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ChEMBL ligand: CHEMBL125021 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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]