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 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]