CGP 36742 [Ligand Id: 1085] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL112797 (CGP-36742, LU-AE-58479, Sgs 742, Sgs-742, Sgs742, SGS742) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| GABAB2/GABAB1/GABA-B receptor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111463] [GtoPdb: 241, 240] [UniProtKB: O75899, Q9UBS5] | ||||||||
| ChEMBL | Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique | F | 4.42 | pIC50 | 38000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 11-16 [PMID:24900248] |
| GABAB1/GABA-B receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2753] [GtoPdb: 240] [UniProtKB: Q9Z0U4] | ||||||||
| ChEMBL | Inhibition of binding of [3H]CGP-27492 to gamma-aminobutyric acid type B receptor of rat cortex. | B | 4.42 | pIC50 | 38000 | nM | IC50 | J Med Chem (1995) 38: 3313-3331 [PMID:7650685] |
| GABAA receptor ρ1 subunit/GABA receptor rho-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3561] [GtoPdb: 420] [UniProtKB: P24046] | ||||||||
| ChEMBL | Antagonist activity at human GABAc Rho1 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method | F | 4.21 | pIC50 | 62000 | nM | IC50 | J Med Chem (2008) 51: 3825-3840 [PMID:18528996] |
| ChEMBL | Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique | F | 4.21 | pIC50 | 62000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 11-16 [PMID:24900248] |
| GABAB receptor in Rat [GtoPdb: 242] | ||||||||
| GtoPdb | - | - | 5.6 | pIC50 | - | - | - | Pharmacol Rev (2002) 54: 247-64 [PMID:12037141] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
