Target family: 1C. Peroxisome proliferator-activated receptors (type: nhr)
Target: Peroxisome proliferator-activated receptor-&alpha;

Ligand: chiglitazar (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: China (2022)
Primary target: no
Median affinity: 5.920000076293945 pEC50
Reference (Journal): The PPARalpha/gamma dual agonist chiglitazar improves insulin resistance and dyslipidemia in MSG obese rats.
Published in: Br J Pharmacol

Ligand: ciprofibrate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: UK (2009)
Primary target: yes
Median affinity: 6.050000190734863 pEC50
Reference (Journal): Anti-inflammatory and PPAR transactivational effects of secondary metabolites from the roots of Asarum sieboldii.
Published in: Bioorg Med Chem Lett

Ligand: clofibrate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: yes
Median affinity: 4.25 pIC50
Reference (Journal): N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents.
Published in: J Med Chem

Ligand: clofibrate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: yes
Median affinity: 4.25 pIC50
Reference (Journal): Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
Published in: J Med Chem

Ligand: clofibrate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: yes
Median affinity: 4.25 pIC50
Reference (Journal): The PPARs: from orphan receptors to drug discovery.
Published in: J Med Chem

Ligand: CP-775146 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.3 pEC50
Reference (Journal): Molecular characterization of novel and selective peroxisome proliferator-activated receptor alpha agonists with robust hypolipidemic activity in vivo.
Published in: Mol Pharmacol

Ligand: DRF 2519 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 5 pEC50
Reference (Journal): Antidiabetic and hypolipidemic potential of DRF 2519--a dual activator of PPAR-alpha and PPAR-gamma.
Published in: Eur J Pharmacol

Ligand: edaglitazone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.980000019073486 pEC50
Reference (Journal): Comparative molecular profiling of the PPARα/γ activator aleglitazar: PPAR selectivity, activity and interaction with cofactors.
Published in: ChemMedChem

Ligand: eicosatetranoic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.7 pIC50
Reference (Journal): PPAR alpha structure-function relationships derived from species-specific differences in responsiveness to hypolipidemic agents.
Published in: Biol Chem

Ligand: eicosatetranoic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.7 pIC50
Reference (Journal): Fatty acids and retinoids control lipid metabolism through activation of peroxisome proliferator-activated receptor-retinoid X receptor heterodimers.
Published in: Proc Natl Acad Sci USA

Ligand: elafibranor (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2024)
Primary target: no
Median affinity: 8.220000267028809 pEC50
Reference (Journal): New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease.
Published in: Expert Opin Pharmacother

Ligand: farglitazar (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.35 pEC50
Reference (Journal): The PPARs: from orphan receptors to drug discovery.
Published in: J Med Chem

Ligand: GW9578 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.3 pEC50
Reference (Journal): A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-gamma reverses the diabetic phenotype of the Zucker diabetic fatty rat.
Published in: Diabetes

Ligand: GW9578 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.3 pEC50
Reference (Journal): Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.
Published in: Bioorg Med Chem Lett

Ligand: GW9578 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.3 pEC50
Reference (Journal): A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.
Published in: J Med Chem

Ligand: imiglitazar (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.17 pEC50
Reference (Journal): Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone.
Published in: Biochem Biophys Res Commun

Ligand: lanifibranor (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.809999942779541 pEC50
Reference (Journal): Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) &#x3b1;/&#x3b3;/&#x3b4; Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate.
Published in: J Med Chem

Ligand: LTB4 (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): Fatty acids, eicosanoids, and hypolipidemic agents identified as ligands of peroxisome proliferator-activated receptors by coactivator-dependent receptor ligand assay.
Published in: Mol Endocrinol

Ligand: LTB4 (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): The PPARalpha-leukotriene B4 pathway to inflammation control.
Published in: Nature

Ligand: LY-465608 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.8 pIC50
Reference (Journal): Design and synthesis of 2-methyl-2-[4-(2-[5-methyl-2-aryloxazol-4-yl]ethoxy)phenoxy]propionic acids: a new class of dual PPARalpha/gamma agonists.
Published in: J Med Chem

Ligand: LY-465608 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.8 pIC50
Reference (Journal): Design and synthesis of alpha-aryloxy-alpha-methylhydrocinnamic acids: a novel class of dual peroxisome proliferator-activated receptor alpha/gamma agonists.
Published in: J Med Chem

Ligand: LY-510929 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.55 pIC50
Reference (Journal): Design and synthesis of alpha-aryloxy-alpha-methylhydrocinnamic acids: a novel class of dual peroxisome proliferator-activated receptor alpha/gamma agonists.
Published in: J Med Chem

Ligand: LY-518674 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.6 pIC50
Reference (Journal): Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
Published in: J Med Chem

Ligand: MK-0767 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): A novel insulin sensitizer acts as a coligand for peroxisome proliferator-activated receptor-alpha (PPAR-alpha) and PPAR-gamma: effect of PPAR-alpha activation on abnormal lipid metabolism in liver of Zucker fatty rats.
Published in: Diabetes

Ligand: MK-0767 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Evidence for direct binding of fatty acids and eicosanoids to human peroxisome proliferators-activated receptor alpha.
Published in: Biochem Biophys Res Commun

Ligand: MK-0767 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): MK-0767, a novel dual PPARalpha/gamma agonist, displays robust antihyperglycemic and hypolipidemic activities.
Published in: Biochem Biophys Res Commun

Ligand: MK-886 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6 pIC50
Reference (Journal): Peroxisomal bifunctional enzyme binds and activates the activation function-1 region of the peroxisome proliferator-activated receptor alpha.
Published in: Biochem J

Ligand: N-oleoylethanolamide (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.92 pIC50
Reference (Journal): Oleylethanolamide regulates feeding and body weight through activation of the nuclear receptor PPAR-alpha.
Published in: Nature

Ligand: N-oleoylethanolamide (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.92 pIC50
Reference (Journal): Oleoylethanolamide, an endogenous PPAR-alpha agonist, lowers body weight and hyperlipidemia in obese rats.
Published in: Neuropharmacology