PSB-12062 [Ligand Id: 9542] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2180160
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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 pIC50 >=10000 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]
ChEMBL Antagonist activity at human P2X4R transfected in 1321N1 cells B 5.48 pIC50 3300 nM IC50 J Nat Prod (2019) 82: 2559-2567 [PMID:31532206]
ChEMBL Antagonist activity at human P2X4R transfected in HEK293 cells B 5.85 pIC50 1400 nM IC50 J Nat Prod (2019) 82: 2559-2567 [PMID:31532206]
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 5.86 pIC50 1380 nM IC50 J Med Chem (2012) 55: 9576-9588 [PMID:23075067]
GtoPdb - - 6 pIC50 - - - Mol Pharmacol (2013) 83: 759-69 [PMID:23253448];
Neuropharmacology (2016) 104: 31-49 [PMID:26686393]
ChEMBL Antagonist activity at human P2X4R transfected in HEK293 cells assessed as inhibition of ATP-mediated calcium influx measured after 10 mins by YOPRO-1 dye uptake assay B 6.12 pIC50 760 nM IC50 J Nat Prod (2019) 82: 2559-2567 [PMID:31532206]
ChEMBL Antagonist activity at human P2X4R transfected in 1321N1 cells assessed as inhibition of ATP-mediated calcium influx measured after 10 mins by Fura-2AM assay B 6.38 pIC50 420 nM IC50 J Nat Prod (2019) 82: 2559-2567 [PMID:31532206]
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 1760 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 6.03 pIC50 928 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]