Roles > EC 3.4.22.52 (calpain-1) inhibitor
Page last updated: 2024-08-05 15:37:46

EC 3.4.22.52 (calpain-1) inhibitor

A calpain inhibitor that interferes with the action of calpain-1 (EC 3.4.22.52).

ChEBI ID: 79050

Members (2)

MemberDefinitionClass
calpastatinA 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 aldehydeA 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

Research

Studies (1,004)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-199076 (7.57)18.7374
1990's280 (27.89)18.2507
2000's342 (34.06)29.6817
2010's273 (27.19)24.3611
2020's33 (3.29)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials5 (0.49%)5.53%
Reviews51 (5.01%)6.00%
Case Studies3 (0.29%)4.05%
Observational0 (0.00%)0.25%
Other959 (94.20%)84.16%

Protein Targets (44)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency22.387211
arylsulfatase AHomo sapiens (human)Potency2.393411
Bloom syndrome protein isoform 1Homo sapiens (human)Potency0.000422
Chain A, CruzipainTrypanosoma cruziPotency0.031622
cytochrome P450 2C9 precursorHomo sapiens (human)Potency39.810711
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency6.309623
D(1A) dopamine receptorHomo sapiens (human)Potency2.059511
DNA polymerase eta isoform 1Homo sapiens (human)Potency0.281811
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency15.568633
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency41.456812
GABA theta subunitRattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency6.309612
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency6.309612
gemininHomo sapiens (human)Potency14.125411
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency39.810713
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency35.481311
lamin isoform A-delta10Homo sapiens (human)Potency18.854122
M-phase phosphoprotein 8Homo sapiens (human)Potency56.234111
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.014111
NFKB1 protein, partialHomo sapiens (human)Potency1.778322
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency10.691011
TDP1 proteinHomo sapiens (human)Potency34.304422
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.501211
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency1.584911
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency70.794611

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 1BRattus norvegicus (Norway rat)IC500.300011
Calpain-1 catalytic subunitHomo sapiens (human)IC500.300011
Calpain-1 catalytic subunitHomo sapiens (human)Ki0.008011
Calpain-1 catalytic subunitSus scrofa (pig)Ki0.010011
Cathepsin BHomo sapiens (human)Ki0.024011
Chymotrypsinogen ABos taurus (cattle)Ki54.000011
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC5020.000011
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