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

Ligand: BADGE (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Median affinity: 4 pKi
Reference (Journal): A synthetic antagonist for the peroxisome proliferator-activated receptor gamma inhibits adipocyte differentiation.
Published in: J Biol Chem

Ligand: BADGE (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Median affinity: 4 pKd
Reference (Journal): A synthetic antagonist for the peroxisome proliferator-activated receptor gamma inhibits adipocyte differentiation.
Published in: J Biol Chem

Ligand: BADGE (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Median affinity: 4 pKd
Reference (Journal): Bisphenol A diglycidyl ether (BADGE) is a PPARgamma agonist in an ECV304 cell line.
Published in: Br J Pharmacol

Ligand: bardoxolone (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8 pKi
Reference (Journal): A synthetic triterpenoid, 2-cyano-3,12-dioxooleana-1,9-dien-28-oic acid (CDDO), is a ligand for the peroxisome proliferator-activated receptor gamma.
Published in: Mol Endocrinol

Ligand: bexarotene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2001)
Primary target: no
Median affinity: 5.519999980926514 pIC50
Reference (Journal): Identification of Bexarotene as a PPARγ Antagonist with HDX.
Published in: PPAR Res

Ligand: CDDO-Me (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.900000095367432 pKi
Reference (Journal): A synthetic triterpenoid, 2-cyano-3,12-dioxooleana-1,9-dien-28-oic acid (CDDO), is a ligand for the peroxisome proliferator-activated receptor gamma.
Published in: Mol Endocrinol

Ligand: chiglitazar (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: China (2022)
Primary target: no
Median affinity: 7.099999904632568 pEC50
Reference (Journal): The PPARalpha/gamma dual agonist chiglitazar improves insulin resistance and dyslipidemia in MSG obese rats.
Published in: Br J Pharmacol

Ligand: ciglitazone (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.599999904632568 pEC50
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: compound 10 [O'Mahony et al., 2022] (Synthetic organic)
Interaction type: None
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.619999885559082 pIC50
Reference (Journal): Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation
Published in: ACS Medicinal Chemistry Letters

Ligand: COOH (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): PPAR-gamma activation mediates adipose depot-specific effects on gene expression and lipoprotein lipase activity: mechanisms for modulation of postprandial lipemia and differential adipose accretion.
Published in: Diabetes

Ligand: COOH (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Treatment of type 2 diabetic db/db mice with a novel PPARgamma agonist improves cardiac metabolism but not contractile function.
Published in: Am J Physiol Endocrinol Metab

Ligand: diclofenac (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1988)
Median affinity: 6.2 pKi
Reference (Journal): Diclofenac antagonizes peroxisome proliferator-activated receptor-gamma signaling.
Published in: Mol Pharmacol

Ligand: diclofenac (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1988)
Median affinity:  -
Reference (Journal): Evaluation of human peroxisome proliferator-activated receptor (PPAR) subtype selectivity of a variety of anti-inflammatory drugs based on a novel assay for PPAR delta(beta).
Published in: J Pharmacol Sci

Ligand: DRF 2519 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
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: yes
Median affinity: 7.449999809265137 pEC50
Reference (Journal): Comparative molecular profiling of the PPARα/γ activator aleglitazar: PPAR selectivity, activity and interaction with cofactors.
Published in: ChemMedChem

Ligand: elafibranor (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2024)
Primary target: no
Median affinity: 7.329999923706055 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: Partial agonist
Ligand approved: no
Median affinity: 7.47 pKd
Reference (Journal): Binding analyses between Human PPARgamma-LBD and ligands.
Published in: Eur J Biochem

Ligand: farglitazar (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.47 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: FMOC-L-Leucine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): A unique PPARgamma ligand with potent insulin-sensitizing yet weak adipogenic activity.
Published in: Mol Cell

Ligand: GW0072 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7 pIC50
Reference (Journal): A peroxisome proliferator-activated receptor gamma ligand inhibits adipocyte differentiation.
Published in: Proc Natl Acad Sci USA

Ligand: GW1929 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
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: 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: GW409544 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.55 pEC50
Reference (Journal): Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
Published in: J Med Chem

Ligand: GW409544 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.55 pEC50
Reference (Journal): Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors.
Published in: Proc Natl Acad Sci USA

Ligand: GW7845 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.43 pKi
Reference (Journal): N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 3. Structure-activity relationship and optimization of the N-aryl substituent.
Published in: J Med Chem

Ligand: GW7845 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.43 pKi
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: GW9578 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6 pEC50
Reference (Journal): Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.
Published in: Bioorg Med Chem Lett

Ligand: GW9662 (Synthetic organic)
Interaction type: Antagonist
Action: Irreversible inhibition
Ligand approved: no
Median affinity: 8.1 pIC50
Reference (Journal): Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662.
Published in: Biochemistry

Ligand: ibuprofen (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1974), EMA (2004)
Median affinity:  -
Reference (Journal): Activation of peroxisome proliferator-activated receptor isoforms and inhibition of prostaglandin H(2) synthases by ibuprofen, naproxen, and indomethacin.
Published in: Biochem Pharmacol

Ligand: ibuprofen (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1974), EMA (2004)
Median affinity:  -
Reference (Journal): Evaluation of human peroxisome proliferator-activated receptor (PPAR) subtype selectivity of a variety of anti-inflammatory drugs based on a novel assay for PPAR delta(beta).
Published in: J Pharmacol Sci

Ligand: indomethacin (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1965)
Median affinity: 7.38 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: indomethacin (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1965)
Median affinity: 7.38 pKd
Reference (Journal): Binding of prostaglandins to human PPARgamma: tool assessment and new natural ligands.
Published in: Eur J Pharmacol