A804598 [Ligand Id: 4121] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1628690 (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 at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced YO-PRO-1 Iodide uptake measured every 30 secs for 1 hr by fluorescence assay B 7.03 pIC50 93 nM IC50 Eur J Med Chem (2017) 130: 433-439 [PMID:28279849]
GtoPdb - - 8 pIC50 ~10 nM IC50
ChEMBL Antagonist activity at P2X7 receptor in LPS-stimulated human THP1 cells assessed as inhibition of LPS/BzATP-induced IL-1beta release preincubated for 30 mins followed by BzATP addition measured after 30 mins by ELISA B 8.05 pIC50 9 nM IC50 Eur J Med Chem (2017) 130: 433-439 [PMID:28279849]
ChEMBL Antagonist activity at human P2X7 receptor expressed in 1321N1 cells assessed as inhibition of agonist-induced calcium flux pretreated for 3 mins followed by BzATP addition after 3 mins measured every 1 sec for 60 secs and at 5 secs interval throughout testing by Flou-4-AM dye based FLIPR assay B 8.05 pIC50 9 nM IC50 Eur J Med Chem (2017) 130: 433-439 [PMID:28279849]
P2X7/P2X purinoceptor 7 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5183] [GtoPdb: 484] [UniProtKB: Q9Z1M0]
ChEMBL Antagonist activity at mouse P2X7 receptor expressed in 1321N1 cells assessed as inhibition of agonist-induced calcium flux pretreated for 3 mins followed by BzATP addition after 3 mins measured every 1 sec for 60 secs and at 5 secs interval throughout testing by Flou-4-AM dye based FLIPR assay B 8.05 pIC50 9 nM IC50 Eur J Med Chem (2017) 130: 433-439 [PMID:28279849]
P2X7/P2X purinoceptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663]
ChEMBL Antagonist activity at rat P2X7 receptor expressed in 1321N1 cells assessed as inhibition of agonist-induced calcium flux pretreated for 3 mins followed by BzATP addition after 3 mins measured every 1 sec for 60 secs and at 5 secs interval throughout testing by Flou-4-AM dye based FLIPR assay B 8.05 pIC50 9 nM IC50 Eur J Med Chem (2017) 130: 433-439 [PMID:28279849]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]