Page last updated: 2024-08-05 15:36:13

EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor

An EC 3.4.24.* (metalloendopeptidase) inhibitor that interferes with the action of anthrax lethal factor endopeptidase (EC 3.4.24.83).

ChEBI ID: 77255

Members (2)

MemberDefinitionClass
mevastatinA carboxylic ester that is pravastatin that is lacking the allylic hydroxy group. A hydroxymethylglutaryl-CoA reductase inhibitor (statin) isolated from Penicillium citrinum and from Penicillium brevicompactum, its clinical use as a lipid-regulating drug ceased following reports of toxicity in animals.mevastatin
simvastatinA member of the class of hexahydronaphthalenes that is lovastatin in which the 2-methylbutyrate ester moiety has been replaced by a 2,2-dimethylbutyrate ester group. It is used as a cholesterol-lowering and anti-cardiovascular disease drug.simvastatin

Research

Studies (8,481)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-1990210 (2.48)18.7374
1990's1,125 (13.26)18.2507
2000's3,080 (36.32)29.6817
2010's3,344 (39.43)24.3611
2020's722 (8.51)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials1,733 (19.39%)5.53%
Reviews599 (6.70%)6.00%
Case Studies487 (5.45%)4.05%
Observational49 (0.55%)0.25%
Other6,069 (67.91%)84.16%

Protein Targets (82)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency44.668411
AR proteinHomo sapiens (human)Potency22.254559
ATAD5 protein, partialHomo sapiens (human)Potency10.318311
Ataxin-2Homo sapiens (human)Potency8.041411
ATPase family AAA domain-containing protein 5Homo sapiens (human)Potency8.041411
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency79.432811
Cellular tumor antigen p53Homo sapiens (human)Potency12.363013
Chain A, Beta-lactamaseEscherichia coli K-12Potency24.318124
Chain A, Ferritin light chainEquus caballus (horse)Potency35.481312
Chain A, JmjC domain-containing histone demethylation protein 3AHomo sapiens (human)Potency25.118911
cytochrome P450 2C9, partialHomo sapiens (human)Potency1.949711
cytochrome P450 2D6Homo sapiens (human)Potency27.540411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency2.130722
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency13.103613
D(1A) dopamine receptorHomo sapiens (human)Potency4.109211
D(1A) dopamine receptorSus scrofa (pig)Potency16.481611
DNA dC->dU-editing enzyme APOBEC-3G isoform 1Homo sapiens (human)Potency3.548111
estrogen nuclear receptor alphaHomo sapiens (human)Potency15.1794615
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency32.343523
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency7.4612812
EWS/FLI fusion proteinHomo sapiens (human)Potency14.408144
farnesoid X nuclear receptorHomo sapiens (human)Potency8.134922
GVesicular stomatitis virusPotency1.949711
gemininHomo sapiens (human)Potency4.108724
GLI family zinc finger 3Homo sapiens (human)Potency20.502624
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency9.942534
heat shock protein beta-1Homo sapiens (human)Potency45.310724
Histone H2A.xCricetulus griseus (Chinese hamster)Potency40.095411
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency1.949711
huntingtin isoform 2Homo sapiens (human)Potency1.000011
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency26.832511
IDH1Homo sapiens (human)Potency5.708712
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency1.949712
Interferon betaHomo sapiens (human)Potency1.949711
mitogen-activated protein kinase 1Homo sapiens (human)Potency31.622811
neuropeptide S receptor isoform AHomo sapiens (human)Potency15.848911
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency15.472824
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency22.142712
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency27.627422
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency14.125411
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency12.046212
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency33.491511
ParkinHomo sapiens (human)Potency18.162034
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency42.816133
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency30.895611
PINK1Homo sapiens (human)Potency24.035312
plasminogen precursorMus musculus (house mouse)Potency2.210612
RAR-related orphan receptor gammaMus musculus (house mouse)Potency2.815824
regulator of G-protein signaling 4Homo sapiens (human)Potency50.118711
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency26.939635
retinoid X nuclear receptor alphaHomo sapiens (human)Potency31.317924
serine/threonine-protein kinase mTOR isoform 1Homo sapiens (human)Potency12.875022
serine/threonine-protein kinase PLK1Homo sapiens (human)Potency29.934911
SMAD family member 2Homo sapiens (human)Potency30.106511
SMAD family member 3Homo sapiens (human)Potency30.106511
Smad3Homo sapiens (human)Potency11.294712
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency0.932822
survival motor neuron protein isoform dHomo sapiens (human)Potency12.589311
TAR DNA-binding protein 43Homo sapiens (human)Potency14.125411
TDP1 proteinHomo sapiens (human)Potency20.476926
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency24.013024
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency2.210612
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency2.210612
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency23.914511
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency15.365422
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency50.118711

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)IC500.53901012
3-hydroxy-3-methylglutaryl-coenzyme A reductaseSchizosaccharomyces pombe 972h-IC5095.200011
3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)Ki34.001322
3-hydroxy-3-methylglutaryl-coenzyme A reductase Rattus norvegicus (Norway rat)IC500.11171111
3-hydroxy-3-methylglutaryl-coenzyme A reductase Rattus norvegicus (Norway rat)Ki0.001011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50133.000012
ATP-dependent translocase ABCB1Homo sapiens (human)IC5029.580055
Bile salt export pumpHomo sapiens (human)IC5022.220045
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC5097.000023
Insulin receptor Rattus norvegicus (Norway rat)IC500.061212
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000012
photoreceptor-specific nuclear receptorHomo sapiens (human)IC501.164011
Potassium channel subfamily K member 9Homo sapiens (human)IC50159.000011
Prostaglandin G/H synthase 2Homo sapiens (human)IC500.061212
Sigma non-opioid intracellular receptor 1Cavia porcellus (domestic guinea pig)IC500.049011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC507.775044
transactivating tegument protein VP16 [Human herpesvirus 1]Human alphaherpesvirus 1 (Herpes simplex virus type 1)IC504.426011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Nuclear receptor subfamily 4 group A member 2Homo sapiens (human)EC505.100011