YD-3 [Ligand Id: 9458] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL125021
  • PAR1/Proteinase-activated receptor 1 in Human [ChEMBL: CHEMBL3974] [GtoPdb: 347] [UniProtKB: P25116]
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  • PAR4/Proteinase activated receptor 4 in Human [ChEMBL: CHEMBL4691] [GtoPdb: 350] [UniProtKB: Q96RI0]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
PAR1/Proteinase-activated receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3974] [GtoPdb: 347] [UniProtKB: P25116]
ChEMBL Antagonist activity at PAR1 in PAR-1-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2014) 24: 4708-4713 [PMID:25176330]
ChEMBL Inhibition of PAR1 (unknown origin) B 5 pIC50 >10000 nM IC50 J Med Chem (2016) 59: 7690-7695 [PMID:27482618]
PAR4/Proteinase activated receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4691] [GtoPdb: 350] [UniProtKB: Q96RI0]
ChEMBL Antagonist activity at PAR4 in PAR-4-AP-stimulated human platelets compound pretreated for 5 mins by fluorescent PAC1 integrin alpha2bb3 activation assay B 6.89 pIC50 130 nM IC50 Bioorg Med Chem Lett (2014) 24: 4708-4713 [PMID:25176330]
ChEMBL Antagonist activity PAR4 (unknown origin) B 6.89 pIC50 130 nM IC50 J Med Chem (2016) 59: 7690-7695 [PMID:27482618]
GtoPdb Antagonism of PAR4-AP-stimulated human platelet aggregation. - 6.89 pIC50 130 nM IC50 Bioorg Med Chem Lett (2014) 24: 4708-13 [PMID:25176330]

ChEMBL data shown on this page come from version 32:

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]