Page last updated: 2024-08-07 15:32:18
Coagulation factor X
A coagulation factor X that is encoded in the genome of human. [PRO:DNx, UniProtKB:P00742]
Synonyms
EC 3.4.21.6;
Stuart factor;
Stuart-Prower factor
Research
Bioassay Publications (93)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 16 (17.20) | 18.2507 |
| 2000's | 42 (45.16) | 29.6817 |
| 2010's | 30 (32.26) | 24.3611 |
| 2020's | 5 (5.38) | 2.80 |
Compounds (49)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 4-iodine-benzo(b)thiophene-2-carboxamidine | Homo sapiens (human) | Ki | 22.0000 | 1 | 1 |
| 5-(n,n-hexamethylene)amiloride | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| benzamidine | Homo sapiens (human) | Ki | 0.3050 | 2 | 2 |
| bis(5-amidino-2-benzimidazolyl)methane | Homo sapiens (human) | IC50 | 4.5000 | 1 | 1 |
| bis(5-amidino-2-benzimidazolyl)methane | Homo sapiens (human) | Ki | 238.7599 | 1 | 12 |
| gabexate | Homo sapiens (human) | IC50 | 4.6100 | 1 | 1 |
| fidexaban | Homo sapiens (human) | Ki | 0.0401 | 6 | 7 |
| nafamostat | Homo sapiens (human) | IC50 | 21.1000 | 1 | 1 |
| pentamidine | Homo sapiens (human) | IC50 | 10.4000 | 1 | 1 |
| ro 15-4513 | Homo sapiens (human) | Ki | 0.0026 | 1 | 1 |
| amiloride | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| 1,2-di(5-amidino-2-benzofuranyl)ethane | Homo sapiens (human) | IC50 | 0.1000 | 1 | 1 |
| 1,2,3,4,6-pentakis-O-galloyl-beta-D-glucose | Homo sapiens (human) | IC50 | 0.1700 | 1 | 1 |
| 1,2,3,4,6-pentakis-O-galloyl-beta-D-glucose | Homo sapiens (human) | Ki | 0.5700 | 1 | 1 |
| mci 9038 | Homo sapiens (human) | IC50 | 134.0000 | 1 | 1 |
| mci 9038 | Homo sapiens (human) | Ki | 53.0000 | 1 | 1 |
| isosteviol | Homo sapiens (human) | IC50 | 0.6417 | 1 | 1 |
| isosteviol | Homo sapiens (human) | Ki | 13.3850 | 1 | 1 |
| sepimostate mesilate | Homo sapiens (human) | Ki | 20.4000 | 1 | 1 |
| dx 9065 | Homo sapiens (human) | IC50 | 0.0850 | 6 | 6 |
| dx 9065 | Homo sapiens (human) | Ki | 0.0503 | 8 | 9 |
| efegatran | Homo sapiens (human) | IC50 | 2.0080 | 2 | 2 |
| melagatran | Homo sapiens (human) | IC50 | 18.5333 | 2 | 3 |
| melagatran | Homo sapiens (human) | Ki | 3.6800 | 1 | 1 |
| razaxaban | Homo sapiens (human) | Ki | 3.2268 | 14 | 24 |
| dabigatran | Homo sapiens (human) | Ki | 2.8533 | 3 | 3 |
| Pedunculagin | Homo sapiens (human) | IC50 | 0.5600 | 1 | 1 |
| Pedunculagin | Homo sapiens (human) | Ki | 0.9900 | 1 | 1 |
| benzamidine | Homo sapiens (human) | Ki | 155.1385 | 3 | 13 |
| sr 90107 | Homo sapiens (human) | IC50 | 9.5976 | 2 | 2 |
| darutigenol | Homo sapiens (human) | IC50 | 11.4180 | 1 | 1 |
| fondaparinux | Homo sapiens (human) | IC50 | 0.0110 | 1 | 1 |
| otamixaban | Homo sapiens (human) | IC50 | 0.0008 | 12 | 0 |
| otamixaban | Homo sapiens (human) | Ki | 0.0004 | 2 | 2 |
| bms 740808 | Homo sapiens (human) | Ki | 0.0000 | 7 | 7 |
| ym 60828 | Homo sapiens (human) | IC50 | 0.0020 | 1 | 1 |
| ym 60828 | Homo sapiens (human) | Ki | 0.0016 | 3 | 3 |
| rivaroxaban | Homo sapiens (human) | IC50 | 0.0038 | 9 | 9 |
| rivaroxaban | Homo sapiens (human) | Ki | 0.0009 | 6 | 6 |
| n-alpha-(2,4,6-triisopropyl-phenylsulfonyl)-3-amidino-(l)-phenyl-alanine-4-ethoxycarbonyl-piperazide hydrochloride | Homo sapiens (human) | Ki | 1.7000 | 1 | 2 |
| dpc 423 | Homo sapiens (human) | Ki | 2.1202 | 6 | 11 |
| gw 813893 | Homo sapiens (human) | Ki | 0.0040 | 6 | 6 |
| darexaban | Homo sapiens (human) | IC50 | 0.0546 | 1 | 1 |
| darexaban | Homo sapiens (human) | Ki | 0.0310 | 1 | 1 |
| lb 30057 | Homo sapiens (human) | Ki | 1.1000 | 1 | 1 |
| ly517717 | Homo sapiens (human) | Ki | 0.0046 | 1 | 1 |
| darexaban glucuronide | Homo sapiens (human) | IC50 | 0.0286 | 1 | 1 |
| darexaban glucuronide | Homo sapiens (human) | Ki | 0.0200 | 1 | 1 |
| apixaban | Homo sapiens (human) | IC50 | 0.2200 | 2 | 2 |
| apixaban | Homo sapiens (human) | Ki | 0.1939 | 11 | 16 |
| betrixaban | Homo sapiens (human) | IC50 | 0.0035 | 3 | 3 |
| betrixaban | Homo sapiens (human) | Ki | 0.0001 | 2 | 2 |
| edoxaban | Homo sapiens (human) | IC50 | 0.0034 | 2 | 2 |
| edoxaban | Homo sapiens (human) | Ki | 0.0006 | 1 | 1 |
| rpr 120844 | Homo sapiens (human) | Ki | 0.0070 | 3 | 3 |
| (z,z)-babch | Homo sapiens (human) | Ki | 0.0062 | 7 | 8 |
| anabaenopeptin b | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| pd 0348292 | Homo sapiens (human) | IC50 | 0.0004 | 2 | 2 |
| kirenol | Homo sapiens (human) | IC50 | 2.5340 | 2 | 2 |
| dihydroisosteviol | Homo sapiens (human) | Ki | 27.5580 | 1 | 1 |
| pf-429242 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| e-52862 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| grassystatin a | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| otamixaban | Homo sapiens (human) | Kd | 0.0531 | 2 | 0 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bms-262084 | Homo sapiens (human) | Selectivity | 8.2500 | 1 | 1 |
PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors.Journal of medicinal chemistry, , Mar-14, Volume: 45, Issue:6, 2002
Solid-phase synthesis of N-substituted amidinophenoxy pyridines as factor XA inhibitors.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 8, Issue:14, 1998
Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 16, Issue:11, 2006
Design of potent selective zinc-mediated serine protease inhibitors.Nature, , Feb-05, Volume: 391, Issue:6667, 1998
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Preparation, characterization, and the crystal structure of the inhibitor ZK-807834 (CI-1031) complexed with factor Xa.Biochemistry, , Oct-17, Volume: 39, Issue:41, 2000
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.Journal of medicinal chemistry, , Dec-30, Volume: 42, Issue:26, 1999
Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme faJournal of medicinal chemistry, , Sep-10, Volume: 41, Issue:19, 1998
Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 8, Issue:16, 1998
Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.Journal of medicinal chemistry, , Dec-18, Volume: 46, Issue:26, 2003
Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Solution-phase and solid-phase synthesis of novel transition state inhibitors of coagulation enzymes incorporating a piperidinyl moiety.Bioorganic & medicinal chemistry letters, , May-03, Volume: 9, Issue:9, 1999
Synthesis and biological evaluation of Isosteviol derivatives as FXa inhibitors.Bioorganic & medicinal chemistry letters, , 01-15, Volume: 30, Issue:2, 2020
Discovery of novel, potent, isosteviol-based antithrombotic agents.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa.Bioorganic & medicinal chemistry, , Feb-01, Volume: 17, Issue:3, 2009
Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.Bioorganic & medicinal chemistry, , Mar-15, Volume: 16, Issue:6, 2008
Discovery of sulfonylalkylamides: A new class of orally active factor Xa inhibitors.Bioorganic & medicinal chemistry, , Mar-01, Volume: 16, Issue:5, 2008
Prodrug-based design, synthesis, and biological evaluation of N-benzenesulfonylpiperidine derivatives as novel, orally active factor Xa inhibitors.Bioorganic & medicinal chemistry, , Jun-15, Volume: 15, Issue:12, 2007
PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors.Journal of medicinal chemistry, , Mar-14, Volume: 45, Issue:6, 2002
GRID/CPCA: a new computational tool to design selective ligands.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin.Acta crystallographica. Section D, Biological crystallography, , Volume: 55, Issue:Pt 8, 1999
Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.Journal of medicinal chemistry, , Dec-30, Volume: 42, Issue:26, 1999
Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.Journal of medicinal chemistry, , May-20, Volume: 42, Issue:10, 1999
Design of benzamidine-type inhibitors of factor Xa.Journal of medicinal chemistry, , Oct-22, Volume: 41, Issue:22, 1998
Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors.Journal of medicinal chemistry, , Apr-15, Volume: 37, Issue:8, 1994
Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.Bioorganic & medicinal chemistry letters, , Nov-04, Volume: 12, Issue:21, 2002
Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.Journal of medicinal chemistry, , Jul-08, Volume: 37, Issue:14, 1994
Design, synthesis, and SAR of a series of activated protein C (APC) inhibitors with selectivity against thrombin for the treatment of haemophilia.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 24, Issue:3, 2014
Antithrombotic effects of LB30870, a potent, orally active, selective and direct thrombin inhibitor, and pharmacokinetics of its prodrug.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.Bioorganic & medicinal chemistry letters, , May-15, Volume: 16, Issue:10, 2006
Orally active thrombin inhibitors. Part 2: optimization of the P2-moiety.Bioorganic & medicinal chemistry letters, , May-15, Volume: 16, Issue:10, 2006
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Phenyltriazolinones as potent factor Xa inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 2010
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 19, Issue:2, 2009
Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 18, Issue:14, 2008
7-fluoroindazoles as potent and selective inhibitors of factor Xa.Journal of medicinal chemistry, , Jan-24, Volume: 51, Issue:2, 2008
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation faJournal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 16, Issue:14, 2006
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blooBioorganic & medicinal chemistry letters, , Aug-01, Volume: 16, Issue:15, 2006
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 16, Issue:7, 2006
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 16, Issue:21, 2006
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Acylated 1Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor.Journal of medicinal chemistry, , Dec-12, Volume: 56, Issue:23, 2013
Structure-based design of novel potent nonpeptide thrombin inhibitors.Journal of medicinal chemistry, , Apr-25, Volume: 45, Issue:9, 2002
Dissecting and designing inhibitor selectivity determinants at the S1 site using an artificial Ala190 protease (Ala190 uPA).Journal of molecular biology, , Nov-19, Volume: 344, Issue:2, 2004
A novel serine protease inhibition motif involving a multi-centered short hydrogen bonding network at the active site.Journal of molecular biology, , Apr-13, Volume: 307, Issue:5, 2001
Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.Chemistry & biology, , Volume: 7, Issue:4, 2000
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.Bioorganic & medicinal chemistry letters, , Jun-17, Volume: 12, Issue:12, 2002
[no title available],
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation faJournal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
1-[3-Aminobenzisoxazol-5'-yl]-3-trifluoromethyl-6-[2'-(3-(R)-hydroxy-N-pyrrolidinyl)methyl-[1,1']-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4-c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blooBioorganic & medicinal chemistry letters, , Aug-01, Volume: 16, Issue:15, 2006
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 16, Issue:21, 2006
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors.Bioorganic & medicinal chemistry letters, , Feb-10, Volume: 13, Issue:3, 2003
PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors.Journal of medicinal chemistry, , Mar-14, Volume: 45, Issue:6, 2002
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Acylated 1Journal of medicinal chemistry, , 11-12, Volume: 63, Issue:21, 2020
Discovery of novel, potent, isosteviol-based antithrombotic agents.European journal of medicinal chemistry, , Dec-01, Volume: 183, 2019
Design of Small-Molecule Active-Site Inhibitors of the S1A Family Proteases as Procoagulant and Anticoagulant Drugs.Journal of medicinal chemistry, , 05-10, Volume: 61, Issue:9, 2018
Design, synthesis and structure-activity relationship of oxazolidinone derivatives containing novel S4 ligand as FXa inhibitors.European journal of medicinal chemistry, , Volume: 96, 2015
Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.European journal of medicinal chemistry, , Aug-28, Volume: 101, 2015
Design, synthesis, and structure-activity and structure-pharmacokinetic relationship studies of novel [6,6,5] tricyclic fused oxazolidinones leading to the discovery of a potent, selective, and orally bioavailable FXa inhibitor.Journal of medicinal chemistry, , Sep-25, Volume: 57, Issue:18, 2014
Low molecular weight dual inhibitors of factor Xa and fibrinogen binding to GPIIb/IIIa with highly overlapped pharmacophores.European journal of medicinal chemistry, , Volume: 64, 2013
5-Chlorothiophene-2-carboxylic acid [(S)-2-[2-methyl-3-(2-oxopyrrolidin-1-yl)benzenesulfonylamino]-3-(4-methylpiperazin-1-yl)-3-oxopropyl]amide (SAR107375), a selective and potent orally active dual thrombin and factor Xa inhibitor.Journal of medicinal chemistry, , Dec-12, Volume: 56, Issue:23, 2013
Synthesis and structure-activity relationship of potent, selective and orally active anthranilamide-based factor Xa inhibitors: application of weakly basic sulfoximine group as novel S4 binding element.European journal of medicinal chemistry, , Volume: 58, 2012
Polysulfated xanthones: multipathway development of a new generation of dual anticoagulant/antiplatelet agents.Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Discovery of the novel antithrombotic agent 5-chloro-N-({(5S)-2-oxo-3- [4-(3-oxomorpholin-4-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene- 2-carboxamide (BAY 59-7939): an oral, direct factor Xa inhibitor.Journal of medicinal chemistry, , Sep-22, Volume: 48, Issue:19, 2005
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Phenyltriazolinones as potent factor Xa inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 2010
Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues.Bioorganic & medicinal chemistry letters, , Mar-01, Volume: 17, Issue:5, 2007
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 21, Issue:6, 2011
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 20, Issue:2, 2010
Selective and dual action orally active inhibitors of thrombin and factor Xa.Bioorganic & medicinal chemistry letters, , May-15, Volume: 17, Issue:10, 2007
Factor Xa inhibitors: S1 binding interactions of a series of N-{(3S)-1-[(1S)-1-methyl-2-morpholin-4-yl-2-oxoethyl]-2-oxopyrrolidin-3-yl}sulfonamides.Journal of medicinal chemistry, , Apr-05, Volume: 50, Issue:7, 2007
Design, synthesis, and biological activity of novel tetrahydropyrazolopyridone derivatives as FXa inhibitors with potent anticoagulant activity.Bioorganic & medicinal chemistry, , 05-15, Volume: 25, Issue:10, 2017
Design, synthesis, and structure-activity relationship of novel and effective apixaban derivatives as FXa inhibitors containing 1,2,4-triazole/pyrrole derivatives as P2 binding element.Bioorganic & medicinal chemistry, , 11-01, Volume: 24, Issue:21, 2016
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 24, Issue:15, 2014
Apixaban inhibition of factor Xa: Microscopic rate constants and inhibition mechanism in purified protein systems and in human plasma.Journal of enzyme inhibition and medicinal chemistry, , Volume: 26, Issue:4, 2011
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Phenyltriazolinones as potent factor Xa inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 2010
Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 19, Issue:2, 2009
Structure-activity relationships of anthranilamide-based factor Xa inhibitors containing piperidinone and pyridinone P4 moieties.Bioorganic & medicinal chemistry letters, , May-01, Volume: 18, Issue:9, 2008
SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 17, Issue:16, 2007
Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation faJournal of medicinal chemistry, , Nov-01, Volume: 50, Issue:22, 2007
Design, synthesis and biological evaluation of anthranilamide derivatives as potential factor Xa (fXa) inhibitors.Bioorganic & medicinal chemistry, , 12-15, Volume: 26, Issue:23-24, 2018
Design, synthesis and biological evaluation of novel 2,3-dihydroquinazolin- 4(1H)-one derivatives as potential fXa inhibitors.European journal of medicinal chemistry, , Jan-05, Volume: 125, 2017
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 19, Issue:8, 2009
Semisynthesis of epoxy-pimarane diterpenoids from kirenol and their FXa inhibition activities.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Semisynthesis of ent-norstrobane diterpenoids as potential inhibitor for factor Xa.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 28, Issue:23-24, 2018
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization.Journal of medicinal chemistry, , Sep-09, Volume: 42, Issue:18, 1999
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.Journal of medicinal chemistry, , Sep-09, Volume: 42, Issue:18, 1999
Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors.Bioorganic & medicinal chemistry letters, , May-01, Volume: 10, Issue:9, 2000
Crystallographic analysis of potent and selective factor Xa inhibitors complexed to bovine trypsin.Acta crystallographica. Section D, Biological crystallography, , Volume: 55, Issue:Pt 8, 1999
Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors.Journal of medicinal chemistry, , Dec-30, Volume: 42, Issue:26, 1999
Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme faJournal of medicinal chemistry, , Sep-10, Volume: 41, Issue:19, 1998
Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.Bioorganic & medicinal chemistry letters, , Aug-18, Volume: 8, Issue:16, 1998
Solid-phase synthesis of N-substituted amidinophenoxy pyridines as factor XA inhibitors.Bioorganic & medicinal chemistry letters, , Jul-21, Volume: 8, Issue:14, 1998
(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa.Journal of medicinal chemistry, , Sep-10, Volume: 41, Issue:19, 1998
Factor Xa inhibitors: next-generation antithrombotic agents.Journal of medicinal chemistry, , Sep-09, Volume: 53, Issue:17, 2010
Exploration of 4,4-disubstituted pyrrolidine-1,2-dicarboxamides as potent, orally active Factor Xa inhibitors with extended duration of action.Bioorganic & medicinal chemistry, , Mar-15, Volume: 17, Issue:6, 2009
Semisynthesis of epoxy-pimarane diterpenoids from kirenol and their FXa inhibition activities.Bioorganic & medicinal chemistry, , 04-01, Volume: 27, Issue:7, 2019
Semisynthesis of ent-norstrobane diterpenoids as potential inhibitor for factor Xa.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 28, Issue:23-24, 2018
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| serine-type endopeptidase activity | molecular function | Catalysis of the hydrolysis of internal, alpha-peptide bonds in a polypeptide chain by a catalytic mechanism that involves a catalytic triad consisting of a serine nucleophile that is activated by a proton relay involving an acidic residue (e.g. aspartate or glutamate) and a basic residue (usually histidine). [GOC:mah, https://www.ebi.ac.uk/merops/about/glossary.shtml#CATTYPE] |
| calcium ion binding | molecular function | Binding to a calcium ion (Ca2+). [GOC:ai] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| phospholipid binding | molecular function | Binding to a phospholipid, a class of lipids containing phosphoric acid as a mono- or diester. [ISBN:0198506732] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
| endoplasmic reticulum lumen | cellular component | The volume enclosed by the membranes of the endoplasmic reticulum. [ISBN:0198547684] |
| Golgi lumen | cellular component | The volume enclosed by the membranes of any cisterna or subcompartment of the Golgi apparatus, including the cis- and trans-Golgi networks. [GOC:mah] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| external side of plasma membrane | cellular component | The leaflet of the plasma membrane that faces away from the cytoplasm and any proteins embedded or anchored in it or attached to its surface. [GOC:dos, GOC:tb] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
Involved In
This protein is involved in 4 target(s):
| Target | Category | Definition |
|---|
| proteolysis | biological process | The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah] |
| blood coagulation | biological process | The sequential process in which the multiple coagulation factors of the blood interact, ultimately resulting in the formation of an insoluble fibrin clot; it may be divided into three stages: stage 1, the formation of intrinsic and extrinsic prothrombin converting principle; stage 2, the formation of thrombin; stage 3, the formation of stable fibrin polymers. [PMID:30700128] |
| positive regulation of cell migration | biological process | Any process that activates or increases the frequency, rate or extent of cell migration. [GOC:go_curators] |
| positive regulation of TOR signaling | biological process | Any process that activates or increases the frequency, rate or extent of TOR signaling. [GOC:mah] |