Page last updated: 2024-08-05 15:01:40

anticholesteremic drug

A substance used to lower plasma cholesterol levels.

ChEBI ID: 35821

Members (16)

MemberDefinitionClass
5,7-dihydroxy-2-methyl-8-(4-(3-hydroxy-1-methyl)-piperidinyl)-4h-1-benzopyran-4-oneA member of the class of chromones that is 4H-chromen-4-one in which the hydrogens at positions 2,5,7 and 8 are replaced by methyl, hydroxy, hydroxy, and (3S,4R)-3-hydroxy-1-methylpiperidin-4-yl groups, respectively. It is an alkaloid initially isolated from Amoora rohituka and is a precursor of the anti-cancer compound flavopiridol.rohitukine
bms201038A member of the class of benzamides obtained by formal condensation of the carboxy group of 4'-(trifluoromethyl)biphenyl-2-carboxylic acid with the primary amino group of 9-[4-(4-aminopiperidin-1-yl)butyl]-N-(2,2,2-trifluoroethyl)-9H-fluorene-9-carboxamide. Used (as its mesylate salt) as a complement to a low-fat diet and other lipid-lowering treatments in patients with homozygous familial hypercholesterolemia.lomitapide
clofibrateThe ethyl ester of clofibric acid.clofibrate
clofibric acidA monocarboxylic acid that is isobutyric acid substituted at position 2 by a p-chlorophenoxy group. It is a metabolite of the drug clofibrate.clofibric acid
eicosapentaenoic acidAn icosapentaenoic acid having five cis-double bonds at positions 5, 8, 11, 14 and 17.all-cis-5,8,11,14,17-icosapentaenoic acid
ezetimibeA beta-lactam that is azetidin-2-one which is substituted at 1, 3, and 4 by p-fluorophenyl, 3-(p-fluorophenyl)-3-hydroxypropyl, and 4-hydroxyphenyl groups, respectively (the 3R,3'S,4S enantiomer).ezetimibe
lovastatinA fatty acid ester that is mevastatin carrying an additional methyl group on the carbobicyclic skeleton. It is used in as an anticholesteremic drug and has been found in fungal species such as Aspergillus terreus and Pleurotus ostreatus (oyster mushroom).lovastatin
meglutolA dicarboxylic acid that is glutaric acid in which one of the two hydrogens at position 3 is substituted by a hydroxy group, while the other is substituted by a methyl group. It has been found to accumulate in urine of patients suffering from HMG-CoA lyase (3-hydroxy-3-methylglutaryl-CoA lyase, EC 4.1.3.4) deficiency. It occurs as a plant metabolite in Crotalaria dura.3-hydroxy-3-methylglutaric acid
ml 236aA carbobicyclic compound that is ML-236C substituted by a hydroxy group at position 8S. It is a fungal metabolite isolated from Penicillium citrinum and exhibits anticholesteremic activity.compactin diol lactone
monacolin lA polyketide that is 1-ethyl-2,6-dimethyl-1,2,6,7,8,8a-hexahydronaphthalene in which one of the methyl hydrogens from the ethyl group is replaced by a 4-hydroxy-6-ketopyran-2-yl group.monacolin L
pravastatinA carboxylic ester resulting from the formal condensation of (S)-2-methylbutyric acid with the hydroxy group adjacent to the ring junction of (3R,5R)-7-[(1S,2S,6S,8S,8aR)-6,8-dihydroxy-2-methyl-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid. Derived from microbial transformation of mevastatin, pravastatin is a reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA). The sodium salt is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.pravastatin
pravastatin sodiumAn organic sodium salt that is the sodium salt of pravastatin. A reversible inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA), it is used for lowering cholesterol and preventing cardiovascular disease. It is one of the lower potency statins, but has the advantage of fewer side effects compared with lovastatin and simvastatin.pravastatin sodium
probucolA dithioketal that is propane-2,2-dithiol in which the hydrogens attached to both sulfur atoms are replaced by 3,5-di-tert-butyl-4-hydroxyphenyl groups. An anticholesteremic drug with antioxidant and anti-inflammatory properties, it is used to treat high levels of cholesterol in blood.probucol
sitosterol, (3beta)-isomerA member of the class of phytosterols that is stigmast-5-ene substituted by a beta-hydroxy group at position 3.sitosterol
stigmastanolA 3-hydroxy steroid that is 5alpha-stigmastane which is substituted at the 3beta position by a hydroxy group.stigmastanol
torcetrapibtorcetrapib

Research

Studies (22,987)

TimeframeStudies, Drugs with This Role(%)All Drugs %
pre-19903,947 (17.17)18.7374
1990's4,926 (21.43)18.2507
2000's6,002 (26.11)29.6817
2010's6,249 (27.18)24.3611
2020's1,863 (8.10)2.80

Study Types

Publication TypeStudies, Drugs with this Role (%)All Drugs (%)
Trials4,266 (16.65%)5.53%
Reviews2,809 (10.97%)6.00%
Case Studies757 (2.96%)4.05%
Observational88 (0.34%)0.25%
Other17,696 (69.08%)84.16%

Protein Targets (206)

Potency Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
15-lipoxygenase, partialHomo sapiens (human)Potency31.622812
activating transcription factor 6Homo sapiens (human)Potency31.252612
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.810711
AR proteinHomo sapiens (human)Potency23.8925924
aryl hydrocarbon receptorHomo sapiens (human)Potency21.591222
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency0.169411
caspase 7, apoptosis-related cysteine proteaseHomo sapiens (human)Potency46.412912
caspase-3Homo sapiens (human)Potency46.412912
Cellular tumor antigen p53Homo sapiens (human)Potency66.534624
Chain A, 2-oxoglutarate OxygenaseHomo sapiens (human)Potency39.810711
Chain A, Beta-lactamaseEscherichia coli K-12Potency11.867525
Chain A, CruzipainTrypanosoma cruziPotency25.118912
Chain A, Ferritin light chainEquus caballus (horse)Potency31.832622
Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASEHomo sapiens (human)Potency21.450912
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency15.811411
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency22.387211
chromobox protein homolog 1Homo sapiens (human)Potency52.969323
cytochrome P450 2C19 precursorHomo sapiens (human)Potency0.794311
cytochrome P450 2C9, partialHomo sapiens (human)Potency10.510513
cytochrome P450 2D6Homo sapiens (human)Potency16.244814
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency5.011911
cytochrome P450 3A4 isoform 1Homo sapiens (human)Potency15.039626
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency6.830127
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency24.636513
DNA polymerase kappa isoform 1Homo sapiens (human)Potency11.220211
estrogen nuclear receptor alphaHomo sapiens (human)Potency25.2543926
estrogen receptor 2 (ER beta)Homo sapiens (human)Potency19.774526
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency20.1369620
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency15.723015
EWS/FLI fusion proteinHomo sapiens (human)Potency20.2757414
farnesoid X nuclear receptorHomo sapiens (human)Potency46.694333
Fumarate hydrataseHomo sapiens (human)Potency5.623411
GVesicular stomatitis virusPotency10.510513
GABA theta subunitRattus norvegicus (Norway rat)Potency15.039613
GALC proteinHomo sapiens (human)Potency50.118711
Gamma-aminobutyric acid receptor subunit alpha-1Rattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit alpha-2Rattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit alpha-3Rattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit alpha-4Rattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit alpha-5Rattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit alpha-6Rattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit beta-1Rattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit beta-2Rattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit beta-3Rattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit deltaRattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit epsilonRattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit gamma-1Rattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit gamma-2Rattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit gamma-3Rattus norvegicus (Norway rat)Potency15.039613
Gamma-aminobutyric acid receptor subunit piRattus norvegicus (Norway rat)Potency15.039613
gemininHomo sapiens (human)Potency4.634624
GLI family zinc finger 3Homo sapiens (human)Potency22.358627
GLS proteinHomo sapiens (human)Potency31.622811
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency32.9228511
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency18.646714
heat shock protein beta-1Homo sapiens (human)Potency53.291024
histone-lysine N-methyltransferase 2A isoform 2 precursorHomo sapiens (human)Potency50.118711
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency10.510513
hypoxia-inducible factor 1 alpha subunitHomo sapiens (human)Potency59.891823
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)Homo sapiens (human)Potency33.144333
IDH1Homo sapiens (human)Potency12.832112
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency10.510516
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency14.125411
Interferon betaHomo sapiens (human)Potency10.510513
isocitrate dehydrogenase 1, partialHomo sapiens (human)Potency50.118711
lamin isoform A-delta10Homo sapiens (human)Potency8.421812
M-phase phosphoprotein 8Homo sapiens (human)Potency0.125911
Microtubule-associated protein tauHomo sapiens (human)Potency20.425124
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.006311
neuropeptide S receptor isoform AHomo sapiens (human)Potency5.011911
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency38.865837
nuclear factor erythroid 2-related factor 2 isoform 2Homo sapiens (human)Potency23.109311
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency44.482823
Nuclear receptor ROR-gammaHomo sapiens (human)Potency4.730811
nuclear receptor ROR-gamma isoform 1Mus musculus (house mouse)Potency11.370523
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency12.589311
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency72.403223
ParkinHomo sapiens (human)Potency11.220211
peripheral myelin protein 22 isoform 1Homo sapiens (human)Potency84.921411
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency40.375845
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency15.526024
phosphopantetheinyl transferaseBacillus subtilisPotency74.338513
PINK1Homo sapiens (human)Potency11.220211
plasminogen precursorMus musculus (house mouse)Potency0.891311
polyproteinZika virusPotency5.623411
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency25.940413
pregnane X nuclear receptorHomo sapiens (human)Potency25.983334
pregnane X receptorRattus norvegicus (Norway rat)Potency44.668411
progesterone receptorHomo sapiens (human)Potency31.773825
Rap guanine nucleotide exchange factor 4Homo sapiens (human)Potency35.481311
RAR-related orphan receptor gammaMus musculus (house mouse)Potency9.1821210
regulator of G-protein signaling 4Homo sapiens (human)Potency23.043412
retinoic acid nuclear receptor alpha variant 1Homo sapiens (human)Potency40.390437
retinoid X nuclear receptor alphaHomo sapiens (human)Potency25.296634
SMAD family member 2Homo sapiens (human)Potency46.944622
SMAD family member 3Homo sapiens (human)Potency46.944622
Smad3Homo sapiens (human)Potency9.180412
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency15.691026
survival motor neuron protein isoform dHomo sapiens (human)Potency15.848911
TDP1 proteinHomo sapiens (human)Potency20.8048212
thioredoxin glutathione reductaseSchistosoma mansoniPotency44.668411
thioredoxin reductaseRattus norvegicus (Norway rat)Potency0.398111
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency41.7345310
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency3.981111
thyroid stimulating hormone receptorHomo sapiens (human)Potency20.671634
thyrotropin-releasing hormone receptorHomo sapiens (human)Potency41.377822
urokinase plasminogen activator surface receptor precursorMus musculus (house mouse)Potency0.891311
urokinase-type plasminogen activator precursorMus musculus (house mouse)Potency0.891311
USP1 protein, partialHomo sapiens (human)Potency50.149124
v-jun sarcoma virus 17 oncogene homolog (avian)Homo sapiens (human)Potency32.614824
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency22.908824
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency56.454113
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency18.646714

Inhibition Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)IC502.87151316
3-hydroxy-3-methylglutaryl-coenzyme A reductaseHomo sapiens (human)Ki0.023511
3-hydroxy-3-methylglutaryl-coenzyme A reductase Rattus norvegicus (Norway rat)IC500.03911618
Acyl-CoA:cholesterol acyltransferase Oryctolagus cuniculus (rabbit)IC5016.800011
Adenosine receptor A1Homo sapiens (human)IC5026.720011
Adenosine receptor A1Homo sapiens (human)Ki15.586011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC508.753011
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)Ki8.680011
Androgen receptorRattus norvegicus (Norway rat)IC5030.164011
Androgen receptorRattus norvegicus (Norway rat)Ki20.110011
AromataseHomo sapiens (human)IC5053.200011
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50131.000014
ATP-dependent translocase ABCB1Homo sapiens (human)IC5050.020055
bcl-2-related protein A1Mus musculus (house mouse)IC50100.000022
Bile salt export pumpHomo sapiens (human)IC50194.085747
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50133.000014
Canalicular multispecific organic anion transporter 1Rattus norvegicus (Norway rat)Ki172.000011
Chain A, Antigen Cd11a (p180)Homo sapiens (human)IC502.400011
Chain A, Protein (peroxisome Proliferator Activated Receptor (ppar-delta))Homo sapiens (human)IC504.000011
Cholesteryl ester transfer proteinHomo sapiens (human)IC500.015244
Coagulation factor VIIHomo sapiens (human)IC5078.000011
Cyclin-A2Homo sapiens (human)IC507.300033
Cyclin-dependent kinase 2Homo sapiens (human)IC507.300033
Cyclin-dependent kinase 9Homo sapiens (human)IC500.300033
Cyclin-T1Homo sapiens (human)IC500.300033
Cytochrome P450 1A2Homo sapiens (human)Ki7.632011
Cytochrome P450 2C9 Homo sapiens (human)IC5050.000011
Cytochrome P450 2D6Homo sapiens (human)IC50100.000011
Cytochrome P450 2J2Homo sapiens (human)IC5050.000011
Cytochrome P450 3A4Homo sapiens (human)IC50100.000011
Delta-type opioid receptorMus musculus (house mouse)IC500.000811
DNA polymerase betaHomo sapiens (human)IC5026.300011
Fatty acid-binding protein, intestinalHomo sapiens (human)Ki17.700011
Fatty acid-binding protein, liverRattus norvegicus (Norway rat)Ki6.920011
Histone deacetylase 1Homo sapiens (human)IC5011.911011
Histone deacetylase 2Homo sapiens (human)IC5025.933011
Histone deacetylase 6Homo sapiens (human)IC5016.285011
Insulin receptor Rattus norvegicus (Norway rat)IC500.012812
Integrin alpha-LHomo sapiens (human)IC503.090022
Integrin beta-2Homo sapiens (human)IC503.090022
Intercellular adhesion molecule 1Homo sapiens (human)IC503.780011
Lanosterol 14-alpha demethylaseHomo sapiens (human)IC50200.000011
Microsomal triglyceride transfer protein large subunitHomo sapiens (human)IC500.005633
Multidrug resistance-associated protein 4Homo sapiens (human)IC50133.000014
NAD-dependent protein deacylase sirtuin-5, mitochondrialHomo sapiens (human)IC501.600011
Neutrophil elastaseHomo sapiens (human)IC500.027011
NPC1-like intracellular cholesterol transporter 1Homo sapiens (human)IC500.370011
NPC1-like intracellular cholesterol transporter 1Rattus norvegicus (Norway rat)Ki0.200011
Oxoeicosanoid receptor 1Homo sapiens (human)IC502.000011
Polyunsaturated fatty acid lipoxygenase ALOX15Homo sapiens (human)IC5014.000011
Prostaglandin G/H synthase 1 Bos taurus (cattle)IC5013.000011
Prostaglandin G/H synthase 2Homo sapiens (human)IC500.012812
Prostaglandin G/H synthase 2Ovis aries (sheep)IC507.100011
ProthrombinHomo sapiens (human)IC50754.925044
ProthrombinHomo sapiens (human)Ki0.267211
Retinoic acid receptor RXR-alphaHomo sapiens (human)Ki7.632011
Sodium-dependent dopamine transporter Homo sapiens (human)IC5010.104011
Sodium-dependent dopamine transporter Homo sapiens (human)Ki8.028011
Sodium-dependent noradrenaline transporter Homo sapiens (human)IC508.753011
Sodium-dependent noradrenaline transporter Homo sapiens (human)Ki8.680011
Sodium/bile acid cotransporterHomo sapiens (human)Ki25.000011
Solute carrier family 22 member 11Homo sapiens (human)IC50591.000011
Solute carrier family 22 member 6Homo sapiens (human)IC50408.000011
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)Ki601.000022
Solute carrier family 22 member 7Homo sapiens (human)IC50352.000011
Solute carrier family 22 member 7Rattus norvegicus (Norway rat)IC50449.000011
Solute carrier family 22 member 8Homo sapiens (human)IC5013.700011
Solute carrier family 22 member 8Rattus norvegicus (Norway rat)IC5015.600011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC5015.800022
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Ki3.400011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC5062.000011
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Ki57.000011
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)IC50190.000011
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)Ki180.000011
Substance-K receptorHomo sapiens (human)IC5028.224011
Substance-K receptorHomo sapiens (human)Ki9.408011
Tissue factorHomo sapiens (human)IC5078.000011
TrypsinSus scrofa (pig)IC50200.000011
Vascular cell adhesion protein 1Homo sapiens (human)IC5050.000011

Activation Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
5-hydroxytryptamine receptor 4Cavia porcellus (domestic guinea pig)EC5055.000011
Fatty acid-binding protein, liverRattus norvegicus (Norway rat)Kd8.662588
Glutamate receptor ionotropic, NMDA 1Homo sapiens (human)EC50300.000011
Glutamate receptor ionotropic, NMDA 2AHomo sapiens (human)EC50300.000011
Glutamate receptor ionotropic, NMDA 2BHomo sapiens (human)EC50300.000011
Glutamate receptor ionotropic, NMDA 2CHomo sapiens (human)EC50300.000011
Glutamate receptor ionotropic, NMDA 2DHomo sapiens (human)EC50300.000011
Glutamate receptor ionotropic, NMDA 3AHomo sapiens (human)EC50300.000011
Glutamate receptor ionotropic, NMDA 3BHomo sapiens (human)EC50300.000011
Integrin alpha-LHomo sapiens (human)Kd12.900011
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)EC50500.000012
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)EC50500.000012
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)EC50500.000012
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)EC50500.000012
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)EC50500.000012
Neuronal acetylcholine receptor subunit alpha-7Rattus norvegicus (Norway rat)EC500.042011
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)EC5052.88331212
Peroxisome proliferator-activated receptor alphaMus musculus (house mouse)EC5037.760544
Peroxisome proliferator-activated receptor deltaHomo sapiens (human)EC5055.000011
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)EC50332.800055
Peroxisome proliferator-activated receptor gammaMus musculus (house mouse)EC50466.666733
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)Kd2.000011

Other Measurements

ProteinTaxonomyMeasurementAverage (mM)Bioassay(s)Drugs
Canalicular multispecific organic anion transporter 1Rattus norvegicus (Norway rat)Km223.000011
Solute carrier family 22 member 8Rattus norvegicus (Norway rat)Km13.400011
Solute carrier organic anion transporter family member 1A1Rattus norvegicus (Norway rat)Km30.000011
Solute carrier organic anion transporter family member 1A4Rattus norvegicus (Norway rat)Km37.500011
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Km59.700022
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)Km2,250.000011
UDP-glucuronosyltransferase 1A1 Homo sapiens (human)Km64.000011
UDP-glucuronosyltransferase 1A3Homo sapiens (human)Km42.000011
UDP-glucuronosyltransferase 2B7Homo sapiens (human)Km21.000011