[3H]A804598 [Ligand Id: 5408] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL574539 (A-804598)
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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 Antagonist activity against human P2X7R expressed in human 1321N1 cell membrane incubated for 1 hrs by radioligand binding assay B 7.96 pIC50 11 nM IC50 ACS Med Chem Lett (2022) 13: 1564-1567 [PMID:36262403]
ChEMBL Binding affinity at human P2X7 receptor B 8 pIC50 10 nM IC50 Bioorg Med Chem (2009) 17: 4861-4865 [PMID:19540765]
P2X7/P2X purinoceptor 7 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5183] [GtoPdb: 484] [UniProtKB: Q9Z1M0]
ChEMBL Binding affinity at mouse P2X7 receptor B 8 pIC50 10 nM IC50 Bioorg Med Chem (2009) 17: 4861-4865 [PMID:19540765]
ChEMBL Antagonist activity against mouse P2X7R expressed in human 1321N1 cell membrane incubated for 1 hrs by radioligand binding assay B 8.05 pIC50 9 nM IC50 ACS Med Chem Lett (2022) 13: 1564-1567 [PMID:36262403]
P2X7/P2X purinoceptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663]
ChEMBL Binding affinity at rat P2X7 receptor B 8 pIC50 10 nM IC50 Bioorg Med Chem (2009) 17: 4861-4865 [PMID:19540765]
ChEMBL Antagonist activity against rat P2X7R expressed in human 1321N1 cell membrane incubated for 1 hrs by radioligand binding assay B 8 pIC50 10 nM IC50 ACS Med Chem Lett (2022) 13: 1564-1567 [PMID:36262403]

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]