ChEMBL ligand: CHEMBL493982 (SCH-530348, Vorapaxar)
GPR183/G-protein coupled receptor 183 in Human [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249] There should be some charts here, you may need to enable JavaScript!
GPR35/G-protein coupled receptor 35 in Human [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97] There should be some charts here, you may need to enable JavaScript!
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
GPR183/G-protein coupled receptor 183 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249]
ChEMBL	GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183	F	5.32	pIC50	4765.24	nM	IC50	EUbOPEN Chemogenomics Library - GPCR Dose-Respose
GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97]
ChEMBL	GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR35	F	5.12	pIC50	7574	nM	IC50	EUbOPEN Chemogenomics Library - GPCR Dose-Respose
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 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]