A740003 [Ligand Id: 4119] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL255787 (A-740003)
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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 recombinant P2X7 receptor expressed in human THP1 cells assessed as inhibition of BzATP-induced IL1-beta release by enzyme-linked immunosorbent assay F 6.81 pIC50 156 nM IC50 Bioorg. Med. Chem. (2009) 17: 4861-4865 [PMID:19540765]
ChEMBL Antagonist activity at human P2X7R expressed in HEK293 cells assessed as inhibition of ATP-induced ethidium iodide uptake preincubated for 10 mins followed by ATP induction measured after 25 mins by fluorescence assay B 6.96 pIC50 109 nM IC50 Eur J Med Chem (2018) 143: 1361-1372 [PMID:29133043]
ChEMBL Antagonist activity at human recombinant P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of BzATP-induced pore formation flux by fluorometric assay F 7.04 pIC50 92 nM IC50 Bioorg. Med. Chem. (2009) 17: 4861-4865 [PMID:19540765]
ChEMBL Antagonist activity at P2X7 receptor in LPS/IFNc-differentiated human THP-1 cells assessed as inhibition of ATP-induced IL-1beta release preincubated for 30 mins followed by LPS stimulation for 4 hrs using cells treated with ATP for 30 mins by ELISA B 7.05 pIC50 89 nM IC50 Eur J Med Chem (2017) 139: 698-717 [PMID:28858765]
ChEMBL Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of ATP-induced ethidium iodide uptake preincubated for 10 mins followed by ATP addition measured after 20 mins by spectrofluorometric analysis B 7.07 pIC50 86 nM IC50 Eur J Med Chem (2017) 139: 698-717 [PMID:28858765]
ChEMBL Antagonist activity at human P2X7 receptor expressed in HEK293 cells assessed as inhibition of ATP-induced IL-1beta release preincubated for 30 mins followed by ATP addition measured after 30 mins by ELISA B 7.09 pIC50 82 nM IC50 Eur J Med Chem (2017) 139: 698-717 [PMID:28858765]
ChEMBL Antagonist activity at human recombinant P2X7 receptor assessed as inhibition of calcium flux by FLIPR assay F 7.36 pIC50 44 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 2093-2096 [PMID:18272365]
ChEMBL Antagonist activity at human recombinant P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of agonist-induced calcium flux by fluorometric assay F 7.4 pIC50 40 nM IC50 Bioorg. Med. Chem. (2009) 17: 4861-4865 [PMID:19540765]
GtoPdb - - 7.4 pIC50 40 nM IC50 J. Pharmacol. Exp. Ther. (2006) 319: 1376-85 [PMID:16982702]
ChEMBL Antagonist activity at human cloned P2X7 receptor expressed in HEK293 cells assessed as inhibition of calcium flux by FLIPR assay F 7.4 pIC50 39.81 nM IC50 J. Med. Chem. (2009) 52: 3366-3376 [PMID:19397270]
ChEMBL Antagonist activity at P2X7 receptor in human THP1 cells assessed as inhibition of BzATP-induced ethidium uptake F 7.4 pIC50 39.81 nM IC50 J. Med. Chem. (2009) 52: 3123-3141 [PMID:19191585]
P2X7/P2X purinoceptor 7 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5183] [GtoPdb: 484] [UniProtKB: Q9Z1M0]
ChEMBL Antagonist activity at P2X7R in Swiss Webster mouse peritoneal macrophages assessed as inhibition of ATP-induced propidium iodide uptake preincubated for 10 mins followed by ATP induction measured after 25 mins by fluorescence assay B 6.05 pIC50 897 nM IC50 Eur J Med Chem (2018) 143: 1361-1372 [PMID:29133043]
ChEMBL Antagonist activity at P2X7 receptor in LPS/IFNc-differentiated Swiss mouse peritoneal macrophages assessed as inhibition of ATP-induced IL-1beta release preincubated for 30 mins followed by LPS stimulation for 4 hrs using cells treated with ATP for 15 mins by ELISA B 6.95 pIC50 112 nM IC50 Eur J Med Chem (2017) 139: 698-717 [PMID:28858765]
ChEMBL Antagonist activity at P2X7 receptor in Swiss mouse peritoneal macrophages assessed as inhibition of BzATP-induced ethidium iodide uptake after 30 mins by spectrofluorometric analysis B 7.2 pIC50 63.33 nM IC50 Eur J Med Chem (2017) 139: 698-717 [PMID:28858765]
ChEMBL Antagonist activity at P2X7 receptor in Swiss mouse peritoneal macrophages assessed as inhibition of BzATP-induced current at holding potential of -60 mV preincubated for 5 mins followed by BzATP addition measured after 5 mins by Whole cell patch-clamp analysis B 7.33 pIC50 46.91 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 cloned P2X7 receptor expressed in HEK293 cells assessed as inhibition of calcium flux by FLIPR assay F 7.7 pIC50 19.95 nM IC50 J. Med. Chem. (2009) 52: 3366-3376 [PMID:19397270]
ChEMBL Activity at rat P2X7 receptor expressed in HEK cells assessed as effect on BzATP-induced ethidium uptake B 7.7 pIC50 19.95 nM IC50 J. Med. Chem. (2009) 52: 3123-3141 [PMID:19191585]
ChEMBL Antagonist activity at rat recombinant P2X7 receptor assessed as inhibition of calcium flux by FLIPR assay F 7.74 pIC50 18 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 2093-2096 [PMID:18272365]
ChEMBL Antagonist activity at rat recombinant P2X7 receptor expressed in human 1321N1 cells assessed as inhibition of agonist-induced calcium flux by fluorometric assay F 7.74 pIC50 18 nM IC50 Bioorg. Med. Chem. (2009) 17: 4861-4865 [PMID:19540765]

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]