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)

MemberDefinitionClass
3,4-dichloroisocoumarinA 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
benzamidineA carboxamidine that is benzene carrying an amidino group.benzamidine
camostatA 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 mesylateA 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
leupeptinA 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
melagatranA 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 0348292A 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
ximelagatranA 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)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990455 (21.72)18.7374
1990's556 (26.54)18.2507
2000's725 (34.61)29.6817
2010's274 (13.08)24.3611
2020's85 (4.06)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials125 (5.48%)5.53%
Reviews248 (10.88%)6.00%
Case Studies15 (0.66%)4.05%
Observational0 (0.00%)0.25%
Other1,891 (82.97%)84.16%

Protein Targets (165)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-lipoxygenase, partialHomo sapiens (human)Potency12.589311
acetylcholinesteraseHomo sapiens (human)Potency38.901811
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency0.293624
Amyloid-beta precursor proteinHomo sapiens (human)Potency23.109311
apical membrane antigen 1, AMA1Plasmodium falciparum 3D7Potency39.810711
arylsulfatase AHomo sapiens (human)Potency0.952811
ATAD5 protein, partialHomo sapiens (human)Potency29.081011
atrial natriuretic peptide receptor 1 precursorHomo sapiens (human)Potency37.933011
atrial natriuretic peptide receptor 2 precursorHomo sapiens (human)Potency13.091811
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.100022
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency89.125111
cellular tumor antigen p53 isoform aHomo sapiens (human)Potency12.589322
Chain A, Ferritin light chainEquus caballus (horse)Potency39.810711
Chain A, HADH2 proteinHomo sapiens (human)Potency3.162311
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency89.125111
Chain B, HADH2 proteinHomo sapiens (human)Potency3.162311
chromobox protein homolog 1Homo sapiens (human)Potency39.810711
cytochrome P450 2C19 precursorHomo sapiens (human)Potency25.118911
cytochrome P450 2C9 precursorHomo sapiens (human)Potency15.848911
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency31.622811
D(1A) dopamine receptorSus scrofa (pig)Potency18.492711
DNA polymerase betaHomo sapiens (human)Potency35.481311
DNA polymerase iota isoform a (long)Homo sapiens (human)Potency31.622811
endonuclease IVEscherichia coliPotency15.848911
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency31.195433
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency5.145514
EWS/FLI fusion proteinHomo sapiens (human)Potency8.587044
flap endonuclease 1Homo sapiens (human)Potency8.436811
gemininHomo sapiens (human)Potency4.190333
GLI family zinc finger 3Homo sapiens (human)Potency16.478422
GLS proteinHomo sapiens (human)Potency2.818411
heat shock 70kDa protein 5 (glucose-regulated protein, 78kDa)Homo sapiens (human)Potency18.492711
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency15.848913
histone deacetylase 9 isoform 3Homo sapiens (human)Potency0.151822
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency31.622822
Integrin alpha-IIbHomo sapiens (human)Potency12.589311
Integrin beta-3Homo sapiens (human)Potency12.589311
lamin isoform A-delta10Homo sapiens (human)Potency24.035322
M-phase phosphoprotein 8Homo sapiens (human)Potency25.118911
Microtubule-associated protein tauHomo sapiens (human)Potency9.327724
neuropeptide S receptor isoform AHomo sapiens (human)Potency12.589311
NFKB1 protein, partialHomo sapiens (human)Potency6.309622
Nrf2Homo sapiens (human)Potency25.929011
Ornithine decarboxylaseRattus norvegicus (Norway rat)Potency0.063111
parathyroid hormone/parathyroid hormone-related peptide receptor precursorHomo sapiens (human)Potency50.118711
ParkinHomo sapiens (human)Potency20.596211
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency4.256211
phosphopantetheinyl transferaseBacillus subtilisPotency35.481311
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency2.818411
pyruvate kinase PKM isoform bHomo sapiens (human)Potency0.063122
Rap guanine nucleotide exchange factor 3Homo sapiens (human)Potency89.125111
regulator of G-protein signaling 4Homo sapiens (human)Potency10.621311
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency21.094244
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency0.335911
survival motor neuron protein isoform dHomo sapiens (human)Potency28.183811
TAR DNA-binding protein 43Homo sapiens (human)Potency35.481311
TDP1 proteinHomo sapiens (human)Potency3.086822
thioredoxin glutathione reductaseSchistosoma mansoniPotency3.162311
thioredoxin reductaseRattus norvegicus (Norway rat)Potency6.139924
ThrombopoietinHomo sapiens (human)Potency12.589322
USP1 protein, partialHomo sapiens (human)Potency10.014822
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency19.348256

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AcrosinSus scrofa (pig)Ki4.000011
Calpain-1 catalytic subunitSus scrofa (pig)IC500.080011
Cathepsin BBos taurus (cattle)IC500.310011
Cathepsin BHomo sapiens (human)IC500.028222
Cathepsin BHomo sapiens (human)Ki0.006333
Cathepsin B Capra hircus (goat)Ki0.006322
Cathepsin GHomo sapiens (human)IC5096.500022
Cathepsin KHomo sapiens (human)Ki0.024011
Cationic trypsinBos taurus (cattle)IC504.055622
Cationic trypsinBos taurus (cattle)Ki18.266067
Chain A, PROTEIN (TRYPSIN)Bos taurus (cattle)Ki127.7714114
Chain A, TRYPSINRattus rattus (black rat)Ki15,000.000011
Chain A, trypsinStreptomyces griseusKi16.400011
Chain A, Trypsin II, anionicRattus norvegicus (Norway rat)Ki106.066719
Chain A, TRYPSIN IVAHomo sapiens (human)Ki22.000011
Chain A, UROKINASE-TYPE PLASMINOGEN ACTIVATORHomo sapiens (human)Ki180.000012
Chain B, PROTEIN (UROKINASE-TYPE PLASMINOGEN ACTIVATOR)Homo sapiens (human)Ki146.000019
Chain H, ProthrombinHomo sapiens (human)Ki0.004012
Chain H, Thrombin heavy chainHomo sapiens (human)Ki146.000016
Chain T, TrypsinBos taurus (cattle)Ki265.0000184
Chain T, Trypsin II, anionicRattus norvegicus (Norway rat)Ki106.066713
Chain U, UROKINASE-TYPE PLASMINOGEN ACTIVATORHomo sapiens (human)Ki180.000011
Chymotrypsinogen ABos taurus (cattle)IC5051.750022
Coagulation factor VIIHomo sapiens (human)IC503.300011
Coagulation factor VIIHomo sapiens (human)Ki240.000011
Coagulation factor XHomo sapiens (human)IC5011.120245
Coagulation factor XBos taurus (cattle)Ki160.000011
Coagulation factor XHomo sapiens (human)Ki1.430033
Coagulation factor XIHomo sapiens (human)IC5020.000011
Cysteine proteaseLeishmania donovaniIC500.010011
Cysteine protease falcipain-3Plasmodium falciparum (malaria parasite P. falciparum)IC500.092522
Cysteine proteinase falcipain 2a Plasmodium falciparum (malaria parasite P. falciparum)IC500.063633
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)IC5017.300012
Fatty acid synthase Rattus norvegicus (Norway rat)IC50250.000011
FurinHomo sapiens (human)IC500.018011
FurinHomo sapiens (human)Ki3.439416
Hepatocyte growth factor activatorHomo sapiens (human)IC5032.000011
Hepatocyte growth factor activatorHomo sapiens (human)Ki0.188011
Kallikrein-1Homo sapiens (human)IC5034.100011
Liver carboxylesteraseSus scrofa (pig)IC50250.000011
Lysosomal protective proteinHomo sapiens (human)IC500.600011
Multidrug and toxin extrusion protein 1Homo sapiens (human)IC502.900011
Multidrug and toxin extrusion protein 2Homo sapiens (human)IC5012.700011
Neutrophil elastaseHomo sapiens (human)IC5051.500022
PapainCarica papaya (papaya)IC500.002211
Plasma kallikreinHomo sapiens (human)IC5040.000011
PlasminogenHomo sapiens (human)IC502.440023
PlasminogenHomo sapiens (human)Ki1.250022
Plasminogen Bos taurus (cattle)IC503.700011
Plasminogen Rattus norvegicus (Norway rat)IC502.620011
Pro-cathepsin HHomo sapiens (human)Ki9.200022
Procathepsin LHomo sapiens (human)IC500.009033
Procathepsin LHomo sapiens (human)Ki3.439416
ProthrombinHomo sapiens (human)IC502.89511113
ProthrombinHomo sapiens (human)Ki18.69901015
Prothrombin Bos taurus (cattle)IC5012.000011
Prothrombin Bos taurus (cattle)Ki890.000011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC5035.000022
Rhomboid protease AarAProvidencia stuartiiIC5016.8145111
Rhomboid protease GlpGEscherichia coli K-12IC5016.8145111
Rhomboid protease GluPBacillus subtilis subsp. subtilis str. 168IC5016.8145111
Rhomboid-related protein 1Mus musculus (house mouse)IC5016.8145111
Rhomboid-related protein 3Mus musculus (house mouse)IC5016.8145111
Serine protease hepsinHomo sapiens (human)IC500.023522
Serine protease hepsinHomo sapiens (human)Ki2.956827
Solute carrier family 22 member 2Homo sapiens (human)IC5016.500011
Suppressor of tumorigenicity 14 proteinHomo sapiens (human)Ki134.198733
Tissue factorHomo sapiens (human)Ki240.000011
Tissue-type plasminogen activatorHomo sapiens (human)Ki304.136733
TPA: protein transporter TIM10Saccharomyces cerevisiae S288CIC5060.050022
TPA: protein transporter TIM23Saccharomyces cerevisiae S288CIC503.830011
Transmembrane protease serine 2Homo sapiens (human)IC500.018011
Transmembrane protease serine 2Homo sapiens (human)Ki3.439416
Transmembrane protease serine 6Homo sapiens (human)IC500.018011
Transmembrane protease serine 6Homo sapiens (human)Ki3.392138
TrypsinSus scrofa (pig)IC500.350022
Trypsin-1Homo sapiens (human)IC500.135645
Trypsin-1Homo sapiens (human)Ki0.004311
Trypsin-2Homo sapiens (human)IC500.156834
Trypsin-2Homo sapiens (human)Ki0.004311
Trypsin-3Homo sapiens (human)IC500.156834
Trypsin-3Homo sapiens (human)Ki0.004311
Urokinase-type plasminogen activatorHomo sapiens (human)Ki93.150022
Vitamin K-dependent protein CHomo sapiens (human)IC501.300011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Angiotensin-converting enzyme 2 Homo sapiens (human)EC5010.000012
Chain A, Coagulation factor X, heavy chainHomo sapiens (human)Kd0.000311
Procathepsin LHomo sapiens (human)EC5010.000012
ProthrombinHomo sapiens (human)Kd270.000433
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusEC5010.000012
Replicase polyprotein 1abBetacoronavirus England 1EC5010.000012
Replicase polyprotein 1abHuman coronavirus 229EEC5010.000012
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC506.670323
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusEC5010.000012
Spike glycoproteinBetacoronavirus England 1EC5010.000012
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusEC5010.000012
Transmembrane protease serine 2Homo sapiens (human)EC507.000023

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Aldehyde oxidaseHomo sapiens (human)Kii1,620.000011
Aldehyde oxidaseHomo sapiens (human)Kis1,240.000011
Liver carboxylesterase 1Homo sapiens (human)Km707.000011