Page last updated: 2024-08-05 15:00:50
serine protease inhibitor
Any protease inhibitor that restricts the action of a serine protease.
ChEBI ID: 64926
Members (8)
| Member | Definition | Class |
|---|---|---|
| 3,4-dichloroisocoumarin | A member of the class of isocoumarins that is isocoumarin substituted by chloro groups at positions 3 and 4. It is a serine protease inhibitor. | 3,4-dichloroisocoumarin |
| benzamidine | A carboxamidine that is benzene carrying an amidino group. | benzamidine |
| camostat | A benzoate ester resulting from the formal condensation of the carboxy group of 4-guanidinobenzoic acid with the hydroxy group of 2-(dimethylamino)-2-oxoethyl (4-hydroxyphenyl)acetate. It is a potent inhibitor of the human transmembrane protease serine 2 (TMPRSS2) and its mesylate salt is currently under investigation for its effectiveness in COVID-19 patients. | camostat |
| camostat mesylate | A methanesulfonate (mesylate) salt prepared from equimolar amounts of camostat and methanesulfonic acid. It is a serine protease inhibitor approved and marketed in Japan in 1985 for the alleviation of acute symptoms associated with chronic pancreatitis. In 1994, it was approved for the treatment of postoperative reflux esophagitis. | camostat mesylate |
| leupeptin | A tripeptide composed of N-acetylleucyl, leucyl and argininal residues joined in sequenceby peptide linkages. It is an inhibitor of the calpains, a family of calcium-activated proteases which promote cell death. | leupeptin |
| melagatran | A member of the class of azetidines that is (2S)-azetidine 2-carboxylic acid in which the carboxylic acid has been converted to the amide corresponding to formal condensation with 4-(aminomethyl)benzenecarboximidamide and in which the hydrogen attached to the azetidine nitrogen is replaced by a (2R)-2-cyclohexyl-2-[(carboxymethyl)amino]acetyl group. | melagatran |
| pd 0348292 | A member of the class of pyrrolidines that is (2R,4R)-N(1)-(p-chlorophenyl)-4-methoxypyrrolidine-1,2-dicarboxamide in which the nitrogen of the 2-carbamoyl group has been substituted by a 2-fluoro-4-(2-oxopyridin-1(2H)-yl)phenyl group. It is a synthetic organic anticoagulant compound that targets activated factor Xa in the coagulation cascade. | eribaxaban |
| ximelagatran | A member of the class of azetidines that is melagatran in which the carboxylic acid group has been converted to the corresponding ethyl ester and in which the amidine group has been converted into the corresponding amidoxime. A prodrug for melagatran, ximelagatran was the first orally available direct thrombin inhibitor to be brought to market as an anticoagulant, but was withdrawn in 2006 following reports of it causing liver damage. | ximelagatran (hydroxylamine form); ximelagatran |
Research
Studies (2,095)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 455 (21.72) | 18.7374 |
| 1990's | 556 (26.54) | 18.2507 |
| 2000's | 725 (34.61) | 29.6817 |
| 2010's | 274 (13.08) | 24.3611 |
| 2020's | 85 (4.06) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 125 (5.48%) | 5.53% |
| Reviews | 248 (10.88%) | 6.00% |
| Case Studies | 15 (0.66%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 1,891 (82.97%) | 84.16% |
Protein Targets (165)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 38.9018 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 0.2936 | 2 | 4 |
| Amyloid-beta precursor protein | Homo sapiens (human) | Potency | 23.1093 | 1 | 1 |
| apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 39.8107 | 1 | 1 |
| arylsulfatase A | Homo sapiens (human) | Potency | 0.9528 | 1 | 1 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 29.0810 | 1 | 1 |
| atrial natriuretic peptide receptor 1 precursor | Homo sapiens (human) | Potency | 37.9330 | 1 | 1 |
| atrial natriuretic peptide receptor 2 precursor | Homo sapiens (human) | Potency | 13.0918 | 1 | 1 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 0.1000 | 2 | 2 |
| bromodomain adjacent to zinc finger domain 2B | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 12.5893 | 2 | 2 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 39.8107 | 1 | 1 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| D(1A) dopamine receptor | Sus scrofa (pig) | Potency | 18.4927 | 1 | 1 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| endonuclease IV | Escherichia coli | Potency | 15.8489 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 31.1954 | 3 | 3 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 5.1455 | 1 | 4 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 8.5870 | 4 | 4 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 8.4368 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 4.1903 | 3 | 3 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 16.4784 | 2 | 2 |
| GLS protein | Homo sapiens (human) | Potency | 2.8184 | 1 | 1 |
| heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa) | Homo sapiens (human) | Potency | 18.4927 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 15.8489 | 1 | 3 |
| histone deacetylase 9 isoform 3 | Homo sapiens (human) | Potency | 0.1518 | 2 | 2 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 31.6228 | 2 | 2 |
| Integrin alpha-IIb | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| Integrin beta-3 | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 24.0353 | 2 | 2 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 9.3277 | 2 | 4 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 6.3096 | 2 | 2 |
| Nrf2 | Homo sapiens (human) | Potency | 25.9290 | 1 | 1 |
| Ornithine decarboxylase | Rattus norvegicus (Norway rat) | Potency | 0.0631 | 1 | 1 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| Parkin | Homo sapiens (human) | Potency | 20.5962 | 1 | 1 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 4.2562 | 1 | 1 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 35.4813 | 1 | 1 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 2.8184 | 1 | 1 |
| pyruvate kinase PKM isoform b | Homo sapiens (human) | Potency | 0.0631 | 2 | 2 |
| Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 10.6213 | 1 | 1 |
| serine/threonine-protein kinase mTOR isoform 1 | Homo sapiens (human) | Potency | 21.0942 | 4 | 4 |
| serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 0.3359 | 1 | 1 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| TAR DNA-binding protein 43 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 3.0868 | 2 | 2 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 3.1623 | 1 | 1 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 6.1399 | 2 | 4 |
| Thrombopoietin | Homo sapiens (human) | Potency | 12.5893 | 2 | 2 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 10.0148 | 2 | 2 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 19.3482 | 5 | 6 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Acrosin | Sus scrofa (pig) | Ki | 4.0000 | 1 | 1 |
| Calpain-1 catalytic subunit | Sus scrofa (pig) | IC50 | 0.0800 | 1 | 1 |
| Cathepsin B | Bos taurus (cattle) | IC50 | 0.3100 | 1 | 1 |
| Cathepsin B | Homo sapiens (human) | IC50 | 0.0282 | 2 | 2 |
| Cathepsin B | Homo sapiens (human) | Ki | 0.0063 | 3 | 3 |
| Cathepsin B | Capra hircus (goat) | Ki | 0.0063 | 2 | 2 |
| Cathepsin G | Homo sapiens (human) | IC50 | 96.5000 | 2 | 2 |
| Cathepsin K | Homo sapiens (human) | Ki | 0.0240 | 1 | 1 |
| Cationic trypsin | Bos taurus (cattle) | IC50 | 4.0556 | 2 | 2 |
| Cationic trypsin | Bos taurus (cattle) | Ki | 18.2660 | 6 | 7 |
| Chain A, PROTEIN (TRYPSIN) | Bos taurus (cattle) | Ki | 127.7714 | 1 | 14 |
| Chain A, TRYPSIN | Rattus rattus (black rat) | Ki | 15,000.0000 | 1 | 1 |
| Chain A, trypsin | Streptomyces griseus | Ki | 16.4000 | 1 | 1 |
| Chain A, Trypsin II, anionic | Rattus norvegicus (Norway rat) | Ki | 106.0667 | 1 | 9 |
| Chain A, TRYPSIN IVA | Homo sapiens (human) | Ki | 22.0000 | 1 | 1 |
| Chain A, UROKINASE-TYPE PLASMINOGEN ACTIVATOR | Homo sapiens (human) | Ki | 180.0000 | 1 | 2 |
| Chain B, PROTEIN (UROKINASE-TYPE PLASMINOGEN ACTIVATOR) | Homo sapiens (human) | Ki | 146.0000 | 1 | 9 |
| Chain H, Prothrombin | Homo sapiens (human) | Ki | 0.0040 | 1 | 2 |
| Chain H, Thrombin heavy chain | Homo sapiens (human) | Ki | 146.0000 | 1 | 6 |
| Chain T, Trypsin | Bos taurus (cattle) | Ki | 265.0000 | 1 | 84 |
| Chain T, Trypsin II, anionic | Rattus norvegicus (Norway rat) | Ki | 106.0667 | 1 | 3 |
| Chain U, UROKINASE-TYPE PLASMINOGEN ACTIVATOR | Homo sapiens (human) | Ki | 180.0000 | 1 | 1 |
| Chymotrypsinogen A | Bos taurus (cattle) | IC50 | 51.7500 | 2 | 2 |
| Coagulation factor VII | Homo sapiens (human) | IC50 | 3.3000 | 1 | 1 |
| Coagulation factor VII | Homo sapiens (human) | Ki | 240.0000 | 1 | 1 |
| Coagulation factor X | Homo sapiens (human) | IC50 | 11.1202 | 4 | 5 |
| Coagulation factor X | Bos taurus (cattle) | Ki | 160.0000 | 1 | 1 |
| Coagulation factor X | Homo sapiens (human) | Ki | 1.4300 | 3 | 3 |
| Coagulation factor XI | Homo sapiens (human) | IC50 | 20.0000 | 1 | 1 |
| Cysteine protease | Leishmania donovani | IC50 | 0.0100 | 1 | 1 |
| Cysteine protease falcipain-3 | Plasmodium falciparum (malaria parasite P. falciparum) | IC50 | 0.0925 | 2 | 2 |
| Cysteine proteinase falcipain 2a | Plasmodium falciparum (malaria parasite P. falciparum) | IC50 | 0.0636 | 3 | 3 |
| Disintegrin and metalloproteinase domain-containing protein 17 | Homo sapiens (human) | IC50 | 17.3000 | 1 | 2 |
| Fatty acid synthase | Rattus norvegicus (Norway rat) | IC50 | 250.0000 | 1 | 1 |
| Furin | Homo sapiens (human) | IC50 | 0.0180 | 1 | 1 |
| Furin | Homo sapiens (human) | Ki | 3.4394 | 1 | 6 |
| Hepatocyte growth factor activator | Homo sapiens (human) | IC50 | 32.0000 | 1 | 1 |
| Hepatocyte growth factor activator | Homo sapiens (human) | Ki | 0.1880 | 1 | 1 |
| Kallikrein-1 | Homo sapiens (human) | IC50 | 34.1000 | 1 | 1 |
| Liver carboxylesterase | Sus scrofa (pig) | IC50 | 250.0000 | 1 | 1 |
| Lysosomal protective protein | Homo sapiens (human) | IC50 | 0.6000 | 1 | 1 |
| Multidrug and toxin extrusion protein 1 | Homo sapiens (human) | IC50 | 2.9000 | 1 | 1 |
| Multidrug and toxin extrusion protein 2 | Homo sapiens (human) | IC50 | 12.7000 | 1 | 1 |
| Neutrophil elastase | Homo sapiens (human) | IC50 | 51.5000 | 2 | 2 |
| Papain | Carica papaya (papaya) | IC50 | 0.0022 | 1 | 1 |
| Plasma kallikrein | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| Plasminogen | Homo sapiens (human) | IC50 | 2.4400 | 2 | 3 |
| Plasminogen | Homo sapiens (human) | Ki | 1.2500 | 2 | 2 |
| Plasminogen | Bos taurus (cattle) | IC50 | 3.7000 | 1 | 1 |
| Plasminogen | Rattus norvegicus (Norway rat) | IC50 | 2.6200 | 1 | 1 |
| Pro-cathepsin H | Homo sapiens (human) | Ki | 9.2000 | 2 | 2 |
| Procathepsin L | Homo sapiens (human) | IC50 | 0.0090 | 3 | 3 |
| Procathepsin L | Homo sapiens (human) | Ki | 3.4394 | 1 | 6 |
| Prothrombin | Homo sapiens (human) | IC50 | 2.8951 | 11 | 13 |
| Prothrombin | Homo sapiens (human) | Ki | 18.6990 | 10 | 15 |
| Prothrombin | Bos taurus (cattle) | IC50 | 12.0000 | 1 | 1 |
| Prothrombin | Bos taurus (cattle) | Ki | 890.0000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 | 35.0000 | 2 | 2 |
| Rhomboid protease AarA | Providencia stuartii | IC50 | 16.8145 | 1 | 11 |
| Rhomboid protease GlpG | Escherichia coli K-12 | IC50 | 16.8145 | 1 | 11 |
| Rhomboid protease GluP | Bacillus subtilis subsp. subtilis str. 168 | IC50 | 16.8145 | 1 | 11 |
| Rhomboid-related protein 1 | Mus musculus (house mouse) | IC50 | 16.8145 | 1 | 11 |
| Rhomboid-related protein 3 | Mus musculus (house mouse) | IC50 | 16.8145 | 1 | 11 |
| Serine protease hepsin | Homo sapiens (human) | IC50 | 0.0235 | 2 | 2 |
| Serine protease hepsin | Homo sapiens (human) | Ki | 2.9568 | 2 | 7 |
| Solute carrier family 22 member 2 | Homo sapiens (human) | IC50 | 16.5000 | 1 | 1 |
| Suppressor of tumorigenicity 14 protein | Homo sapiens (human) | Ki | 134.1987 | 3 | 3 |
| Tissue factor | Homo sapiens (human) | Ki | 240.0000 | 1 | 1 |
| Tissue-type plasminogen activator | Homo sapiens (human) | Ki | 304.1367 | 3 | 3 |
| TPA: protein transporter TIM10 | Saccharomyces cerevisiae S288C | IC50 | 60.0500 | 2 | 2 |
| TPA: protein transporter TIM23 | Saccharomyces cerevisiae S288C | IC50 | 3.8300 | 1 | 1 |
| Transmembrane protease serine 2 | Homo sapiens (human) | IC50 | 0.0180 | 1 | 1 |
| Transmembrane protease serine 2 | Homo sapiens (human) | Ki | 3.4394 | 1 | 6 |
| Transmembrane protease serine 6 | Homo sapiens (human) | IC50 | 0.0180 | 1 | 1 |
| Transmembrane protease serine 6 | Homo sapiens (human) | Ki | 3.3921 | 3 | 8 |
| Trypsin | Sus scrofa (pig) | IC50 | 0.3500 | 2 | 2 |
| Trypsin-1 | Homo sapiens (human) | IC50 | 0.1356 | 4 | 5 |
| Trypsin-1 | Homo sapiens (human) | Ki | 0.0043 | 1 | 1 |
| Trypsin-2 | Homo sapiens (human) | IC50 | 0.1568 | 3 | 4 |
| Trypsin-2 | Homo sapiens (human) | Ki | 0.0043 | 1 | 1 |
| Trypsin-3 | Homo sapiens (human) | IC50 | 0.1568 | 3 | 4 |
| Trypsin-3 | Homo sapiens (human) | Ki | 0.0043 | 1 | 1 |
| Urokinase-type plasminogen activator | Homo sapiens (human) | Ki | 93.1500 | 2 | 2 |
| Vitamin K-dependent protein C | Homo sapiens (human) | IC50 | 1.3000 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Angiotensin-converting enzyme 2 | Homo sapiens (human) | EC50 | 10.0000 | 1 | 2 |
| Chain A, Coagulation factor X, heavy chain | Homo sapiens (human) | Kd | 0.0003 | 1 | 1 |
| Procathepsin L | Homo sapiens (human) | EC50 | 10.0000 | 1 | 2 |
| Prothrombin | Homo sapiens (human) | Kd | 270.0004 | 3 | 3 |
| Replicase polyprotein 1a | Severe acute respiratory syndrome-related coronavirus | EC50 | 10.0000 | 1 | 2 |
| Replicase polyprotein 1ab | Betacoronavirus England 1 | EC50 | 10.0000 | 1 | 2 |
| Replicase polyprotein 1ab | Human coronavirus 229E | EC50 | 10.0000 | 1 | 2 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | EC50 | 6.6703 | 2 | 3 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | EC50 | 10.0000 | 1 | 2 |
| Spike glycoprotein | Betacoronavirus England 1 | EC50 | 10.0000 | 1 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | EC50 | 10.0000 | 1 | 2 |
| Transmembrane protease serine 2 | Homo sapiens (human) | EC50 | 7.0000 | 2 | 3 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Aldehyde oxidase | Homo sapiens (human) | Kii | 1,620.0000 | 1 | 1 |
| Aldehyde oxidase | Homo sapiens (human) | Kis | 1,240.0000 | 1 | 1 |
| Liver carboxylesterase 1 | Homo sapiens (human) | Km | 707.0000 | 1 | 1 |