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Cationic trypsin
A protein that is a translation product of any of the following genes in cow
Synonyms
EC 3.4.21.4;
Beta-trypsin
Research
Bioassay Publications (40)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (2.50) | 18.7374 |
| 1990's | 19 (47.50) | 18.2507 |
| 2000's | 17 (42.50) | 29.6817 |
| 2010's | 2 (5.00) | 24.3611 |
| 2020's | 1 (2.50) | 2.80 |
Compounds (48)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| phenethylamine | Bos taurus (cattle) | Ki | 11.0000 | 1 | 1 |
| benzamidine | Bos taurus (cattle) | Ki | 18.2660 | 6 | 7 |
| bis(5-amidino-2-benzimidazolyl)methane | Bos taurus (cattle) | Ki | 0.0170 | 1 | 1 |
| fidexaban | Bos taurus (cattle) | Ki | 0.2100 | 3 | 4 |
| nafamostat | Bos taurus (cattle) | IC50 | 0.0170 | 1 | 1 |
| 1,2-Dihydroquinolin-2-imine | Bos taurus (cattle) | Ki | 390.0000 | 1 | 2 |
| 2-aminobenzimidazole | Bos taurus (cattle) | Ki | 155.0000 | 1 | 2 |
| phenylguanidine | Bos taurus (cattle) | Ki | 162.9650 | 2 | 2 |
| amiloride | Bos taurus (cattle) | Ki | 345.7667 | 1 | 3 |
| 3-phenylpropylamine | Bos taurus (cattle) | Ki | 32.5000 | 1 | 1 |
| 2,4-diaminoquinazoline | Bos taurus (cattle) | Ki | 1,466.6667 | 1 | 3 |
| inogatran | Bos taurus (cattle) | Ki | 0.6750 | 1 | 1 |
| 4-fluorobenzylamine | Bos taurus (cattle) | Ki | 0.4300 | 1 | 1 |
| 4-hydroxyquinoline | Bos taurus (cattle) | Ki | 2,000.0000 | 1 | 2 |
| leupeptin | Bos taurus (cattle) | IC50 | 8.1000 | 1 | 1 |
| 1-aminoisoquinoline | Bos taurus (cattle) | Ki | 495.0000 | 1 | 2 |
| 2-amino-1-methylbenzimidazole | Bos taurus (cattle) | Ki | 1,085.0000 | 1 | 2 |
| 4-phenylbutylamine | Bos taurus (cattle) | Ki | 20.0000 | 1 | 1 |
| mci 9038 | Bos taurus (cattle) | Ki | 2.9000 | 1 | 1 |
| dx 9065 | Bos taurus (cattle) | Ki | 0.2600 | 3 | 4 |
| efegatran | Bos taurus (cattle) | IC50 | 0.0065 | 2 | 2 |
| efegatran | Bos taurus (cattle) | Ki | 0.0065 | 2 | 2 |
| 5-amidinoindole | Bos taurus (cattle) | Ki | 29.1000 | 1 | 1 |
| n(alpha)-tosyl-(3-amidinophenyl)alanine piperidide | Bos taurus (cattle) | Ki | 1.2000 | 1 | 1 |
| 4-guanidinobenzoate | Bos taurus (cattle) | IC50 | 342.5000 | 1 | 4 |
| 4-guanidinobenzoate | Bos taurus (cattle) | Ki | 10,000.0000 | 2 | 2 |
| melagatran | Bos taurus (cattle) | IC50 | 0.0112 | 1 | 1 |
| razaxaban | Bos taurus (cattle) | Ki | 7.0400 | 2 | 11 |
| benzamidine | Bos taurus (cattle) | Ki | 196.0533 | 3 | 15 |
| 2-(4-chlorophenyl)guanidine | Bos taurus (cattle) | Ki | 119.9750 | 2 | 2 |
| quercetin | Bos taurus (cattle) | IC50 | 24.4200 | 2 | 5 |
| apigenin | Bos taurus (cattle) | IC50 | 141.5000 | 1 | 1 |
| luteolin | Bos taurus (cattle) | IC50 | 35.3000 | 1 | 1 |
| kaempferol | Bos taurus (cattle) | IC50 | 105.9000 | 1 | 1 |
| morin | Bos taurus (cattle) | IC50 | 110.8000 | 1 | 1 |
| myricetin | Bos taurus (cattle) | IC50 | 10.2000 | 1 | 1 |
| rutin | Bos taurus (cattle) | IC50 | 42.2000 | 1 | 5 |
| napsagatran | Bos taurus (cattle) | Ki | 1.9000 | 1 | 1 |
| n,n-(4-xylylidene)bisaminoguanidine | Bos taurus (cattle) | Ki | 55.3333 | 1 | 3 |
| glyoxal bis(guanylhydrazone) | Bos taurus (cattle) | Ki | 565.2500 | 1 | 4 |
| bms-262084 | Bos taurus (cattle) | IC50 | 0.0720 | 1 | 1 |
| ym 60828 | Bos taurus (cattle) | Ki | 0.1590 | 1 | 1 |
| n-alpha-(2,4,6-triisopropyl-phenylsulfonyl)-3-amidino-(l)-phenyl-alanine-4-ethoxycarbonyl-piperazide hydrochloride | Bos taurus (cattle) | Ki | 0.0370 | 1 | 1 |
| dpc 423 | Bos taurus (cattle) | Ki | 3.8869 | 1 | 6 |
| lb 30057 | Bos taurus (cattle) | Ki | 12.0777 | 3 | 3 |
| rpr 120844 | Bos taurus (cattle) | Ki | 0.0069 | 1 | 1 |
| (z,z)-babch | Bos taurus (cattle) | Ki | 0.0271 | 5 | 6 |
| m-chlorophenylguanidine | Bos taurus (cattle) | Ki | 1,099.5050 | 2 | 2 |
| grassystatin a | Bos taurus (cattle) | IC50 | 10.0000 | 1 | 1 |
| cycloviolacin o2 | Bos taurus (cattle) | Ki | 0.0000 | 1 | 1 |
Synthesis of 2-guanidinyl pyridines and their trypsin inhibition and docking.Bioorganic & medicinal chemistry, , 08-15, Volume: 28, Issue:16, 2020
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
Simple, intuitive calculations of free energy of binding for protein-ligand complexes. 1. Models without explicit constrained water.Journal of medicinal chemistry, , Jun-06, Volume: 45, Issue:12, 2002
GRID/CPCA: a new computational tool to design selective ligands.Journal of medicinal chemistry, , Aug-10, Volume: 43, Issue:16, 2000
Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.Journal of medicinal chemistry, , Dec-31, Volume: 41, Issue:27, 1998
Design and synthesis of potent and highly selective thrombin inhibitors.Journal of medicinal chemistry, , Nov-11, Volume: 37, Issue:23, 1994
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
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
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
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
Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors.Journal of medicinal chemistry, , May-20, Volume: 42, Issue:10, 1999
In-depth study of tripeptide-based alpha-ketoheterocycles as inhibitors of thrombin. Effective utilization of the S1' subsite and its implications to structure-based drug design.Journal of medicinal chemistry, , Mar-24, Volume: 48, Issue:6, 2005
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
Potent thrombin inhibitors that probe the S1 subsite: tripeptide transition state analogues based on a heterocycle-activated carbonyl group.Journal of medicinal chemistry, , Aug-02, Volume: 39, Issue:16, 1996
Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions.Journal of medicinal chemistry, , Oct-27, Volume: 38, Issue:22, 1995
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
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
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
Crystals of the urokinase type plasminogen activator variant beta(c)-uPAin complex with small molecule inhibitors open the way towards structure-based drug design.Journal of molecular biology, , Aug-11, Volume: 301, Issue:2, 2000
Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator.Chemistry & biology, , Volume: 7, Issue:4, 2000
Noncovalent thrombin inhibitors incorporating an imidazolylethynyl P1.Bioorganic & medicinal chemistry letters, , Dec-18, Volume: 10, Issue:24, 2000
Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption.Bioorganic & medicinal chemistry letters, , Sep-06, Volume: 9, Issue:17, 1999
Potent and efficacious thienylamidine-incorporated thrombin inhibitors.Bioorganic & medicinal chemistry letters, , Jul-07, Volume: 8, Issue:13, 1998
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
(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
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