vorapaxar [Ligand Id: 4047] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL493982 (Vorapaxar, SCH-530348)
  • PAR1/Proteinase-activated receptor 1 in Human [ChEMBL: CHEMBL3974] [GtoPdb: 347] [UniProtKB: P25116]
  • 8.09
1 CHEMBL493982_lig_chart_1 Proteinase-activated receptor 1 Human
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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 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 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 B 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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]