stiripentol [Ligand Id: 5469] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1983350 (BCX 2600, BCX-2600, Diacomit, Stiripentol)
  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2095172] [GtoPdb: 404414411] [UniProtKB: P14867P18507P47870]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095172] [GtoPdb: 404414411] [UniProtKB: P14867P18507P47870]
ChEMBL Agonist activity at GABA alpha1beta2gamma2 receptor in human HEK293T at -50 mV holding potential by whole cell voltage clamp assay B 4.34 pEC50 46000 nM EC50 Eur J Med Chem (2019) 183: 111650-111650 [PMID:31539780]

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]