AZ11645373 [Ligand Id: 4142] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL338117
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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 In vitro antagonism of P2X 7 receptor in THP-1 (human pre-monocytic) cells. F 7.7 pKd 19.95 nM Kd Bioorg Med Chem Lett (2003) 13: 4043-4046 [PMID:14592504]
ChEMBL Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake F 7.7 pKd 19.95 nM Kd J Med Chem (2009) 52: 3123-3141 [PMID:19191585]
ChEMBL Inhibition of human P2X7 receptor B 7.51 pIC50 31 nM IC50 Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538]
P2X7/P2X purinoceptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663]
ChEMBL Inhibition of rat P2X7 receptor B 4 pIC50 >100000 nM IC50 Bioorg Med Chem Lett (2015) 25: 3164-3167 [PMID:26099538]

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]