An agent which overcomes insulin resistance by activation of the peroxisome proliferator activated receptor gamma (PPAR-gamma).
ChEBI ID: 50864
| Member | Definition | Class |
|---|---|---|
| 15-deoxy-delta(12,14)-prostaglandin j2 | A prostaglandin J derivative comprising prostaglandin J2 lacking the 15-hydroxy group and having C=C double bonds at the 12- and 14-positions. | 15-deoxy-Delta(12,14)-prostaglandin J2 |
| ciglitazone | An aromatic ether that consists of 1,3-thiazolidine-2,4-dione with position 5 substituted by a 4-[(1-methylcyclohexyl)methoxy]benzyl group. A selective PPARgamma agonist. | ciglitazone |
| 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 |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 30 (0.33) | 18.7374 |
| 1990's | 271 (3.02) | 18.2507 |
| 2000's | 4,090 (45.54) | 29.6817 |
| 2010's | 3,867 (43.05) | 24.3611 |
| 2020's | 724 (8.06) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 1,381 (13.64%) | 5.53% |
| Reviews | 887 (8.76%) | 6.00% |
| Case Studies | 199 (1.97%) | 4.05% |
| Observational | 26 (0.26%) | 0.25% |
| Other | 7,631 (75.38%) | 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 | 43.6486 | 1 | 1 |
| aldehyde dehydrogenase 1 family, member A1 | Homo sapiens (human) | Potency | 22.0289 | 1 | 3 |
| AR protein | Homo sapiens (human) | Potency | 20.0973 | 6 | 6 |
| aryl hydrocarbon receptor | Homo sapiens (human) | Potency | 32.8366 | 2 | 2 |
| Bloom syndrome protein isoform 1 | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| Cellular tumor antigen p53 | Homo sapiens (human) | Potency | 34.1376 | 3 | 4 |
| Chain A, 2-oxoglutarate Oxygenase | Homo sapiens (human) | Potency | 28.1838 | 1 | 1 |
| Chain A, ATP-DEPENDENT DNA HELICASE Q1 | Homo sapiens (human) | Potency | 24.0893 | 2 | 5 |
| Chain A, Cruzipain | Trypanosoma cruzi | Potency | 35.4813 | 1 | 1 |
| Chain A, Ferritin light chain | Equus caballus (horse) | Potency | 21.2440 | 2 | 3 |
| Chain A, HADH2 protein | Homo sapiens (human) | Potency | 31.6228 | 1 | 1 |
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 17.3729 | 1 | 3 |
| Chain A, TYROSYL-DNA PHOSPHODIESTERASE | Homo sapiens (human) | Potency | 19.2084 | 1 | 3 |
| Chain B, HADH2 protein | Homo sapiens (human) | Potency | 31.6228 | 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 | 17.5822 | 2 | 3 |
| cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a | Homo sapiens (human) | Potency | 10.5909 | 1 | 1 |
| DNA polymerase kappa isoform 1 | Homo sapiens (human) | Potency | 7.1912 | 1 | 2 |
| estrogen nuclear receptor alpha | Homo sapiens (human) | Potency | 18.9635 | 6 | 8 |
| estrogen receptor 2 (ER beta) | Homo sapiens (human) | Potency | 6.0602 | 2 | 2 |
| estrogen-related nuclear receptor alpha | Homo sapiens (human) | Potency | 23.5899 | 3 | 4 |
| euchromatic histone-lysine N-methyltransferase 2 | Homo sapiens (human) | Potency | 21.1699 | 1 | 2 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 4.3550 | 2 | 4 |
| farnesoid X nuclear receptor | Homo sapiens (human) | Potency | 32.9391 | 3 | 3 |
| 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 | 8.4144 | 1 | 1 |
| glucocorticoid receptor [Homo sapiens] | Homo sapiens (human) | Potency | 29.4852 | 5 | 6 |
| histone acetyltransferase KAT2A isoform 1 | Homo sapiens (human) | Potency | 24.1969 | 1 | 3 |
| lamin isoform A-delta10 | Homo sapiens (human) | Potency | 0.0022 | 1 | 1 |
| Luciferase | Photinus pyralis (common eastern firefly) | Potency | 25.2913 | 2 | 3 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 26.8088 | 2 | 4 |
| nuclear factor erythroid 2-related factor 2 isoform 1 | Homo sapiens (human) | Potency | 38.8314 | 3 | 3 |
| nuclear receptor ROR-gamma isoform 1 | Mus musculus (house mouse) | Potency | 24.0353 | 2 | 2 |
| nuclear receptor subfamily 1, group I, member 3 | Homo sapiens (human) | Potency | 20.1994 | 3 | 5 |
| peripheral myelin protein 22 | Rattus norvegicus (Norway rat) | Potency | 18.1056 | 1 | 1 |
| peroxisome proliferator activated receptor gamma | Homo sapiens (human) | Potency | 2.2867 | 4 | 6 |
| Peroxisome proliferator-activated receptor alpha | Homo sapiens (human) | Potency | 44.6684 | 1 | 1 |
| peroxisome proliferator-activated receptor delta | Homo sapiens (human) | Potency | 31.2256 | 2 | 2 |
| phosphopantetheinyl transferase | Bacillus subtilis | Potency | 67.8334 | 1 | 2 |
| potassium voltage-gated channel subfamily H member 2 isoform d | Homo sapiens (human) | Potency | 35.4813 | 1 | 1 |
| pregnane X nuclear receptor | Homo sapiens (human) | Potency | 23.5303 | 3 | 3 |
| progesterone receptor | Homo sapiens (human) | Potency | 14.9601 | 1 | 1 |
| prostaglandin E2 receptor EP2 subtype | Homo sapiens (human) | Potency | 41.7629 | 1 | 1 |
| regulator of G-protein signaling 4 | Homo sapiens (human) | Potency | 1.5912 | 1 | 2 |
| retinoic acid nuclear receptor alpha variant 1 | Homo sapiens (human) | Potency | 12.7968 | 2 | 2 |
| retinoid X nuclear receptor alpha | Homo sapiens (human) | Potency | 10.7941 | 3 | 3 |
| SMAD family member 2 | Homo sapiens (human) | Potency | 8.4852 | 1 | 1 |
| SMAD family member 3 | Homo sapiens (human) | Potency | 8.4852 | 1 | 1 |
| TDP1 protein | Homo sapiens (human) | Potency | 25.0965 | 2 | 6 |
| thyroid hormone receptor beta isoform 2 | Rattus norvegicus (Norway rat) | Potency | 18.6597 | 2 | 4 |
| 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 | 12.4822 | 1 | 2 |
| v-jun sarcoma virus 17 oncogene homolog (avian) | Homo sapiens (human) | Potency | 0.0007 | 1 | 1 |
| vitamin D (1,25- dihydroxyvitamin D3) receptor | Homo sapiens (human) | Potency | 2.6601 | 1 | 1 |
| vitamin D3 receptor isoform VDRA | Homo sapiens (human) | Potency | 15.5346 | 1 | 4 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| 15-hydroxyprostaglandin dehydrogenase [NAD(+)] | Homo sapiens (human) | IC50 | 2.7000 | 1 | 1 |
| Acetylcholinesterase | Homo sapiens (human) | IC50 | 15.0260 | 1 | 1 |
| Adenosine receptor A3 | Homo sapiens (human) | IC50 | 3.0470 | 1 | 1 |
| Adenosine receptor A3 | Homo sapiens (human) | Ki | 1.7220 | 1 | 1 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | IC50 | 2.2200 | 1 | 1 |
| Aldo-keto reductase family 1 member B1 | Rattus norvegicus (Norway rat) | Ki | 2.2010 | 1 | 1 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 3.0470 | 1 | 1 |
| Alpha-1A adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 1.7220 | 1 | 1 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | IC50 | 3.0470 | 1 | 1 |
| Alpha-1B adrenergic receptor | Rattus norvegicus (Norway rat) | Ki | 1.7220 | 1 | 1 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | IC50 | 16.5510 | 1 | 1 |
| Alpha-2A adrenergic receptor | Homo sapiens (human) | Ki | 6.2070 | 1 | 1 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | IC50 | 13.2580 | 1 | 1 |
| Alpha-2B adrenergic receptor | Homo sapiens (human) | Ki | 6.0530 | 1 | 1 |
| Amine oxidase [flavin-containing] A | Homo sapiens (human) | IC50 | 32.1310 | 1 | 2 |
| Amine oxidase [flavin-containing] A | Homo sapiens (human) | Ki | 27.6000 | 1 | 1 |
| Amine oxidase [flavin-containing] A | Rattus norvegicus (Norway rat) | Ki | 16.4354 | 2 | 2 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | IC50 | 0.4517 | 2 | 6 |
| Amine oxidase [flavin-containing] B | Homo sapiens (human) | Ki | 1.2926 | 3 | 4 |
| Amine oxidase [flavin-containing] B | Rattus norvegicus (Norway rat) | Ki | 2.0926 | 3 | 4 |
| ATP-binding cassette sub-family C member 3 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 3 |
| ATP-binding cassette sub-family C member 8 | Homo sapiens (human) | IC50 | 0.0480 | 1 | 1 |
| ATP-sensitive inward rectifier potassium channel 11 | Homo sapiens (human) | IC50 | 0.0480 | 1 | 1 |
| Beta-3 adrenergic receptor | Homo sapiens (human) | IC50 | 17.8710 | 1 | 1 |
| Beta-3 adrenergic receptor | Homo sapiens (human) | Ki | 13.4030 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 7.5096 | 6 | 14 |
| Bile salt export pump | Rattus norvegicus (Norway rat) | IC50 | 21.0000 | 1 | 2 |
| C-C chemokine receptor type 2 | Homo sapiens (human) | Ki | 32.6000 | 1 | 1 |
| Canalicular multispecific organic anion transporter 1 | Homo sapiens (human) | IC50 | 133.0000 | 1 | 1 |
| Carbonic anhydrase 2 | Homo sapiens (human) | IC50 | 1.4230 | 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 |
| D(1A) dopamine receptor | Homo sapiens (human) | IC50 | 19.7850 | 1 | 1 |
| D(1A) dopamine receptor | Homo sapiens (human) | Ki | 9.8930 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | IC50 | 26.7040 | 1 | 1 |
| D(3) dopamine receptor | Homo sapiens (human) | Ki | 9.0690 | 1 | 1 |
| Delta-type opioid receptor | Homo sapiens (human) | IC50 | 26.8940 | 1 | 1 |
| Delta-type opioid receptor | Homo sapiens (human) | Ki | 9.4810 | 1 | 1 |
| Enoyl-[acyl-carrier-protein] reductase [NADH] | Francisella tularensis subsp. tularensis SCHU S4 | IC50 | 79.0000 | 1 | 1 |
| Epidermal growth factor receptor | Homo sapiens (human) | IC50 | 4.6550 | 1 | 1 |
| Melanocortin receptor 5 | Homo sapiens (human) | IC50 | 28.6210 | 1 | 1 |
| Melanocortin receptor 5 | Homo sapiens (human) | Ki | 26.8480 | 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 | 67.8333 | 1 | 3 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | IC50 | 21.1070 | 1 | 1 |
| Muscarinic acetylcholine receptor M2 | Homo sapiens (human) | Ki | 7.5050 | 1 | 1 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | IC50 | 14.9470 | 1 | 1 |
| Muscarinic acetylcholine receptor M3 | Homo sapiens (human) | Ki | 3.1680 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | IC50 | 16.2240 | 1 | 1 |
| Muscarinic acetylcholine receptor M4 | Homo sapiens (human) | Ki | 2.2630 | 1 | 1 |
| 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 | 1.4585 | 51 | 56 |
| 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 | 0.3565 | 22 | 26 |
| Potassium voltage-gated channel subfamily H member 2 | Homo sapiens (human) | IC50 | 29.5000 | 1 | 1 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | IC50 | 2.2200 | 1 | 1 |
| Sodium-dependent noradrenaline transporter | Homo sapiens (human) | Ki | 2.2010 | 1 | 1 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | IC50 | 14.9480 | 1 | 1 |
| Sodium-dependent serotonin transporter | Homo sapiens (human) | Ki | 7.9410 | 1 | 1 |
| Sodium/bile acid cotransporter | Homo sapiens (human) | IC50 | 5.1000 | 1 | 1 |
| Steryl-sulfatase | Homo sapiens (human) | IC50 | 0.8000 | 1 | 1 |
| Substance-K receptor | Homo sapiens (human) | IC50 | 12.5760 | 1 | 1 |
| Substance-K receptor | Homo sapiens (human) | Ki | 4.1920 | 1 | 1 |
| Thromboxane-A synthase | Homo sapiens (human) | IC50 | 3.5600 | 1 | 1 |
| Tyrosine-protein phosphatase non-receptor type 1 | Homo sapiens (human) | IC50 | 216.6667 | 2 | 3 |
| 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 |
| Muscarinic acetylcholine receptor M1 | Rattus norvegicus (Norway rat) | EC50 | 0.3130 | 1 | 4 |
| Muscarinic acetylcholine receptor M2 | Rattus norvegicus (Norway rat) | EC50 | 0.3130 | 1 | 4 |
| Muscarinic acetylcholine receptor M3 | Rattus norvegicus (Norway rat) | EC50 | 0.3130 | 1 | 4 |
| Muscarinic acetylcholine receptor M4 | Rattus norvegicus (Norway rat) | EC50 | 0.3130 | 1 | 4 |
| Muscarinic acetylcholine receptor M5 | Rattus norvegicus (Norway rat) | EC50 | 0.3130 | 1 | 4 |
| Nuclear receptor subfamily 1 group I member 2 | Homo sapiens (human) | EC50 | 9.5333 | 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 | 56.2902 | 173 | 185 |
| Peroxisome proliferator-activated receptor gamma | Mus musculus (house mouse) | EC50 | 0.7343 | 3 | 6 |
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | Kd | 1.2602 | 9 | 9 |
| Thrombin | Oryctolagus cuniculus (rabbit) | EC50 | 0.0110 | 1 | 1 |
| Transient receptor potential cation channel subfamily A member 1 | Homo sapiens (human) | EC50 | 5.6000 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| Peroxisome proliferator-activated receptor gamma | Homo sapiens (human) | Activity | 1.6475 | 4 | 4 |