 1 Human 7.8 pKi = 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20354177
4017 235 0 None - 1 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20354177
123797 2751 23 None -1 4 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12242085
123797 2751 23 None -1 4 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12421602
123797 2751 23 None -1 4 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17011599
1479 2751 23 None -1 4 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12242085
1479 2751 23 None -1 4 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12421602
1479 2751 23 None -1 4 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17011599
CHEMBL429731 2751 23 None -1 4 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12242085
CHEMBL429731 2751 23 None -1 4 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12421602
CHEMBL429731 2751 23 None -1 4 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17011599
4016 3273 0 None 28 2 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12242085
4016 3273 0 None 28 2 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12421602
4016 3273 0 None 28 2 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17337079
1480 2954 0 None -707 2 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11024015
1480 2954 0 None -707 2 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12421602
1485 624 27 None -4 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 11024015
1485 624 27 None -4 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 12242085
1485 624 27 None -4 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 12421602
3474 624 27 None -4 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 11024015
3474 624 27 None -4 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 12242085
3474 624 27 None -4 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 12421602
5311023 624 27 None -4 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 11024015
5311023 624 27 None -4 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 12242085
5311023 624 27 None -4 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 12421602
CHEMBL332347 624 27 None -4 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 11024015
CHEMBL332347 624 27 None -4 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 12242085
CHEMBL332347 624 27 None -4 4 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 473 11 5 4 2.4 O=C([C@H](NC(=O)C(c1ccccc1)c1ccccc1)CCCN=C(N)N)NCc1ccc(cc1)O 12421602
132709 33 0 None -3 2 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11024015
132709 33 0 None -3 2 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12421602
132709 33 0 None -3 2 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17011599
1477 33 0 None -3 2 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11024015
1477 33 0 None -3 2 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12421602
1477 33 0 None -3 2 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17011599
1482 4065 0 None 25 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12242085
1482 4065 0 None 25 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12421602
155817415 4065 0 None 25 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12242085
155817415 4065 0 None 25 2 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12421602