PSB-0739 [Ligand Id: 5904] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL455536 (PSB-0739)
  • P2Y12 receptor/Purinergic receptor P2Y12 in Human [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
P2Y12 receptor/Purinergic receptor P2Y12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2001] [GtoPdb: 328] [UniProtKB: Q9H244]
ChEMBL Competitive antagonist activity at human P2Y12 receptor expressed in CHO cells assessed as forskolin/ 2-methylthio-ADP-induced cAMP production preincubated for 10 mins followed 2-methylthio-ADP addition measured after 3.5 hrs by luciferase reporter gene assay F 9.8 pKd 0.16 nM Kd J Med Chem (2017) 60: 3020-3038 [PMID:28306255]
GtoPdb - - 7.6 pKi 24.9 nM Ki J Med Chem (2009) 52: 3784-93 [PMID:19463000]
ChEMBL Displacement of [3H]PSB0413 from human platelet P2Y12 receptor B 7.6 pKi 24.9 nM Ki J Med Chem (2009) 52: 3784-3793 [PMID:19463000]
GtoPdb - - 9.8 pA2 - - - J Pharmacol Exp Ther (2009) 331: 648-55 [PMID:19690189]

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]