GSK1370319A [Ligand Id: 10503] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2218759
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572]
ChEMBL Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method B 6.75 pKi 176 nM Ki J Med Chem (2020) 63: 2074-2094 [PMID:31525963]
ChEMBL Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method B 6.06 pIC50 861.8 nM IC50 J Med Chem (2020) 63: 2074-2094 [PMID:31525963]
GtoPdb - - 6.32 pIC50 474 nM IC50 J Med Chem (2020) 63: 2074-2094 [PMID:31525963]
ChEMBL Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction in BzATP-stimulated TO-PRO-3 incorporation preincubated with compound and TO-PRO-3 for 15 mins prior to BzATP addition and measured after 1 hr by Fluo-3AM dye based flow cytometry B 6.32 pIC50 474 nM IC50 J Med Chem (2020) 63: 2074-2094 [PMID:31525963]
ChEMBL SUPPLEMENTARY: Inhibition of human P2X7 receptor assessed as inhibition of ethidium bromide accumulation. Same assay as CHEMBL1103860 B 7.9 pIC50 12.59 nM IC50 Structure-activity relationship data for chemical series of antagonists of the P2X7 receptor (Supplementary Bioactivity Data for publication CHEMBL1157114)

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]