Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
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
1067 1679 121 None -4 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
ChEMBL 103 3 2 2 -0.2 NCCCC(=O)O 10.1021/jm7015842
119 1679 121 None -4 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
ChEMBL 103 3 2 2 -0.2 NCCCC(=O)O 10.1021/jm7015842
1262 1679 121 None -4 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
ChEMBL 103 3 2 2 -0.2 NCCCC(=O)O 10.1021/jm7015842
5410 1679 121 None -4 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
ChEMBL 103 3 2 2 -0.2 NCCCC(=O)O 10.1021/jm7015842
6992099 1679 121 None -4 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
ChEMBL 103 3 2 2 -0.2 NCCCC(=O)O 10.1021/jm7015842
CHEMBL96 1679 121 None -4 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
ChEMBL 103 3 2 2 -0.2 NCCCC(=O)O 10.1021/jm7015842
DB02530 1679 121 None -4 4 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
ChEMBL 103 3 2 2 -0.2 NCCCC(=O)O 10.1021/jm7015842
11701095 188121 2 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
ChEMBL 161 1 2 2 0.9 CP(=O)(O)C1=CCC(N)C1 10.1021/jm7015842
CHEMBL504482 188121 2 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
ChEMBL 161 1 2 2 0.9 CP(=O)(O)C1=CCC(N)C1 10.1021/jm7015842
24895101 171473 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
ChEMBL 161 1 2 2 0.9 CP(=O)(O)C1=CC[C@H](N)C1 10.1021/jm7015842
CHEMBL447171 171473 0 None - 1 Human 4.3 pEC50 = 4.3 Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
ChEMBL 161 1 2 2 0.9 CP(=O)(O)C1=CC[C@H](N)C1 10.1021/jm7015842
24895106 170325 1 None - 1 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
ChEMBL 161 1 2 2 0.9 CP(=O)(O)C1=CC[C@@H](N)C1 10.1021/jm7015842
CHEMBL445449 170325 1 None - 1 Human 4.1 pEC50 = 4.1 Functional
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp methodAgonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
ChEMBL 161 1 2 2 0.9 CP(=O)(O)C1=CC[C@@H](N)C1 10.1021/jm7015842
16686147 2264 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 141 3 2 2 -0.3 NC[C@H](CP(=O)O)F None
7705 2264 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 141 3 2 2 -0.3 NC[C@H](CP(=O)O)F None
CHEMBL448343 2264 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 141 3 2 2 -0.3 NC[C@H](CP(=O)O)F None
DB11920 2264 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 141 3 2 2 -0.3 NC[C@H](CP(=O)O)F None
1067 1679 121 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
119 1679 121 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
1262 1679 121 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
5410 1679 121 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
6992099 1679 121 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
CHEMBL96 1679 121 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
DB02530 1679 121 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
1064 562 0 None - 1 Rat 4.5 pIC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
3428 562 0 None - 1 Rat 4.5 pIC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
44602 562 0 None - 1 Rat 4.5 pIC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
6918881 562 0 None - 1 Rat 4.5 pIC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
CHEMBL301742 562 0 None - 1 Rat 4.5 pIC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
DB00181 562 0 None - 1 Rat 4.5 pIC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
DB08891 562 0 None - 1 Rat 4.5 pIC50 = 4.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
1069 879 40 None - 1 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 7650685
1069 879 40 None - 1 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 9069281
107699 879 40 None - 1 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 7650685
107699 879 40 None - 1 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 9069281
CHEMBL40157 879 40 None - 1 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 7650685
CHEMBL40157 879 40 None - 1 Rat 4.7 pIC50 = 4.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 9069281
1081 96 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 122 3 2 2 0.1 NCCC[P+](=O)O 9069281
5381 96 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 122 3 2 2 0.1 NCCC[P+](=O)O 9069281
6335948 96 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 122 3 2 2 0.1 NCCC[P+](=O)O 9069281
1075 3499 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 2 3 0.2 OC(=O)C[C@@H]1OCC(NC1)(C)C 7562513
5311429 3499 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 2 3 0.2 OC(=O)C[C@@H]1OCC(NC1)(C)C 7562513
86294992 3499 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 2 3 0.2 OC(=O)C[C@@H]1OCC(NC1)(C)C 7562513
CHEMBL1895916 3499 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 2 2 3 0.2 OC(=O)C[C@@H]1OCC(NC1)(C)C 7562513
1072 884 0 None - 1 Rat 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 421 10 3 5 3.2 COc1ccc(cc1)CP(=O)(C[C@H](CN([C@@H](c1cccc(c1)C(=O)O)C)C)O)O 9069281
3429 884 0 None - 1 Rat 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 421 10 3 5 3.2 COc1ccc(cc1)CP(=O)(C[C@H](CN([C@@H](c1cccc(c1)C(=O)O)C)C)O)O 9069281
5310936 884 0 None - 1 Rat 8.9 pIC50 = 8.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 421 10 3 5 3.2 COc1ccc(cc1)CP(=O)(C[C@H](CN([C@@H](c1cccc(c1)C(=O)O)C)C)O)O 9069281
1078 3402 0 None - 1 Rat 3.5 pIC50 None 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 249 4 2 3 1.3 NCC(c1ccc(cc1)Cl)CS(=O)(=O)O 9069281
122150 3402 0 None - 1 Rat 3.5 pIC50 None 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 249 4 2 3 1.3 NCC(c1ccc(cc1)Cl)CS(=O)(=O)O 9069281
CHEMBL312403 3402 0 None - 1 Rat 3.5 pIC50 None 3.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 249 4 2 3 1.3 NCC(c1ccc(cc1)Cl)CS(=O)(=O)O 9069281
1068 68 0 None - 1 Rat 4.1 pIC50 None 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 265 4 3 4 0.4 NCC(c1ccc(cc1)Cl)(CS(=O)(=O)O)O 9069281
1564 68 0 None - 1 Rat 4.1 pIC50 None 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 265 4 3 4 0.4 NCC(c1ccc(cc1)Cl)(CS(=O)(=O)O)O 9069281
CHEMBL1256573 68 0 None - 1 Rat 4.1 pIC50 None 4.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 265 4 3 4 0.4 NCC(c1ccc(cc1)Cl)(CS(=O)(=O)O)O 9069281
1067 1679 121 None 4 4 Rat 4.6 pIC50 None 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
119 1679 121 None 4 4 Rat 4.6 pIC50 None 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
1262 1679 121 None 4 4 Rat 4.6 pIC50 None 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
5410 1679 121 None 4 4 Rat 4.6 pIC50 None 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
6992099 1679 121 None 4 4 Rat 4.6 pIC50 None 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
CHEMBL96 1679 121 None 4 4 Rat 4.6 pIC50 None 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
DB02530 1679 121 None 4 4 Rat 4.6 pIC50 None 4.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
10154248 881 0 None - 1 Human 4.9 pIC50 None 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 4 2 2 0.8 NCCCP(=O)(C(F)F)O 9069281
1066 881 0 None - 1 Human 4.9 pIC50 None 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 4 2 2 0.8 NCCCP(=O)(C(F)F)O 9069281
CHEMBL113553 881 0 None - 1 Human 4.9 pIC50 None 4.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 173 4 2 2 0.8 NCCCP(=O)(C(F)F)O 9069281
1074 887 0 None - 1 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 659 15 6 7 4.5 [N-]=[N+]=Nc1cc(O)c(cc1I)C(=O)NCCCCCP(=O)(C[C@H](CN[C@@H](c1cccc(c1)C(=O)O)C)O)O 9069281
6324595 887 0 None - 1 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 659 15 6 7 4.5 [N-]=[N+]=Nc1cc(O)c(cc1I)C(=O)NCCCCCP(=O)(C[C@H](CN[C@@H](c1cccc(c1)C(=O)O)C)O)O 9069281
CHEMBL1909011 887 0 None - 1 Rat 8.4 pIC50 None 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 659 15 6 7 4.5 [N-]=[N+]=Nc1cc(O)c(cc1I)C(=O)NCCCCCP(=O)(C[C@H](CN[C@@H](c1cccc(c1)C(=O)O)C)O)O 9069281
1073 885 0 None - 1 Rat 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 646 16 6 6 3.9 O=C(CCc1ccc(c(c1)I)O)NCCCCCP(=O)(C[C@H](CN[C@@H](c1cccc(c1)C(=O)O)C)O)O 9069281
5311043 885 0 None - 1 Rat 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 646 16 6 6 3.9 O=C(CCc1ccc(c(c1)I)O)NCCCCCP(=O)(C[C@H](CN[C@@H](c1cccc(c1)C(=O)O)C)O)O 9069281
CHEMBL1909010 885 0 None - 1 Rat 8.6 pIC50 None 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 646 16 6 6 3.9 O=C(CCc1ccc(c(c1)I)O)NCCCCCP(=O)(C[C@H](CN[C@@H](c1cccc(c1)C(=O)O)C)O)O 9069281
1070 882 9 None 3 2 Rat 8.8 pIC50 None 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 407 8 3 3 4.9 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@H](c1ccc(c(c1)Cl)Cl)C 9069281
1090 882 9 None 3 2 Rat 8.8 pIC50 None 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 407 8 3 3 4.9 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@H](c1ccc(c(c1)Cl)Cl)C 9069281
197584 882 9 None 3 2 Rat 8.8 pIC50 None 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 407 8 3 3 4.9 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@H](c1ccc(c(c1)Cl)Cl)C 9069281
CHEMBL1213187 882 9 None 3 2 Rat 8.8 pIC50 None 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 407 8 3 3 4.9 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@H](c1ccc(c(c1)Cl)Cl)C 9069281
1071 883 0 None - 1 Rat 9.2 pIC50 None 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 383 9 4 4 3.2 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@@H](c1cccc(c1)C(=O)O)C 9069281
9800175 883 0 None - 1 Rat 9.2 pIC50 None 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 383 9 4 4 3.2 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@@H](c1cccc(c1)C(=O)O)C 9069281




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
5446 1838 50 None - 0 Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alonePositive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alone
ChEMBL 337 6 2 7 3.8 CSc1nc(NC2CCCC2)c(c(n1)NC1CCCC1)[N+](=O)[O-] 10.1016/j.bmcl.2017.03.084
6604928 1838 50 None - 0 Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alonePositive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alone
ChEMBL 337 6 2 7 3.8 CSc1nc(NC2CCCC2)c(c(n1)NC1CCCC1)[N+](=O)[O-] 10.1016/j.bmcl.2017.03.084
CHEMBL392394 1838 50 None - 0 Human 7.1 pEC50 = 7.1 Binding
Positive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alonePositive allosteric modulation at human GABA-B 1b expressed in CHO cells co-expressing rat GABA-B2 assessed as potentiation of GABA-induced inhibition of 7beta forskolin-stimulated cyclic AMP formation after 2 hrs in presence of 0.3 uM GABA relative to 100 uM GABA alone
ChEMBL 337 6 2 7 3.8 CSc1nc(NC2CCCC2)c(c(n1)NC1CCCC1)[N+](=O)[O-] 10.1016/j.bmcl.2017.03.084
9964332 9947 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 193 6 2 3 0.6 CC(=O)CCP(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL115162 9947 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 193 6 2 3 0.6 CC(=O)CCP(=O)(O)CCCN 10.1021/jm00017a016
9813169 9690 2 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 213 5 2 2 1.8 NCCCP(=O)(O)Cc1ccccc1 10.1021/jm00017a016
CHEMBL113613 9690 2 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 213 5 2 2 1.8 NCCCP(=O)(O)Cc1ccccc1 10.1021/jm00017a016
28560001 109916 8 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 227 6 2 2 1.8 NCCCP(=O)(O)CCc1ccccc1 10.1021/jm00017a016
659968 109916 8 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 227 6 2 2 1.8 NCCCP(=O)(O)CCc1ccccc1 10.1021/jm00017a016
CHEMBL324407 109916 8 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 227 6 2 2 1.8 NCCCP(=O)(O)CCc1ccccc1 10.1021/jm00017a016
9883500 141797 1 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay.
ChEMBL 318 1 1 2 4.6 CC(=O)[C@H]1CCC2C3CC[C@H]4C[C@H](O)CC[C@]4(C)C3CC[C@@]21C nan
CHEMBL38856 141797 1 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay.
ChEMBL 318 1 1 2 4.6 CC(=O)[C@H]1CCC2C3CC[C@H]4C[C@H](O)CC[C@]4(C)C3CC[C@@]21C nan
10377028 108120 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 241 8 3 5 -0.1 CCOC(OCC)P(=O)(O)C[C@@H](O)CN 10.1021/jm00017a016
CHEMBL320533 108120 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 241 8 3 5 -0.1 CCOC(OCC)P(=O)(O)C[C@@H](O)CN 10.1021/jm00017a016
58227083 124090 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay.
ChEMBL 321 1 1 3 4.0 C[C@]12CC[C@@H](O)C[C@@H]1CCC1C2CC[C@@]2(C)C1CC[C@@H]2[N+](=O)[O-] nan
CHEMBL3640615 124090 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay.
ChEMBL 321 1 1 3 4.0 C[C@]12CC[C@@H](O)C[C@@H]1CCC1C2CC[C@@]2(C)C1CC[C@@H]2[N+](=O)[O-] nan
9920531 109832 2 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 179 5 2 2 1.3 CC(C)CP(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL323887 109832 2 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 179 5 2 2 1.3 CC(C)CP(=O)(O)CCCN 10.1021/jm00017a016
10352529 110178 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 191 5 2 3 0.2 NCC(=O)CP(=O)(O)CC1CC1 10.1021/jm00017a016
CHEMBL325932 110178 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 191 5 2 3 0.2 NCC(=O)CP(=O)(O)CC1CC1 10.1021/jm00017a016
28559746 9548 46 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 137 3 2 2 0.2 CP(=O)(O)CCCN 10.1021/jm00017a016
5230 9548 46 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 137 3 2 2 0.2 CP(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL112710 9548 46 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 137 3 2 2 0.2 CP(=O)(O)CCCN 10.1021/jm00017a016
9920471 9372 2 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 165 5 2 2 1.0 CCCP(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL111890 9372 2 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 165 5 2 2 1.0 CCCP(=O)(O)CCCN 10.1021/jm00017a016
9964768 109886 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 241 8 3 5 -0.1 CCOC(OCC)P(=O)(O)CC(O)CN 10.1021/jm00017a016
CHEMBL324244 109886 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 241 8 3 5 -0.1 CCOC(OCC)P(=O)(O)CC(O)CN 10.1021/jm00017a016
58227084 124091 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay.
ChEMBL 335 1 1 3 4.4 C[C@]12CC[C@@](C)(O)C[C@@H]1CCC1C2CC[C@@]2(C)C1CC[C@@H]2[N+](=O)[O-] nan
CHEMBL3640616 124091 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay.
ChEMBL 335 1 1 3 4.4 C[C@]12CC[C@@](C)(O)C[C@@H]1CCC1C2CC[C@@]2(C)C1CC[C@@H]2[N+](=O)[O-] nan
9815542 9481 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 195 6 3 3 0.7 CCCC(O)P(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL112408 9481 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 195 6 3 3 0.7 CCCC(O)P(=O)(O)CCCN 10.1021/jm00017a016
9878233 110812 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 253 8 2 4 1.7 CC(C)OC(OC(C)C)P(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL326622 110812 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 253 8 2 4 1.7 CC(C)OC(OC(C)C)P(=O)(O)CCCN 10.1021/jm00017a016
10105390 9486 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 233 6 2 2 2.6 NCCCP(=O)(O)CCC1CCCCC1 10.1021/jm00017a016
CHEMBL112460 9486 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 233 6 2 2 2.6 NCCCP(=O)(O)CCC1CCCCC1 10.1021/jm00017a016
10466591 9530 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 235 6 2 3 1.6 NCCCP(=O)(O)CCC1CCCCO1 10.1021/jm00017a016
CHEMBL112639 9530 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 235 6 2 3 1.6 NCCCP(=O)(O)CCC1CCCCO1 10.1021/jm00017a016
44341174 9678 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 343 9 5 5 -0.5 NCCCP(=O)(O)CC(O)CNC(=O)c1ccccc1C(N)=O 10.1021/jm00017a016
CHEMBL113540 9678 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 343 9 5 5 -0.5 NCCCP(=O)(O)CC(O)CNC(=O)c1ccccc1C(N)=O 10.1021/jm00017a016
9898878 110176 15 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 151 4 2 2 0.6 CCP(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL325921 110176 15 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 151 4 2 2 0.6 CCP(=O)(O)CCCN 10.1021/jm00017a016
130023 9684 8 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 207 8 2 2 2.2 CCCCCCP(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL113571 9684 8 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 207 8 2 2 2.2 CCCCCCP(=O)(O)CCCN 10.1021/jm00017a016
9878836 10031 2 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 281 12 2 4 2.5 CCCCOC(OCCCC)P(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL115664 10031 2 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 281 12 2 4 2.5 CCCCOC(OCCCC)P(=O)(O)CCCN 10.1021/jm00017a016
9923821 9887 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 335 9 2 4 3.0 CCOC(OCC)P(=O)(O)CC(CN)c1ccc(Cl)cc1 10.1021/jm00017a016
CHEMBL114812 9887 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 335 9 2 4 3.0 CCOC(OCC)P(=O)(O)CC(CN)c1ccc(Cl)cc1 10.1021/jm00017a016
9877786 9554 1 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 215 6 2 2 2.0 CCCC(F)(F)P(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL112741 9554 1 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 215 6 2 2 2.0 CCCC(F)(F)P(=O)(O)CCCN 10.1021/jm00017a016
1069 879 40 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 10.1021/jm00017a016
107699 879 40 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 10.1021/jm00017a016
CHEMBL40157 879 40 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 10.1021/jm00017a016
9856380 9746 2 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 253 10 2 4 1.7 CCCOC(OCCC)P(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL114027 9746 2 None - 0 Rat 4.6 pIC50 = 4.6 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 253 10 2 4 1.7 CCCOC(OCCC)P(=O)(O)CCCN 10.1021/jm00017a016
10219796 9363 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 195 6 3 3 0.4 CCCCP(=O)(O)CC(O)CN 10.1021/jm00017a016
CHEMBL111817 9363 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 195 6 3 3 0.4 CCCCP(=O)(O)CC(O)CN 10.1021/jm00017a016
15134818 9453 2 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 180 6 3 3 -0.0 NCCCP(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL112291 9453 2 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 180 6 3 3 -0.0 NCCCP(=O)(O)CCCN 10.1021/jm00017a016
58227082 124092 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay.
ChEMBL 322 1 1 2 5.1 CS[C@H]1CCC2C3CC[C@H]4C[C@H](O)CC[C@]4(C)C3CC[C@@]21C nan
CHEMBL3640617 124092 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay.
ChEMBL 322 1 1 2 5.1 CS[C@H]1CCC2C3CC[C@H]4C[C@H](O)CC[C@]4(C)C3CC[C@@]21C nan
10466077 9484 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 221 5 2 3 1.2 NCCCP(=O)(O)CC1CCCCO1 10.1021/jm00017a016
CHEMBL112451 9484 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 221 5 2 3 1.2 NCCCP(=O)(O)CC1CCCCO1 10.1021/jm00017a016
10082524 9796 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 229 5 3 3 0.8 NC[C@@H](O)CP(=O)(O)Cc1ccccc1 10.1021/jm00017a016
CHEMBL114288 9796 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 229 5 3 3 0.8 NC[C@@H](O)CP(=O)(O)Cc1ccccc1 10.1021/jm00017a016
9877609 109972 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 193 4 2 3 0.7 NCCCP(=O)(O)C1CCCO1 10.1021/jm00017a016
CHEMBL324694 109972 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 193 4 2 3 0.7 NCCCP(=O)(O)C1CCCO1 10.1021/jm00017a016
10219657 9536 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 177 5 2 2 1.0 NCCCP(=O)(O)CC1CC1 10.1021/jm00017a016
CHEMBL112658 9536 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 177 5 2 2 1.0 NCCCP(=O)(O)CC1CC1 10.1021/jm00017a016
9834206 96291 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 195 6 3 3 0.7 CCCCP(=O)(O)C(O)CCN 10.1021/jm00017a016
CHEMBL264396 96291 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 195 6 3 3 0.7 CCCCP(=O)(O)C(O)CCN 10.1021/jm00017a016
130021 9563 29 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 179 6 2 2 1.4 CCCCP(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL112797 9563 29 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 179 6 2 2 1.4 CCCCP(=O)(O)CCCN 10.1021/jm00017a016
10058852 9438 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 207 4 2 3 1.1 NCCCP(=O)(O)C1CCCCO1 10.1021/jm00017a016
CHEMBL112213 9438 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 207 4 2 3 1.1 NCCCP(=O)(O)C1CCCCO1 10.1021/jm00017a016
130022 9470 30 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 219 5 2 2 2.2 NCCCP(=O)(O)CC1CCCCC1 10.1021/jm00017a016
CHEMBL112362 9470 30 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 219 5 2 2 2.2 NCCCP(=O)(O)CC1CCCCC1 10.1021/jm00017a016
10465678 168766 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 209 6 3 3 0.8 CCCCP(=O)(O)CC(C)(O)CN 10.1021/jm00017a016
CHEMBL441821 168766 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 209 6 3 3 0.8 CCCCP(=O)(O)CC(C)(O)CN 10.1021/jm00017a016
121956 9436 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 123 3 2 2 -0.2 NCCC[PH](=O)O 10.1021/jm00017a016
CHEMBL112203 9436 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 123 3 2 2 -0.2 NCCC[PH](=O)O 10.1021/jm00017a016
10354046 9397 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 235 5 3 3 1.2 NCC(O)CP(=O)(O)CC1CCCCC1 10.1021/jm00017a016
CHEMBL112019 9397 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 235 5 3 3 1.2 NCC(O)CP(=O)(O)CC1CCCCC1 10.1021/jm00017a016
10376775 9653 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 235 5 3 3 1.2 NC[C@H](O)CP(=O)(O)CC1CCCCC1 10.1021/jm00017a016
CHEMBL113435 9653 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 235 5 3 3 1.2 NC[C@H](O)CP(=O)(O)CC1CCCCC1 10.1021/jm00017a016
10398919 9909 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 229 5 3 3 0.8 NC[C@H](O)CP(=O)(O)Cc1ccccc1 10.1021/jm00017a016
CHEMBL114918 9909 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 229 5 3 3 0.8 NC[C@H](O)CP(=O)(O)Cc1ccccc1 10.1021/jm00017a016
15134810 9444 1 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 152 4 3 3 -0.5 NCCCP(=O)(O)CN 10.1021/jm00017a016
CHEMBL112248 9444 1 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 152 4 3 3 -0.5 NCCCP(=O)(O)CN 10.1021/jm00017a016
10243064 9472 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 233 5 2 3 1.4 NCC(=O)CP(=O)(O)CC1CCCCC1 10.1021/jm00017a016
CHEMBL112376 9472 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 233 5 2 3 1.4 NCC(=O)CP(=O)(O)CC1CCCCC1 10.1021/jm00017a016
10331452 109702 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 231 5 2 2 1.9 NCCCP(=O)(O)Cc1ccc(F)cc1 10.1021/jm00017a016
CHEMBL323713 109702 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 231 5 2 2 1.9 NCCCP(=O)(O)Cc1ccc(F)cc1 10.1021/jm00017a016
1070 882 9 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrsDisplacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrs
ChEMBL 407 8 3 3 4.9 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@H](c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2013.01.025
1090 882 9 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrsDisplacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrs
ChEMBL 407 8 3 3 4.9 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@H](c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2013.01.025
197584 882 9 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrsDisplacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrs
ChEMBL 407 8 3 3 4.9 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@H](c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2013.01.025
CHEMBL1213187 882 9 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrsDisplacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrs
ChEMBL 407 8 3 3 4.9 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@H](c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2013.01.025
10059083 9529 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 214 5 2 3 1.2 NCCCP(=O)(O)Cc1ccccn1 10.1021/jm00017a016
CHEMBL112638 9529 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 214 5 2 3 1.2 NCCCP(=O)(O)Cc1ccccn1 10.1021/jm00017a016
10084142 9633 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 263 4 3 3 1.4 CP(=O)(O)CC(O)(CN)c1ccc(Cl)cc1 10.1021/jm00017a016
CHEMBL113305 9633 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 263 4 3 3 1.4 CP(=O)(O)CC(O)(CN)c1ccc(Cl)cc1 10.1021/jm00017a016
5310935 9634 4 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 235 5 3 3 1.2 NC[C@@H](O)CP(=O)(O)CC1CCCCC1 10.1021/jm00017a016
CHEMBL113308 9634 4 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 235 5 3 3 1.2 NC[C@@H](O)CP(=O)(O)CC1CCCCC1 10.1021/jm00017a016
9882973 108725 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 305 7 3 3 2.6 CCCCP(=O)(O)CC(O)(CN)c1ccc(Cl)cc1 10.1021/jm00017a016
CHEMBL321688 108725 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 305 7 3 3 2.6 CCCCP(=O)(O)CC(O)(CN)c1ccc(Cl)cc1 10.1021/jm00017a016
9942295 109245 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 179 3 2 2 1.4 CC(C)(C)P(=O)(O)CCCN 10.1021/jm00017a016
CHEMBL322965 109245 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 179 3 2 2 1.4 CC(C)(C)P(=O)(O)CCCN 10.1021/jm00017a016
10105202 9978 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 229 5 3 3 0.8 NCC(O)CP(=O)(O)Cc1ccccc1 10.1021/jm00017a016
CHEMBL115354 9978 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 229 5 3 3 0.8 NCC(O)CP(=O)(O)Cc1ccccc1 10.1021/jm00017a016
10059688 162859 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 229 5 3 3 1.3 NCCCP(=O)(O)C(O)c1ccccc1 10.1021/jm00017a016
CHEMBL419582 162859 1 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 229 5 3 3 1.3 NCCCP(=O)(O)C(O)c1ccccc1 10.1021/jm00017a016
58227081 124093 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay.
ChEMBL 440 3 1 4 5.5 CN(C)c1ccc([C@H]2C[C@@]3(C)C(CC[C@@H]3[N+](=O)[O-])C3CC[C@H]4C[C@](C)(O)CCC4C32)cc1 nan
CHEMBL3640618 124093 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Binding Assay: [35S]TBPS binding assay.Binding Assay: [35S]TBPS binding assay.
ChEMBL 440 3 1 4 5.5 CN(C)c1ccc([C@H]2C[C@@]3(C)C(CC[C@@H]3[N+](=O)[O-])C3CC[C@H]4C[C@](C)(O)CCC4C32)cc1 nan
9813635 9768 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 247 4 2 2 2.3 CP(=O)(O)CC(CN)c1ccc(Cl)cc1 10.1021/jm00017a016
CHEMBL114128 9768 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex.
ChEMBL 247 4 2 2 2.3 CP(=O)(O)CC(CN)c1ccc(Cl)cc1 10.1021/jm00017a016
1070 882 9 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrsDisplacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrs
ChEMBL 407 8 3 3 4.9 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@H](c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2013.01.025
1090 882 9 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrsDisplacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrs
ChEMBL 407 8 3 3 4.9 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@H](c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2013.01.025
197584 882 9 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrsDisplacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrs
ChEMBL 407 8 3 3 4.9 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@H](c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2013.01.025
CHEMBL1213187 882 9 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrsDisplacement of [3H]CGP54626 from human recombinant GABAB1A receptor expressed in CHO cells after 3 hrs
ChEMBL 407 8 3 3 4.9 O[C@H](CP(=O)(CC1CCCCC1)O)CN[C@H](c1ccc(c(c1)Cl)Cl)C 10.1016/j.bmcl.2013.01.025