Page last updated: 2024-08-05 15:01:40
anticholesteremic drug
A substance used to lower plasma cholesterol levels.
ChEBI ID: 35821
Members (16)
| Member | Definition | Class |
|---|---|---|
| 5,7-dihydroxy-2-methyl-8-(4-(3-hydroxy-1-methyl)-piperidinyl)-4h-1-benzopyran-4-one | A 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 |
| bms201038 | A 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 |
| clofibrate | The ethyl ester of clofibric acid. | clofibrate |
| clofibric acid | A 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 acid | An icosapentaenoic acid having five cis-double bonds at positions 5, 8, 11, 14 and 17. | all-cis-5,8,11,14,17-icosapentaenoic acid |
| ezetimibe | A 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 |
| lovastatin | A 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 |
| meglutol | A 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 236a | A 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 l | A 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 |
| pravastatin | A 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 sodium | An 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 |
| probucol | A 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)-isomer | A member of the class of phytosterols that is stigmast-5-ene substituted by a beta-hydroxy group at position 3. | sitosterol |
| stigmastanol | A 3-hydroxy steroid that is 5alpha-stigmastane which is substituted at the 3beta position by a hydroxy group. | stigmastanol |
| torcetrapib | torcetrapib |
Research
Studies (22,987)
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 3,947 (17.17) | 18.7374 |
| 1990's | 4,926 (21.43) | 18.2507 |
| 2000's | 6,002 (26.11) | 29.6817 |
| 2010's | 6,249 (27.18) | 24.3611 |
| 2020's | 1,863 (8.10) | 2.80 |
Study Types
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 4,266 (16.65%) | 5.53% |
| Reviews | 2,809 (10.97%) | 6.00% |
| Case Studies | 757 (2.96%) | 4.05% |
| Observational | 88 (0.34%) | 0.25% |
| Other | 17,696 (69.08%) | 84.16% |
Protein Targets (206)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-lipoxygenase, partial | Homo sapiens (human) | Potency | 31.6228 | 1 | 2 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 31.2526 | 1 | 2 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 23.8925 | 9 | 24 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 21.5912 | 2 | 2 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 0.1694 | 1 | 1 |
| caspase 7, apoptosis-related cysteine protease | Homo sapiens (human) | Potency | 46.4129 | 1 | 2 |
| caspase-3 | Homo sapiens (human) | Potency | 46.4129 | 1 | 2 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 66.5346 | 2 | 4 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 39.8107 | 1 | 1 |
| Chain A, Beta-lactamase | Escherichia coli K-12 | Potency | 11.8675 | 2 | 5 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 25.1189 | 1 | 2 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 31.8326 | 2 | 2 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 21.4509 | 1 | 2 |
| Chain A, Putative fructose-1,6-bisphosphate aldolase | Giardia intestinalis | Potency | 15.8114 | 1 | 1 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 22.3872 | 1 | 1 |
| chromobox protein homolog 1 | Homo sapiens (human) | Potency | 52.9693 | 2 | 3 |
| cytochrome P450 2C19 precursor | Homo sapiens (human) | Potency | 0.7943 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 10.5105 | 1 | 3 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 16.2448 | 1 | 4 |
| cytochrome P450 2D6 isoform 1 | Homo sapiens (human) | Potency | 5.0119 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 15.0396 | 2 | 6 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 6.8301 | 2 | 7 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 24.6365 | 1 | 3 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 25.2543 | 9 | 26 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 19.7745 | 2 | 6 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 20.1369 | 6 | 20 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 15.7230 | 1 | 5 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 20.2757 | 4 | 14 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 46.6943 | 3 | 3 |
| Fumarate hydratase | Homo sapiens (human) | Potency | 5.6234 | 1 | 1 |
| G | Vesicular stomatitis virus | Potency | 10.5105 | 1 | 3 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| GALC protein | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 15.0396 | 1 | 3 |
| geminin | Homo sapiens (human) | Potency | 4.6346 | 2 | 4 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 22.3586 | 2 | 7 |
| GLS protein | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 32.9228 | 5 | 11 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 18.6467 | 1 | 4 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 53.2910 | 2 | 4 |
| histone-lysine N-methyltransferase 2A isoform 2 precursor | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 10.5105 | 1 | 3 |
| hypoxia-inducible factor 1 alpha subunit | Homo sapiens (human) | Potency | 59.8918 | 2 | 3 |
| hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor) | Homo sapiens (human) | Potency | 33.1443 | 3 | 3 |
| IDH1 | Homo sapiens (human) | Potency | 12.8321 | 1 | 2 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 10.5105 | 1 | 6 |
| Inositol monophosphatase 1 | Rattus norvegicus (Norway rat) | Potency | 14.1254 | 1 | 1 |
| Interferon beta | Homo sapiens (human) | Potency | 10.5105 | 1 | 3 |
| isocitrate dehydrogenase 1, partial | Homo sapiens (human) | Potency | 50.1187 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 8.4218 | 1 | 2 |
| M-phase phosphoprotein 8 | Homo sapiens (human) | Potency | 0.1259 | 1 | 1 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 20.4251 | 2 | 4 |
| muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | Potency | 0.0063 | 1 | 1 |
| neuropeptide S receptor isoform A | Homo sapiens (human) | Potency | 5.0119 | 1 | 1 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 38.8658 | 3 | 7 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 23.1093 | 1 | 1 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 44.4828 | 2 | 3 |
| Nuclear receptor ROR-gamma | Homo sapiens (human) | Potency | 4.7308 | 1 | 1 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 11.3705 | 2 | 3 |
| nuclear receptor subfamily 1, group I, member 2 | Rattus norvegicus (Norway rat) | Potency | 12.5893 | 1 | 1 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 72.4032 | 2 | 3 |
| Parkin | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| peripheral myelin protein 22 isoform 1 | Homo sapiens (human) | Potency | 84.9214 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 40.3758 | 4 | 5 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 15.5260 | 2 | 4 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 74.3385 | 1 | 3 |
| PINK1 | Homo sapiens (human) | Potency | 11.2202 | 1 | 1 |
| plasminogen precursor | Mus musculus (house mouse) | Potency | 0.8913 | 1 | 1 |
| polyprotein | Zika virus | Potency | 5.6234 | 1 | 1 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 25.9404 | 1 | 3 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 25.9833 | 3 | 4 |
| pregnane X receptor | Rattus norvegicus (Norway rat) | Potency | 44.6684 | 1 | 1 |
| progesterone receptor | Homo sapiens (human) | Potency | 31.7738 | 2 | 5 |
| Rap guanine nucleotide exchange factor 4 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 9.1821 | 2 | 10 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 23.0434 | 1 | 2 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 40.3904 | 3 | 7 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 25.2966 | 3 | 4 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 46.9446 | 2 | 2 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 46.9446 | 2 | 2 |
| Smad3 | Homo sapiens (human) | Potency | 9.1804 | 1 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 15.6910 | 2 | 6 |
| survival motor neuron protein isoform d | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 20.8048 | 2 | 12 |
| thioredoxin glutathione reductase | Schistosoma mansoni | Potency | 44.6684 | 1 | 1 |
| thioredoxin reductase | Rattus norvegicus (Norway rat) | Potency | 0.3981 | 1 | 1 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 41.7345 | 3 | 10 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 3.9811 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 20.6716 | 3 | 4 |
| thyrotropin-releasing hormone receptor | Homo sapiens (human) | Potency | 41.3778 | 2 | 2 |
| urokinase plasminogen activator surface receptor precursor | Mus musculus (house mouse) | Potency | 0.8913 | 1 | 1 |
| urokinase-type plasminogen activator precursor | Mus musculus (house mouse) | Potency | 0.8913 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 50.1491 | 2 | 4 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 32.6148 | 2 | 4 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 22.9088 | 2 | 4 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 56.4541 | 1 | 3 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 18.6467 | 1 | 4 |
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase | Homo sapiens (human) | IC50 | 2.8715 | 13 | 16 |
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase | Homo sapiens (human) | Ki | 0.0235 | 1 | 1 |
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase | Rattus norvegicus (Norway rat) | IC50 | 0.0391 | 16 | 18 |
| Acyl-CoA:cholesterol acyltransferase | Oryctolagus cuniculus (rabbit) | IC50 | 16.8000 | 1 | 1 |
| Adenosine receptor A1 | Homo sapiens (human) | IC50 | 26.7200 | 1 | 1 |
| Adenosine receptor A1 | Homo sapiens (human) | Ki | 15.5860 | 1 | 1 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | IC50 | 8.7530 | 1 | 1 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | Ki | 8.6800 | 1 | 1 |
| Androgen receptor | Rattus norvegicus (Norway rat) | IC50 | 30.1640 | 1 | 1 |
| Androgen receptor | Rattus norvegicus (Norway rat) | Ki | 20.1100 | 1 | 1 |
| Aromatase | Homo sapiens (human) | IC50 | 53.2000 | 1 | 1 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 131.0000 | 1 | 4 |
| ATP-dependent translocase ABCB1 | Homo sapiens (human) | IC50 | 50.0200 | 5 | 5 |
| bcl-2-related protein A1 | Mus musculus (house mouse) | IC50 | 100.0000 | 2 | 2 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 194.0857 | 4 | 7 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 4 |
| Canalicular multispecific organic anion transporter 1 | Rattus norvegicus (Norway rat) | Ki | 172.0000 | 1 | 1 |
| Chain A, Antigen Cd11a (p180) | Homo sapiens (human) | IC50 | 2.4000 | 1 | 1 |
| Chain A, Protein (peroxisome Proliferator Activated Receptor (ppar-delta)) | Homo sapiens (human) | IC50 | 4.0000 | 1 | 1 |
| Cholesteryl ester transfer protein | Homo sapiens (human) | IC50 | 0.0152 | 4 | 4 |
| Coagulation factor VII | Homo sapiens (human) | IC50 | 78.0000 | 1 | 1 |
| Cyclin-A2 | Homo sapiens (human) | IC50 | 7.3000 | 3 | 3 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 | 7.3000 | 3 | 3 |
| Cyclin-dependent kinase 9 | Homo sapiens (human) | IC50 | 0.3000 | 3 | 3 |
| Cyclin-T1 | Homo sapiens (human) | IC50 | 0.3000 | 3 | 3 |
| Cytochrome P450 1A2 | Homo sapiens (human) | Ki | 7.6320 | 1 | 1 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Cytochrome P450 2D6 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Cytochrome P450 2J2 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| Delta-type opioid receptor | Mus musculus (house mouse) | IC50 | 0.0008 | 1 | 1 |
| DNA polymerase beta | Homo sapiens (human) | IC50 | 26.3000 | 1 | 1 |
| Fatty acid-binding protein, intestinal | Homo sapiens (human) | Ki | 17.7000 | 1 | 1 |
| Fatty acid-binding protein, liver | Rattus norvegicus (Norway rat) | Ki | 6.9200 | 1 | 1 |
| Histone deacetylase 1 | Homo sapiens (human) | IC50 | 11.9110 | 1 | 1 |
| Histone deacetylase 2 | Homo sapiens (human) | IC50 | 25.9330 | 1 | 1 |
| Histone deacetylase 6 | Homo sapiens (human) | IC50 | 16.2850 | 1 | 1 |
| Insulin receptor | Rattus norvegicus (Norway rat) | IC50 | 0.0128 | 1 | 2 |
| Integrin alpha-L | Homo sapiens (human) | IC50 | 3.0900 | 2 | 2 |
| Integrin beta-2 | Homo sapiens (human) | IC50 | 3.0900 | 2 | 2 |
| Intercellular adhesion molecule 1 | Homo sapiens (human) | IC50 | 3.7800 | 1 | 1 |
| Lanosterol 14-alpha demethylase | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
| Microsomal triglyceride transfer protein large subunit | Homo sapiens (human) | IC50 | 0.0056 | 3 | 3 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 4 |
| NAD-dependent protein deacylase sirtuin-5, mitochondrial | Homo sapiens (human) | IC50 | 1.6000 | 1 | 1 |
| Neutrophil elastase | Homo sapiens (human) | IC50 | 0.0270 | 1 | 1 |
| NPC1-like intracellular cholesterol transporter 1 | Homo sapiens (human) | IC50 | 0.3700 | 1 | 1 |
| NPC1-like intracellular cholesterol transporter 1 | Rattus norvegicus (Norway rat) | Ki | 0.2000 | 1 | 1 |
| Oxoeicosanoid receptor 1 | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
| Polyunsaturated fatty acid lipoxygenase ALOX15 | Homo sapiens (human) | IC50 | 14.0000 | 1 | 1 |
| Prostaglandin G/H synthase 1 | Bos taurus (cattle) | IC50 | 13.0000 | 1 | 1 |
| Prostaglandin G/H synthase 2 | Homo sapiens (human) | IC50 | 0.0128 | 1 | 2 |
| Prostaglandin G/H synthase 2 | Ovis aries (sheep) | IC50 | 7.1000 | 1 | 1 |
| Prothrombin | Homo sapiens (human) | IC50 | 754.9250 | 4 | 4 |
| Prothrombin | Homo sapiens (human) | Ki | 0.2672 | 1 | 1 |
| Retinoic acid receptor RXR-alpha | Homo sapiens (human) | Ki | 7.6320 | 1 | 1 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | IC50 | 10.1040 | 1 | 1 |
| Sodium-dependent dopamine transporter | Homo sapiens (human) | Ki | 8.0280 | 1 | 1 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | IC50 | 8.7530 | 1 | 1 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | Ki | 8.6800 | 1 | 1 |
| Sodium/bile acid cotransporter | Homo sapiens (human) | Ki | 25.0000 | 1 | 1 |
| Solute carrier family 22 member 11 | Homo sapiens (human) | IC50 | 591.0000 | 1 | 1 |
| Solute carrier family 22 member 6 | Homo sapiens (human) | IC50 | 408.0000 | 1 | 1 |
| Solute carrier family 22 member 6 | Rattus norvegicus (Norway rat) | Ki | 601.0000 | 2 | 2 |
| Solute carrier family 22 member 7 | Homo sapiens (human) | IC50 | 352.0000 | 1 | 1 |
| Solute carrier family 22 member 7 | Rattus norvegicus (Norway rat) | IC50 | 449.0000 | 1 | 1 |
| Solute carrier family 22 member 8 | Homo sapiens (human) | IC50 | 13.7000 | 1 | 1 |
| Solute carrier family 22 member 8 | Rattus norvegicus (Norway rat) | IC50 | 15.6000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1B1 | Homo sapiens (human) | IC50 | 15.8000 | 2 | 2 |
| Solute carrier organic anion transporter family member 1B1 | Homo sapiens (human) | Ki | 3.4000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1B3 | Homo sapiens (human) | IC50 | 62.0000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1B3 | Homo sapiens (human) | Ki | 57.0000 | 1 | 1 |
| Solute carrier organic anion transporter family member 2B1 | Homo sapiens (human) | IC50 | 190.0000 | 1 | 1 |
| Solute carrier organic anion transporter family member 2B1 | Homo sapiens (human) | Ki | 180.0000 | 1 | 1 |
| Substance-K receptor | Homo sapiens (human) | IC50 | 28.2240 | 1 | 1 |
| Substance-K receptor | Homo sapiens (human) | Ki | 9.4080 | 1 | 1 |
| Tissue factor | Homo sapiens (human) | IC50 | 78.0000 | 1 | 1 |
| Trypsin | Sus scrofa (pig) | IC50 | 200.0000 | 1 | 1 |
| Vascular cell adhesion protein 1 | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
Activation Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 4 | Cavia porcellus (domestic guinea pig) | EC50 | 55.0000 | 1 | 1 |
| Fatty acid-binding protein, liver | Rattus norvegicus (Norway rat) | Kd | 8.6625 | 8 | 8 |
| Glutamate receptor ionotropic, NMDA 1 | Homo sapiens (human) | EC50 | 300.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2A | Homo sapiens (human) | EC50 | 300.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2B | Homo sapiens (human) | EC50 | 300.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2C | Homo sapiens (human) | EC50 | 300.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2D | Homo sapiens (human) | EC50 | 300.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 3A | Homo sapiens (human) | EC50 | 300.0000 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 3B | Homo sapiens (human) | EC50 | 300.0000 | 1 | 1 |
| Integrin alpha-L | Homo sapiens (human) | Kd | 12.9000 | 1 | 1 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | EC50 | 500.0000 | 1 | 2 |
| Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | EC50 | 500.0000 | 1 | 2 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | EC50 | 500.0000 | 1 | 2 |
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | EC50 | 500.0000 | 1 | 2 |
| Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | EC50 | 500.0000 | 1 | 2 |
| Neuronal acetylcholine receptor subunit alpha-7 | Rattus norvegicus (Norway rat) | EC50 | 0.0420 | 1 | 1 |
| Peroxisome proliferator-activated receptor alpha | Homo sapiens (human) | EC50 | 52.8833 | 12 | 12 |
| Peroxisome proliferator-activated receptor alpha | Mus musculus (house mouse) | EC50 | 37.7605 | 4 | 4 |
| Peroxisome proliferator-activated receptor delta | Homo sapiens (human) | EC50 | 55.0000 | 1 | 1 |
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | EC50 | 332.8000 | 5 | 5 |
| Peroxisome proliferator-activated receptor gamma | Mus musculus (house mouse) | EC50 | 466.6667 | 3 | 3 |
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | Kd | 2.0000 | 1 | 1 |
Other Measurements
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Canalicular multispecific organic anion transporter 1 | Rattus norvegicus (Norway rat) | Km | 223.0000 | 1 | 1 |
| Solute carrier family 22 member 8 | Rattus norvegicus (Norway rat) | Km | 13.4000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1A1 | Rattus norvegicus (Norway rat) | Km | 30.0000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1A4 | Rattus norvegicus (Norway rat) | Km | 37.5000 | 1 | 1 |
| Solute carrier organic anion transporter family member 1B1 | Homo sapiens (human) | Km | 59.7000 | 2 | 2 |
| Solute carrier organic anion transporter family member 2B1 | Homo sapiens (human) | Km | 2,250.0000 | 1 | 1 |
| UDP-glucuronosyltransferase 1A1 | Homo sapiens (human) | Km | 64.0000 | 1 | 1 |
| UDP-glucuronosyltransferase 1A3 | Homo sapiens (human) | Km | 42.0000 | 1 | 1 |
| UDP-glucuronosyltransferase 2B7 | Homo sapiens (human) | Km | 21.0000 | 1 | 1 |