protease inhibitor

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

ChEBI ID: 37670

Members (9)

Member	Definition	Class
acetyl-aspartyl-glutamyl-valyl-aspartal	A 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
amastatin	A tetrapeptide comprising (2S,3R)-3-amino-2-hydroxy-5-methylhexanoyl, L-valyl, L-valyl and L-aspartic acid units joined in sequence	amastatin
bortezomib	L-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
cilastatin	The 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 sodium	The 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 64		E64 zwitterion; E64
GRL-0617	A 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
KOM70144	A 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)-fluoromethylketone	A 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)

Timeframe	Studies, Drugs with This Role(%)	All Drugs %
pre-1990	373 (4.35)	18.7374
1990's	652 (7.60)	18.2507
2000's	2,044 (23.83)	29.6817
2010's	4,238 (49.42)	24.3611
2020's	1,269 (14.80)	2.80

Study Types

Publication Type	Studies, Drugs with this Role (%)	All Drugs (%)
Trials	1,131 (12.77%)	5.53%
Reviews	1,049 (11.85%)	6.00%
Case Studies	990 (11.18%)	4.05%
Observational	43 (0.49%)	0.25%
Other	5,642 (63.72%)	84.16%

Protein Targets (182)

Potency Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
AR protein	Homo sapiens (human)	Potency	0.8203	7	12
Ataxin-2	Homo sapiens (human)	Potency	0.0200	1	2
ATPase family AAA domain-containing protein 5	Homo sapiens (human)	Potency	0.0204	2	4
caspase 7, apoptosis-related cysteine protease	Homo sapiens (human)	Potency	0.2113	1	1
caspase-3	Cricetulus griseus (Chinese hamster)	Potency	0.0067	1	1
caspase-3	Homo sapiens (human)	Potency	0.2113	1	1
Caspase-7	Cricetulus griseus (Chinese hamster)	Potency	0.0067	1	1
Cellular tumor antigen p53	Homo sapiens (human)	Potency	1.5095	2	5
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE	Homo sapiens (human)	Potency	75.1930	1	1
chromobox protein homolog 1	Homo sapiens (human)	Potency	100.0000	1	1
cytochrome P450 family 3 subfamily A polypeptide 4	Homo sapiens (human)	Potency	3.8849	2	2
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a	Homo sapiens (human)	Potency	0.0180	1	2
DNA polymerase kappa isoform 1	Homo sapiens (human)	Potency	29.9349	1	1
estrogen nuclear receptor alpha	Homo sapiens (human)	Potency	0.1326	9	15
estrogen receptor 2 (ER beta)	Homo sapiens (human)	Potency	1.5092	2	2
estrogen-related nuclear receptor alpha	Homo sapiens (human)	Potency	0.0194	6	7
EWS/FLI fusion protein	Homo sapiens (human)	Potency	9.8972	4	7
farnesoid X nuclear receptor	Homo sapiens (human)	Potency	6.0492	2	2
Fumarate hydratase	Homo sapiens (human)	Potency	0.0332	1	1
geminin	Homo sapiens (human)	Potency	16.7185	2	2
glucocorticoid receptor [Homo sapiens]	Homo sapiens (human)	Potency	0.0127	2	4
Glutamate receptor 2	Rattus norvegicus (Norway rat)	Potency	0.0596	1	1
GTP-binding nuclear protein Ran isoform 1	Homo sapiens (human)	Potency	6.5131	1	1
heat shock protein beta-1	Homo sapiens (human)	Potency	0.2881	2	2
Histone H2A.x	Cricetulus griseus (Chinese hamster)	Potency	15.5565	1	1
importin subunit beta-1 isoform 1	Homo sapiens (human)	Potency	6.5131	1	1
Interferon beta	Homo sapiens (human)	Potency	0.0498	2	4
nuclear factor erythroid 2-related factor 2 isoform 1	Homo sapiens (human)	Potency	0.0216	2	2
nuclear receptor subfamily 1, group I, member 2	Rattus norvegicus (Norway rat)	Potency	0.0106	1	2
nuclear receptor subfamily 1, group I, member 3	Homo sapiens (human)	Potency	0.1111	3	3
peroxisome proliferator activated receptor gamma	Homo sapiens (human)	Potency	0.0472	3	4
peroxisome proliferator-activated receptor delta	Homo sapiens (human)	Potency	0.2684	3	3
phosphopantetheinyl transferase	Bacillus subtilis	Potency	79.4328	1	1
polyprotein	Zika virus	Potency	0.0332	1	1
PPM1D protein	Homo sapiens (human)	Potency	0.0415	1	2
pregnane X nuclear receptor	Homo sapiens (human)	Potency	0.0084	1	1
progesterone receptor	Homo sapiens (human)	Potency	0.9439	1	1
RAR-related orphan receptor gamma	Mus musculus (house mouse)	Potency	0.0386	2	2
retinoic acid nuclear receptor alpha variant 1	Homo sapiens (human)	Potency	0.0094	1	1
retinoid X nuclear receptor alpha	Homo sapiens (human)	Potency	0.0668	2	2
snurportin-1	Homo sapiens (human)	Potency	6.5131	1	1
TDP1 protein	Homo sapiens (human)	Potency	0.0092	2	4
thioredoxin glutathione reductase	Schistosoma mansoni	Potency	0.7943	1	1
thioredoxin reductase	Rattus norvegicus (Norway rat)	Potency	70.7946	1	1
thyroid hormone receptor beta isoform 2	Rattus norvegicus (Norway rat)	Potency	0.0250	3	5
transcriptional regulator ERG isoform 3	Homo sapiens (human)	Potency	3.1623	1	1
vitamin D (1,25- dihydroxyvitamin D3) receptor	Homo sapiens (human)	Potency	1.8738	3	3
Voltage-dependent calcium channel gamma-2 subunit	Mus musculus (house mouse)	Potency	0.0596	1	1

Inhibition Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
26S proteasome complex subunit SEM1	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome non-ATPase regulatory subunit 1	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome non-ATPase regulatory subunit 11	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome non-ATPase regulatory subunit 12	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome non-ATPase regulatory subunit 13	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome non-ATPase regulatory subunit 14	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome non-ATPase regulatory subunit 2	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome non-ATPase regulatory subunit 3	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome non-ATPase regulatory subunit 4	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome non-ATPase regulatory subunit 6	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome non-ATPase regulatory subunit 7	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome non-ATPase regulatory subunit 8	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome regulatory subunit 10B	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome regulatory subunit 4	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome regulatory subunit 6A	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome regulatory subunit 6B	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome regulatory subunit 7	Homo sapiens (human)	IC50	0.5335	4	4
26S proteasome regulatory subunit 8	Homo sapiens (human)	IC50	0.5335	4	4
Aminopeptidase N	Sus scrofa (pig)	IC50	1.1000	1	1
Aminopeptidase N	Homo sapiens (human)	Ki	0.2000	1	1
Aminopeptidase N	Sus scrofa (pig)	Ki	0.6800	3	3
Angiotensin-converting enzyme	Rattus norvegicus (Norway rat)	IC50	1.1000	1	1
Angiotensin-converting enzyme 2	Homo sapiens (human)	IC50	0.5800	1	2
ATP-binding cassette sub-family C member 3	Homo sapiens (human)	IC50	133.0000	1	1
ATP-dependent Clp protease proteolytic subunit	Staphylococcus aureus subsp. aureus NCTC 8325	IC50	5.3000	1	1
Beta-1 adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.1700	1	3
Beta-2 adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.1700	1	3
Beta-3 adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.1700	1	3
Beta-carbonic anhydrase 1	Mycobacterium tuberculosis H37Rv	Ki	7.3000	1	1
Bile salt export pump	Homo sapiens (human)	IC50	133.0000	1	1
Calpain-1 catalytic subunit	Homo sapiens (human)	IC50	0.1000	1	1
Calpain-1 catalytic subunit	Sus scrofa (pig)	Ki	3.9600	1	1
Calpain-9	Homo sapiens (human)	IC50	55.7900	1	2
Canalicular multispecific organic anion transporter 1	Homo sapiens (human)	IC50	133.0000	1	1
Carbonic anhydrase 1	Homo sapiens (human)	Ki	1.2900	2	2
Carbonic anhydrase 12	Homo sapiens (human)	Ki	5.8700	1	1
Carbonic anhydrase 13	Homo sapiens (human)	Ki	8.4500	1	1
Carbonic anhydrase 14	Homo sapiens (human)	Ki	3.2800	1	1
Carbonic anhydrase 15	Mus musculus (house mouse)	Ki	2.6800	1	1
Carbonic anhydrase 2	Homo sapiens (human)	Ki	1.1600	2	2
Carbonic anhydrase 3	Homo sapiens (human)	Ki	4.5700	1	1
Carbonic anhydrase 4	Homo sapiens (human)	Ki	6.5100	1	1
Carbonic anhydrase 5A, mitochondrial	Homo sapiens (human)	Ki	6.9200	1	1
Carbonic anhydrase 5B, mitochondrial	Homo sapiens (human)	Ki	6.8300	1	1
Carbonic anhydrase 6	Homo sapiens (human)	Ki	4.3800	1	1
Carbonic anhydrase 7	Homo sapiens (human)	Ki	6.9400	1	1
Carbonic anhydrase 9	Homo sapiens (human)	Ki	3.3800	1	1
Caspase-1	Homo sapiens (human)	IC50	7.0641	5	10
Caspase-1	Homo sapiens (human)	Ki	0.0091	1	2
Caspase-2	Homo sapiens (human)	IC50	0.0210	1	1
Caspase-3	Homo sapiens (human)	IC50	0.0340	17	22
Caspase-3	Homo sapiens (human)	Ki	0.0091	1	2
Caspase-6	Homo sapiens (human)	IC50	0.0077	3	5
Caspase-7	Homo sapiens (human)	IC50	0.0560	10	15
Caspase-8	Homo sapiens (human)	IC50	0.0602	5	10
Cathepsin B	Homo sapiens (human)	IC50	6.0141	5	5
Cathepsin B	Homo sapiens (human)	Ki	16.0000	1	1
Cathepsin G	Homo sapiens (human)	IC50	1.8100	2	2
Cathepsin G	Homo sapiens (human)	Ki	0.6300	1	1
Cathepsin S	Homo sapiens (human)	IC50	0.0070	1	1
Chain A, caspase-3, p17 subunit	Homo sapiens (human)	Ki	0.0013	1	3
Chain B, caspase-3, p12 subunit	Homo sapiens (human)	Ki	0.0013	1	3
Chain H, Proteasome component PUP1	Saccharomyces cerevisiae (brewer's yeast)	Ki	0.0006	1	1
Chain I, Proteasome component PUP3	Saccharomyces cerevisiae (brewer's yeast)	Ki	0.0006	1	1
Chain K, Proteasome component PRE2	Saccharomyces cerevisiae (brewer's yeast)	Ki	0.0006	1	2
Chain L, Proteasome component C5	Saccharomyces cerevisiae (brewer's yeast)	Ki	0.0006	1	2
Chymase	Homo sapiens (human)	IC50	1.1900	1	1
Chymotrypsinogen A	Bos taurus (cattle)	Ki	2.4000	1	1
Chymotrypsinogen B	Homo sapiens (human)	Ki	0.3200	1	1
Cruzipain	Trypanosoma cruzi	IC50	0.2100	2	2
Cysteine protease	Trypanosoma brucei rhodesiense	IC50	0.0031	1	1
Cysteine protease	Trypanosoma brucei rhodesiense	Ki	0.0350	1	1
Cysteine protease falcipain-3	Plasmodium falciparum (malaria parasite P. falciparum)	IC50	0.1972	3	3
Cysteine proteinase falcipain 2a	Plasmodium falciparum (malaria parasite P. falciparum)	IC50	0.0828	6	6
Cysteine proteinase falcipain 2a	Plasmodium falciparum (malaria parasite P. falciparum)	Ki	13.6267	3	3
Cytosol aminopeptidase	Homo sapiens (human)	Ki	5.1125	4	4
Dipeptidase 1	Sus scrofa (pig)	Ki	0.1700	1	3
Dipeptidyl peptidase 1	Homo sapiens (human)	IC50	0.7700	1	1
Fatty acid synthase	Rattus norvegicus (Norway rat)	IC50	300.0000	1	1
Glutamyl aminopeptidase	Homo sapiens (human)	Ki	8.0000	1	1
Histone deacetylase 1	Homo sapiens (human)	IC50	0.6200	1	1
Histone deacetylase 2	Homo sapiens (human)	IC50	0.8000	1	1
Histone deacetylase 3	Homo sapiens (human)	IC50	1.1800	1	1
Histone deacetylase 6	Homo sapiens (human)	IC50	69.4400	1	1
Histone deacetylase 8	Homo sapiens (human)	IC50	0.0720	1	1
Leucyl-cystinyl aminopeptidase	Rattus norvegicus (Norway rat)	Ki	0.1200	2	2
Leukotriene B4 receptor 1	Homo sapiens (human)	Ki	0.0300	1	2
Liver carboxylesterase	Sus scrofa (pig)	IC50	300.0000	1	1
Lon protease homolog, mitochondrial	Homo sapiens (human)	IC50	0.1830	1	1
Lysosomal protective protein	Homo sapiens (human)	IC50	154.6000	2	2
Multidrug resistance-associated protein 4	Homo sapiens (human)	IC50	133.0000	1	1
NACHT, LRR and PYD domains-containing protein 3	Mus musculus (house mouse)	IC50	0.0407	1	1
Neutrophil elastase	Homo sapiens (human)	IC50	300.0000	1	1
Neutrophil elastase	Homo sapiens (human)	Ki	2.3000	1	1
Nuclear factor NF-kappa-B p100 subunit	Homo sapiens (human)	IC50	0.0850	1	1
Nuclear factor NF-kappa-B p105 subunit	Homo sapiens (human)	IC50	0.0850	1	1
Papain	Carica papaya (papaya)	IC50	0.0187	3	3
Papain	Carica papaya (papaya)	Ki	5.0800	1	1
Polyunsaturated fatty acid 5-lipoxygenase	Homo sapiens (human)	Ki	0.0300	1	1
Pro-cathepsin H	Homo sapiens (human)	IC50	0.1900	1	1
Procathepsin L	Homo sapiens (human)	IC50	0.1856	6	7
Procathepsin L	Homo sapiens (human)	Ki	0.0300	1	1
Proteasomal ubiquitin receptor ADRM1	Homo sapiens (human)	IC50	0.5335	4	4
Proteasome subunit alpha type-1	Homo sapiens (human)	IC50	0.3213	7	7
Proteasome subunit alpha type-2	Homo sapiens (human)	IC50	0.3213	7	7
Proteasome subunit alpha type-3	Homo sapiens (human)	IC50	0.3213	7	7
Proteasome subunit alpha type-4	Homo sapiens (human)	IC50	0.3213	7	7
Proteasome subunit alpha type-5	Homo sapiens (human)	IC50	0.3213	7	7
Proteasome subunit alpha type-6	Homo sapiens (human)	IC50	0.3213	7	7
Proteasome subunit alpha type-7	Homo sapiens (human)	IC50	0.3213	7	7
Proteasome subunit alpha-type 8	Homo sapiens (human)	IC50	0.3213	7	7
Proteasome subunit beta type-1	Homo sapiens (human)	IC50	0.2149	18	18
Proteasome subunit beta type-10	Homo sapiens (human)	IC50	0.5359	10	10
Proteasome subunit beta type-11	Homo sapiens (human)	IC50	0.3213	7	7
Proteasome subunit beta type-2	Homo sapiens (human)	IC50	2.9860	19	19
Proteasome subunit beta type-3	Homo sapiens (human)	IC50	0.3213	7	7
Proteasome subunit beta type-4	Homo sapiens (human)	IC50	0.3213	7	7
Proteasome subunit beta type-5	Homo sapiens (human)	IC50	15,084.2836	32	34
Proteasome subunit beta type-5	Homo sapiens (human)	Ki	0.0067	3	3
Proteasome subunit beta type-6	Homo sapiens (human)	IC50	0.2842	8	8
Proteasome subunit beta type-7	Homo sapiens (human)	IC50	1.8772	8	8
Proteasome subunit beta type-8	Homo sapiens (human)	IC50	0.1681	14	14
Proteasome subunit beta type-8	Mus musculus (house mouse)	IC50	0.0168	1	1
Proteasome subunit beta type-9	Homo sapiens (human)	IC50	0.2059	11	11
Prothrombin	Homo sapiens (human)	Ki	13.0000	1	1
Replicase polyprotein 1a	Severe acute respiratory syndrome-related coronavirus	IC50	0.5800	1	2
Replicase polyprotein 1ab	Betacoronavirus England 1	IC50	0.5800	1	2
Replicase polyprotein 1ab	Human coronavirus 229E	IC50	0.5800	1	2
Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2	IC50	2.7993	12	15
Replicase polyprotein 1ab	Severe acute respiratory syndrome-related coronavirus	IC50	0.9180	3	5
Solute carrier family 22 member 6	Homo sapiens (human)	IC50	2,550.0000	1	1
Solute carrier family 22 member 6	Rattus norvegicus (Norway rat)	IC50	2,387.0000	1	1
Solute carrier family 22 member 6	Homo sapiens (human)	Ki	1,470.0000	1	1
Solute carrier family 22 member 8	Homo sapiens (human)	IC50	249.0000	1	1
Solute carrier family 22 member 8	Rattus norvegicus (Norway rat)	IC50	742.0000	1	1
Solute carrier family 22 member 8	Homo sapiens (human)	Ki	231.0000	1	1
Spike glycoprotein	Betacoronavirus England 1	IC50	0.5800	1	2
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	IC50	0.5800	1	2
Transcription factor p65	Homo sapiens (human)	IC50	0.0850	1	1
Transmembrane protease serine 2	Homo sapiens (human)	IC50	0.5800	1	2

Activation Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
Angiotensin-converting enzyme 2	Homo sapiens (human)	EC50	20.0000	1	1
ATP-dependent Clp protease proteolytic subunit	Staphylococcus aureus subsp. aureus NCTC 8325	EC50	23.5000	1	1
Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2	EC50	24.3000	1	2
Replicase polyprotein 1ab	Severe acute respiratory syndrome coronavirus 2	Kd	6.7450	2	2

Other Measurements

Protein	Taxonomy	Measurement	Average (mM)	Bioassay(s)	Drugs
Proteasome subunit beta type-1	Homo sapiens (human)	Ki50	0.0250	2	2
Proteasome subunit beta type-2	Homo sapiens (human)	Ki50	1.0750	2	2
Proteasome subunit beta type-5	Homo sapiens (human)	Ki50	0.0100	2	2

chemdatabank.com

protease inhibitor

Members (9)

Research

Studies (8,576)

Study Types

Protein Targets (182)

Potency Measurements

Inhibition Measurements

Activation Measurements

Other Measurements