Page last updated: 2024-08-05 15:19:26
hepatitis C protease inhibitor
An inhibitor of hepatitis C protease, an enzyme required for production of proteins needed for viral assembly.
ChEBI ID: 64924
Members (9)
| Member | Definition | Class |
|---|---|---|
| 5-o-methylembelin | A member of the class of monohydroxy-1,4-benzoquinones that is embelin in which the hydroxy group at position 5 is replaced by a methoxy group. Isolated from Lysimachia punctata and Embelia ribes, it exhibits antileishmanial activity as well as inhibitory activity towards hepatitis C protease. | 5-O-methyl embelin |
| embelin | A member of the class of dihydroxy-1,4-benzoquinones that is 2,5-dihydroxy-1,4-benzoquinone which is substituted by an undecyl group at position 3. Isolated from Lysimachia punctata and Embelia ribes, it exhibits antimicrobial, antineoplastic and inhibitory activity towards hepatitis C protease. | embelin |
| grazoprevir | An azamacrocyclic compound that is a hepatitis C protease inhibitor used in combination with elbasvir (under the brand name Zepatier) for treatment of chronic HCV genotypes 1 or 4 infection in adults. | grazoprevir |
| ledipasvir | A benzimidazole derivative that is used in combination with sofosbuvir (under the trade name Harvoni) for the treatment of chronic hepatitis C genotype 1 infection. | ledipasvir |
| mk-7009 | An azamacrocyclic compound that is a hepatitis C virus (HCV) NS3/4A protease inhibitor which is approved for the treatment of hepatitis C virus infections in Japan. | vaniprevir |
| n-(3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl)-3-(2-((((1,1-dimethylethyl)amino)carbonyl)amino)-3,3-dimethyl-1-oxobutyl)-6,6-dimethyl-3-azabicyclo(3.1.0)hexan-2-carboxamide | A synthetic tripeptide consisting of N-(tert-butylcarbamoyl)-3-methyl-L-valyl, a cyclopropyl-fused prolyl and 3-amino-4-cyclobutyl-2-oxobutanamide residues joined in sequence. Used for treatment of chronic hepatitis C virus genotype 1 infection. | boceprevir |
| narlaprevir | An azabicyclohexane that is (1R,5S)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane substituted by [(3S)-1-(cyclopropylamino)-1,2-dioxoheptan-3-yl]aminoacyl and N-({1-[(tert-butylsulfonyl)methyl]cyclohexyl}carbamoyl)-3-methyl-L-valyl groups at positions 2S and 3, respectively. It is a hepatitis C virus (HCV) NS3/4A serine protease inhibitor (Ki = 6 nM) that is used for the treatment of chronic hepatitis C. | narlaprevir |
| sofosbuvir | A nucleotide conjugate that is used in combination with ledipasvir (under the trade name Harvoni) for the treatment of chronic hepatitis C genotype 1 infection. | sofosbuvir |
| telaprevir | An oligopeptide consisting of N-(pyrazin-2-ylcarbonyl)cyclohexylalanyl, 3-methylvalyl, octahydrocyclopenta[c]pyrrole-1-carboxy, and 3-amino-N-cyclopropyl-2-oxohexanamide residues joined in sequence. Used for treatment of chronic hepatitis C virus genotype 1 infection. | telaprevir |
Research
Studies (3,431)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 13 (0.38) | 18.7374 |
| 1990's | 9 (0.26) | 18.2507 |
| 2000's | 99 (2.89) | 29.6817 |
| 2010's | 2,635 (76.80) | 24.3611 |
| 2020's | 675 (19.67) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 579 (14.36%) | 5.53% |
| Reviews | 551 (13.66%) | 6.00% |
| Case Studies | 378 (9.37%) | 4.05% |
| Observational | 204 (5.06%) | 0.25% |
| Other | 2,321 (57.55%) | 84.16% |
Protein Targets (108)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 19.6222 | 1 | 2 |
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 5.0119 | 1 | 1 |
| 67.9K protein | Vaccinia virus | Potency | 12.3564 | 2 | 3 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 27.8397 | 1 | 3 |
| apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 39.8107 | 1 | 1 |
| cellular tumor antigen p53 isoform a | Homo sapiens (human) | Potency | 12.5893 | 2 | 2 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 12.2097 | 1 | 2 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 21.4865 | 2 | 2 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 33.9972 | 1 | 2 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 25.0594 | 1 | 1 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 5.0119 | 1 | 1 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 21.4865 | 2 | 2 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 26.6320 | 1 | 2 |
| ClpP | Bacillus subtilis | Potency | 10.0000 | 1 | 1 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 25.1189 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 30.1116 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 6.7412 | 1 | 1 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 16.8090 | 1 | 2 |
| D(2) dopamine receptor isoform long | Homo sapiens (human) | Potency | 22.2803 | 1 | 2 |
| Disintegrin and metalloproteinase domain-containing protein 17 | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 89.7164 | 1 | 2 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 20.2676 | 1 | 2 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 29.9439 | 3 | 3 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 17.7828 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 30.1116 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 0.1032 | 1 | 1 |
| GLS protein | Homo sapiens (human) | Potency | 17.7828 | 1 | 2 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 27.7205 | 2 | 5 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 30.1116 | 1 | 1 |
| importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 125.8920 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 30.1116 | 1 | 2 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 1.5849 | 1 | 1 |
| Integrin alpha-IIb | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| Integrin beta-3 | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| Interferon beta | Homo sapiens (human) | Potency | 17.3809 | 2 | 4 |
| lethal factor (plasmid) | Bacillus anthracis str. A2012 | Potency | 7.5506 | 1 | 2 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 29.0839 | 2 | 6 |
| mitogen-activated protein kinase 1 | Homo sapiens (human) | Potency | 0.1259 | 1 | 1 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| polyunsaturated fatty acid lipoxygenase ALOX12 | Homo sapiens (human) | Potency | 8.9125 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| PPM1D protein | Homo sapiens (human) | Potency | 13.1373 | 1 | 2 |
| Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) | Potency | 84.2180 | 2 | 2 |
| serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 29.9349 | 1 | 1 |
| Smad3 | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| snurportin-1 | Homo sapiens (human) | Potency | 125.8920 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 28.1838 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 23.7246 | 2 | 2 |
| ubiquitin carboxyl-terminal hydrolase 2 isoform a | Homo sapiens (human) | Potency | 3.1623 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 46.1437 | 1 | 2 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cathepsin B | Homo sapiens (human) | IC50 | 1,669.4017 | 3 | 6 |
| Cathepsin F | Homo sapiens (human) | IC50 | 7.0333 | 1 | 3 |
| Cathepsin K | Homo sapiens (human) | IC50 | 3.5567 | 1 | 3 |
| Cathepsin L2 | Homo sapiens (human) | IC50 | 3.8083 | 1 | 3 |
| Cathepsin S | Homo sapiens (human) | IC50 | 48.0700 | 2 | 6 |
| Cereblon isoform 4 | Magnetospirillum gryphiswaldense | Ki | 24.5000 | 2 | 2 |
| Chain A, Genome polyprotein | Ki | 0.9580 | 1 | 3 | |
| Chain A, NS3 protease, NS4A protein | Ki | 0.9580 | 1 | 11 | |
| Chain A, NS3 protease,NS4A protein | Ki | 0.9580 | 1 | 1 | |
| Chymase | Homo sapiens (human) | IC50 | 3.3527 | 1 | 3 |
| Chymotrypsin-like elastase family member 1 | Homo sapiens (human) | IC50 | 6.6767 | 1 | 3 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Cytochrome P450 1A2 | Homo sapiens (human) | Ki | 6.1000 | 1 | 1 |
| Cytochrome P450 2C19 | Homo sapiens (human) | Ki | 0.0820 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 60.0000 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | Ki | 0.0039 | 1 | 1 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Cytochrome P450 2D6 | Homo sapiens (human) | Ki | 6.1000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 8.4000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | Ki | 0.0820 | 1 | 1 |
| E3 ubiquitin-protein ligase XIAP | Homo sapiens (human) | IC50 | 4.1000 | 3 | 3 |
| E3 ubiquitin-protein ligase XIAP | Homo sapiens (human) | Ki | 0.4000 | 1 | 1 |
| G-protein coupled receptor 84 | Homo sapiens (human) | Ki | 0.0236 | 1 | 1 |
| Genome polyprotein | Hepatitis C virus (isolate H77) | Ki | 0.0095 | 3 | 3 |
| Genome polyprotein | IC50 | 0.0007 | 3 | 3 | |
| Genome polyprotein | Ki | 0.0106 | 24 | 29 | |
| Histone acetyltransferase KAT2B | Homo sapiens (human) | IC50 | 7.2000 | 1 | 1 |
| Macrophage-expressed gene 1 protein | Homo sapiens (human) | IC50 | 3.1733 | 2 | 3 |
| Neutrophil elastase | Homo sapiens (human) | IC50 | 31.7100 | 3 | 8 |
| Non-structural protein 4A | IC50 | 0.0007 | 3 | 3 | |
| Non-structural protein 4A | Ki | 0.0099 | 5 | 7 | |
| Nonstructural protein 5A | IC50 | 0.0310 | 2 | 2 | |
| NS3 protease | IC50 | 0.9757 | 7 | 7 | |
| NS3 protease | Hepatitis C virus subtype 1b | IC50 | 0.0044 | 4 | 4 |
| NS3 protease | Ki | 0.0039 | 1 | 1 | |
| NS3 protease | Hepatitis C virus subtype 1b | Ki | 3.0910 | 2 | 2 |
| Plasminogen | Homo sapiens (human) | IC50 | 69.5667 | 1 | 3 |
| Polyunsaturated fatty acid 5-lipoxygenase | Homo sapiens (human) | IC50 | 1.4875 | 5 | 8 |
| Procathepsin L | Homo sapiens (human) | IC50 | 3,334.7533 | 1 | 3 |
| Prostaglandin E synthase | Homo sapiens (human) | IC50 | 0.2000 | 1 | 1 |
| Protein cereblon | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
| Prothrombin | Homo sapiens (human) | IC50 | 34.0000 | 1 | 3 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 | 7.9647 | 12 | 19 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | IC50 | 8.6257 | 3 | 7 |
| Trypsin-1 | Homo sapiens (human) | IC50 | 10.0000 | 1 | 2 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cytochrome P450 2C9 | Homo sapiens (human) | EC50 | 0.2300 | 1 | 1 |
| G-protein coupled receptor 84 | Homo sapiens (human) | EC50 | 2.0886 | 10 | 10 |
| Nonstructural protein 5A | EC50 | 0.1551 | 31 | 31 | |
| NS5 | Zika virus | EC50 | 15.5100 | 2 | 2 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | EC50 | 5.6550 | 2 | 2 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | EC50 | 1.3100 | 1 | 1 |
| RNA-directed RNA polymerase | EC50 | 0.1454 | 12 | 12 | |
| streptokinase A precursor | Streptococcus pyogenes M1 GAS | EC50 | 1.6710 | 1 | 1 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Aldo-keto reductase family 1 member C2 | Homo sapiens (human) | Km | 52.2600 | 1 | 1 |
| Aldo-keto reductase family 1 member C3 | Homo sapiens (human) | Km | 43.5500 | 1 | 1 |
| Cathepsin S | Homo sapiens (human) | IC90 | 100.0000 | 1 | 3 |
| Neutrophil elastase | Homo sapiens (human) | IC90 | 100.0000 | 1 | 3 |
| NS3 protease | Km | 262.6667 | 3 | 3 | |
| Plasminogen | Homo sapiens (human) | IC90 | 103.3333 | 1 | 3 |
| Prothrombin | Homo sapiens (human) | IC90 | 34.1333 | 1 | 3 |
| RNA-directed RNA polymerase | EC90 | 0.8343 | 7 | 7 |