Page last updated: 2024-08-05 15:39:41

protease inhibitor

A compound which inhibits or antagonizes the biosynthesis or actions of proteases (endopeptidases).

ChEBI ID: 37670

Members (9)

MemberDefinitionClass
acetyl-aspartyl-glutamyl-valyl-aspartalA tetrapeptide consisting of two L-aspartic acid residues, an L-glutamyl residue and an L-valine residue with an acetyl group at the N-terminal and with the C-terminal carboxy group reduced to an aldehyde. It is an inhibitor of caspase-3/7.Ac-Asp-Glu-Val-Asp-H
amastatinA tetrapeptide comprising (2S,3R)-3-amino-2-hydroxy-5-methylhexanoyl, L-valyl, L-valyl and L-aspartic acid units joined in sequenceamastatin
bortezomibL-Phenylalaninamide substituted at the amide nitrogen by a 1-(dihydroxyboranyl)-3-methylbutyl group and at N(alpha) by a pyrazin-2-ylcarbonyl group. It is a dipeptidyl boronic acid that reversibly inhibits the 26S proteasome.bortezomib
cilastatinThe thioether resulting from the formal oxidative coupling of the thiol group of L-cysteine with the 7-position of (2Z)-2-({[(1S)-2,2-dimethylcyclopropyl]carbonyl}amino)hept-2-enoic acid. It is an inhibitor of dehydropeptidase I (membrane dipeptidase, 3.4.13.19), an enzyme found in the brush border of renal tubes and responsible for degrading the antibiotic imipenem. Cilastatin is therefore administered (as the sodium salt) with imipenem to prolong the antibacterial effect of the latter by preventing its renal metabolism to inactive and potentially nephrotoxic products. Cilastatin also acts as a leukotriene D4 dipeptidase inhibitor, preventing the metabolism of leukotriene D4 to leukotriene E4.cilastatin
cilastatin sodiumThe monosodium salt of cilastatin. It is an inhibitor of dehydropeptidase I (membrane dipeptidase, 3.4.13.19), an enzyme found in the brush border of renal tubes and responsible for degrading the antibiotic imipenem. Cilastatin sodium is therefore administered with imipenem to prolong the antibacterial effect of the latter by preventing its renal metabolism to microbiologically inactive and potentially nephrotoxic products.cilastatin sodium
e 64E64 zwitterion; E64
GRL-0617A benzamide resulting from the formal condensation of the carboxy group of 5-amino-2-methylbenzoic acid with the amino group of (1R)-1-(naphthalen-1-yl)ethan-1-amine. It is a potent noncovalent inhibitor (IC50 = 600 nM) of severe acute respiratory syndrome-coronavirus papain-like protease (SARS-CoV PLpro).GRL-0617
KOM70144A benzamide that is GRL-0617 in which one of the hydrogen's of the primary amino group is replaced by an acetyl group. It an inhibitor of SARS-CoV and SARS-CoV-2 papain-like protease (PLpro) with an IC50 of 2.6 muM and 5.0 muM, respectively. It also inhibits SARS-CoV and SARS-CoV-2 infection of Vero E6 cells in vitro (EC50 values are 13.1 and 21 muM, respectively).KOM70144
z-val-ala-asp(ome)-fluoromethylketoneA tripeptide consisting of Z-Val-Ala-Asp(OMe) in which the C-terminal OH group has been replaced by a fluoromethyl group. An irreversible pan-caspase inhibitor.Z-Val-Ala-Asp(OMe)-CH2F

Research

Studies (8,576)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990373 (4.35)18.7374
1990's652 (7.60)18.2507
2000's2,044 (23.83)29.6817
2010's4,238 (49.42)24.3611
2020's1,269 (14.80)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1,131 (12.77%)5.53%
Reviews1,049 (11.85%)6.00%
Case Studies990 (11.18%)4.05%
Observational43 (0.49%)0.25%
Other5,642 (63.72%)84.16%

Protein Targets (182)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
AR proteinHomo sapiens (human)Potency0.8203712
Ataxin-2Homo sapiens (human)Potency0.020012
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency0.020424
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency0.211311
caspase-3Cricetulus griseus (Chinese hamster)Potency0.006711
caspase-3Homo sapiens (human)Potency0.211311
Caspase-7Cricetulus griseus (Chinese hamster)Potency0.006711
Cellular tumor antigen p53Homo sapiens (human)Potency1.509525
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency75.193011
chromobox protein homolog 1Homo sapiens (human)Potency100.000011
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency3.884922
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency0.018012
DNA polymerase kappa isoform 1Homo sapiens (human)Potency29.934911
estrogen nuclear receptor alphaHomo sapiens (human)Potency0.1326915
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency1.509222
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency0.019467
EWS/FLI fusion proteinHomo sapiens (human)Potency9.897247
farnesoid X nuclear receptorHomo sapiens (human)Potency6.049222
Fumarate hydrataseHomo sapiens (human)Potency0.033211
gemininHomo sapiens (human)Potency16.718522
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency0.012724
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency0.059611
GTP-binding nuclear protein Ran isoform 1Homo sapiens (human)Potency6.513111
heat shock protein beta-1Homo sapiens (human)Potency0.288122
Histone H2A.xCricetulus griseus (Chinese hamster)Potency15.556511
importin subunit beta-1 isoform 1Homo sapiens (human)Potency6.513111
Interferon betaHomo sapiens (human)Potency0.049824
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency0.021622
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency0.010612
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency0.111133
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency0.047234
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency0.268433
phosphopantetheinyl transferaseBacillus subtilisPotency79.432811
polyproteinZika virusPotency0.033211
PPM1D proteinHomo sapiens (human)Potency0.041512
pregnane X nuclear receptorHomo sapiens (human)Potency0.008411
progesterone receptorHomo sapiens (human)Potency0.943911
RAR-related orphan receptor gammaMus musculus (house mouse)Potency0.038622
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency0.009411
retinoid X nuclear receptor alphaHomo sapiens (human)Potency0.066822
snurportin-1Homo sapiens (human)Potency6.513111
TDP1 proteinHomo sapiens (human)Potency0.009224
thioredoxin glutathione reductaseSchistosoma mansoniPotency0.794311
thioredoxin reductaseRattus norvegicus (Norway rat)Potency70.794611
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency0.025035
transcriptional regulator ERG isoform 3Homo sapiens (human)Potency3.162311
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency1.873833
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency0.059611

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
26S proteasome complex subunit SEM1Homo sapiens (human)IC500.533544
26S proteasome non-ATPase regulatory subunit 1Homo sapiens (human)IC500.533544
26S proteasome non-ATPase regulatory subunit 11Homo sapiens (human)IC500.533544
26S proteasome non-ATPase regulatory subunit 12Homo sapiens (human)IC500.533544
26S proteasome non-ATPase regulatory subunit 13Homo sapiens (human)IC500.533544
26S proteasome non-ATPase regulatory subunit 14Homo sapiens (human)IC500.533544
26S proteasome non-ATPase regulatory subunit 2Homo sapiens (human)IC500.533544
26S proteasome non-ATPase regulatory subunit 3Homo sapiens (human)IC500.533544
26S proteasome non-ATPase regulatory subunit 4Homo sapiens (human)IC500.533544
26S proteasome non-ATPase regulatory subunit 6Homo sapiens (human)IC500.533544
26S proteasome non-ATPase regulatory subunit 7Homo sapiens (human)IC500.533544
26S proteasome non-ATPase regulatory subunit 8Homo sapiens (human)IC500.533544
26S proteasome regulatory subunit 10BHomo sapiens (human)IC500.533544
26S proteasome regulatory subunit 4Homo sapiens (human)IC500.533544
26S proteasome regulatory subunit 6AHomo sapiens (human)IC500.533544
26S proteasome regulatory subunit 6BHomo sapiens (human)IC500.533544
26S proteasome regulatory subunit 7Homo sapiens (human)IC500.533544
26S proteasome regulatory subunit 8Homo sapiens (human)IC500.533544
Aminopeptidase NSus scrofa (pig)IC501.100011
Aminopeptidase NHomo sapiens (human)Ki0.200011
Aminopeptidase NSus scrofa (pig)Ki0.680033
Angiotensin-converting enzymeRattus norvegicus (Norway rat)IC501.100011
Angiotensin-converting enzyme 2 Homo sapiens (human)IC500.580012
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000011
ATP-dependent Clp protease proteolytic subunitStaphylococcus aureus subsp. aureus NCTC 8325IC505.300011
Beta-1 adrenergic receptorRattus norvegicus (Norway rat)Ki0.170013
Beta-2 adrenergic receptorRattus norvegicus (Norway rat)Ki0.170013
Beta-3 adrenergic receptorRattus norvegicus (Norway rat)Ki0.170013
Beta-carbonic anhydrase 1Mycobacterium tuberculosis H37RvKi7.300011
Bile salt export pumpHomo sapiens (human)IC50133.000011
Calpain-1 catalytic subunitHomo sapiens (human)IC500.100011
Calpain-1 catalytic subunitSus scrofa (pig)Ki3.960011
Calpain-9Homo sapiens (human)IC5055.790012
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000011
Carbonic anhydrase 1Homo sapiens (human)Ki1.290022
Carbonic anhydrase 12Homo sapiens (human)Ki5.870011
Carbonic anhydrase 13Homo sapiens (human)Ki8.450011
Carbonic anhydrase 14Homo sapiens (human)Ki3.280011
Carbonic anhydrase 15Mus musculus (house mouse)Ki2.680011
Carbonic anhydrase 2Homo sapiens (human)Ki1.160022
Carbonic anhydrase 3Homo sapiens (human)Ki4.570011
Carbonic anhydrase 4Homo sapiens (human)Ki6.510011
Carbonic anhydrase 5A, mitochondrialHomo sapiens (human)Ki6.920011
Carbonic anhydrase 5B, mitochondrialHomo sapiens (human)Ki6.830011
Carbonic anhydrase 6Homo sapiens (human)Ki4.380011
Carbonic anhydrase 7Homo sapiens (human)Ki6.940011
Carbonic anhydrase 9Homo sapiens (human)Ki3.380011
Caspase-1Homo sapiens (human)IC507.0641510
Caspase-1Homo sapiens (human)Ki0.009112
Caspase-2Homo sapiens (human)IC500.021011
Caspase-3Homo sapiens (human)IC500.03401722
Caspase-3Homo sapiens (human)Ki0.009112
Caspase-6Homo sapiens (human)IC500.007735
Caspase-7Homo sapiens (human)IC500.05601015
Caspase-8Homo sapiens (human)IC500.0602510
Cathepsin BHomo sapiens (human)IC506.014155
Cathepsin BHomo sapiens (human)Ki16.000011
Cathepsin GHomo sapiens (human)IC501.810022
Cathepsin GHomo sapiens (human)Ki0.630011
Cathepsin SHomo sapiens (human)IC500.007011
Chain A, caspase-3, p17 subunitHomo sapiens (human)Ki0.001313
Chain B, caspase-3, p12 subunitHomo sapiens (human)Ki0.001313
Chain H, Proteasome component PUP1Saccharomyces cerevisiae (brewer's yeast)Ki0.000611
Chain I, Proteasome component PUP3Saccharomyces cerevisiae (brewer's yeast)Ki0.000611
Chain K, Proteasome component PRE2Saccharomyces cerevisiae (brewer's yeast)Ki0.000612
Chain L, Proteasome component C5Saccharomyces cerevisiae (brewer's yeast)Ki0.000612
ChymaseHomo sapiens (human)IC501.190011
Chymotrypsinogen ABos taurus (cattle)Ki2.400011
Chymotrypsinogen BHomo sapiens (human)Ki0.320011
CruzipainTrypanosoma cruziIC500.210022
Cysteine protease Trypanosoma brucei rhodesienseIC500.003111
Cysteine protease Trypanosoma brucei rhodesienseKi0.035011
Cysteine protease falcipain-3Plasmodium falciparum (malaria parasite P. falciparum)IC500.197233
Cysteine proteinase falcipain 2a Plasmodium falciparum (malaria parasite P. falciparum)IC500.082866
Cysteine proteinase falcipain 2a Plasmodium falciparum (malaria parasite P. falciparum)Ki13.626733
Cytosol aminopeptidaseHomo sapiens (human)Ki5.112544
Dipeptidase 1Sus scrofa (pig)Ki0.170013
Dipeptidyl peptidase 1Homo sapiens (human)IC500.770011
Fatty acid synthase Rattus norvegicus (Norway rat)IC50300.000011
Glutamyl aminopeptidaseHomo sapiens (human)Ki8.000011
Histone deacetylase 1Homo sapiens (human)IC500.620011
Histone deacetylase 2Homo sapiens (human)IC500.800011
Histone deacetylase 3Homo sapiens (human)IC501.180011
Histone deacetylase 6Homo sapiens (human)IC5069.440011
Histone deacetylase 8Homo sapiens (human)IC500.072011
Leucyl-cystinyl aminopeptidaseRattus norvegicus (Norway rat)Ki0.120022
Leukotriene B4 receptor 1Homo sapiens (human)Ki0.030012
Liver carboxylesteraseSus scrofa (pig)IC50300.000011
Lon protease homolog, mitochondrialHomo sapiens (human)IC500.183011
Lysosomal protective proteinHomo sapiens (human)IC50154.600022
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000011
NACHT, LRR and PYD domains-containing protein 3 Mus musculus (house mouse)IC500.040711
Neutrophil elastaseHomo sapiens (human)IC50300.000011
Neutrophil elastaseHomo sapiens (human)Ki2.300011
Nuclear factor NF-kappa-B p100 subunit Homo sapiens (human)IC500.085011
Nuclear factor NF-kappa-B p105 subunitHomo sapiens (human)IC500.085011
PapainCarica papaya (papaya)IC500.018733
PapainCarica papaya (papaya)Ki5.080011
Polyunsaturated fatty acid 5-lipoxygenaseHomo sapiens (human)Ki0.030011
Pro-cathepsin HHomo sapiens (human)IC500.190011
Procathepsin LHomo sapiens (human)IC500.185667
Procathepsin LHomo sapiens (human)Ki0.030011
Proteasomal ubiquitin receptor ADRM1Homo sapiens (human)IC500.533544
Proteasome subunit alpha type-1Homo sapiens (human)IC500.321377
Proteasome subunit alpha type-2Homo sapiens (human)IC500.321377
Proteasome subunit alpha type-3Homo sapiens (human)IC500.321377
Proteasome subunit alpha type-4Homo sapiens (human)IC500.321377
Proteasome subunit alpha type-5Homo sapiens (human)IC500.321377
Proteasome subunit alpha type-6Homo sapiens (human)IC500.321377
Proteasome subunit alpha type-7Homo sapiens (human)IC500.321377
Proteasome subunit alpha-type 8Homo sapiens (human)IC500.321377
Proteasome subunit beta type-1Homo sapiens (human)IC500.21491818
Proteasome subunit beta type-10Homo sapiens (human)IC500.53591010
Proteasome subunit beta type-11Homo sapiens (human)IC500.321377
Proteasome subunit beta type-2Homo sapiens (human)IC502.98601919
Proteasome subunit beta type-3Homo sapiens (human)IC500.321377
Proteasome subunit beta type-4Homo sapiens (human)IC500.321377
Proteasome subunit beta type-5Homo sapiens (human)IC5015,084.28363234
Proteasome subunit beta type-5Homo sapiens (human)Ki0.006733
Proteasome subunit beta type-6Homo sapiens (human)IC500.284288
Proteasome subunit beta type-7Homo sapiens (human)IC501.877288
Proteasome subunit beta type-8Homo sapiens (human)IC500.16811414
Proteasome subunit beta type-8Mus musculus (house mouse)IC500.016811
Proteasome subunit beta type-9Homo sapiens (human)IC500.20591111
ProthrombinHomo sapiens (human)Ki13.000011
Replicase polyprotein 1aSevere acute respiratory syndrome-related coronavirusIC500.580012
Replicase polyprotein 1abBetacoronavirus England 1IC500.580012
Replicase polyprotein 1abHuman coronavirus 229EIC500.580012
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC502.79931215
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusIC500.918035
Solute carrier family 22 member 6Homo sapiens (human)IC502,550.000011
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)IC502,387.000011
Solute carrier family 22 member 6Homo sapiens (human)Ki1,470.000011
Solute carrier family 22 member 8Homo sapiens (human)IC50249.000011
Solute carrier family 22 member 8Rattus norvegicus (Norway rat)IC50742.000011
Solute carrier family 22 member 8Homo sapiens (human)Ki231.000011
Spike glycoproteinBetacoronavirus England 1IC500.580012
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusIC500.580012
Transcription factor p65Homo sapiens (human)IC500.085011
Transmembrane protease serine 2Homo sapiens (human)IC500.580012

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Angiotensin-converting enzyme 2 Homo sapiens (human)EC5020.000011
ATP-dependent Clp protease proteolytic subunitStaphylococcus aureus subsp. aureus NCTC 8325EC5023.500011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2EC5024.300012
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2Kd6.745022

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Proteasome subunit beta type-1Homo sapiens (human)Ki500.025022
Proteasome subunit beta type-2Homo sapiens (human)Ki501.075022
Proteasome subunit beta type-5Homo sapiens (human)Ki500.010022