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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]