saclofen [Ligand Id: 1078] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL312403
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  • GABAB receptor in Human [GtoPdb: 242]
  • GABAB receptor in Rat [GtoPdb: 242]
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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: 241240] [UniProtKB: O75899Q9UBS5]
ChEMBL Inhibition of Gamma-aminobutyric acid type B receptor B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (1995) 5: 237-240
ChEMBL Inhibition of Gamma-aminobutyric acid type B receptor B 4.48 pIC50 33000 nM IC50 Bioorg Med Chem Lett (1995) 5: 237-240
GABAB2/GABAB1 in Rat [GtoPdb: 241240] [UniProtKB: O88871Q9Z0U4]
GtoPdb - - 3.5 pIC50 - - - Nature (1997) 386: 239-46 [PMID:9069281]
GABAB receptor in Human [GtoPdb: 242]
GtoPdb - - 4.3 pKi - - - Br J Pharmacol (2000) 131: 1050-4 [PMID:11082110];
Biochem Pharmacol (2003) 65: 1103-13 [PMID:12663046]
GABAB receptor in Rat [GtoPdb: 242]
GtoPdb - - 5.4 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]