An EC 6.2.1.* (acid-thiol ligase) inhibitor that interferes with the action of a long-chain-fatty-acid--CoA ligase (EC 6.2.1.3).
ChEBI ID: 83157
| Member | Definition | Class |
|---|---|---|
| pioglitazone | A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity. | pioglitazone |
| rosiglitazone | rosiglitazone | |
| triacsin c | A nitroso compound that is N-undecylnitrous hydrazide carrying double bonds at positions 1,2,4, and 7. It is a long-chain fatty acyl CoA synthetase inhibitor and interferes with lipid metabolism by inhibiting the de novo synthesis of glycerolipids and cholesterol esters. | triacsin C |
| troglitazone | troglitazone |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 7 (0.07) | 18.7374 |
| 1990's | 604 (6.20) | 18.2507 |
| 2000's | 4,429 (45.46) | 29.6817 |
| 2010's | 3,954 (40.58) | 24.3611 |
| 2020's | 749 (7.69) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1,526 (13.79%) | 5.53% |
| Reviews | 1,049 (9.48%) | 6.00% |
| Case Studies | 245 (2.21%) | 4.05% |
| Observational | 26 (0.23%) | 0.25% |
| Other | 8,218 (74.28%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1 | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| acetylcholinesterase | Homo sapiens (human) | Potency | 89.3584 | 1 | 1 |
| activating transcription factor 6 | Homo sapiens (human) | Potency | 54.9410 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 15.8489 | 1 | 1 |
| AR protein | Homo sapiens (human) | Potency | 31.4768 | 10 | 16 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 39.4104 | 3 | 6 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| Chain A, ATP-DEPENDENT DNA HELICASE Q1 | Homo sapiens (human) | Potency | 52.7397 | 2 | 4 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 1.2582 | 1 | 2 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 49.2885 | 1 | 2 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 6.9178 | 1 | 1 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 38.9018 | 1 | 1 |
| cytochrome P450 3A4 isoform 1 | Homo sapiens (human) | Potency | 7.9433 | 2 | 2 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 18.2888 | 2 | 2 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 45.4900 | 1 | 2 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 29.2039 | 10 | 20 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 16.6350 | 2 | 3 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 43.7779 | 6 | 9 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 22.5358 | 1 | 2 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 4.3550 | 2 | 4 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 59.6426 | 2 | 2 |
| G | Vesicular stomatitis virus | Potency | 6.9178 | 1 | 1 |
| GABA theta subunit | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-4 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-5 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit alpha-6 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit beta-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit delta | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit epsilon | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-1 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-2 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit gamma-3 | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| Gamma-aminobutyric acid receptor subunit pi | Rattus norvegicus (Norway rat) | Potency | 7.9433 | 1 | 1 |
| geminin | Homo sapiens (human) | Potency | 13.3359 | 1 | 1 |
| GLI family zinc finger 3 | Homo sapiens (human) | Potency | 35.7375 | 2 | 3 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 37.0314 | 2 | 4 |
| Glutamate receptor 2 | Rattus norvegicus (Norway rat) | Potency | 26.9546 | 1 | 2 |
| heat shock protein beta-1 | Homo sapiens (human) | Potency | 58.2929 | 2 | 2 |
| Histamine H2 receptor | Cavia porcellus (domestic guinea pig) | Potency | 10.0000 | 1 | 2 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 32.1841 | 1 | 3 |
| Histone H2A.x | Cricetulus griseus (Chinese hamster) | Potency | 126.7930 | 1 | 1 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 6.9178 | 1 | 1 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 6.9178 | 1 | 2 |
| Interferon beta | Homo sapiens (human) | Potency | 6.9178 | 1 | 1 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 0.0022 | 1 | 1 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 32.1968 | 1 | 2 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 20.0850 | 1 | 2 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 14.2070 | 3 | 5 |
| nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_a | Homo sapiens (human) | Potency | 35.0650 | 1 | 2 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 15.8489 | 1 | 1 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 15.5566 | 2 | 2 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 10.1815 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 0.3739 | 4 | 9 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 13.5186 | 2 | 3 |
| Polyunsaturated fatty acid lipoxygenase ALOX15B | Homo sapiens (human) | Potency | 10.0000 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 33.9679 | 3 | 3 |
| progesterone receptor | Homo sapiens (human) | Potency | 21.5851 | 1 | 2 |
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 14.6764 | 2 | 4 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 23.7781 | 1 | 1 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 41.1779 | 2 | 4 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 14.0115 | 3 | 5 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 5.6404 | 2 | 2 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 5.6404 | 2 | 2 |
| Spike glycoprotein | Severe acute respiratory syndrome-related coronavirus | Potency | 17.7828 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 21.1096 | 2 | 8 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 23.9487 | 3 | 7 |
| thyroid hormone receptor beta isoform a | Homo sapiens (human) | Potency | 19.9526 | 1 | 1 |
| thyroid stimulating hormone receptor | Homo sapiens (human) | Potency | 61.1306 | 2 | 2 |
| thyrotropin-releasing hormone receptor | Homo sapiens (human) | Potency | 3.3786 | 1 | 1 |
| tyrosine-protein kinase Yes | Homo sapiens (human) | Potency | 1.7291 | 1 | 1 |
| USP1 protein, partial | Homo sapiens (human) | Potency | 30.6230 | 1 | 2 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 30.8228 | 1 | 2 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 6.9012 | 1 | 2 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| Voltage-dependent calcium channel gamma-2 subunit | Mus musculus (house mouse) | Potency | 26.9546 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | IC50 | 1.3120 | 1 | 1 |
| 5-hydroxytryptamine receptor 2B | Homo sapiens (human) | Ki | 0.8350 | 1 | 1 |
| Adenosine receptor A3 | Homo sapiens (human) | IC50 | 5.2080 | 1 | 1 |
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 2.9430 | 1 | 1 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 5.2080 | 1 | 1 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 2.9430 | 1 | 1 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 5.2080 | 1 | 1 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 2.9430 | 1 | 1 |
| Amine oxidase [flavin-containing] A | Homo sapiens (human) | IC50 | 35.0690 | 1 | 1 |
| Amine oxidase [flavin-containing] A | Homo sapiens (human) | Ki | 19.0500 | 2 | 2 |
| Amine oxidase [flavin-containing] A | Rattus norvegicus (Norway rat) | Ki | 12.5569 | 3 | 3 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | IC50 | 1.0667 | 2 | 6 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | Ki | 2.9340 | 4 | 5 |
| Amine oxidase [flavin-containing] B | Rattus norvegicus (Norway rat) | Ki | 3.8540 | 4 | 5 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 99.0000 | 1 | 3 |
| ATP-binding cassette sub-family C member 8 | Homo sapiens (human) | IC50 | 0.6665 | 1 | 2 |
| ATP-sensitive inward rectifier potassium channel 11 | Homo sapiens (human) | IC50 | 0.6665 | 1 | 2 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 6.6439 | 7 | 19 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 | 14.1250 | 2 | 4 |
| C-C chemokine receptor type 2 | Homo sapiens (human) | Ki | 32.6000 | 1 | 1 |
| Carbonic anhydrase 2 | Homo sapiens (human) | IC50 | 1.7177 | 1 | 3 |
| Carnitine O-palmitoyltransferase 1, liver isoform | Homo sapiens (human) | IC50 | 10.0000 | 1 | 2 |
| Carnitine O-palmitoyltransferase 2, mitochondrial | Homo sapiens (human) | IC50 | 100.0000 | 1 | 2 |
| Carnitine O-palmitoyltransferase 2, mitochondrial | Rattus norvegicus (Norway rat) | IC50 | 100.0000 | 1 | 2 |
| CDGSH iron-sulfur domain-containing protein 1 | Homo sapiens (human) | IC50 | 4.6905 | 1 | 2 |
| CDGSH iron-sulfur domain-containing protein 1 | Rattus norvegicus (Norway rat) | IC50 | 1.0500 | 1 | 2 |
| CDGSH iron-sulfur domain-containing protein 1 | Homo sapiens (human) | Ki | 0.2005 | 1 | 2 |
| CDGSH iron-sulfur domain-containing protein 2 | Homo sapiens (human) | IC50 | 3.5450 | 1 | 2 |
| Cytochrome P450 2C9 | Homo sapiens (human) | IC50 | 4.0000 | 1 | 1 |
| Enoyl-[acyl-carrier-protein] reductase [NADH] | Francisella tularensis subsp. tularensis SCHU S4 | IC50 | 79.0000 | 1 | 1 |
| Forkhead box protein M1 | Homo sapiens (human) | IC50 | 122.4000 | 1 | 1 |
| Forkhead box protein M1 | Homo sapiens (human) | Ki | 0.0520 | 1 | 1 |
| Indoleamine 2,3-dioxygenase 1 | Mus musculus (house mouse) | IC50 | 61.0000 | 1 | 1 |
| Indoleamine 2,3-dioxygenase 2 | Mus musculus (house mouse) | IC50 | 4.5000 | 1 | 1 |
| Mitogen-activated protein kinase 1 | Homo sapiens (human) | IC50 | 1.2380 | 1 | 1 |
| Mu-type opioid receptor | Cavia porcellus (domestic guinea pig) | IC50 | 0.0380 | 1 | 1 |
| Multidrug resistance-associated protein 4 | Homo sapiens (human) | IC50 | 43.8333 | 1 | 3 |
| Peroxisome proliferator-activated receptor alpha | Homo sapiens (human) | IC50 | 25.5266 | 18 | 19 |
| Peroxisome proliferator-activated receptor alpha | Mus musculus (house mouse) | IC50 | 0.6150 | 1 | 2 |
| Peroxisome proliferator-activated receptor alpha | Homo sapiens (human) | Ki | 33.3000 | 1 | 1 |
| Peroxisome proliferator-activated receptor delta | Homo sapiens (human) | IC50 | 32.0010 | 5 | 5 |
| Peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Ki | 33.3000 | 1 | 1 |
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | IC50 | 1.3583 | 52 | 61 |
| Peroxisome proliferator-activated receptor gamma | Mus musculus (house mouse) | IC50 | 0.7000 | 1 | 1 |
| Peroxisome proliferator-activated receptor gamma | Rattus norvegicus (Norway rat) | IC50 | 0.7000 | 1 | 1 |
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | Ki | 0.2588 | 25 | 30 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 29.5000 | 1 | 1 |
| Sodium/bile acid cotransporter | Homo sapiens (human) | IC50 | 5.1000 | 1 | 1 |
| Steryl-sulfatase | Homo sapiens (human) | IC50 | 0.8000 | 1 | 1 |
| Thromboxane-A synthase | Homo sapiens (human) | IC50 | 3.2630 | 1 | 2 |
| Tyrosine-protein phosphatase non-receptor type 1 | Homo sapiens (human) | IC50 | 176.2500 | 2 | 4 |
| UDP-glucuronosyltransferase 1-6 | Homo sapiens (human) | Ki | 20.0000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Cannabinoid receptor 2 | Mus musculus (house mouse) | EC50 | 0.0330 | 1 | 1 |
| Catechol O-methyltransferase | Rattus norvegicus (Norway rat) | EC50 | 0.2200 | 1 | 3 |
| Cytochrome P450 2C9 | Homo sapiens (human) | EC50 | 0.0110 | 1 | 1 |
| Cytochrome P450 3A4 | Homo sapiens (human) | EC50 | 0.0110 | 1 | 1 |
| Cytochrome P450 3A5 | Homo sapiens (human) | EC50 | 0.0110 | 1 | 1 |
| Free fatty acid receptor 1 | Homo sapiens (human) | EC50 | 412.1562 | 1 | 2 |
| Glutamate receptor ionotropic, NMDA 1 | Homo sapiens (human) | EC50 | 0.0210 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 1 | Rattus norvegicus (Norway rat) | EC50 | 0.0210 | 1 | 2 |
| Glutamate receptor ionotropic, NMDA 2A | Homo sapiens (human) | EC50 | 0.0210 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2B | Homo sapiens (human) | EC50 | 0.0210 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2C | Homo sapiens (human) | EC50 | 0.0210 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 2D | Homo sapiens (human) | EC50 | 0.0210 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 3A | Homo sapiens (human) | EC50 | 0.0210 | 1 | 1 |
| Glutamate receptor ionotropic, NMDA 3B | Homo sapiens (human) | EC50 | 0.0210 | 1 | 1 |
| Mitogen-activated protein kinase 14 | Homo sapiens (human) | EC50 | 1.0000 | 1 | 1 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | EC50 | 0.4687 | 1 | 6 |
| Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | EC50 | 0.4687 | 1 | 6 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | EC50 | 0.4687 | 1 | 6 |
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | EC50 | 0.4687 | 1 | 6 |
| Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | EC50 | 0.4687 | 1 | 6 |
| Nuclear receptor subfamily 1 group I member 2 | Homo sapiens (human) | EC50 | 15.8000 | 3 | 3 |
| Peroxisome proliferator-activated receptor alpha | Homo sapiens (human) | EC50 | 6.7705 | 41 | 43 |
| Peroxisome proliferator-activated receptor alpha | Mus musculus (house mouse) | EC50 | 3.0000 | 1 | 1 |
| Peroxisome proliferator-activated receptor delta | Homo sapiens (human) | EC50 | 6.1110 | 10 | 10 |
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | EC50 | 51.4692 | 185 | 202 |
| Peroxisome proliferator-activated receptor gamma | Mus musculus (house mouse) | EC50 | 0.4551 | 4 | 7 |
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | Kd | 1.1677 | 8 | 8 |
| Thrombin | Oryctolagus cuniculus (rabbit) | EC50 | 0.0110 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Peroxisome proliferator-activated receptor alpha | Homo sapiens (human) | Fold activation | 1.1200 | 1 | 1 |
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | Activity | 1.6475 | 4 | 4 |
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | Fold activation | 3.1600 | 1 | 1 |
| UDP-glucuronosyltransferase 1A1 | Homo sapiens (human) | Km | 58.0000 | 1 | 1 |
| UDP-glucuronosyltransferase 1A10 | Homo sapiens (human) | Km | 11.0000 | 1 | 1 |