ChEMBL ligand: CHEMBL2103856 (Atopaxar, E-5555, E5555, ER-172594-00)
PAR1/Proteinase-activated receptor 1 in Human [ChEMBL: CHEMBL3974] [GtoPdb: 347] [UniProtKB: P25116] There should be some charts here, you may need to enable JavaScript!

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 human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay	F	7.48	pIC50	33	nM	IC50	Bioorg Med Chem (2018) 26: 2514-2529 [PMID:29685684]
ChEMBL	Antagonist activity at PAR1 in human EAhy926 cells assessed as inhibition of TFLLRN-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by TFLLRN-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay	F	7.5	pIC50	31.62	nM	IC50	Bioorg Med Chem (2018) 26: 2514-2529 [PMID:29685684]
GtoPdb	-	-	7.72	pIC50	19	nM	IC50	Eur J Pharmacol (2011) 657: 131-7 [PMID:21300059]

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]