dwb2023/gtopdb-target-family-interaction-detail huggingface dataset:
Target family: 1.14.11.- Histone demethylases (type: enzyme)
Target: lysine demethylase 4C

Ligand: zavondemstat (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Patent): Histone demethylase inhibitors

Ligand: IOX1 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.21999979019165 pIC50
Reference (Journal): A cell-permeable ester derivative of the JmjC histone demethylase inhibitor IOX1.
Published in: ChemMedChem
Target family: 1.14.11.- Histone demethylases (type: enzyme)
Target: lysine demethylase 4A

Ligand: ML324 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6 pIC50
Reference (Journal): Discovery of ML324, a JMJD2 demethylase inhibitor with demonstrated antiviral activity
Published in: Probe Reports from the NIH Molecular Libraries Program

Ligand: KDM5 inhibitor N71 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.28000020980835 pIC50
Reference (Journal): Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A.
Published in: J Med Chem

Ligand: compound 6a [PMID: 18942826] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.150000095367432 pIC50
Reference (Journal): Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
Published in: J Med Chem
Target family: 1.14.13.9 Kynurenine 3-monooxygenase (type: enzyme)
Target: kynurenine 3-monooxygenase

Ligand: GSK065 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 10.300000190734863 pKi
Reference (Journal): Structural and mechanistic basis of differentiated inhibitors of the acute pancreatitis target kynurenine-3-monooxygenase.
Published in: Nat Commun

Ligand: GSK065 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pIC50
Reference (Journal): Structural and mechanistic basis of differentiated inhibitors of the acute pancreatitis target kynurenine-3-monooxygenase.
Published in: Nat Commun

Ligand: GSK180 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 8.199999809265137 pIC50
Reference (Journal): Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis.
Published in: Nat Med
Target family: 1.17.4.1 Ribonucleoside-diphosphate reductases (type: enzyme)
Target: ribonucleotide reductase catalytic subunit M1

Ligand: clofarabine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2004), EMA (2009)
Primary target: no
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Effects of 2-chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)adenine on K562 cellular metabolism and the inhibition of human ribonucleotide reductase and DNA polymerases by its 5'-triphosphate.
Published in: Cancer Res

Ligand: fludarabine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1991)
Primary target: yes
Median affinity: 6 pIC50
Reference (Journal): In vitro biological activity of 9-beta-D-arabinofuranosyl-2-fluoroadenine and the biochemical actions of its triphosphate on DNA polymerases and ribonucleotide reductase from HeLa cells.
Published in: Mol Pharmacol

Ligand: gemcitabine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity:  -
Reference (Journal): Inhibition of ribonucleotide reduction in CCRF-CEM cells by 2',2'-difluorodeoxycytidine.
Published in: Mol Pharmacol

Ligand: hydroxyurea (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1967), EMA (2007)
Primary target: yes
Median affinity: 3.8299999237060547 pIC50
Reference (Journal): Determination of the potency and subunit-selectivity of ribonucleotide reductase inhibitors with a recombinant-holoenzyme-based in vitro assay.
Published in: Biochem Pharmacol

Ligand: TAS1553 (Synthetic organic)
Interaction type: Inhibitor
Action: Binding
Ligand approved: no
Primary target: no
Median affinity: 7.460000038146973 pKd
Reference (Journal): TAS1553, a small molecule subunit interaction inhibitor of ribonucleotide reductase, exhibits antitumor activity by causing DNA replication stress.
Published in: Commun Biol
Target family: 1.17.4.1 Ribonucleoside-diphosphate reductases (type: enzyme)
Target: ribonucleotide reductase regulatory subunit M2

Ligand: clofarabine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (2004), EMA (2009)
Primary target: yes
Median affinity: 8.300000190734863 pIC50
Reference (Journal): Effects of 2-chloro-9-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)adenine on K562 cellular metabolism and the inhibition of human ribonucleotide reductase and DNA polymerases by its 5'-triphosphate.
Published in: Cancer Res

Ligand: fludarabine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1991)
Primary target: yes
Median affinity: 6 pIC50
Reference (Journal): In vitro biological activity of 9-beta-D-arabinofuranosyl-2-fluoroadenine and the biochemical actions of its triphosphate on DNA polymerases and ribonucleotide reductase from HeLa cells.
Published in: Mol Pharmacol

Ligand: gemcitabine (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity:  -
Reference (Journal): Inhibition of ribonucleotide reduction in CCRF-CEM cells by 2',2'-difluorodeoxycytidine.
Published in: Mol Pharmacol

Ligand: hydroxyurea (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1967), EMA (2007)
Primary target: yes
Median affinity: 3.8299999237060547 pIC50
Reference (Journal): Determination of the potency and subunit-selectivity of ribonucleotide reductase inhibitors with a recombinant-holoenzyme-based in vitro assay.
Published in: Biochem Pharmacol
Target family: 1.2.3.1 Aldehyde oxidase (type: enzyme)
Target: aldehyde oxidase 1

Ligand: raloxifene (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: yes
Approval source: FDA (1997), EMA (1998)
Primary target: no
Median affinity: 7.349999904632568 pIC50
Reference (Patent): Therapeutic agent for nonalcoholic fatty liver disease
Target family: 1.4.3.13 Lysyl oxidases (type: enzyme)
Target: lysyl oxidase

Ligand: CCT365623 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 6.050000190734863 pIC50
Reference (Journal): Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships.
Published in: J Med Chem

Ligand: compound 21b [PMID: 31430136] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.480000019073486 pIC50
Reference (Journal): 2-Aminomethylene-5-sulfonylthiazole Inhibitors of Lysyl Oxidase (LOX) and LOXL2 Show Significant Efficacy in Delaying Tumor Growth.
Published in: J Med Chem
Target family: 1.4.3.13 Lysyl oxidases (type: enzyme)
Target: lysyl oxidase like 2

Ligand: CCT365623 (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: no
Median affinity: 5.820000171661377 pIC50
Reference (Journal): Anti-metastatic Inhibitors of Lysyl Oxidase (LOX): Design and Structure-Activity Relationships.
Published in: J Med Chem

Ligand: compound 21b [PMID: 31430136] (Synthetic organic)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 6.820000171661377 pIC50
Reference (Journal): 2-Aminomethylene-5-sulfonylthiazole Inhibitors of Lysyl Oxidase (LOX) and LOXL2 Show Significant Efficacy in Delaying Tumor Growth.
Published in: J Med Chem

Ligand: simtuzumab (Antibody)
Interaction type: Inhibitor
Action: Inhibition
Ligand approved: no
Primary target: yes
Median affinity: 7.170000076293945 pKi
Reference (Patent): LOX and LOXL2 inhibitors and uses thereof.
Target family: 1A. Thyroid hormone receptors (type: nhr)
Target: Thyroid hormone receptor-&alpha;

Ligand: sobetirome (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.36 pKd
Reference (Journal): Binding of 3,5,3'-triiodothyronine (T3) and its analogs to the in vitro translational products of c-erbA protooncogenes: differences in the affinity of the alpha- and beta-forms for the acetic acid analog and failure of the human testis and kidney alpha-2 products to bind T3.
Published in: Mol Endocrinol

Ligand: rT3 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Binding of 3,5,3'-triiodothyronine (T3) and its analogs to the in vitro translational products of c-erbA protooncogenes: differences in the affinity of the alpha- and beta-forms for the acetic acid analog and failure of the human testis and kidney alpha-2 products to bind T3.
Published in: Mol Endocrinol

Ligand: resmetirom (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2024)
Primary target: no
Median affinity: 5.429999828338623 pEC50
Reference (Journal): Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dyslipidemia.
Published in: J Med Chem

Ligand: NH-3 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.62 pKd
Reference (Journal): Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.
Published in: J Med Chem

Ligand: KB-141 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.6 pIC50
Reference (Journal): Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.
Published in: J Med Chem

Ligand: dextrothyroxine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1967)
Primary target: yes
Median affinity:  -
Reference (Journal): Effects of dextrothyroxine on the pituitary-thyroid axis in hypercholesterolemic children and goitrous adults.
Published in: J Clin Endocrinol Metab
Target family: 1A. Thyroid hormone receptors (type: nhr)
Target: Thyroid hormone receptor-&alpha;

Ligand: VK2809 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.449999809265137 pKi
Reference (Journal): Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.
Published in: J Med Chem

Ligand: T4 (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2000)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): Binding of 3,5,3'-triiodothyronine (T3) and its analogs to the in vitro translational products of c-erbA protooncogenes: differences in the affinity of the alpha- and beta-forms for the acetic acid analog and failure of the human testis and kidney alpha-2 products to bind T3.
Published in: Mol Endocrinol

Ligand: tiratricol (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Binding of 3,5,3'-triiodothyronine (T3) and its analogs to the in vitro translational products of c-erbA protooncogenes: differences in the affinity of the alpha- and beta-forms for the acetic acid analog and failure of the human testis and kidney alpha-2 products to bind T3.
Published in: Mol Endocrinol

Ligand: triiodothyronine (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1956)
Primary target: yes
Median affinity: 10 pKd
Reference (Journal): Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.
Published in: J Med Chem
Target family: 1B. Retinoic acid receptors (type: nhr)
Target: Retinoic acid receptor-&gamma;

Ligand: BMS270394 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.3 pIC50
Reference (Journal): Structural basis for isotype selectivity of the human retinoic acid nuclear receptor.
Published in: J Mol Biol

Ligand: BMS270394 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.3 pIC50
Reference (Journal): Enantiomer discrimination illustrated by high-resolution crystal structures of the human nuclear receptor hRARgamma.
Published in: Proc Natl Acad Sci USA

Ligand: alitretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity: 9 pKd
Reference (Journal): Activation of retinoid X receptors induces apoptosis in HL-60 cell lines.
Published in: Mol Cell Biol

Ligand: alitretinoin (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1999), EMA (2000)
Primary target: yes
Median affinity: 9 pKd
Reference (Journal): Structural basis for isotype selectivity of the human retinoic acid nuclear receptor.
Published in: J Mol Biol

Ligand: AHPN (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.11 pKi
Reference (Journal): Synthesis, structure-affinity relationships, and biological activities of ligands binding to retinoic acid receptor subtypes.
Published in: J Med Chem

Ligand: AGN193109 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): Recruitment of nuclear receptor corepressor and coactivator to the retinoic acid receptor by retinoid ligands. Influence of DNA-heterodimer interactions.
Published in: J Biol Chem

Ligand: AGN193109 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): Identification and functional separation of retinoic acid receptor neutral antagonists and inverse agonists.
Published in: J Biol Chem

Ligand: AGN193109 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pIC50
Reference (Journal): Therapeutic applications for ligands of retinoid receptors.
Published in: Curr Pharm Des

Ligand: adapalene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1996)
Primary target: yes
Median affinity: 6.889999866485596 pKi
Reference (Journal): Synthesis, structure-affinity relationships, and biological activities of ligands binding to retinoic acid receptor subtypes.
Published in: J Med Chem
Target family: 1C. Peroxisome proliferator-activated receptors (type: nhr)
Target: Peroxisome proliferator-activated receptor-&alpha;

Ligand: NS-220 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.73 pEC50
Reference (Journal): A novel selective peroxisome proliferator-activated receptor alpha agonist, 2-methyl-c-5-[4-[5-methyl-2-(4-methylphenyl)-4-oxazolyl]butyl]-1,3-dioxane-r-2-carboxylic acid (NS-220), potently decreases plasma triglyceride and glucose levels and modifies lipoprotein profiles in KK-Ay mice.
Published in: J Pharmacol Exp Ther
Target family: 1C. Peroxisome proliferator-activated receptors (type: nhr)
Target: Peroxisome proliferator-activated receptor-&beta;/&delta;

Ligand: GSK0660 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pIC50
Reference (Journal): Identification and characterization of a selective peroxisome proliferator-activated receptor beta/delta (NR1C2) antagonist.
Published in: Mol Endocrinol
Target family: 1C. Peroxisome proliferator-activated receptors (type: nhr)
Target: Peroxisome proliferator-activated receptor-&gamma;

Ligand: 15-deoxy-Δ-12,14-prostaglandin J2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 pIC50
Reference (Journal): Development of a scintillation proximity assay for peroxisome proliferator-activated receptor gamma ligand binding domain.
Published in: Anal Biochem

Ligand: 15-deoxy-Δ-12,14-prostaglandin J2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 pIC50
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
Target family: 1C. Peroxisome proliferator-activated receptors (type: nhr)
Target: Peroxisome proliferator-activated receptor-&gamma;

Ligand: 15-deoxy-Δ-12,14-prostaglandin J2 (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.3 pIC50
Reference (Journal): Covalent binding of 15-deoxy-delta12,14-prostaglandin J2 to PPARgamma.
Published in: Biochem Biophys Res Commun
Target family: 1C. Peroxisome proliferator-activated receptors (type: nhr)
Target: Peroxisome proliferator-activated receptor-&alpha;

Ligand: pirinixic acid (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pEC50
Reference (Journal): The PPARs: from orphan receptors to drug discovery.
Published in: J Med Chem

Ligand: pristanic acid (Metabolite)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 4.4 pEC50
Reference (Journal): Pristanic acid and phytanic acid: naturally occurring ligands for the nuclear receptor peroxisome proliferator-activated receptor alpha.
Published in: J Lipid Res

Ligand: pterostilbene (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity:  -

Ligand: (R)-16 [PMID: 32267688] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.369999885559082 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: Agonist
Ligand approved: no
Median affinity: 6 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: Agonist
Ligand approved: no
Median affinity: 5.72 pEC50
Reference (Journal): Pharmacological profiles of a novel oral antidiabetic agent, JTT-501, an isoxazolidinedione derivative.
Published in: Eur J Pharmacol

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: TZD18 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.6 pIC50
Reference (Journal): A novel peroxisome proliferator-activated receptor alpha/gamma dual agonist demonstrates favorable effects on lipid homeostasis.
Published in: Endocrinology
Target family: 1C. Peroxisome proliferator-activated receptors (type: nhr)
Target: Peroxisome proliferator-activated receptor-&beta;/&delta;

Ligand: compound 25 [PMID: 32687365] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.820000171661377 pEC50
Reference (Journal): Design and Structural Optimization of Dual FXR/PPARδ Activators.
Published in: J Med Chem
Target family: 1C. Peroxisome proliferator-activated receptors (type: nhr)
Target: Peroxisome proliferator-activated receptor-&alpha;

Ligand: GW7647 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 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: farglitazar (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.35 pEC50
Reference (Journal): Novel PPARgamma agonists GI 262570, GW 7845, GW 1929, and pioglitazone decrease calcium channel function and myogenic tone in rat mesenteric arteries.
Published in: Pharmacology

Ligand: fenofibrate (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1993), EMA (2011)
Primary target: yes
Median affinity: 4.519999980926514 pEC50
Reference (Journal): Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
Published in: J Med Chem

Ligand: gemfibrozil (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1993)
Primary target: yes
Median affinity: 4.230000019073486 pEC50
Reference (Journal): Discovery of gemfibrozil analogues that activate PPARα and enhance the expression of gene CPT1A involved in fatty acids catabolism.
Published in: Eur J Med Chem

Ligand: GW2331 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 6.8 pKd
Reference (Journal): Convergence of 9-cis retinoic acid and peroxisome proliferator signalling pathways through heterodimer formation of their receptors.
Published in: Nature

Ligand: GW409544 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.7 pIC50
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: Agonist
Ligand approved: no
Median affinity: 8.7 pIC50
Reference (Journal): Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors.
Published in: Proc Natl Acad Sci USA

Ligand: GW6471 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.6 pIC50
Reference (Journal): Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha.
Published in: Nature

Ligand: GW7647 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pEC50
Reference (Journal): Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis.
Published in: Bioorg Med Chem Lett