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 33:

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]