ChEMBL ligand: CHEMBL198362 (BAY 59-7939, BAY-59-7939, JNJ-39039039, JNJ39039039, Rivaroxaban, Xarelto)
coagulation factor X/Coagulation factor X in Human [ChEMBL: CHEMBL244] [GtoPdb: 2359] [UniProtKB: P00742] Coagulation factor X in Rabbit [ChEMBL: CHEMBL5062] [UniProtKB: O19045] There should be some charts here, you may need to enable JavaScript!
coagulation factor XII/Coagulation factor XII in Human [ChEMBL: CHEMBL2821] [GtoPdb: 2361] [UniProtKB: P00748] There should be some charts here, you may need to enable JavaScript!
ST14 transmembrane serine protease matriptase /Matriptase in Human [ChEMBL: CHEMBL3018] [GtoPdb: 2418] [UniProtKB: Q9Y5Y6] There should be some charts here, you may need to enable JavaScript!
coagulation factor II, thrombin/Thrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734] 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
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	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	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 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 Xa using S-2765 as chromogenic substrate preincubated for 10 mins followed by substrate addition and measured after 10 mins	B	8.22	pIC50	6	nM	IC50	Eur J Med Chem (2023) 246: 114855-114855 [PMID:36462436]
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	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]
ChEMBL	Inhibition of human coagulation factor Xa using Boc-Ile-Glu-Gly-Arg-AMC as fluorogenic substrate measured at 1 min interval for 1 hr by fluorometric assay	B	9.15	pIC50	0.7	nM	IC50	J Med Chem (2020) 63: 13159-13186 [PMID:33089691]
ChEMBL	Inhibition of factor Xa (unknown origin)	B	9.15	pIC50	0.7	nM	IC50	Bioorg Med Chem Lett (2023) 80: 129127-129127 [PMID:36634753]
ChEMBL	Inhibition of factor 10a	B	9.15	pIC50	0.7	nM	IC50	J Med Chem (2010) 53: 6243-6274 [PMID:20503967]
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]
coagulation factor XII/Coagulation factor XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2821] [GtoPdb: 2361] [UniProtKB: P00748]
ChEMBL	Inhibition of human coagulation factor XIIA using Boc-Gln-Gly-Arg-AMC as fluorogenic substrate measured at 1 min interval for 1 hr by fluorometric assay	B	4.48	pIC50	>33000	nM	IC50	J Med Chem (2020) 63: 13159-13186 [PMID:33089691]
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	Inhibition of human thrombin using S-2238 as chromogenic substrate preincubated for 10 mins followed by substrate addition and measured after 10 mins by absorbance based assay	B	4	pIC50	>100000	nM	IC50	Eur J Med Chem (2023) 246: 114855-114855 [PMID:36462436]

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]