Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type

 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
1067 1707 None 128 Human Functional pEC50 = 5.8 5.8 -4 4
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 1707 None 128 Human Functional pEC50 = 5.8 5.8 -4 4
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 1707 None 128 Human Functional pEC50 = 5.8 5.8 -4 4
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 1707 None 128 Human Functional pEC50 = 5.8 5.8 -4 4
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 1707 None 128 Human Functional pEC50 = 5.8 5.8 -4 4
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 1707 None 128 Human Functional pEC50 = 5.8 5.8 -4 4
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 1707 None 128 Human Functional pEC50 = 5.8 5.8 -4 4
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 188705 None 2 Human Functional pEC50 = 4.3 4.3 - 1
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 188705 None 2 Human Functional pEC50 = 4.3 4.3 - 1
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 172037 None 0 Human Functional pEC50 = 4.3 4.3 - 1
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 172037 None 0 Human Functional pEC50 = 4.3 4.3 - 1
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 170890 None 1 Human Functional pEC50 = 4.1 4.1 - 1
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 170890 None 1 Human Functional pEC50 = 4.1 4.1 - 1
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 2294 None 0 Human Functional pEC50 = 8.1 8.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 141 3 2 2 -0.3 NC[C@H](CP(=O)O)F None
7705 2294 None 0 Human Functional pEC50 = 8.1 8.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 141 3 2 2 -0.3 NC[C@H](CP(=O)O)F None
CHEMBL448343 2294 None 0 Human Functional pEC50 = 8.1 8.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 141 3 2 2 -0.3 NC[C@H](CP(=O)O)F None
DB11920 2294 None 0 Human Functional pEC50 = 8.1 8.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 141 3 2 2 -0.3 NC[C@H](CP(=O)O)F None
1067 1707 None 128 Rat Functional pIC50 = 8.3 8.3 4 4
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
119 1707 None 128 Rat Functional pIC50 = 8.3 8.3 4 4
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
1262 1707 None 128 Rat Functional pIC50 = 8.3 8.3 4 4
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
5410 1707 None 128 Rat Functional pIC50 = 8.3 8.3 4 4
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
6992099 1707 None 128 Rat Functional pIC50 = 8.3 8.3 4 4
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
CHEMBL96 1707 None 128 Rat Functional pIC50 = 8.3 8.3 4 4
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
DB02530 1707 None 128 Rat Functional pIC50 = 8.3 8.3 4 4
NoneNone
Drug Central 103 3 2 2 -0.2 NCCCC(=O)O None
1064 568 None 0 Rat Functional pIC50 = 4.5 4.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
3428 568 None 0 Rat Functional pIC50 = 4.5 4.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
44602 568 None 0 Rat Functional pIC50 = 4.5 4.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
6918881 568 None 0 Rat Functional pIC50 = 4.5 4.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
CHEMBL301742 568 None 0 Rat Functional pIC50 = 4.5 4.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
DB00181 568 None 0 Rat Functional pIC50 = 4.5 4.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
DB08891 568 None 0 Rat Functional pIC50 = 4.5 4.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 213 4 2 2 1.9 NC[C@@H](c1ccc(cc1)Cl)CC(=O)O 9069281
1069 891 None 49 Rat Functional pIC50 = 4.7 4.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 7650685
1069 891 None 49 Rat Functional pIC50 = 4.7 4.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 9069281
107699 891 None 49 Rat Functional pIC50 = 4.7 4.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 7650685
107699 891 None 49 Rat Functional pIC50 = 4.7 4.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 9069281
CHEMBL40157 891 None 49 Rat Functional pIC50 = 4.7 4.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 7650685
CHEMBL40157 891 None 49 Rat Functional pIC50 = 4.7 4.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 225 8 2 4 1.0 NCCCP(=O)(C(OCC)OCC)O 9069281
1081 96 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 122 3 2 2 0.1 NCCC[P+](=O)O 9069281
5381 96 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 122 3 2 2 0.1 NCCC[P+](=O)O 9069281
6335948 96 None 0 Rat Functional pIC50 = 5.6 5.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 122 3 2 2 0.1 NCCC[P+](=O)O 9069281
1075 3553 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 173 2 2 3 0.2 OC(=O)C[C@@H]1OCC(NC1)(C)C 7562513
5311429 3553 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 173 2 2 3 0.2 OC(=O)C[C@@H]1OCC(NC1)(C)C 7562513
86294992 3553 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 173 2 2 3 0.2 OC(=O)C[C@@H]1OCC(NC1)(C)C 7562513
CHEMBL1895916 3553 None 0 Rat Functional pIC50 = 6.4 6.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 173 2 2 3 0.2 OC(=O)C[C@@H]1OCC(NC1)(C)C 7562513
1072 896 None 0 Rat Functional pIC50 = 8.9 8.9 - 1
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 896 None 0 Rat Functional pIC50 = 8.9 8.9 - 1
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 896 None 0 Rat Functional pIC50 = 8.9 8.9 - 1
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 3456 None 0 Rat Functional pIC50 None 3.5 3.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 249 4 2 3 1.3 NCC(c1ccc(cc1)Cl)CS(=O)(=O)O 9069281
122150 3456 None 0 Rat Functional pIC50 None 3.5 3.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 249 4 2 3 1.3 NCC(c1ccc(cc1)Cl)CS(=O)(=O)O 9069281
CHEMBL312403 3456 None 0 Rat Functional pIC50 None 3.5 3.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 249 4 2 3 1.3 NCC(c1ccc(cc1)Cl)CS(=O)(=O)O 9069281
1068 68 None 0 Rat Functional pIC50 None 4.1 4.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 265 4 3 4 0.4 NCC(c1ccc(cc1)Cl)(CS(=O)(=O)O)O 9069281
1564 68 None 0 Rat Functional pIC50 None 4.1 4.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 265 4 3 4 0.4 NCC(c1ccc(cc1)Cl)(CS(=O)(=O)O)O 9069281
CHEMBL1256573 68 None 0 Rat Functional pIC50 None 4.1 4.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 265 4 3 4 0.4 NCC(c1ccc(cc1)Cl)(CS(=O)(=O)O)O 9069281
1067 1707 None 128 Rat Functional pIC50 None 4.6 4.6 4 4
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
119 1707 None 128 Rat Functional pIC50 None 4.6 4.6 4 4
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
1262 1707 None 128 Rat Functional pIC50 None 4.6 4.6 4 4
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
5410 1707 None 128 Rat Functional pIC50 None 4.6 4.6 4 4
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
6992099 1707 None 128 Rat Functional pIC50 None 4.6 4.6 4 4
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
CHEMBL96 1707 None 128 Rat Functional pIC50 None 4.6 4.6 4 4
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
DB02530 1707 None 128 Rat Functional pIC50 None 4.6 4.6 4 4
UnclassifiedUnclassified
Guide to Pharmacology 103 3 2 2 -0.2 NCCCC(=O)O 9069281
10154248 893 None 0 Human Functional pIC50 None 4.9 4.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 173 4 2 2 0.8 NCCCP(=O)(C(F)F)O 9069281
1066 893 None 0 Human Functional pIC50 None 4.9 4.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 173 4 2 2 0.8 NCCCP(=O)(C(F)F)O 9069281
CHEMBL113553 893 None 0 Human Functional pIC50 None 4.9 4.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 173 4 2 2 0.8 NCCCP(=O)(C(F)F)O 9069281
1074 899 None 0 Rat Functional pIC50 None 8.4 8.4 - 1
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 899 None 0 Rat Functional pIC50 None 8.4 8.4 - 1
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 899 None 0 Rat Functional pIC50 None 8.4 8.4 - 1
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 897 None 0 Rat Functional pIC50 None 8.6 8.6 - 1
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 897 None 0 Rat Functional pIC50 None 8.6 8.6 - 1
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 897 None 0 Rat Functional pIC50 None 8.6 8.6 - 1
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 894 None 12 Rat Functional pIC50 None 8.8 8.8 3 2
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 894 None 12 Rat Functional pIC50 None 8.8 8.8 3 2
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 894 None 12 Rat Functional pIC50 None 8.8 8.8 3 2
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 894 None 12 Rat Functional pIC50 None 8.8 8.8 3 2
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 895 None 0 Rat Functional pIC50 None 9.2 9.2 - 1
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 895 None 0 Rat Functional pIC50 None 9.2 9.2 - 1
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


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
2284 204071 None 114 Human Binding pAC50 = 5.6 5.6 - 0
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 204071 None 114 Human Binding pAC50 = 5.6 5.6 - 0
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
DB00181 204071 None 114 Human Binding pAC50 = 5.6 5.6 - 0
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 1866 None 57 Human Binding pEC50 = 7.1 7.1 - 0
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 1866 None 57 Human Binding pEC50 = 7.1 7.1 - 0
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 1866 None 57 Human Binding pEC50 = 7.1 7.1 - 0
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 10040 None 0 Rat Binding pIC50 = 6 6.0 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 10040 None 0 Rat Binding pIC50 = 6 6.0 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9781 None 2 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9781 None 2 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110403 None 8 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110403 None 8 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110403 None 8 Rat Binding pIC50 = 5 5.0 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 142327 None 1 Rat Binding pIC50 = 7.9 7.9 - 0
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 142327 None 1 Rat Binding pIC50 = 7.9 7.9 - 0
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 108605 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 108605 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 124608 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 124608 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
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 110319 None 2 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110319 None 2 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110665 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110665 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9637 None 55 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9637 None 55 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9637 None 55 Rat Binding pIC50 = 7.8 7.8 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9461 None 3 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9461 None 3 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110373 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110373 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 124609 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
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 124609 None 0 Rat Binding pIC50 = 7.8 7.8 - 0
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 9570 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9570 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 111298 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 111298 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9575 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9575 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9619 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9619 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9768 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9768 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110663 None 21 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110663 None 21 Rat Binding pIC50 = 5.7 5.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9774 None 9 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9774 None 9 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 10124 None 2 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 10124 None 2 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9980 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9980 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9643 None 1 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9643 None 1 Rat Binding pIC50 = 4.7 4.7 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 891 None 49 Rat Binding pIC50 = 4.6 4.6 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 891 None 49 Rat Binding pIC50 = 4.6 4.6 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 891 None 49 Rat Binding pIC50 = 4.6 4.6 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9837 None 2 Rat Binding pIC50 = 4.6 4.6 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9837 None 2 Rat Binding pIC50 = 4.6 4.6 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9452 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9452 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9542 None 2 Rat Binding pIC50 = 4.5 4.5 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9542 None 2 Rat Binding pIC50 = 4.5 4.5 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 124610 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 124610 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
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 9573 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9573 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9887 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9887 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110459 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110459 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9625 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9625 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 96737 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 96737 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9652 None 37 Rat Binding pIC50 = 4.4 4.4 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9652 None 37 Rat Binding pIC50 = 4.4 4.4 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9527 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9527 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9559 None 38 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9559 None 38 Rat Binding pIC50 = 5.4 5.4 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 169330 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 169330 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9525 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9525 None 0 Rat Binding pIC50 = 8.3 8.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9486 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9486 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9743 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9743 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 10002 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 10002 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9533 None 1 Rat Binding pIC50 = 4.3 4.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9533 None 1 Rat Binding pIC50 = 4.3 4.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9561 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9561 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110189 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 110189 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 894 None 12 Human Binding pIC50 = 8.2 8.2 - 1
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 894 None 12 Human Binding pIC50 = 8.2 8.2 - 1
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 894 None 12 Human Binding pIC50 = 8.2 8.2 - 1
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 894 None 12 Human Binding pIC50 = 8.2 8.2 - 1
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 9618 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9618 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9723 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9723 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9724 None 4 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9724 None 4 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 109210 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 109210 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 109731 None 0 Rat Binding pIC50 = 4.1 4.1 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 109731 None 0 Rat Binding pIC50 = 4.1 4.1 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 10071 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 10071 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 163409 None 1 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 163409 None 1 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 124611 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
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 124611 None 0 Rat Binding pIC50 = 8.0 8.0 - 0
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 9859 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 9859 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid 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 894 None 12 Human Binding pKi = 8.5 8.5 - 1
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 894 None 12 Human Binding pKi = 8.5 8.5 - 1
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 894 None 12 Human Binding pKi = 8.5 8.5 - 1
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 894 None 12 Human Binding pKi = 8.5 8.5 - 1
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