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ChEMBL ligand: CHEMBL493982 (SCH-530348, Vorapaxar) |
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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 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]