Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Common
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
Relation
Activity
Value
AssayType

Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

1067 8490 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 8490 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 8490 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 8490 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 8490 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 8490 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 8490 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 195486 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 195486 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 178818 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 178818 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 177671 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 177671 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 9076 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 9076 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 9076 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 9076 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 8490 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 8490 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 8490 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 8490 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 8490 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 8490 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 8490 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 7356 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 7356 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 7356 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 7356 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 7356 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 7356 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 7356 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 7679 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 7679 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 7679 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 7679 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 7679 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 7679 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 6884 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 6884 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 6884 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 10328 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 10328 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 10328 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 10328 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 7684 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 7684 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 7684 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 10231 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 10231 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 10231 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 6856 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 6856 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 6856 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 8490 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 8490 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 8490 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 8490 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 8490 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 8490 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 8490 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 7681 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 7681 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 7681 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 7687 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 7687 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 7687 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 7685 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 7685 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 7685 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 7682 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 7682 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 7682 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 7682 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 7683 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 7683 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
Sel. page Similar-
ity
Common
name
GPCRdb
ID
#Vendors

Reference
ligand
Fold
selectivity
# Tested
GPCRs
Species

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

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

2284 210852 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 210852 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 8649 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 8649 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 8649 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 16814 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 16814 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 16555 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 16555 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 117182 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 117182 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 117182 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 149107 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 149107 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 115384 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 115384 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 131388 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 131388 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 117098 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 117098 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 117444 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 117444 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 16411 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 16411 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 16411 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 16235 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 16235 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 117152 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 117152 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 131389 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 131389 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 16344 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 16344 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 118077 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 118077 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 16349 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 16349 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 16393 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 16393 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 16542 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 16542 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 117442 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 117442 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 16548 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 16548 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 16898 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 16898 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 16754 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 16754 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 16417 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 16417 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 7679 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 7679 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 7679 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 16611 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 16611 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 16226 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 16226 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 16316 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 16316 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 131390 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 131390 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 16347 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 16347 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 16661 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 16661 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 117238 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 117238 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 16399 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 16399 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 103514 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 103514 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 16426 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 16426 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 16301 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 16301 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 16333 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 16333 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 176111 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 176111 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 16299 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 16299 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 16260 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 16260 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 16517 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 16517 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 16776 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 16776 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 16307 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 16307 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 16335 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 16335 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 116968 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 116968 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 7682 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 7682 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 7682 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 7682 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 16392 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 16392 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 16497 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 16497 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 16498 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 16498 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 115989 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 115989 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 116510 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 116510 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 16845 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 16845 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 170190 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 170190 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 131391 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 131391 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 16633 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 16633 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 7682 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 7682 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 7682 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 7682 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