An inhibitor of hepatitis C protease, an enzyme required for production of proteins needed for viral assembly.
| 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 |
| 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 |