Page last updated: 2024-08-05 15:37:48

EC 3.4.23.46 (memapsin 2) inhibitor

An EC 3.4.23.* (aspartic endopeptidase) inhibitor that interferes with the activity of memapsin 2 (EC 3.4.23.46).

ChEBI ID: 74925

Members (6)

MemberDefinitionClass
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
l 685458A peptide and carboxamide that is L-leucyl-L-phenylalaninamide, L-Leu-L-Phe-NH2, which has been acylated on the N-terminus by a Phe-Phe hydroxyethylene dipeptide isotere, 2R-benzyl-5S-tert-butoxycarbonylamino-4R-hydroxy-6-phenylhexanoic acid. Compounds based on the structure of L-685,458 are potent inhibitors of gamma-secretase, which mediates the final catalytic step that generates the amyloid beta-peptide (Abeta), which assembles into the neurotoxic aggregates in the brains of sufferers of Alzheimer's disease.L-685,458
loganinAn iridoid monoterpenoid with formula C17H26O10 that is isolated from several plant species and exhibits neuroprotective and anti-inflammatory properties.loganin
ly 411575A dibenzoazepine that is 5,7-dihydro-6H-dibenzo[b,d]azepin-6-one which is substituted at the 7 pro-S position by the C-terminal carboxamide nitrogen of N(2)-[(2S)-2-(3,5-difluorophenyl)-2-hydroxyacetyl]-L-alaninamide. It is a potent, cell permeable and selective gamma-secretase inhibitor. It has been tested as a possible treatment for Alzheimer's disease and shows promise for its potential to counteract severe hearing loss.LY-411575
n-(n-(3,5-difluorophenacetyl)alanyl)phenylglycine tert-butyl esterA dipeptide consisting of alanylphenylglycine derivatised as a 3,5-difluorophenylacetamide at the amino terminal and a tert-butyl ester at the carboxy terminal. A gamma-secretase inhibitor.DAPT
ro 4929097A member of the class of dibenzoazepines that is the amide formed from formal condensation of the carboxy group of 2,2-dimethyl-3-oxo-3-[(2,2,3,3,3-pentafluoropropyl)amino]propanoic acid with the amino group of (7S)-7-amino-5,7-dihydrodibenzo[b,d]azepin-6-one.RO4929097

Research

Studies (582)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19902 (0.34)18.7374
1990's5 (0.86)18.2507
2000's153 (26.29)29.6817
2010's354 (60.82)24.3611
2020's68 (11.68)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1 (0.16%)5.53%
Reviews20 (3.16%)6.00%
Case Studies1 (0.16%)4.05%
Observational0 (0.00%)0.25%
Other611 (96.52%)84.16%

Protein Targets (56)

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
EWS/FLI fusion proteinHomo sapiens (human)Potency18.339745
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
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency11.232222
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
Beta-secretase 1Homo sapiens (human)IC500.300011
Beta-secretase 2Homo sapiens (human)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
Gamma-secretase subunit APH-1AHomo sapiens (human)IC505.68751418
Gamma-secretase subunit APH-1BHomo sapiens (human)IC505.68751418
Gamma-secretase subunit PEN-2Homo sapiens (human)IC505.40401519
NicastrinHomo sapiens (human)IC505.68751418
Presenilin-1Homo sapiens (human)IC505.68751418
Presenilin-2Homo sapiens (human)IC505.68751418
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2IC5020.000011
Signal peptide peptidase-like 2AHomo sapiens (human)IC500.010011
Signal transducer and activator of transcription 3Homo sapiens (human)IC5014.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Gamma-secretase subunit APH-1AHomo sapiens (human)EC500.006433
Gamma-secretase subunit APH-1BHomo sapiens (human)EC500.006433
Gamma-secretase subunit PEN-2Homo sapiens (human)EC500.006433
NicastrinHomo sapiens (human)EC500.006433
Presenilin-1Homo sapiens (human)EC500.003955
Presenilin-2Homo sapiens (human)EC500.006433

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Gamma-secretase subunit PEN-2Homo sapiens (human)ED500.025022