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

Ligand: L-165461 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Novel peroxisome proliferator-activated receptor (PPAR) gamma and PPARdelta ligands produce distinct biological effects.
Published in: J Biol Chem

Ligand: L-764406 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.15 pIC50
Reference (Journal): L-764406 is a partial agonist of human peroxisome proliferator-activated receptor gamma. The role of Cys313 in ligand binding.
Published in: J Biol Chem

Ligand: L-783483 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.85 pKi
Reference (Journal): Novel peroxisome proliferator-activated receptor (PPAR) gamma and PPARdelta ligands produce distinct biological effects.
Published in: J Biol Chem

Ligand: L-796449 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): Novel peroxisome proliferator-activated receptor (PPAR) gamma and PPARdelta ligands produce distinct biological effects.
Published in: J Biol Chem

Ligand: lanifibranor (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.690000057220459 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: LG100754 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): The antidiabetic agent LG100754 sensitizes cells to low concentrations of peroxisome proliferator-activated receptor gamma ligands.
Published in: J Biol Chem

Ligand: LG100754 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): The rexinoid LG100754 is a novel RXR:PPARgamma agonist and decreases glucose levels in vivo.
Published in: Mol Endocrinol

Ligand: linoleic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.3 pKd
Reference (Journal): Binding of prostaglandins to human PPARgamma: tool assessment and new natural ligands.
Published in: Eur J Pharmacol

Ligand: linoleic acid (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.3 pKd
Reference (Journal): Binding analyses between Human PPARgamma-LBD and ligands.
Published in: Eur J Biochem

Ligand: LY-465608 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.26 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-510929 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 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: Full agonist
Ligand approved: no
Median affinity: 8 pIC50
Reference (Journal): Bombesin-like peptides in health and disease. Proceedings of an international symposium. October 13-16, 1987, Rome, Italy. A tribute to Vittorio Erspamer, M.D.
Published in: Ann NY Acad Sci

Ligand: MDG 548 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.670000076293945 pEC50
Reference (Journal): Integrated virtual screening for the identification of novel and selective peroxisome proliferator-activated receptor (PPAR) scaffolds.
Published in: J Med Chem

Ligand: mesalazine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1987)
Primary target: yes
Median affinity: 1.8200000524520874 pIC50
Reference (Journal): Intestinal antiinflammatory effect of 5-aminosalicylic acid is dependent on peroxisome proliferator-activated receptor-gamma.
Published in: J Exp Med

Ligand: MK-0767 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.49 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: Full agonist
Ligand approved: no
Median affinity: 6.49 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: Full agonist
Ligand approved: no
Median affinity: 7 pEC50
Reference (Journal): MK-0767, a novel dual PPARalpha/gamma agonist, displays robust antihyperglycemic and hypolipidemic activities.
Published in: Biochem Biophys Res Commun

Ligand: MRL20 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Benzoyl 2-methyl indoles as selective PPARgamma modulators.
Published in: Bioorg Med Chem Lett

Ligand: MRL24 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9 pIC50
Reference (Journal): Benzoyl 2-methyl indoles as selective PPARgamma modulators.
Published in: Bioorg Med Chem Lett

Ligand: netoglitazone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 pKd
Reference (Journal): A potent antidiabetic thiazolidinedione with unique peroxisome proliferator-activated receptor gamma-activating properties.
Published in: J Biol Chem

Ligand: nTzDpa (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): Distinct properties and advantages of a novel peroxisome proliferator-activated protein [gamma] selective modulator.
Published in: Mol Endocrinol

Ligand: PAT5A (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.35 pKd
Reference (Journal): PAT5A: a partial agonist of peroxisome proliferator-activated receptor gamma is a potent antidiabetic thiazolidinedione yet weakly adipogenic.
Published in: J Pharmacol Exp Ther

Ligand: PAT5A (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.35 pKd
Reference (Journal): Euglycemic and hypolipidemic activity of PAT5A: a unique thiazolidinedione with weak peroxisome proliferator activated receptor gamma activity.
Published in: Metab Clin Exp

Ligand: pioglitazone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity: 6.199999809265137 pIC50
Reference (Journal): Identification of high-affinity binding sites for the insulin sensitizer rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand for peroxisomal proliferator-activated receptor gamma.
Published in: J Pharmacol Exp Ther

Ligand: pioglitazone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity: 6.199999809265137 pIC50
Reference (Journal): Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone.
Published in: Biochem Biophys Res Commun

Ligand: pioglitazone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity: 6.199999809265137 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: (R)-16 [PMID: 32267688] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pEC50
Reference (Journal): A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode.
Published in: J Med Chem

Ligand: ragaglitazar (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.03 pIC50
Reference (Journal): Ragaglitazar: a novel PPAR alpha PPAR gamma agonist with potent lipid-lowering and insulin-sensitizing efficacy in animal models.
Published in: Br J Pharmacol

Ligand: ragaglitazar (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.03 pIC50
Reference (Journal): The dual PPARalpha/gamma agonist, ragaglitazar, improves insulin sensitivity and metabolic profile equally with pioglitazone in diabetic and dietary obese ZDF rats.
Published in: Br J Pharmacol

Ligand: ragaglitazar (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.03 pIC50
Reference (Journal): Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar.
Published in: J Med Chem

Ligand: reglitazar (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 pEC50
Reference (Journal): Pharmacological profiles of a novel oral antidiabetic agent, JTT-501, an isoxazolidinedione derivative.
Published in: Eur J Pharmacol

Ligand: resveratrol (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.849999904632568 pKd
Reference (Journal): Resveratrol and its metabolites bind to PPARs.
Published in: Chembiochem

Ligand: rosiglitazone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity: 7.400000095367432 pKd
Reference (Journal): Identification of high-affinity binding sites for the insulin sensitizer rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand for peroxisomal proliferator-activated receptor gamma.
Published in: J Pharmacol Exp Ther

Ligand: rosiglitazone (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity: 6.920000076293945 pKi
Reference (Journal): Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.
Published in: Bioorg Med Chem Lett

Ligand: rosiglitazone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity: 7.400000095367432 pKd
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: rosiglitazone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity: 7.400000095367432 pKd
Reference (Journal): Peroxisome proliferator-activated receptors alpha and gamma are activated by indomethacin and other non-steroidal anti-inflammatory drugs.
Published in: J Biol Chem

Ligand: SB-219993 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.5 pIC50
Reference (Journal): Identification of high-affinity binding sites for the insulin sensitizer rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand for peroxisomal proliferator-activated receptor gamma.
Published in: J Pharmacol Exp Ther

Ligand: SB-219994 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.68 pIC50
Reference (Journal): Identification of high-affinity binding sites for the insulin sensitizer rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand for peroxisomal proliferator-activated receptor gamma.
Published in: J Pharmacol Exp Ther

Ligand: seladelpar (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6 pEC50
Reference (Journal): Discovery of para-alkylthiophenoxyacetic acids as a novel series of potent and selective PPARdelta agonists.
Published in: Bioorg Med Chem Lett

Ligand: [125I]SB-236636 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.1 pKd
Reference (Journal): Identification of high-affinity binding sites for the insulin sensitizer rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand for peroxisomal proliferator-activated receptor gamma.
Published in: J Pharmacol Exp Ther

Ligand: [3H]AD5075 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.66 pKi
Reference (Journal): Thiazolidinediones produce a conformational change in peroxisomal proliferator-activated receptor-gamma: binding and activation correlate with antidiabetic actions in db/db mice.
Published in: Endocrinology

Ligand: [3H]GW2331 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.52 pKd
Reference (Journal): Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors alpha and gamma.
Published in: Proc Natl Acad Sci USA

Ligand: T0070907 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): T0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities.
Published in: J Biol Chem

Ligand: tagitinin A (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.260000228881836 pIC50
Reference (Journal): Sesquiterpene lactones from Tithonia diversifolia act as peroxisome proliferator-activated receptor agonists.
Published in: Bioorg Med Chem Lett

Ligand: tirotundin (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.570000171661377 pIC50
Reference (Journal): Sesquiterpene lactones from Tithonia diversifolia act as peroxisome proliferator-activated receptor agonists.
Published in: Bioorg Med Chem Lett

Ligand: triple modulator 10 [PMID: 29878767] (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 6.519999980926514 pEC50
Reference (Journal): Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology.
Published in: J Med Chem

Ligand: troglitazone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity: 6.300000190734863 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: troglitazone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity: 5.800000190734863 pKi
Reference (Journal): Thiazolidinediones produce a conformational change in peroxisomal proliferator-activated receptor-gamma: binding and activation correlate with antidiabetic actions in db/db mice.
Published in: Endocrinology

Ligand: troglitazone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1997)
Primary target: yes
Median affinity: 6.300000190734863 pIC50
Reference (Journal): Identification of high-affinity binding sites for the insulin sensitizer rosiglitazone (BRL-49653) in rodent and human adipocytes using a radioiodinated ligand for peroxisomal proliferator-activated receptor gamma.
Published in: J Pharmacol Exp Ther

Ligand: TZD18 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.24 pIC50
Reference (Journal): A novel peroxisome proliferator-activated receptor alpha/gamma dual agonist demonstrates favorable effects on lipid homeostasis.
Published in: Endocrinology

Ligand: VCE-004.3 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.460000038146973 pIC50
Reference (Journal): VCE-004.3, a cannabidiol aminoquinone derivative, prevents bleomycin-induced skin fibrosis and inflammation through PPARγ- and CB<sub>2</sub> receptor-dependent pathways.
Published in: Br J Pharmacol

Ligand: zafirlukast (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: no
Median affinity: 5.610000133514404 pEC50
Reference (Journal): Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology.
Published in: J Med Chem