An EC 3.4.22.* (cysteine endopeptidase) inhibitor that interferes with the action of any calpain.
ChEBI ID: 82824
| Member | Definition | Class |
|---|---|---|
| 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 |
| pd 150606 | An organoiodine compound that is acrylic acid in which the vinylic hydrogens at positions 2 and 3 are replaced by mercapto and 4-iodophenyl groups respectively (the Z geoisomer). | (Z)-3-(4-iodophenyl)-2-mercaptoacrylic acid |
| phevalin | A member of the class of pyrazinones that is pyrazin-2(1H)-one substituted by an isopropyl and benzyl groups at position 3 and 6, respectively. It is a natural product found in Staphylococcus aureus that inhibits calpain in a casein hydrolysis assay (IC50 = 1.3 muM), contributes to S. aureus infection in mice, and alters human keratinocyte gene expression. | phevalin |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 325 (31.89) | 18.7374 |
| 1990's | 343 (33.66) | 18.2507 |
| 2000's | 215 (21.10) | 29.6817 |
| 2010's | 119 (11.68) | 24.3611 |
| 2020's | 17 (1.67) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 10 (0.96%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 1,032 (99.04%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Calpain-1 catalytic subunit | Homo sapiens (human) | IC50 | 1.2000 | 1 | 1 |
| Calpain-1 catalytic subunit | Sus scrofa (pig) | IC50 | 12.3933 | 3 | 3 |
| Cathepsin B | Bos taurus (cattle) | IC50 | 0.3100 | 1 | 1 |
| Cathepsin B | Homo sapiens (human) | IC50 | 0.0282 | 2 | 2 |
| Cathepsin B | Homo sapiens (human) | Ki | 0.0063 | 3 | 3 |
| Cathepsin B | Capra hircus (goat) | Ki | 0.0063 | 2 | 2 |
| 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 |
| Hepatocyte growth factor activator | Homo sapiens (human) | Ki | 0.1880 | 1 | 1 |
| Papain | Carica papaya (papaya) | IC50 | 0.0022 | 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 |
| Pro-cathepsin H | Homo sapiens (human) | Ki | 9.2000 | 2 | 2 |
| Procathepsin L | Homo sapiens (human) | IC50 | 0.0046 | 2 | 2 |
| Prothrombin | Bos taurus (cattle) | IC50 | 12.0000 | 1 | 1 |
| Serine protease hepsin | Homo sapiens (human) | Ki | 0.0610 | 1 | 1 |
| Suppressor of tumorigenicity 14 protein | Homo sapiens (human) | Ki | 1.2980 | 2 | 2 |
| 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 |