A calpain inhibitor that interferes with the action of calpain-1 (EC 3.4.22.52).
ChEBI ID: 79050
| Member | Definition | Class |
|---|---|---|
| calpastatin | A 27-membered polypeptide comprising the sequence Ac-Asp-Pro-Met-Ser-Ser-Thr-Tyr-Ile-Glu-Glu-Leu-Gly-Lys-Arg-Glu-Val-Thr-Ile-Pro-Pro-Lys-Tyr-Arg-Glu-Leu-Leu-Ala-NH2. An acetylated synthetic peptide from human calpastatin that strongly inhibits both calpains I and II but not papain (a cysteine protease) or trypsin (a serine protease). | calpastatin peptide Ac 184-210 |
| carbobenzoxyvalylphenylalanine aldehyde | A dipeptide resulting from the formal condensation of the carboxy group of N-benzyloxycarbonyl-L-valine with the amino group of L-phenylalanine aldehyde. It is a potent cell-permeable inhibitor of calpain I and II, and is also a gamma-secretase inhibitor. | Z-Val-Phe-H |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 76 (7.57) | 18.7374 |
| 1990's | 280 (27.89) | 18.2507 |
| 2000's | 342 (34.06) | 29.6817 |
| 2010's | 273 (27.19) | 24.3611 |
| 2020's | 33 (3.29) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 5 (0.49%) | 5.53% |
| Reviews | 51 (5.01%) | 6.00% |
| Case Studies | 3 (0.29%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 959 (94.20%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
| arylsulfatase A | Homo sapiens (human) | Potency | 2.3934 | 1 | 1 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 0.0004 | 2 | 2 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 0.0316 | 2 | 2 |
| cytochrome P450 2C9 precursor | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 6.3096 | 2 | 3 |
| D(1A) dopamine receptor | Homo sapiens (human) | Potency | 2.0595 | 1 | 1 |
| DNA polymerase eta isoform 1 | Homo sapiens (human) | Potency | 0.2818 | 1 | 1 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 15.5686 | 3 | 3 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 41.4568 | 1 | 2 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 6.3096 | 1 | 2 |
| geminin | Homo sapiens (human) | Potency | 14.1254 | 1 | 1 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 39.8107 | 1 | 3 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 18.8541 | 2 | 2 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 56.2341 | 1 | 1 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 0.0141 | 1 | 1 |
| NFKB1 protein, partial | Homo sapiens (human) | Potency | 1.7783 | 2 | 2 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 10.6910 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 34.3044 | 2 | 2 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 0.5012 | 1 | 1 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 1.5849 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 70.7946 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1B | Rattus norvegicus (Norway rat) | IC50 | 0.3000 | 1 | 1 |
| Calpain-1 catalytic subunit | Homo sapiens (human) | IC50 | 0.3000 | 1 | 1 |
| Calpain-1 catalytic subunit | Homo sapiens (human) | Ki | 0.0080 | 1 | 1 |
| Calpain-1 catalytic subunit | Sus scrofa (pig) | Ki | 0.0100 | 1 | 1 |
| Cathepsin B | Homo sapiens (human) | Ki | 0.0240 | 1 | 1 |
| Chymotrypsinogen A | Bos taurus (cattle) | Ki | 54.0000 | 1 | 1 |
| Replicase polyprotein 1ab | Severe acute respiratory syndrome coronavirus 2 | IC50 | 20.0000 | 1 | 1 |