ML354 [Ligand Id: 9459] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1609104
  • 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]
PAR4/Proteinase activated receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4691] [GtoPdb: 350] [UniProtKB: Q96RI0]
GtoPdb Antagonism measured in a novel PAC-1 fluorescent αIIbβ3 activation assay. - 6.85 pIC50 140 nM IC50 Bioorg Med Chem Lett (2014) 24: 4708-13 [PMID:25176330]
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 6.85 pIC50 140 nM IC50 Bioorg Med Chem Lett (2014) 24: 4708-4713 [PMID:25176330]

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]