A839977 [Ligand Id: 4122] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1628691 (A-839977)
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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 human P2X7 receptor expressed in human THP1 cells assessed as reduction in BzATP-induced IL-1beta levels preincubated for 30 mins followed by BzATP addition measured after 30 mins by ELISA B 7.43 pIC50 37.15 nM IC50 Eur J Med Chem (2017) 139: 698-717 [PMID:28858765]
ChEMBL Antagonist activity at human P2X7 receptor expressed in human 1321N1 cells assessed as reduction in agonist-induced intracellular Ca2+ levels preincubated for 3 mins followed by agonist addition measured up to 2 mins by Fluo-4 dye-based FLIPR assay B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2017) 139: 698-717 [PMID:28858765]
GtoPdb - - 7.7 pIC50 ~20 nM IC50 Br. J. Pharmacol. (2007) 151: 571-9 [PMID:17471177];
Br. J. Pharmacol. (2009) 157: 1203-14 [PMID:19558545];
Behav. Brain Res. (2009) 204: 77-81 [PMID:19464323]
ChEMBL Antagonist activity at human P2X7 receptor expressed in human THP1 cells assessed as reduction in BzATP-induced pore formation by measuring YO-PRO uptake by FLIPR assay B 8.18 pIC50 6.61 nM IC50 Eur J Med Chem (2017) 139: 698-717 [PMID:28858765]
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 human 1321N1 cells assessed as reduction in agonist-induced intracellular Ca2+ levels preincubated for 3 mins followed by agonist addition measured up to 2 mins by Fluo-4 dye-based FLIPR assay B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2017) 139: 698-717 [PMID:28858765]
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 human 1321N1 cells assessed as reduction in agonist-induced intracellular Ca2+ levels preincubated for 3 mins followed by agonist addition measured up to 2 mins by Fluo-4 dye-based FLIPR assay B 7.7 pIC50 20 nM IC50 Eur J Med Chem (2017) 139: 698-717 [PMID:28858765]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]