ChEMBL ligand: CHEMBL493982 (SCH-530348, Vorapaxar)
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 human PAR1 in HCASMC assessed as inhibition of thrombin-induced thymidine incorporation	F	7.89	pKi	13	nM	Ki	J Med Chem (2008) 51: 3061-3064 [PMID:18447380]
ChEMBL	Displacement of [3H]haTRAP from PAR-1 isolated from human platelets by liquid scintillation counting analysis	B	8.07	pKi	8.5	nM	Ki	ACS Med Chem Lett (2014) 5: 183-187 [PMID:24900795]
GtoPdb	-	-	8.09	pKi	8.1	nM	Ki	J Med Chem (2008) 51: 3061-4 [PMID:18447380]
ChEMBL	Displacement of [3H]haTRAP from PAR1 in human platelets	B	8.09	pKi	8.1	nM	Ki	J Med Chem (2008) 51: 3061-3064 [PMID:18447380]
ChEMBL	Displacement of high affinity TRAP form human platelet PAR1	B	8.1	pKi	8	nM	Ki	Bioorg Med Chem Lett (2010) 20: 6676-6679 [PMID:20888225]
ChEMBL	Antagonist activity at human PAR1 in HCASMC assessed as inhibition of thrombin-induced calcium efflux	F	8.96	pKi	1.1	nM	Ki	J Med Chem (2008) 51: 3061-3064 [PMID:18447380]
ChEMBL	Antagonist activity at human PAR1 expressed in KNRK cells assessed as inhibition of agonist-induced intracellular calcium mobilization by fluorimetric assay	F	6.6	pIC50	250	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127046-127046 [PMID:32122739]
ChEMBL	Antagonist activity at PAR1 in human platelet rich plasma assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis	B	6.92	pIC50	120	nM	IC50	ACS Med Chem Lett (2013) 4: 1054-1058 [PMID:24900604]
ChEMBL	Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in thrombin-stimulated platelet aggregation preincubated for 3 mins followed by thrombin stimulation measured after 5 mins by aggregometric analysis	B	7.09	pIC50	81	nM	IC50	J Med Chem (2017) 60: 7166-7185 [PMID:28745507]
ChEMBL	Antagonist activity at human PAR1 expressed in HEK293 cells co-expressing Galpha15 assessed as inhibition of haTRAP-induced calcium mobilization preincubated for 15 mins followed by haTRAP addition by calcium-4 dye based FLIPR assay	F	7.19	pIC50	64	nM	IC50	J Med Chem (2017) 60: 7166-7185 [PMID:28745507]
ChEMBL	Antagonist activity at PAR1 in human platelets assessed as inhibition of thrombin-induced platelet aggregation	F	7.33	pIC50	47	nM	IC50	J Med Chem (2008) 51: 3061-3064 [PMID:18447380]
ChEMBL	Antagonist activity at PAR1 in human platelet-rich plasma assessed as reduction in TRAP-stimulated platelet aggregation preincubated for 20 mins followed by TRAP stimulation measured after 5 mins by aggregometric analysis	B	7.51	pIC50	31	nM	IC50	J Med Chem (2017) 60: 7166-7185 [PMID:28745507]
ChEMBL	Antagonist activity at PAR1 in human platelets assessed as inhibition of haTRAP-induced platelet aggregation	F	7.6	pIC50	25	nM	IC50	J Med Chem (2008) 51: 3061-3064 [PMID:18447380]
ChEMBL	Antagonist activity at PAR1 in washed human platelets assessed as inhibition of haTRAP-induced platelet aggregation preincubated for 1 hr followed by haTRAP addition measured for 10 mins by spectrophotometric analysis	B	8.82	pIC50	1.5	nM	IC50	ACS Med Chem Lett (2013) 4: 1054-1058 [PMID:24900604]
ChEMBL	Displacement of [3H]haTRAP from PAR1 in human platelet membranes after 60 mins by scintillation counting analysis	B	8.96	pIC50	1.1	nM	IC50	ACS Med Chem Lett (2013) 4: 1054-1058 [PMID:24900604]

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]