rivaroxaban [Ligand Id: 6388] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL198362 (Rivaroxaban, JNJ-39039039, Xarelto, JNJ39039039, BAY-59-7939, BAY 59-7939)
  • coagulation factor X/Coagulation factor X in Human [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
  • Coagulation factor X in Rabbit [ChEMBL: CHEMBL5062] [UniProtKB: O19045]
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  • ST14 transmembrane serine protease matriptase /Matriptase in Human [ChEMBL: CHEMBL3018] [GtoPdb: 2418] [UniProtKB: Q9Y5Y6]
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  • coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
coagulation factor X/Coagulation factor X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742]
ChEMBL Inhibition of human activated Factor X using S-2765 as substrate incubated for 15 mins followed by substrate addition and measured after 1 hr by chromogenic assay B 8.47 pKi 3.4 nM Ki Eur J Med Chem (2019) 183: 111722-111722 [PMID:31563807]
ChEMBL Inhibition of factor 10a (unknown origin) B 9.15 pKi 0.7 nM Ki MedChemComm (2014) 5: 197-202
ChEMBL Inhibition of F10a (unknown origin) using S-2222 as substrate incubated for 15 mins prior to substrate addition measured every 10 secs by spectrophotometric analysis B 9.18 pKi 0.66 nM Ki Eur. J. Med. Chem. (2013) 64: 302-313 [PMID:23644213]
ChEMBL Inhibition of human factor 10a using pefachrome F10a as substrate preincubated for 10 mins followed by substrate addition and measured for 20 mins B 9.4 pKi 0.4 nM Ki J Med Chem (2018) 61: 3799-3822 [PMID:29072911]
ChEMBL Inhibition of factor-10a (unknown origin) B 9.4 pKi 0.4 nM Ki J. Med. Chem. (2013) 56: 9441-9456 [PMID:24175584]
ChEMBL Inhibition of factor 10a B 9.4 pKi 0.4 nM Ki J. Med. Chem. (2010) 53: 6243-6274 [PMID:20503967]
ChEMBL Inhibition of Factor 10a B 9.4 pKi 0.4 nM Ki Bioorg. Med. Chem. Lett. (2009) 19: 2179-2185 [PMID:19297154]
GtoPdb - - 9.4 pKi 0.4 nM Ki J Thromb Haemost (2005) 3: 514-21 [PMID:15748242]
ChEMBL Enzyme Inhibition Assay: The enzymatic activity of human factor Xa (FXa) was measured using the conversion of a chromogenic substrate specific for FXa. Factor Xa cleaves p-nitroaniline from the chromogenic substrate. The determinations were carried out in microtitre plates as follows.The test substances, in various concentrations, were dissolved in DMSO and incubated at 25 C. with human FXa (0.5 nmol/l dissolved in 50 mmol/l of tris buffer [C,C,C-tris(hydroxymethyl)-aminomethane], 150 mmol/l of NaCl, 0.1% BSA (bovine serum albumin), pH=8.3) for 10 minutes. Pure DMSO was used as control. The chromogenic substrate (150 umol 11 of Pefachrome FXa from Pentapharm) was then added. After an incubation time of 20 minutes at 25 C., the extinction at 405 nm was determined. B 6.15 pIC50 700 nM IC50 US-8822458-B2. Substituted oxazolidinones and their use in the field of blood coagulation (2014)
ChEMBL Inhibition of F10a in human plasma assessed as doubling of activated partial thromboplastin time B 6.15 pIC50 700 nM IC50 Eur. J. Med. Chem. (2015) 96: 369-380 [PMID:25911624]
ChEMBL Inhibition of F10a in human plasma assessed as doubling of prothombin time B 6.4 pIC50 400 nM IC50 Eur. J. Med. Chem. (2015) 96: 369-380 [PMID:25911624]
ChEMBL Inhibition of human F10a using S-2765 as substrate preincubated for 10 mins followed by substrate addition by microplate reader analysis B 7.84 pIC50 14.4 nM IC50 Eur. J. Med. Chem. (2015) 101: 41-51 [PMID:26114810]
ChEMBL Inhibition of human factor 10a using N-Z-D-Arg-Gly-Arg-pNA, S-2765 chromogenic substrate B 8.07 pIC50 8.52 nM IC50 J. Med. Chem. (2014) 57: 7770-7791 [PMID:25179681]
ChEMBL Inhibition of human factor 10a assessed as CBS 31.39 substrate hydrolysis by spectrophotometric analysis B 8.34 pIC50 4.59 nM IC50 J. Med. Chem. (2011) 54: 5373-5384 [PMID:21732671]
ChEMBL Inhibition of human F10a using S-2765 as substrate after 45 mins by spectra max analysis B 8.66 pIC50 2.2 nM IC50 Eur. J. Med. Chem. (2015) 96: 369-380 [PMID:25911624]
ChEMBL Inhibition of human F10a using S-2765 as substrate after 45 mins B 8.8 pIC50 1.6 nM IC50 Eur. J. Med. Chem. (2012) 58: 136-152 [PMID:23124211]
ChEMBL Enzyme Inhibition Assay: The enzymatic activity of human factor Xa (FXa) was measured using the conversion of a chromogenic substrate specific for FXa. Factor Xa cleaves p-nitroaniline from the chromogenic substrate. The determinations were carried out in microtitre plates as follows.The test substances, in various concentrations, were dissolved in DMSO and incubated at 25 C. with human FXa (0.5 nmol/l dissolved in 50 mmol/l of tris buffer [C,C,C-tris(hydroxymethyl)-aminomethane], 150 mmol/l of NaCl, 0.1% BSA (bovine serum albumin), pH=8.3) for 10 minutes. Pure DMSO was used as control. The chromogenic substrate (150 umol 11 of Pefachrome FXa from Pentapharm) was then added. After an incubation time of 20 minutes at 25 C., the extinction at 405 nm was determined. B 8.85 pIC50 1.4 nM IC50 US-8822458-B2. Substituted oxazolidinones and their use in the field of blood coagulation (2014)
ChEMBL Inhibition of factor 10a B 9.15 pIC50 0.7 nM IC50 J. Med. Chem. (2010) 53: 6243-6274 [PMID:20503967]
ChEMBL In vitro inhibition of human coagulation factor Xa after incubation for 10 min at 25 degree C B 9.15 pIC50 0.7 nM IC50 J. Med. Chem. (2005) 48: 5900-5908 [PMID:16161994]
Coagulation factor X in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5062] [UniProtKB: O19045]
ChEMBL Inhibition of F10a in rabbit plasma assessed as doubling of activated partial thromboplastin time B 6.07 pIC50 860 nM IC50 Eur. J. Med. Chem. (2015) 96: 369-380 [PMID:25911624]
ChEMBL Inhibition of F10a in rabbit plasma assessed as doubling of prothombin time B 6.29 pIC50 510 nM IC50 Eur. J. Med. Chem. (2015) 96: 369-380 [PMID:25911624]
ST14 transmembrane serine protease matriptase /Matriptase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3018] [GtoPdb: 2418] [UniProtKB: Q9Y5Y6]
ChEMBL Inhibition of matripase (unknown origin) using Boc-QAR-AMC as substrate incubated for 30 mins prior to substrate addition by fluorescence assay B 5.47 pKi 3350 nM Ki Bioorg. Med. Chem. (2015) 23: 2328-2343 [PMID:25882520]
coagulation factor II, thrombin/Thrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL Inhibition of thrombin (unknown origin) B 6 pKi >1000 nM Ki J. Med. Chem. (2013) 56: 9441-9456 [PMID:24175584]

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]