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|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,677 | MK-0767 | Synthetic organic | 6,320 | Agonist | Agonist | false | 135,650,612 | null | null | pKd | 10,252 | Journal | Biochem Biophys Res Commun | Evidence for direct binding of fatty acids and eicosanoids to human peroxisome proliferators-activated receptor alpha. | 10,403,814 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,677 | MK-0767 | Synthetic organic | 6,320 | Agonist | Agonist | false | 135,650,612 | null | null | pKd | 10,207 | Journal | Biochem Biophys Res Commun | MK-0767, a novel dual PPARalpha/gamma agonist, displays robust antihyperglycemic and hypolipidemic activities. | 15,120,604 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,655 | MK-886 | Synthetic organic | 6,298 | Antagonist | Antagonist | false | 135,650,618 | null | 6 | pIC50 | 10,230 | Journal | Biochem J | Peroxisomal bifunctional enzyme binds and activates the activation function-1 region of the peroxisome proliferator-activated receptor alpha. | 11,139,388 | null | PMC1221566 |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,661 | N-oleoylethanolamide | Metabolite | 6,304 | Agonist | Agonist | false | 135,651,533 | null | 6.92 | pIC50 | 10,215 | Journal | Nature | Oleylethanolamide regulates feeding and body weight through activation of the nuclear receptor PPAR-alpha. | 12,955,147 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,661 | N-oleoylethanolamide | Metabolite | 6,304 | Agonist | Agonist | false | 135,651,533 | null | 6.92 | pIC50 | 10,216 | Journal | Neuropharmacology | Oleoylethanolamide, an endogenous PPAR-alpha agonist, lowers body weight and hyperlipidemia in obese rats. | 15,910,890 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,692 | 15-deoxy-Δ-12,14-prostaglandin J2 | Metabolite | 6,333 | Agonist | Full agonist | false | 135,651,375 | null | 6.3 | pIC50 | 10,395 | Journal | Biochem Biophys Res Commun | Covalent binding of 15-deoxy-delta12,14-prostaglandin J2 to PPARgamma. | 16,198,309 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,666 | pirinixic acid | Synthetic organic | 6,309 | Agonist | Agonist | false | 135,650,834 | false | 5.3 | pEC50 | 10,265 | Journal | J Med Chem | The PPARs: from orphan receptors to drug discovery. | 10,691,680 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,676 | pristanic acid | Metabolite | 6,319 | Agonist | Agonist | false | 135,651,550 | null | 4.4 | pEC50 | 10,278 | Journal | J Lipid Res | Pristanic acid and phytanic acid: naturally occurring ligands for the nuclear receptor peroxisome proliferator-activated receptor alpha. | 11,060,349 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,681 | pterostilbene | Synthetic organic | 6,400 | Agonist | Agonist | false | 135,650,865 | null | null | - | null | null | null | null | null | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 10,751 | (R)-16 [PMID: 32267688] | Synthetic organic | 87,214 | Agonist | Agonist | false | 405,560,192 | false | 6.37 | pEC50 | 39,109 | Journal | J Med Chem | A Selective Modulator of Peroxisome Proliferator-Activated Receptor γ with an Unprecedented Binding Mode. | 32,267,688 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,664 | ragaglitazar | Synthetic organic | 6,307 | Agonist | Agonist | false | 135,650,882 | null | 6 | pIC50 | 10,210 | Journal | J Med Chem | Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor alpha/gamma agonist ragaglitazar. | 12,672,231 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,670 | reglitazar | Synthetic organic | 6,313 | Agonist | Agonist | false | 135,650,893 | null | 5.72 | pEC50 | 10,259 | Journal | Eur J Pharmacol | Pharmacological profiles of a novel oral antidiabetic agent, JTT-501, an isoxazolidinedione derivative. | 9,932,726 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 11,137 | seladelpar | Synthetic organic | 87,365 | Agonist | Agonist | false | 434,122,197 | false | 6 | pEC50 | 39,966 | Journal | Bioorg Med Chem Lett | Discovery of para-alkylthiophenoxyacetic acids as a novel series of potent and selective PPARdelta agonists. | 17,524,639 | null |
||
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,665 | TZD18 | Synthetic organic | 6,308 | Agonist | Agonist | false | 135,651,287 | null | 7.6 | pIC50 | 10,222 | Journal | Endocrinology | A novel peroxisome proliferator-activated receptor alpha/gamma dual agonist demonstrates favorable effects on lipid homeostasis. | 14,701,675 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 594 | Peroxisome proliferator-activated receptor-β/δ | 11,130 | compound 25 [PMID: 32687365] | Synthetic organic | 87,352 | Agonist | Agonist | false | 434,122,190 | false | 5.82 | pEC50 | 39,936 | Journal | J Med Chem | Design and Structural Optimization of Dual FXR/PPARδ Activators. | 32,687,365 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,674 | GW7647 | Synthetic organic | 6,317 | Agonist | Agonist | false | 135,650,339 | false | 8.2 | pEC50 | 10,200 | Journal | Diabetes | A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-gamma reverses the diabetic phenotype of the Zucker diabetic fatty rat. | 10,389,847 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,672 | farglitazar | Synthetic organic | 6,315 | Agonist | Agonist | false | 135,650,251 | null | 6.35 | pEC50 | 10,225 | Journal | Pharmacology | Novel PPARgamma agonists GI 262570, GW 7845, GW 1929, and pioglitazone decrease calcium channel function and myogenic tone in rat mesenteric arteries. | 15,452,359 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 7,186 | fenofibrate | Synthetic organic | 79,393 | Agonist | Agonist | true | FDA (1993), EMA (2011) | 178,103,761 | true | 4.52 | pEC50 | 10,224 | Journal | J Med Chem | Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes. | 15,293,980 | null | null |
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 3,439 | gemfibrozil | Synthetic organic | 79,511 | Agonist | Agonist | true | FDA (1993) | 178,100,439 | true | 4.23 | pEC50 | 24,325 | Journal | Eur J Med Chem | Discovery of gemfibrozil analogues that activate PPARα and enhance the expression of gene CPT1A involved in fatty acids catabolism. | 21,889,235 | null | null |
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,680 | GW2331 | Synthetic organic | 6,323 | Agonist | Agonist | false | 135,650,331 | null | 6.8 | pKd | 10,237 | Journal | Nature | Convergence of 9-cis retinoic acid and peroxisome proliferator signalling pathways through heterodimer formation of their receptors. | 1,324,435 | null | PMC6159883 |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,656 | GW409544 | Synthetic organic | 6,299 | Agonist | Agonist | false | 135,650,335 | null | 8.7 | pIC50 | 10,224 | Journal | J Med Chem | Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes. | 15,293,980 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,656 | GW409544 | Synthetic organic | 6,299 | Agonist | Agonist | false | 135,650,335 | null | 8.7 | pIC50 | 10,267 | Journal | Proc Natl Acad Sci USA | Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors. | 11,698,662 | null | PMC61142 |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 3,440 | GW6471 | Synthetic organic | 7,986 | Antagonist | Antagonist | false | 178,100,440 | null | 6.6 | pIC50 | 14,213 | Journal | Nature | Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARalpha. | 11,845,213 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,674 | GW7647 | Synthetic organic | 6,317 | Agonist | Agonist | false | 135,650,339 | false | 8.2 | pEC50 | 10,202 | Journal | Bioorg Med Chem Lett | Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis. | 11,354,382 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,701 | AD5075 | Synthetic organic | 6,347 | Agonist | Full agonist | false | 135,649,896 | null | 7.66 | pKi | 10,282 | Journal | J Biol Chem | Novel peroxisome proliferator-activated receptor (PPAR) gamma and PPARdelta ligands produce distinct biological effects. | 10,037,770 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,701 | AD5075 | Synthetic organic | 6,347 | Agonist | Full agonist | false | 135,649,896 | null | 7.66 | pKi | 10,316 | Journal | Mol Endocrinol | Distinct properties and advantages of a novel peroxisome proliferator-activated protein [gamma] selective modulator. | 12,554,792 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,663 | AD-5061 | Synthetic organic | 6,340 | Agonist | Full agonist | false | 135,649,895 | null | 7.7 | pIC50 | 10,256 | Journal | Biochem Biophys Res Commun | Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone. | 11,095,972 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,663 | AD-5061 | Synthetic organic | 6,340 | Agonist | Full agonist | false | 135,649,895 | null | 7.7 | pIC50 | 10,257 | Journal | Eur J Pharmacol | A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes. | 15,219,816 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,692 | 15-deoxy-Δ-12,14-prostaglandin J2 | Metabolite | 6,333 | Agonist | Full agonist | false | 135,651,375 | null | 6.3 | pIC50 | 10,373 | Journal | Cell Signal | Natural ligands of PPARgamma: are prostaglandin J(2) derivatives really playing the part? | 11,955,950 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,692 | 15-deoxy-Δ-12,14-prostaglandin J2 | Metabolite | 6,333 | Agonist | Full agonist | false | 135,651,375 | null | 6.3 | pIC50 | 10,351 | Journal | Cell | A prostaglandin J2 metabolite binds peroxisome proliferator-activated receptor gamma and promotes adipocyte differentiation. | 8,521,498 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,668 | bezafibrate | Synthetic organic | 6,311 | Agonist | Agonist | true | 135,649,989 | true | 4.3 | pEC50 | 10,224 | Journal | J Med Chem | Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes. | 15,293,980 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,668 | bezafibrate | Synthetic organic | 6,311 | Agonist | Agonist | true | 135,649,989 | true | 4.3 | pEC50 | 10,226 | Journal | Biochem Biophys Res Commun | Fibrate and statin synergistically increase the transcriptional activities of PPARalpha/RXRalpha and decrease the transactivation of NFkappaB. | 11,779,144 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 7,821 | AZD4619 | Synthetic organic | 80,646 | Agonist | Agonist | false | 223,366,152 | true | 7.1 | pEC50 | 26,013 | Webpage | null | PPARα receptor agonist. | null | null |
||
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,663 | AD-5061 | Synthetic organic | 6,306 | Agonist | Agonist | false | 135,649,895 | null | 5.6 | pIC50 | 10,256 | Journal | Biochem Biophys Res Commun | Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone. | 11,095,972 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,663 | AD-5061 | Synthetic organic | 6,306 | Agonist | Agonist | false | 135,649,895 | null | 5.6 | pIC50 | 10,257 | Journal | Eur J Pharmacol | A novel oxyiminoalkanoic acid derivative, TAK-559, activates human peroxisome proliferator-activated receptor subtypes. | 15,219,816 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,679 | 8S-HETE | Metabolite | 6,322 | Agonist | Agonist | false | 135,651,417 | null | 7 | pKd | 10,272 | Journal | J Biol Chem | Differential activation of peroxisome proliferator-activated receptors by eicosanoids. | 7,592,593 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 593 | Peroxisome proliferator-activated receptor-α | 2,679 | 8S-HETE | Metabolite | 6,322 | Agonist | Agonist | false | 135,651,417 | null | 7 | pKd | 10,213 | Journal | Proc Natl Acad Sci USA | Hypolipidemic drugs, polyunsaturated fatty acids, and eicosanoids are ligands for peroxisome proliferator-activated receptors alpha and delta. | 9,113,986 | null | PMC20719 |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,708 | BADGE | Synthetic organic | 8,006 | Antagonist | Antagonist | null | null | 135,649,978 | null | 4 | pKi | 10,403 | Journal | J Biol Chem | A synthetic antagonist for the peroxisome proliferator-activated receptor gamma inhibits adipocyte differentiation. | 10,636,887 | null | null |
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,708 | BADGE | Synthetic organic | 6,361 | Agonist | Full agonist | null | null | 135,649,978 | null | 4 | pKd | 10,403 | Journal | J Biol Chem | A synthetic antagonist for the peroxisome proliferator-activated receptor gamma inhibits adipocyte differentiation. | 10,636,887 | null | null |
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,708 | BADGE | Synthetic organic | 6,361 | Agonist | Full agonist | null | null | 135,649,978 | null | 4 | pKd | 10,317 | Journal | Br J Pharmacol | Bisphenol A diglycidyl ether (BADGE) is a PPARgamma agonist in an ECV304 cell line. | 11,030,710 | null | PMC1572386 |
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,717 | bardoxolone | Synthetic organic | 6,350 | Agonist | Partial agonist | false | 135,650,061 | false | 8 | pKi | 10,401 | Journal | Mol Endocrinol | 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. | 11,043,571 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,807 | bexarotene | Synthetic organic | 83,093 | Antagonist | Antagonist | true | FDA (1999), EMA (2001) | 135,650,520 | false | 5.52 | pIC50 | 30,138 | Journal | PPAR Res | Identification of Bexarotene as a PPARγ Antagonist with HDX. | 26,451,138 | null | PMC4586960 |
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 3,443 | CDDO-Me | Synthetic organic | 8,004 | Antagonist | Antagonist | false | 178,100,443 | null | 6.9 | pKi | 10,401 | Journal | Mol Endocrinol | 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. | 11,043,571 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 12,287 | chiglitazar | Synthetic organic | 89,029 | Agonist | Agonist | true | China (2022) | 473,153,875 | false | 7.1 | pEC50 | 44,439 | Journal | Br J Pharmacol | The PPARalpha/gamma dual agonist chiglitazar improves insulin resistance and dyslipidemia in MSG obese rats. | 16,751,799 | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,711 | ciglitazone | Synthetic organic | 6,368 | Agonist | Full agonist | false | 135,650,096 | null | 4.6 | pEC50 | 10,223 | Journal | J Med Chem | N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents. | 9,836,620 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 11,974 | compound 10 [O'Mahony <i>et al</i>., 2022] | Synthetic organic | 88,651 | None | Binding | false | 464,244,115 | false | 7.62 | pIC50 | 43,581 | Journal | ACS Medicinal Chemistry Letters | Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation | null | 10.1021/acsmedchemlett.1c00715 | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,715 | COOH | Synthetic organic | 6,376 | Agonist | Full agonist | false | 53,801,056 | null | null | - | 10,357 | Journal | Diabetes | 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. | 12,540,599 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,715 | COOH | Synthetic organic | 6,376 | Agonist | Full agonist | false | 53,801,056 | null | null | - | 10,319 | Journal | Am J Physiol Endocrinol Metab | Treatment of type 2 diabetic db/db mice with a novel PPARgamma agonist improves cardiac metabolism but not contractile function. | 14,600,074 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,714 | diclofenac | Synthetic organic | 8,005 | Antagonist | Antagonist | true | FDA (1988) | 135,650,177 | null | 6.2 | pKi | 14,216 | Journal | Mol Pharmacol | Diclofenac antagonizes peroxisome proliferator-activated receptor-gamma signaling. | 11,752,200 | null | null |
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,714 | diclofenac | Synthetic organic | 6,375 | Agonist | Partial agonist | true | FDA (1988) | 135,650,177 | null | null | - | 10,354 | Journal | J Pharmacol Sci | 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). | 14,646,253 | null | null |
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,671 | DRF 2519 | Synthetic organic | 6,372 | Agonist | Full agonist | false | 135,650,210 | null | null | - | 10,204 | Journal | Eur J Pharmacol | Antidiabetic and hypolipidemic potential of DRF 2519--a dual activator of PPAR-alpha and PPAR-gamma. | 15,140,637 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 8,907 | edaglitazone | Synthetic organic | 83,091 | Agonist | Agonist | false | 310,264,688 | true | 7.45 | pEC50 | 30,109 | Journal | ChemMedChem | Comparative molecular profiling of the PPARα/γ activator aleglitazar: PPAR selectivity, activity and interaction with cofactors. | 22,489,042 | null | PMC3504387 |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 11,135 | elafibranor | Synthetic organic | 87,362 | Agonist | Agonist | true | FDA (2024) | 434,122,195 | false | 7.33 | pEC50 | 39,959 | Journal | Expert Opin Pharmacother | New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease. | 24,428,677 | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,672 | farglitazar | Synthetic organic | 6,362 | Agonist | Partial agonist | false | 135,650,251 | null | 7.47 | pKd | 10,407 | Journal | Eur J Biochem | Binding analyses between Human PPARgamma-LBD and ligands. | 14,717,706 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,672 | farglitazar | Synthetic organic | 6,362 | Agonist | Partial agonist | false | 135,650,251 | null | 7.47 | pKd | 10,223 | Journal | J Med Chem | N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents. | 9,836,620 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,705 | FMOC-L-Leucine | Synthetic organic | 6,356 | Agonist | Partial agonist | false | 135,650,280 | null | 6 | pKi | 10,385 | Journal | Mol Cell | A unique PPARgamma ligand with potent insulin-sensitizing yet weak adipogenic activity. | 11,684,010 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,695 | GW0072 | Synthetic organic | 6,338 | Agonist | Partial agonist | false | 135,651,255 | null | 7 | pIC50 | 10,374 | Journal | Proc Natl Acad Sci USA | A peroxisome proliferator-activated receptor gamma ligand inhibits adipocyte differentiation. | 10,339,548 | null | PMC26842 |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,703 | GW1929 | Synthetic organic | 6,351 | Agonist | Full agonist | false | 135,650,330 | false | 8.8 | pKi | 10,200 | Journal | Diabetes | A novel N-aryl tyrosine activator of peroxisome proliferator-activated receptor-gamma reverses the diabetic phenotype of the Zucker diabetic fatty rat. | 10,389,847 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,680 | GW2331 | Synthetic organic | 6,360 | Agonist | Full agonist | false | 135,650,331 | null | 6.52 | pKd | 10,238 | Journal | Proc Natl Acad Sci USA | Fatty acids and eicosanoids regulate gene expression through direct interactions with peroxisome proliferator-activated receptors alpha and gamma. | 9,113,987 | null | PMC20720 |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,656 | GW409544 | Synthetic organic | 6,369 | Agonist | Full agonist | false | 135,650,335 | null | 9.55 | pEC50 | 10,224 | Journal | J Med Chem | Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes. | 15,293,980 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,656 | GW409544 | Synthetic organic | 6,369 | Agonist | Full agonist | false | 135,650,335 | null | 9.55 | pEC50 | 10,267 | Journal | Proc Natl Acad Sci USA | Structural determinants of ligand binding selectivity between the peroxisome proliferator-activated receptors. | 11,698,662 | null | PMC61142 |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,704 | GW7845 | Synthetic organic | 6,352 | Agonist | Full agonist | false | 135,650,340 | null | 8.43 | pKi | 10,325 | Journal | J Med Chem | N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 3. Structure-activity relationship and optimization of the N-aryl substituent. | 9,836,622 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,704 | GW7845 | Synthetic organic | 6,352 | Agonist | Full agonist | false | 135,650,340 | null | 8.43 | pKi | 10,223 | Journal | J Med Chem | N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents. | 9,836,620 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,673 | GW9578 | Synthetic organic | 6,370 | Agonist | Full agonist | false | 135,650,342 | null | 6 | pEC50 | 10,202 | Journal | Bioorg Med Chem Lett | Identification of a subtype selective human PPARalpha agonist through parallel-array synthesis. | 11,354,382 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 3,442 | GW9662 | Synthetic organic | 8,003 | Antagonist | Irreversible inhibition | false | 178,100,442 | null | 8.1 | pIC50 | 10,360 | Journal | Biochemistry | Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662. | 12,022,867 | null | null |
|
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,713 | ibuprofen | Synthetic organic | 6,374 | Agonist | Full agonist | true | FDA (1974), EMA (2004) | 135,650,365 | null | null | - | 10,348 | Journal | Biochem Pharmacol | Activation of peroxisome proliferator-activated receptor isoforms and inhibition of prostaglandin H(2) synthases by ibuprofen, naproxen, and indomethacin. | 11,755,111 | null | null |
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 2,713 | ibuprofen | Synthetic organic | 6,374 | Agonist | Full agonist | true | FDA (1974), EMA (2004) | 135,650,365 | null | null | - | 10,354 | Journal | J Pharmacol Sci | 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). | 14,646,253 | null | null |
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 1,909 | indomethacin | Synthetic organic | 6,364 | Agonist | Partial agonist | true | FDA (1965) | 135,650,390 | null | 7.38 | pKd | 10,362 | Journal | J Biol Chem | Peroxisome proliferator-activated receptors alpha and gamma are activated by indomethacin and other non-steroidal anti-inflammatory drugs. | 9,013,583 | null | null |
86 | nhr | 1C. Peroxisome proliferator-activated receptors | 595 | Peroxisome proliferator-activated receptor-γ | 1,909 | indomethacin | Synthetic organic | 6,364 | Agonist | Partial agonist | true | FDA (1965) | 135,650,390 | null | 7.38 | pKd | 10,333 | Journal | Eur J Pharmacol | Binding of prostaglandins to human PPARgamma: tool assessment and new natural ligands. | 11,301,062 | null | null |
87 | nhr | 1D. Rev-Erb receptors | 596 | Rev-Erb-α | 2,903 | GSK4112 | Synthetic organic | 6,625 | Agonist | Agonist | false | 135,650,323 | false | 5.64 | pIC50 | 13,216 | Journal | ACS Chem Biol | Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. | 21,043,485 | null | PMC3042041 |
|
87 | nhr | 1D. Rev-Erb receptors | 596 | Rev-Erb-α | 2,903 | GSK4112 | Synthetic organic | 78,631 | Agonist | Agonist | false | 135,650,323 | false | 6.4 | pEC50 | 15,345 | Journal | ACS Chem Biol | GSK4112, a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα. | 20,677,822 | null | null |
|
87 | nhr | 1D. Rev-Erb receptors | 596 | Rev-Erb-α | 4,349 | heme | Metabolite | 9,463 | Agonist | Agonist | false | 178,101,166 | null | null | - | 16,147 | Journal | Science | Rev-erbalpha, a heme sensor that coordinates metabolic and circadian pathways. | 18,006,707 | null | null |
|
87 | nhr | 1D. Rev-Erb receptors | 596 | Rev-Erb-α | 4,349 | heme | Metabolite | 9,463 | Agonist | Agonist | false | 178,101,166 | null | null | - | 16,146 | Journal | Nat Struct Mol Biol | Identification of heme as the ligand for the orphan nuclear receptors REV-ERBalpha and REV-ERBbeta. | 18,037,887 | null | PMC2743565 |
|
87 | nhr | 1D. Rev-Erb receptors | 596 | Rev-Erb-α | 2,904 | SR8278 | Synthetic organic | 6,624 | Antagonist | Antagonist | false | 135,651,083 | false | 6.3 | pEC50 | 13,216 | Journal | ACS Chem Biol | Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. | 21,043,485 | null | PMC3042041 |
|
87 | nhr | 1D. Rev-Erb receptors | 596 | Rev-Erb-α | 2,904 | SR8278 | Synthetic organic | 6,623 | Antagonist | Antagonist | false | 135,651,083 | false | 6.5 | pIC50 | 13,216 | Journal | ACS Chem Biol | Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB. | 21,043,485 | null | PMC3042041 |
|
87 | nhr | 1D. Rev-Erb receptors | 596 | Rev-Erb-α | 8,901 | SR9009 | Synthetic organic | 83,072 | Agonist | Agonist | false | 310,264,682 | false | 6.17 | pIC50 | 30,128 | Journal | Nature | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. | 22,460,951 | null | PMC3343186 |
|
87 | nhr | 1D. Rev-Erb receptors | 596 | Rev-Erb-α | 8,900 | SR9011 | Synthetic organic | 83,073 | Agonist | Agonist | false | 310,264,681 | false | 6.1 | pIC50 | 30,128 | Journal | Nature | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. | 22,460,951 | null | PMC3343186 |
|
87 | nhr | 1D. Rev-Erb receptors | 597 | Rev-Erb-β | 8,902 | cobalt protoporphyrin IX | Synthetic organic | 83,076 | Antagonist | Antagonist | false | 310,264,683 | false | 5.59 | pKd | 30,097 | Journal | J Biol Chem | Structure of REV-ERBβ ligand-binding domain bound to a porphyrin antagonist. | 24,872,411 | null | PMC4106322 |
|
87 | nhr | 1D. Rev-Erb receptors | 597 | Rev-Erb-β | 4,349 | heme | Metabolite | 9,464 | Agonist | Agonist | false | 178,101,166 | false | 6.45 | pKd | 30,097 | Journal | J Biol Chem | Structure of REV-ERBβ ligand-binding domain bound to a porphyrin antagonist. | 24,872,411 | null | PMC4106322 |
|
87 | nhr | 1D. Rev-Erb receptors | 597 | Rev-Erb-β | 4,349 | heme | Metabolite | 9,464 | Agonist | Agonist | false | 178,101,166 | false | 6.45 | pKd | 16,147 | Journal | Science | Rev-erbalpha, a heme sensor that coordinates metabolic and circadian pathways. | 18,006,707 | null | null |
|
87 | nhr | 1D. Rev-Erb receptors | 597 | Rev-Erb-β | 4,349 | heme | Metabolite | 9,464 | Agonist | Agonist | false | 178,101,166 | false | 6.45 | pKd | 16,146 | Journal | Nat Struct Mol Biol | Identification of heme as the ligand for the orphan nuclear receptors REV-ERBalpha and REV-ERBbeta. | 18,037,887 | null | PMC2743565 |
|
87 | nhr | 1D. Rev-Erb receptors | 597 | Rev-Erb-β | 8,901 | SR9009 | Synthetic organic | 83,074 | Agonist | Agonist | false | 310,264,682 | false | 6.1 | pIC50 | 30,128 | Journal | Nature | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. | 22,460,951 | null | PMC3343186 |
|
87 | nhr | 1D. Rev-Erb receptors | 597 | Rev-Erb-β | 8,900 | SR9011 | Synthetic organic | 83,075 | Agonist | Agonist | false | 310,264,681 | false | 6.25 | pIC50 | 30,128 | Journal | Nature | Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists. | 22,460,951 | null | PMC3343186 |
|
87 | nhr | 1D. Rev-Erb receptors | 597 | Rev-Erb-β | 8,903 | zinc protoporphyrin IX | Synthetic organic | 83,077 | Antagonist | Antagonist | false | 310,264,684 | false | null | - | 30,097 | Journal | J Biol Chem | Structure of REV-ERBβ ligand-binding domain bound to a porphyrin antagonist. | 24,872,411 | null | PMC4106322 |
|
88 | nhr | 1F. Retinoic acid-related orphans | 598 | RAR-related orphan receptor-α | 3,432 | 7-hydroxycholesterol | Metabolite | 7,552 | Agonist | Agonist | false | 178,100,434 | null | null | - | 10,464 | Journal | Anal Biochem | Identification of natural ligands of retinoic acid receptor-related orphan receptor alpha ligand-binding domain expressed in Sf9 cells--a mass spectrometry approach. | 14,622,968 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 598 | RAR-related orphan receptor-α | 8,906 | CD2314 | Synthetic organic | 83,089 | Agonist | Agonist | false | 310,264,687 | false | 5.42 | pKd | 30,106 | Journal | Cancer Res | Mechanism of regulation and suppression of melanoma invasiveness by novel retinoic acid receptor-gamma target gene carbohydrate sulfotransferase 10. | 19,470,764 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 598 | RAR-related orphan receptor-α | 2,718 | cholesterol | Metabolite | 6,398 | Agonist | Agonist | false | 135,651,457 | null | null | - | 10,463 | Journal | Structure | X-ray structure of the hRORalpha LBD at 1.63 A: structural and functional data that cholesterol or a cholesterol derivative is the natural ligand of RORalpha. | 12,467,577 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 598 | RAR-related orphan receptor-α | 2,718 | cholesterol | Metabolite | 6,398 | Agonist | Agonist | false | 135,651,457 | null | null | - | 10,462 | Journal | Biochem Biophys Res Commun | The metastasis suppressor candidate nucleotide diphosphate kinase NM23 specifically interacts with members of the ROR/RZR nuclear orphan receptor subfamily. | 8,858,107 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 598 | RAR-related orphan receptor-α | 2,738 | cholesterol sulphate | Metabolite | 6,399 | Agonist | Agonist | false | 135,651,458 | null | null | - | 10,464 | Journal | Anal Biochem | Identification of natural ligands of retinoic acid receptor-related orphan receptor alpha ligand-binding domain expressed in Sf9 cells--a mass spectrometry approach. | 14,622,968 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 598 | RAR-related orphan receptor-α | 2,738 | cholesterol sulphate | Metabolite | 6,399 | Agonist | Agonist | false | 135,651,458 | null | null | - | 10,463 | Journal | Structure | X-ray structure of the hRORalpha LBD at 1.63 A: structural and functional data that cholesterol or a cholesterol derivative is the natural ligand of RORalpha. | 12,467,577 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 598 | RAR-related orphan receptor-α | 10,143 | SR1001 | Synthetic organic | 85,727 | Agonist | Inverse agonist | false | 381,118,853 | true | 6.76 | pKi | 29,073 | Journal | Nature | Suppression of TH17 differentiation and autoimmunity by a synthetic ROR ligand. | 21,499,262 | null | PMC3148894 |
|
88 | nhr | 1F. Retinoic acid-related orphans | 598 | RAR-related orphan receptor-α | 2,755 | T0901317 | Synthetic organic | 87,028 | Agonist | Inverse agonist | false | 135,651,223 | false | 6.88 | pKi | 29,072 | Journal | Mol Pharmacol | The benzenesulfoamide T0901317 [N-(2,2,2-trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide] is a novel retinoic acid receptor-related orphan receptor-alpha/gamma inverse agonist. | 19,887,649 | null | PMC2812071 |
|
88 | nhr | 1F. Retinoic acid-related orphans | 599 | RAR-related orphan receptor-β | 2,741 | all-trans-4-oxo-retinoic acid | Synthetic organic | 6,408 | Antagonist | Antagonist | false | 135,649,918 | null | 6.1 | pKi | 10,456 | Journal | Nat Struct Biol | All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta. | 12,958,591 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 599 | RAR-related orphan receptor-β | 2,741 | all-trans-4-oxo-retinoic acid | Synthetic organic | 6,407 | Antagonist | Antagonist | false | 135,649,918 | null | 9.3 | pIC50 | 10,456 | Journal | Nat Struct Biol | All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta. | 12,958,591 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 599 | RAR-related orphan receptor-β | 2,740 | ALRT 1550 | Synthetic organic | 6,404 | Antagonist | Antagonist | false | 135,649,927 | null | 6.8 | pKi | 10,456 | Journal | Nat Struct Biol | All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta. | 12,958,591 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 599 | RAR-related orphan receptor-β | 2,740 | ALRT 1550 | Synthetic organic | 6,403 | Antagonist | Antagonist | false | 135,649,927 | null | 10.4 | pIC50 | 10,456 | Journal | Nat Struct Biol | All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta. | 12,958,591 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 599 | RAR-related orphan receptor-β | 8,906 | CD2314 | Synthetic organic | 83,090 | Agonist | Agonist | false | 310,264,687 | true | 6.84 | pKd | 30,106 | Journal | Cancer Res | Mechanism of regulation and suppression of melanoma invasiveness by novel retinoic acid receptor-gamma target gene carbohydrate sulfotransferase 10. | 19,470,764 | null | null |
|
88 | nhr | 1F. Retinoic acid-related orphans | 599 | RAR-related orphan receptor-β | 2,644 | tretinoin | Metabolite | 6,406 | Antagonist | Antagonist | true | FDA (1995) | 135,651,435 | null | 6.55 | pKi | 10,456 | Journal | Nat Struct Biol | All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta. | 12,958,591 | null | null |
88 | nhr | 1F. Retinoic acid-related orphans | 599 | RAR-related orphan receptor-β | 2,644 | tretinoin | Metabolite | 7,553 | Agonist | Agonist | true | FDA (1995) | 135,651,435 | null | null | - | 10,456 | Journal | Nat Struct Biol | All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta. | 12,958,591 | null | null |
88 | nhr | 1F. Retinoic acid-related orphans | 599 | RAR-related orphan receptor-β | 2,644 | tretinoin | Metabolite | 6,405 | Antagonist | Antagonist | true | FDA (1995) | 135,651,435 | null | 9.82 | pIC50 | 10,456 | Journal | Nat Struct Biol | All-trans retinoic acid is a ligand for the orphan nuclear receptor ROR beta. | 12,958,591 | null | null |