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 Displacement of [3H]-A-804598 from human P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay B 7.17 pKi 68 nM Ki J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
ChEMBL Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis B 5.68 pIC50 2100 nM IC50 J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
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 Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5183] [GtoPdb: 484] [UniProtKB: Q9Z1M0]
ChEMBL Antagonist activity at mouse P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis B 5.54 pIC50 2900 nM IC50 J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
P2X7/P2X purinoceptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2496] [GtoPdb: 484] [UniProtKB: Q64663]
ChEMBL Displacement of [3H]-A-804598 from rat P2X7 receptor expressed in HEK293 cell membrane by in vitro binding assay B 6.7 pKi 200 nM Ki J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
ChEMBL Antagonist activity at rat P2X7 receptor expressed in HEK293 cells assessed as inhibition of BzATP-induced calcium-flux measured after 60 mins by FLIPR analysis B 6.04 pIC50 910 nM IC50 J Med Chem (2021) 64: 4891-4902 [PMID:33822617]
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 32:

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]