A cysteine protease inhibitor which inhibits cathepsin B (EC 3.4.22.1).
ChEBI ID: 64932
| Member | Definition | Class |
|---|---|---|
| aloxistatin | An L-leucine derivative that is the amide obtained by formal condensation of the carboxy group of (2S,3S)-3-(ethoxycarbonyl)oxirane-2-carboxylic acid with the amino group of N-(3-methylbutyl)-L-leucinamide. | aloxistatin |
| amentoflavone | A biflavonoid that is obtained by oxidative coupling of two molecules of apigenin resulting in a bond between positions C-3 of the hydroxyphenyl ring and C-8 of the chromene ring. A natural product found particularly in Ginkgo biloba and Hypericum perforatum. | amentoflavone |
| leupeptin | A 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 |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 341 (27.11) | 18.7374 |
| 1990's | 373 (29.65) | 18.2507 |
| 2000's | 280 (22.26) | 29.6817 |
| 2010's | 201 (15.98) | 24.3611 |
| 2020's | 63 (5.01) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1 (0.08%) | 5.53% |
| Reviews | 19 (1.45%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 1,294 (98.48%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 14.1254 | 1 | 1 |
| acid sphingomyelinase | Homo sapiens (human) | Potency | 89.1251 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| apical membrane antigen 1, AMA1 | Plasmodium falciparum 3D7 | Potency | 35.4813 | 1 | 1 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 22.3872 | 1 | 1 |
| Chain A, JmjC domain-containing histone demethylation protein 3A | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| ClpP | Bacillus subtilis | Potency | 35.4813 | 1 | 1 |
| DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 25.7953 | 2 | 2 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 79.4328 | 1 | 1 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 46.2116 | 2 | 2 |
| geminin | Homo sapiens (human) | Potency | 12.5893 | 1 | 1 |
| glp-1 receptor, partial | Homo sapiens (human) | Potency | 19.9526 | 1 | 2 |
| GLS protein | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| GTP-binding nuclear protein Ran isoform 1 | Homo sapiens (human) | Potency | 5.1735 | 1 | 1 |
| Guanine nucleotide-binding protein G | Homo sapiens (human) | Potency | 13.4270 | 2 | 2 |
| importin subunit beta-1 isoform 1 | Homo sapiens (human) | Potency | 5.1735 | 1 | 1 |
| Interferon beta | Homo sapiens (human) | Potency | 0.1171 | 1 | 3 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 0.4467 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 26.9680 | 2 | 2 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 10.0000 | 1 | 1 |
| parathyroid hormone/parathyroid hormone-related peptide receptor precursor | Homo sapiens (human) | Potency | 125.8920 | 1 | 1 |
| peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| PPM1D protein | Homo sapiens (human) | Potency | 0.1171 | 1 | 2 |
| Rap guanine nucleotide exchange factor 3 | Homo sapiens (human) | Potency | 70.7946 | 1 | 1 |
| serine/threonine-protein kinase PLK1 | Homo sapiens (human) | Potency | 21.1923 | 1 | 1 |
| Smad3 | Homo sapiens (human) | Potency | 30.3001 | 1 | 2 |
| snurportin-1 | Homo sapiens (human) | Potency | 5.1735 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 18.1526 | 2 | 2 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 39.8107 | 1 | 1 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 56.2341 | 1 | 1 |
| Vpr | Human immunodeficiency virus 1 | Potency | 39.8107 | 1 | 1 |
| WRN | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1 | Bos taurus (cattle) | IC50 | 29.0000 | 1 | 1 |
| 1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1 | Homo sapiens (human) | IC50 | 29.0000 | 1 | 1 |
| 5-hydroxytryptamine receptor 1D | Sus scrofa (pig) | Ki | 4.0940 | 1 | 1 |
| 5-hydroxytryptamine receptor 2C | Homo sapiens (human) | Ki | 2.5550 | 1 | 1 |
| 72 kDa type IV collagenase | Homo sapiens (human) | IC50 | 30.3100 | 1 | 1 |
| Amyloid-beta precursor protein | Homo sapiens (human) | IC50 | 4.8000 | 1 | 1 |
| Angiotensin-converting enzyme 2 | Homo sapiens (human) | IC50 | 8.3000 | 1 | 1 |
| Beta-secretase 1 | Homo sapiens (human) | IC50 | 1.5400 | 1 | 1 |
| calpain II, partial | Sus scrofa (pig) | IC50 | 1.7742 | 1 | 1 |
| Calpain-1 catalytic subunit | Homo sapiens (human) | IC50 | 23.4200 | 3 | 3 |
| Calpain-1 catalytic subunit | Sus scrofa (pig) | IC50 | 0.0800 | 1 | 1 |
| Cannabinoid receptor 2 | Mus musculus (house mouse) | IC50 | 100.0000 | 1 | 1 |
| Cathepsin B | Bos taurus (cattle) | IC50 | 0.3100 | 1 | 1 |
| Cathepsin B | Homo sapiens (human) | IC50 | 4.8155 | 3 | 3 |
| Cathepsin B | Homo sapiens (human) | Ki | 0.0063 | 3 | 3 |
| Cathepsin B | Capra hircus (goat) | Ki | 0.0063 | 2 | 2 |
| Cathepsin G | Homo sapiens (human) | IC50 | 1.1000 | 1 | 1 |
| Cathepsin G | Mus musculus (house mouse) | IC50 | 10.0000 | 1 | 1 |
| Cathepsin K | Homo sapiens (human) | Ki | 0.0240 | 1 | 1 |
| Cationic trypsin | Bos taurus (cattle) | IC50 | 8.1000 | 1 | 1 |
| Cysteine protease | Leishmania donovani | IC50 | 0.0100 | 1 | 1 |
| Cysteine protease falcipain-3 | Plasmodium falciparum (malaria parasite P. falciparum) | IC50 | 0.0925 | 2 | 2 |
| Cysteine proteinase falcipain 2a | Plasmodium falciparum (malaria parasite P. falciparum) | IC50 | 0.0636 | 3 | 3 |
| Cytosolic phospholipase A2 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 1.2410 | 1 | 1 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 0.0362 | 2 | 2 |
| Delta-type opioid receptor | Sus scrofa (pig) | Ki | 0.0365 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Homo sapiens (human) | IC50 | 281,838.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Homo sapiens (human) | IC50 | 281,838.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Homo sapiens (human) | IC50 | 281,838.0000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | IC50 | 0.0149 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Gamma-aminobutyric acid receptor subunit theta | Homo sapiens (human) | Ki | 0.0060 | 2 | 2 |
| Group 10 secretory phospholipase A2 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Hepatocyte growth factor activator | Homo sapiens (human) | Ki | 0.1880 | 1 | 1 |
| hypothetical protein SA1422 | Staphylococcus aureus subsp. aureus N315 | IC50 | 19.3900 | 2 | 2 |
| M1-family alanyl aminopeptidase | Plasmodium falciparum 3D7 | IC50 | 108.3900 | 1 | 1 |
| Matrix metalloproteinase-9 | Homo sapiens (human) | IC50 | 2.5800 | 1 | 1 |
| Mcl-1 | Homo sapiens (human) | IC50 | 1.6341 | 1 | 1 |
| Myeloblastin | Mus musculus (house mouse) | IC50 | 10.0000 | 1 | 1 |
| Neutrophil elastase | Homo sapiens (human) | IC50 | 1.2700 | 1 | 1 |
| Neutrophil elastase | Mus musculus (house mouse) | IC50 | 10.0000 | 1 | 1 |
| Papain | Carica papaya (papaya) | IC50 | 0.0022 | 1 | 1 |
| Papain | Carica papaya (papaya) | Ki | 52.0000 | 1 | 1 |
| Phospholipase A2 | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 1 |
| Phospholipase A2, membrane associated | Homo sapiens (human) | IC50 | 23.8000 | 1 | 1 |
| Plasma kallikrein | Homo sapiens (human) | IC50 | 40.0000 | 1 | 1 |
| Plasminogen | Homo sapiens (human) | IC50 | 1.2000 | 1 | 1 |
| Plasminogen | Bos taurus (cattle) | IC50 | 3.7000 | 1 | 1 |
| Poly [ADP-ribose] polymerase 1 | Homo sapiens (human) | IC50 | 0.1023 | 3 | 3 |
| Poly [ADP-ribose] polymerase 2 | Homo sapiens (human) | IC50 | 10.3000 | 2 | 2 |
| Pro-cathepsin H | Homo sapiens (human) | Ki | 9.2000 | 2 | 2 |
| Procathepsin L | Homo sapiens (human) | IC50 | 2.6798 | 4 | 4 |
| Prothrombin | Bos taurus (cattle) | IC50 | 12.0000 | 1 | 1 |
| Replicase polyprotein 1a | Severe acute respiratory syndrome-related coronavirus | IC50 | 8.3000 | 1 | 1 |
| Replicase polyprotein 1ab | Betacoronavirus England 1 | IC50 | 8.3000 | 1 | 1 |
| Replicase polyprotein 1ab | Human coronavirus 229E | IC50 | 8.3000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 | 8.3000 | 2 | 2 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | IC50 | 8.3000 | 3 | 3 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | Ki | 13.8000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome-related coronavirus | Ki | 13.8000 | 2 | 2 |
| Reverse transcriptase/RNaseH | Human immunodeficiency virus 1 | IC50 | 119.0000 | 1 | 1 |
| Serine protease hepsin | Homo sapiens (human) | Ki | 0.0610 | 1 | 1 |
| Spike glycoprotein | Betacoronavirus England 1 | IC50 | 8.3000 | 1 | 1 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | IC50 | 8.3000 | 1 | 1 |
| Stromelysin-1 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Suppressor of tumorigenicity 14 protein | Homo sapiens (human) | Ki | 1.2980 | 2 | 2 |
| Transmembrane protease serine 2 | Homo sapiens (human) | IC50 | 8.3000 | 1 | 1 |
| Transmembrane protease serine 6 | Homo sapiens (human) | Ki | 3.2500 | 2 | 2 |
| Trypsin | Sus scrofa (pig) | IC50 | 0.3500 | 2 | 2 |
| Trypsin-1 | Homo sapiens (human) | IC50 | 0.6000 | 1 | 1 |
| Trypsin-2 | Homo sapiens (human) | IC50 | 0.6000 | 1 | 1 |
| Trypsin-3 | Homo sapiens (human) | IC50 | 0.6000 | 1 | 1 |
| Tyrosine-protein phosphatase non-receptor type 1 | Homo sapiens (human) | IC50 | 7.4000 | 1 | 1 |
| Tyrosine-protein phosphatase non-receptor type 1 | Homo sapiens (human) | Ki | 7.8000 | 1 | 1 |
| Valosin-containing protein | Homo sapiens (human) | IC50 | 36.3280 | 2 | 3 |
| Xanthine dehydrogenase/oxidase | Bos taurus (cattle) | IC50 | 35.3000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Estrogen receptor | Rattus norvegicus (Norway rat) | EC50 | 150.0000 | 1 | 2 |
| Estrogen receptor beta | Rattus norvegicus (Norway rat) | EC50 | 150.0000 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Homo sapiens (human) | EC50 | 3.6000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Homo sapiens (human) | EC50 | 3.6000 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Homo sapiens (human) | EC50 | 3.6000 | 1 | 1 |
| Matrix metalloproteinase-9 | Homo sapiens (human) | Kd | 2.1800 | 1 | 1 |
| Placenta growth factor | Homo sapiens (human) | Kd | 0.0082 | 1 | 1 |
| streptokinase A precursor | Streptococcus pyogenes M1 GAS | EC50 | 76.1490 | 2 | 2 |
| Vascular endothelial growth factor A | Homo sapiens (human) | Kd | 0.0165 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Delta-type opioid receptor | Homo sapiens (human) | Ke | 6.0000 | 1 | 1 |
| Kappa-type opioid receptor | Homo sapiens (human) | Ke | 0.4900 | 1 | 1 |
| Mu-type opioid receptor | Homo sapiens (human) | Ke | 10.0000 | 1 | 1 |