PSB-12054 [Ligand Id: 12566] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2180137
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
P2X1/P2X purinoceptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2094] [GtoPdb: 478] [UniProtKB: P51575]
ChEMBL Antagonist activity at human P2X1 receptor by cell-based calcium influx assay F 5.19 pIC50 6520 nM IC50 J Med Chem (2012) 55: 9576-9588 [PMID:23075067]
P2X2/P2X purinoceptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2531] [GtoPdb: 479] [UniProtKB: Q9UBL9]
ChEMBL Antagonist activity at human P2X2 receptor by cell-based calcium influx assay F 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 9576-9588 [PMID:23075067]
P2X3/P2X purinoceptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2998] [GtoPdb: 480] [UniProtKB: P56373]
ChEMBL Antagonist activity at human P2X3 receptor by cell-based calcium influx assay F 5 pIC50 10000 nM IC50 J Med Chem (2012) 55: 9576-9588 [PMID:23075067]
P2X4/P2X purinoceptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2104] [GtoPdb: 481] [UniProtKB: Q99571]
GtoPdb - - 6.7 pIC50 199 nM IC50 J Med Chem (2012) 55: 9576-88 [PMID:23075067]
ChEMBL Antagonist activity at human P2X4 receptor expressed in 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx compound preincubated for 30 mins before ATP treatment by Fluo-4 AM fluorescence method F 6.72 pIC50 189 nM IC50 J Med Chem (2012) 55: 9576-9588 [PMID:23075067]
ChEMBL Antagonist activity at human P2X4 receptor expressed in human 1321N1 cells assessed as inhibition of ATP-induced cytosolic calcium influx preincubated for 30 mins followed by ATP addition by Fluo-4 AM dye-based fluorescence assay B 6.72 pIC50 189 nM IC50 Bioorg Med Chem (2014) 22: 1077-1088 [PMID:24411477]
P2X4/P2X purinoceptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176849] [GtoPdb: 481] [UniProtKB: Q9JJX6]
ChEMBL Antagonist activity at mouse P2X4 receptor by cell-based calcium influx assay F 5.75 pIC50 1770 nM IC50 J Med Chem (2012) 55: 9576-9588 [PMID:23075067]
P2X4/P2X purinoceptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2818] [GtoPdb: 481] [UniProtKB: P51577]
ChEMBL Antagonist activity at rat P2X4 receptor by cell-based calcium influx assay F 5.68 pIC50 2100 nM IC50 J Med Chem (2012) 55: 9576-9588 [PMID:23075067]
P2X7/P2X purinoceptor 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4805] [GtoPdb: 484] [UniProtKB: Q99572]
ChEMBL Antagonist activity at human P2X7 receptor by cell-based calcium influx assay F 5 pIC50 >10000 nM IC50 J Med Chem (2012) 55: 9576-9588 [PMID:23075067]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]