Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name
GPCRdb
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#Vendors

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ligand
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selectivity
# Tested
GPCRs
Species

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

Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

1067 1709 128 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 1709 128 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 1709 128 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 1709 128 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 1709 128 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 1709 128 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 1709 128 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 188707 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 188707 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 172039 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 172039 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 170892 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 170892 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 2296 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 2296 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 2296 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 2296 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 1709 128 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
119 1709 128 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
1262 1709 128 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
5410 1709 128 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
6992099 1709 128 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
CHEMBL96 1709 128 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
DB02530 1709 128 None 4 4 Rat 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
1064 568 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 568 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 568 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 568 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 568 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 568 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 568 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 892 49 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 892 49 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 892 49 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 892 49 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 892 49 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 892 49 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 3555 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 3555 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 3555 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 3555 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 897 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 897 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 897 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 3458 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 3458 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 3458 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 1709 128 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 1709 128 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 1709 128 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 1709 128 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 1709 128 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 1709 128 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 1709 128 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 894 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 894 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 894 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 900 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 900 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 900 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 898 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 898 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 898 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 895 12 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 895 12 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 895 12 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 895 12 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 896 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 896 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 (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ity
Common
name
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Reference
ligand
Fold
selectivity
# Tested
GPCRs
Species

p-value
(-log)
Activity
Type
Activity
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Activity
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Type
Assay
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weight
Rot
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H don

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Smiles

DOI

2284 204073 114 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human GABBR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GABBR1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 213 4 2 2 1.9 NCC(CC(=O)O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL701 204073 114 None - 0 Human 5.6 pAC50 = 5.6 Binding
Binding affinity towards human GABBR1 in an in vitro assay with cellular components measured by scintillation proximity assayBinding affinity towards human GABBR1 in an in vitro assay with cellular components measured by scintillation proximity assay
ChEMBL 213 4 2 2 1.9 NCC(CC(=O)O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5446 1868 57 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 1868 57 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 1868 57 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 10042 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 10042 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 9783 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 9783 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 110405 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 110405 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 110405 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 142329 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 142329 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 108607 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 108607 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 124610 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 124610 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 110321 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 110321 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 110667 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 110667 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 9639 55 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 9639 55 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 9639 55 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 9463 3 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 9463 3 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 110375 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 110375 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 124611 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 124611 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 9572 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 9572 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 111300 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 111300 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 9577 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 9577 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 9621 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 9621 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 9770 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 9770 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 110665 21 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 110665 21 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 9776 9 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 9776 9 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 10126 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 10126 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 9982 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 9982 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 9645 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 9645 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 892 49 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 892 49 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 892 49 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 9839 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 9839 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 9454 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 9454 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 9544 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 9544 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 124612 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 124612 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 9575 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 9575 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 9889 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 9889 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 110461 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 110461 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 9627 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 9627 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 96739 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 96739 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 9654 37 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 9654 37 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 9529 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 9529 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 9561 38 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 9561 38 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 169332 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 169332 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 9527 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 9527 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 9488 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 9488 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 9745 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 9745 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 10004 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 10004 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 9535 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 9535 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 9563 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 9563 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 110191 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 110191 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 895 12 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 895 12 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 895 12 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 895 12 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 9620 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 9620 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 9725 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 9725 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 9726 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 9726 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 109212 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 109212 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 109733 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 109733 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 10073 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 10073 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 163411 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 163411 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 124613 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 124613 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 9861 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 9861 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 895 12 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 895 12 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 895 12 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 895 12 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