Proteins > Peroxisome proliferator-activated receptor alpha
Page last updated: 2024-08-07 13:07:15
Peroxisome proliferator-activated receptor alpha
A peroxisome proliferator-activated receptor alpha that is encoded in the genome of mouse. [OMA:P23204, PRO:DNx]
Synonyms
PPAR-alpha;
Nuclear receptor subfamily 1 group C member 1
Research
Bioassay Publications (20)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 2 (10.00) | 18.2507 |
| 2000's | 12 (60.00) | 29.6817 |
| 2010's | 5 (25.00) | 24.3611 |
| 2020's | 1 (5.00) | 2.80 |
Compounds (23)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| pioglitazone | Mus musculus (house mouse) | IC50 | 1.1500 | 1 | 1 |
| pirinixic acid | Mus musculus (house mouse) | Ki | 0.1000 | 1 | 1 |
| rosiglitazone | Mus musculus (house mouse) | IC50 | 0.0800 | 1 | 1 |
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| gw 2433 | Mus musculus (house mouse) | EC50 | 0.2700 | 1 | 1 |
| clofibrate | Mus musculus (house mouse) | EC50 | 50.0000 | 1 | 1 |
| clofibric acid | Mus musculus (house mouse) | EC50 | 33.6807 | 3 | 3 |
| fenofibrate | Mus musculus (house mouse) | EC50 | 18.0000 | 1 | 1 |
| pirinixic acid | Mus musculus (house mouse) | EC50 | 0.4740 | 4 | 5 |
| bezafibrate | Mus musculus (house mouse) | EC50 | 90.0000 | 2 | 2 |
| fenofibric acid | Mus musculus (house mouse) | EC50 | 18.0000 | 1 | 1 |
| telmisartan | Mus musculus (house mouse) | EC50 | 10.0000 | 1 | 1 |
| rosiglitazone | Mus musculus (house mouse) | EC50 | 3.0000 | 1 | 1 |
| mk 767 | Mus musculus (house mouse) | EC50 | 10.0000 | 1 | 1 |
| jtt 501 | Mus musculus (house mouse) | EC50 | 4.3000 | 1 | 1 |
| tesaglitazar | Mus musculus (house mouse) | EC50 | 1.7000 | 1 | 1 |
| gw 7647 | Mus musculus (house mouse) | EC50 | 0.0010 | 1 | 1 |
| gw 501516 | Mus musculus (house mouse) | EC50 | 2.5000 | 1 | 1 |
| gw 9578 | Mus musculus (house mouse) | EC50 | 0.0067 | 3 | 3 |
| l 796449 | Mus musculus (house mouse) | EC50 | 7.6000 | 1 | 1 |
| gw0742 | Mus musculus (house mouse) | EC50 | 8.8000 | 1 | 1 |
| ns-220 | Mus musculus (house mouse) | EC50 | 0.0300 | 1 | 1 |
| gw 590735 | Mus musculus (house mouse) | EC50 | 0.0175 | 2 | 2 |
| aleglitazar | Mus musculus (house mouse) | EC50 | 2.3400 | 1 | 1 |
| lt175 | Mus musculus (house mouse) | EC50 | 0.2440 | 3 | 5 |
| bms 687453 | Mus musculus (house mouse) | EC50 | 4.5138 | 3 | 6 |
Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.Journal of medicinal chemistry, , Aug-25, Volume: 48, Issue:17, 2005
A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.Journal of medicinal chemistry, , Sep-23, Volume: 42, Issue:19, 1999
The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones.Journal of medicinal chemistry, , Feb-02, Volume: 39, Issue:3, 1996
Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.Journal of medicinal chemistry, , Aug-25, Volume: 48, Issue:17, 2005
O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists.Bioorganic & medicinal chemistry letters, , Oct-06, Volume: 13, Issue:19, 2003
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.Journal of medicinal chemistry, , Sep-23, Volume: 42, Issue:19, 1999
The Race to Bash NASH: Emerging Targets and Drug Development in a Complex Liver Disease.Journal of medicinal chemistry, , 05-28, Volume: 63, Issue:10, 2020
Discovery of a peroxisome proliferator activated receptor gamma (PPARgamma) modulator with balanced PPARalpha activity for the treatment of type 2 diabetes and dyslipidemia.Journal of medicinal chemistry, , Jul-23, Volume: 52, Issue:14, 2009
Glycine amides as PPARalpha agonists.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 20, Issue:11, 2010
The PPARs: from orphan receptors to drug discovery.Journal of medicinal chemistry, , Feb-24, Volume: 43, Issue:4, 2000
A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.Journal of medicinal chemistry, , Sep-23, Volume: 42, Issue:19, 1999
Design, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor alpha agonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 18, Issue:2, 2008
Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents.Journal of medicinal chemistry, , Feb-22, Volume: 50, Issue:4, 2007
Crystal structure of the peroxisome proliferator-activated receptor gamma (PPARgamma) ligand binding domain complexed with a novel partial agonist: a new region of the hydrophobic pocket could be exploited for drug design.Journal of medicinal chemistry, , Dec-25, Volume: 51, Issue:24, 2008
Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.Journal of medicinal chemistry, , Aug-25, Volume: 48, Issue:17, 2005
Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARα Selective Agonist.ACS medicinal chemistry letters, , Jun-09, Volume: 7, Issue:6, 2016
Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453).Journal of medicinal chemistry, , Apr-08, Volume: 53, Issue:7, 2010
Novel peroxisome proliferator-activated receptor alpha agonists lower low-density lipoprotein and triglycerides, raise high-density lipoprotein, and synergistically increase cholesterol excretion with a liver X receptor agonist.The Journal of pharmacology and experimental therapeutics, , Volume: 327, Issue:3, 2008