Page last updated: 2024-08-07 15:43:30
Trypsin-1
A serine protease 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P07477]
Synonyms
EC 3.4.21.4;
Beta-trypsin;
Cationic trypsinogen;
Serine protease 1;
Trypsin I
Research
Bioassay Publications (56)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (1.79) | 18.7374 |
| 1990's | 12 (21.43) | 18.2507 |
| 2000's | 26 (46.43) | 29.6817 |
| 2010's | 16 (28.57) | 24.3611 |
| 2020's | 1 (1.79) | 2.80 |
Compounds (54)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| 5-(n,n-hexamethylene)amiloride | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| bis(5-amidino-2-benzimidazolyl)methane | Homo sapiens (human) | IC50 | 4.4000 | 1 | 1 |
| bis(5-amidino-2-benzimidazolyl)methane | Homo sapiens (human) | Ki | 206.0149 | 3 | 14 |
| camostat | Homo sapiens (human) | IC50 | 0.0035 | 1 | 1 |
| n(alpha)-(2-naphthylsulfonylglycyl)-4-amidinophenylalanine piperidide | Homo sapiens (human) | IC50 | 0.1690 | 1 | 1 |
| nafamostat | Homo sapiens (human) | IC50 | 0.0170 | 1 | 1 |
| netropsin | Homo sapiens (human) | IC50 | 35.0000 | 1 | 2 |
| pentamidine | Homo sapiens (human) | IC50 | 43.3333 | 1 | 3 |
| sulfaguanidine | Homo sapiens (human) | Ki | 1.3500 | 1 | 1 |
| benzylamine | Homo sapiens (human) | Ki | 299,916.0000 | 1 | 1 |
| isoquinoline-1,3,4-trione | Homo sapiens (human) | IC50 | 5.0000 | 1 | 1 |
| amiloride | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| 2'-carbomethoxyphenyl 4-guanidinobenzoate | Homo sapiens (human) | IC50 | 0.0650 | 1 | 1 |
| baicalin | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| 4-aminomethylbenzoic acid | Homo sapiens (human) | Ki | 500,035.0000 | 1 | 1 |
| 4-methylbenzylamine | Homo sapiens (human) | Ki | 666,807.0000 | 1 | 1 |
| leupeptin | Homo sapiens (human) | IC50 | 0.6000 | 1 | 1 |
| 4-methoxybenzylamine | Homo sapiens (human) | Ki | 1,000,000.0000 | 1 | 1 |
| p-Aminobenzamidine dihydrochloride | Homo sapiens (human) | Ki | 8.9000 | 1 | 1 |
| mci 9038 | Homo sapiens (human) | Ki | 1.9900 | 1 | 1 |
| sivelestat | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| sepimostate mesilate | Homo sapiens (human) | Ki | 0.2900 | 1 | 1 |
| dx 9065 | Homo sapiens (human) | IC50 | 3.2000 | 1 | 1 |
| dx 9065 | Homo sapiens (human) | Ki | 0.6200 | 3 | 3 |
| efegatran | Homo sapiens (human) | IC50 | 0.0080 | 1 | 1 |
| acetylphenylalanyl-prolyl-boroarginine | Homo sapiens (human) | Ki | 0.0045 | 2 | 2 |
| skullcapflavone ii | Homo sapiens (human) | IC50 | 110.0000 | 1 | 1 |
| foy 251 | Homo sapiens (human) | IC50 | 0.0550 | 1 | 1 |
| melagatran | Homo sapiens (human) | IC50 | 0.0119 | 1 | 2 |
| melagatran | Homo sapiens (human) | Ki | 0.0043 | 1 | 1 |
| beta-naphthamidine | Homo sapiens (human) | Ki | 7.7900 | 2 | 2 |
| razaxaban | Homo sapiens (human) | Ki | 6.9714 | 7 | 7 |
| dabigatran | Homo sapiens (human) | Ki | 0.0502 | 2 | 2 |
| benzamidine | Homo sapiens (human) | Ki | 237.5000 | 1 | 2 |
| 1-(2-Naphthylmethyl)-2,3-dioxo-indoline-5-carboxamide | Homo sapiens (human) | IC50 | 352.0000 | 1 | 1 |
| telaprevir | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| wogonoside | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| silybin | Homo sapiens (human) | IC50 | 3.7000 | 1 | 1 |
| ganhuangenin | Homo sapiens (human) | IC50 | 88.0000 | 1 | 1 |
| quercetin | Homo sapiens (human) | IC50 | 15.4000 | 1 | 1 |
| baicalein | Homo sapiens (human) | IC50 | 3.7000 | 1 | 1 |
| wogonin | Homo sapiens (human) | IC50 | 105.0000 | 1 | 1 |
| camostat mesylate | Homo sapiens (human) | IC50 | 0.0506 | 1 | 1 |
| 5,7-dihydroxy-6-methoxy-2-phenylchromen-4-one | Homo sapiens (human) | IC50 | 61.0000 | 1 | 1 |
| otamixaban | Homo sapiens (human) | Ki | 0.3010 | 1 | 2 |
| bms 740808 | Homo sapiens (human) | Ki | 2.8000 | 2 | 2 |
| bms-262084 | Homo sapiens (human) | IC50 | 0.0272 | 2 | 2 |
| dpc 423 | Homo sapiens (human) | Ki | 0.0600 | 3 | 3 |
| zd 8321 | Homo sapiens (human) | Ki | 66.6000 | 1 | 1 |
| gw 813893 | Homo sapiens (human) | IC50 | 158.0000 | 1 | 1 |
| l 374087 | Homo sapiens (human) | Ki | 3.2000 | 5 | 5 |
| darexaban | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| lb 30057 | Homo sapiens (human) | Ki | 3.2900 | 1 | 1 |
| darexaban glucuronide | Homo sapiens (human) | Ki | 100.0000 | 1 | 1 |
| apixaban | Homo sapiens (human) | Ki | 4.2000 | 1 | 1 |
| mk-7009 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| rpx7009 | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
Amides of xanthurenic acid as zinc-dependent inhibitors of Lp-PLA(2).Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 22, Issue:2, 2012
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
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
Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 18, Issue:16, 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
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Protease inhibitors: current status and future prospects.Journal of medicinal chemistry, , Feb-10, Volume: 43, Issue:3, 2000
Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.Bioorganic & medicinal chemistry letters, , Apr-05, Volume: 9, Issue:7, 1999
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 2: optimization of the P2-moiety.Bioorganic & medicinal chemistry letters, , May-15, Volume: 16, Issue:10, 2006
Orally active thrombin inhibitors. Part 1: optimization of the P1-moiety.Bioorganic & medicinal chemistry letters, , May-15, Volume: 16, Issue:10, 2006
Interaction with the S1 beta-pocket of urokinase: 8-heterocycle substituted and 6,8-disubstituted 2-naphthamidine urokinase inhibitors.Bioorganic & medicinal chemistry letters, , Jun-21, Volume: 14, Issue:12, 2004
Identification of novel binding interactions in the development of potent, selective 2-naphthamidine inhibitors of urokinase. Synthesis, structural analysis, and SAR of N-phenyl amide 6-substitution.Journal of medicinal chemistry, , Jan-15, Volume: 47, Issue:2, 2004
Phenyltriazolinones as potent factor Xa inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 20, Issue:4, 2010
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
7-fluoroindazoles as potent and selective inhibitors of factor Xa.Journal of medicinal chemistry, , Jan-24, Volume: 51, Issue:2, 2008
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
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
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
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
Structure-based design of novel potent nonpeptide thrombin inhibitors.Journal of medicinal chemistry, , Apr-25, Volume: 45, Issue:9, 2002
Structure-activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
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
Factor XIa Inhibitors as New Anticoagulants.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors.Bioorganic & medicinal chemistry letters, , May-03, Volume: 14, Issue:9, 2004
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
The selectivity and bioavailability improvement of novel oral anticoagulants: An overview.European journal of medicinal chemistry, , Feb-25, Volume: 146, 2018
Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.Bioorganic & medicinal chemistry letters, , Oct-20, Volume: 13, Issue:20, 2003
Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates.Journal of medicinal chemistry, , Nov-05, Volume: 41, Issue:23, 1998
C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption.Bioorganic & medicinal chemistry letters, , Jul-07, Volume: 8, Issue:13, 1998
L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor.Bioorganic & medicinal chemistry letters, , Apr-07, Volume: 8, Issue:7, 1998
Enables
This protein enables 2 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] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
Located In
This protein is located in 3 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] |
| collagen-containing extracellular matrix | cellular component | An extracellular matrix consisting mainly of proteins (especially collagen) and glycosaminoglycans (mostly as proteoglycans) that provides not only essential physical scaffolding for the cellular constituents but can also initiate crucial biochemical and biomechanical cues required for tissue morphogenesis, differentiation and homeostasis. The components are secreted by cells in the vicinity and form a sheet underlying or overlying cells such as endothelial and epithelial cells. [GOC:BHF, GOC:rph, PMID:21123617] |
| blood microparticle | cellular component | A phospholipid microvesicle that is derived from any of several cell types, such as platelets, blood cells, endothelial cells, or others, and contains membrane receptors as well as other proteins characteristic of the parental cell. Microparticles are heterogeneous in size, and are characterized as microvesicles free of nucleic acids. [GOC:BHF, GOC:mah, PMID:16373184] |
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 3 target(s):
| Target | Category | Definition |
|---|
| digestion | biological process | The whole of the physical, chemical, and biochemical processes carried out by multicellular organisms to break down ingested nutrients into components that may be easily absorbed and directed into metabolism. [GOC:isa_complete, ISBN:0198506732] |
| extracellular matrix disassembly | biological process | A process that results in the breakdown of the extracellular matrix. [GOC:jid] |
| proteolysis | biological process | The hydrolysis of proteins into smaller polypeptides and/or amino acids by cleavage of their peptide bonds. [GOC:bf, GOC:mah] |