A438079 [Ligand Id: 4118] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL377219 (A-438079)
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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 in expressed in HEK293 cells assessed as inhibition of BzATP-induced EtBr uptake B 6.52 pIC50 300 nM IC50 Eur J Med Chem (2018) 151: 462-481 [PMID:29649742]
GtoPdb - - 6.9 pIC50 ~125 nM IC50 Br J Pharmacol (2007) 151: 571-9 [PMID:17471177]
ChEMBL Antagonist activity at human P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of calcium flux by FLIPR F 6.9 pIC50 125.89 nM IC50 J. Med. Chem. (2006) 49: 3659-3666 [PMID:16759108]
ChEMBL Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake F 6.9 pIC50 125.89 nM IC50 J. Med. Chem. (2009) 52: 3123-3141 [PMID:19191585]
ChEMBL Antagonist activity at human recombinant P2X7 receptor assessed as inhibition of BzATP-induced calcium flux by FLIPR assay F 6.91 pIC50 123.03 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 2089-2092 [PMID:18272366]
ChEMBL Antagonist activity at human recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of benzoylbenzoic ATP-induced calcium production by FLIPR assay F 6.91 pIC50 123.03 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 3297-3300 [PMID:21536435]
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 inhibition of calcium flux by FLIPR F 6.5 pIC50 316.23 nM IC50 J. Med. Chem. (2006) 49: 3659-3666 [PMID:16759108]
ChEMBL Activity at rat P2X7 receptor expressed in HEK cells assessed as effect on BzATP-induced ethidium uptake B 6.5 pIC50 316.23 nM IC50 J. Med. Chem. (2009) 52: 3123-3141 [PMID:19191585]
ChEMBL Antagonist activity at rat recombinant P2X7 receptor assessed as inhibition of BzATP-induced calcium flux by FLIPR assay F 6.51 pIC50 309.03 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 2089-2092 [PMID:18272366]
ChEMBL Antagonist activity at rat recombinant P2X7 receptor expressed in HEK293 cells assessed as inhibition of benzoylbenzoic ATP-induced calcium production by FLIPR assay F 6.51 pIC50 309.03 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 3297-3300 [PMID:21536435]

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]