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Target Report Card

Target Name and Classification

Target ID CHEMBL235
Target Type SINGLE PROTEIN
Preferred Name Peroxisome proliferator-activated receptor gamma
Synonyms NR1C3 | Nuclear receptor subfamily 1 group C member 3 | PPAR-gamma | PPARG | Peroxisome proliferator-activated receptor gamma
Organism Homo sapiens
Species Group No
Protein Target Classification
  • transcription factor > nuclear receptor > nuclear hormone receptor subfamily 1 > nuclear hormone receptor subfamily 1 group c > nuclear hormone receptor subfamily 1 group c member 3

Target Components

Component Description Relationship Accession
Peroxisome proliferator-activated receptor gamma SINGLE PROTEIN P37231

Target Relations

ChEMBL ID Pref Name Target Type
CHEMBL3559683 Peroxisome proliferator-activated receptor PROTEIN FAMILY
CHEMBL2095161 Peroxisome proliferator-activated receptor gamma/Nuclear receptor coactivator 3 PROTEIN-PROTEIN INTERACTION
CHEMBL2095162 Peroxisome proliferator-activated receptor gamma/Nuclear receptor coactivator 1 PROTEIN-PROTEIN INTERACTION
CHEMBL2111394 RXR alpha/PPAR gamma PROTEIN COMPLEX
CHEMBL2111325 PPAR alpha/gamma SELECTIVITY GROUP
CHEMBL2095163 Peroxisome proliferator-activated receptor gamma/Nuclear receptor coactivator 2 PROTEIN-PROTEIN INTERACTION
CHEMBL2096976 Peroxisome proliferator-activated receptor gamma/Nuclear receptor corepressor 2 PROTEIN-PROTEIN INTERACTION
CHEMBL2111371 PPAR delta/gamma SELECTIVITY GROUP

Approved Drugs and Clinical Candidates

ChEMBL ID Name Mechanism of Action Max Phase References
CHEMBL408 TROGLITAZONE Peroxisome proliferator-activated receptor gamma agonist 4 PubMed
CHEMBL704 MESALAMINE Peroxisome proliferator-activated receptor gamma agonist 4 PubMed PubMed PubMed
CHEMBL843 ROSIGLITAZONE MALEATE Peroxisome proliferator-activated receptor gamma agonist 4 DailyMed
CHEMBL1715 PIOGLITAZONE HYDROCHLORIDE Peroxisome proliferator-activated receptor gamma agonist 4 DailyMed
CHEMBL1200760 BALSALAZIDE DISODIUM Peroxisome proliferator-activated receptor gamma agonist 4 PubMed PubMed PubMed
CHEMBL1201013 OLSALAZINE SODIUM Peroxisome proliferator-activated receptor gamma agonist 4 DailyMed PubMed PubMed PubMed
CHEMBL282686 TESAGLITAZAR Peroxisome proliferator-activated receptor gamma agonist 3 PubMed PubMed
CHEMBL186179 MURAGLITAZAR Peroxisome proliferator-activated receptor gamma agonist 3 PubMed PubMed
CHEMBL519504 ALEGLITAZAR Peroxisome proliferator-activated receptor gamma agonist 3 PubMed
CHEMBL592054 IMIGLITAZAR Peroxisome proliferator-activated receptor gamma agonist 3 PubMed PubMed PubMed
CHEMBL1762621 BARDOXOLONE METHYL Peroxisome proliferator-activated receptor gamma antagonist 3 PubMed PubMed
CHEMBL2103991 BALAGLITAZONE Peroxisome proliferator-activated receptor gamma partial agonist 3 PubMed
CHEMBL2104753 RIVOGLITAZONE Peroxisome proliferator-activated receptor gamma agonist 3 Other PubMed PubMed
CHEMBL329123 ETALOCIB Peroxisome proliferator-activated receptor gamma agonist 2 DOI
CHEMBL93747 NETOGLITAZONE Peroxisome proliferator-activated receptor gamma modulator 2 PubMed
CHEMBL107367 FARGLITAZAR Peroxisome proliferator-activated receptor gamma agonist 2 PubMed
CHEMBL181954 NAVEGLITAZAR Peroxisome proliferator-activated receptor gamma agonist 2 KEGG PubMed PubMed
CHEMBL490029 MK-0533 Peroxisome proliferator-activated receptor gamma modulator 2 PubMed
CHEMBL1236924 INT131 Peroxisome proliferator-activated receptor gamma modulator 2 Other PubMed PubMed
CHEMBL2103824 ARHALOFENATE Peroxisome proliferator-activated receptor gamma modulator 2 PubMed
CHEMBL3545020 MBX-2044 Peroxisome proliferator-activated receptor gamma modulator 2
CHEMBL3545277 OMS405 Peroxisome proliferator-activated receptor gamma agonist 2 Other
CHEMBL3545278 ATx08-001 Peroxisome proliferator-activated receptor gamma modulator 2 PubMed PubMed
CHEMBL3545279 Efatutazone hydrochloride Peroxisome proliferator-activated receptor gamma agonist 2 Other Other PubMed
CHEMBL3545176 DB959 Peroxisome proliferator-activated receptor gamma agonist 1 Other Other
CHEMBL3545240 CLX-0921 Peroxisome proliferator-activated receptor gamma agonist 1 PubMed PubMed
CHEMBL3545295 AVE0847 Peroxisome proliferator-activated receptor gamma agonist 1 Other PubMed
More...

Target Associated Bioactivities

Target Associated Assays

Target Ligand Efficiencies

Target Associated Compound Properties

Target Cross References - Gene

Array Express ENSG00000132170
Ensembl ENSG00000132170
GO Cellular Component GO:0005634 (nucleus)
GO:0005654 (nucleoplasm)
GO:0005737 (cytoplasm)
GO:0005794 (Golgi apparatus)
GO:0005829 (cytosol)
GO:0043231 (intracellular membrane-bounded organelle)
GO:0048471 (perinuclear region of cytoplasm)
GO:0090575 (RNA polymerase II transcription factor complex)
GO Molecular Function GO:0001046 (core promoter sequence-specific DNA binding)
GO:0003677 (DNA binding)
GO:0003682 (chromatin binding)
GO:0003700 (transcription factor activity, sequence-specific DNA binding)
GO:0003707 (steroid hormone receptor activity)
GO:0004879 (RNA polymerase II transcription factor activity, ligand-activated sequence-specific DNA binding)
GO:0004955 (prostaglandin receptor activity)
GO:0005515 (protein binding)
GO:0008134 (transcription factor binding)
GO:0008144 (drug binding)
GO:0008270 (zinc ion binding)
GO:0019899 (enzyme binding)
GO:0019903 (protein phosphatase binding)
GO:0030331 (estrogen receptor binding)
GO:0030374 (ligand-dependent nuclear receptor transcription coactivator activity)
GO:0033613 (activating transcription factor binding)
GO:0042802 (identical protein binding)
GO:0043565 (sequence-specific DNA binding)
GO:0044212 (transcription regulatory region DNA binding)
GO:0046872 (metal ion binding)
GO:0046965 (retinoid X receptor binding)
GO:0050544 (arachidonic acid binding)
GO:0051393 (alpha-actinin binding)
GO Biological Process GO:0000122 (negative regulation of transcription from RNA polymerase II promoter)
GO:0001890 (placenta development)
GO:0002674 (negative regulation of acute inflammatory response)
GO:0006351 (transcription, DNA-templated)
GO:0006355 (regulation of transcription, DNA-templated)
GO:0006357 (regulation of transcription from RNA polymerase II promoter)
GO:0006367 (transcription initiation from RNA polymerase II promoter)
GO:0006629 (lipid metabolic process)
GO:0006919 (activation of cysteine-type endopeptidase activity involved in apoptotic process)
GO:0007165 (signal transduction)
GO:0007186 (G-protein coupled receptor signaling pathway)
GO:0007507 (heart development)
GO:0007584 (response to nutrient)
GO:0008217 (regulation of blood pressure)
GO:0008285 (negative regulation of cell proliferation)
GO:0009409 (response to cold)
GO:0009612 (response to mechanical stimulus)
GO:0010033 (response to organic substance)
GO:0010745 (negative regulation of macrophage derived foam cell differentiation)
GO:0010871 (negative regulation of receptor biosynthetic process)
GO:0010887 (negative regulation of cholesterol storage)
GO:0010891 (negative regulation of sequestering of triglyceride)
GO:0014070 (response to organic cyclic compound)
GO:0015909 (long-chain fatty acid transport)
GO:0019216 (regulation of lipid metabolic process)
GO:0019395 (fatty acid oxidation)
GO:0030224 (monocyte differentiation)
GO:0030308 (negative regulation of cell growth)
GO:0030855 (epithelial cell differentiation)
GO:0031000 (response to caffeine)
GO:0031100 (organ regeneration)
GO:0032526 (response to retinoic acid)
GO:0032869 (cellular response to insulin stimulus)
GO:0032966 (negative regulation of collagen biosynthetic process)
GO:0033189 (response to vitamin A)
GO:0033993 (response to lipid)
GO:0035357 (peroxisome proliferator activated receptor signaling pathway)
GO:0035902 (response to immobilization stress)
GO:0036270 (response to diuretic)
GO:0042493 (response to drug)
GO:0042593 (glucose homeostasis)
GO:0042594 (response to starvation)
GO:0042752 (regulation of circadian rhythm)
GO:0042953 (lipoprotein transport)
GO:0043065 (positive regulation of apoptotic process)
GO:0043401 (steroid hormone mediated signaling pathway)
GO:0043627 (response to estrogen)
GO:0045087 (innate immune response)
GO:0045165 (cell fate commitment)
GO:0045598 (regulation of fat cell differentiation)
GO:0045600 (positive regulation of fat cell differentiation)
GO:0045713 (low-density lipoprotein particle receptor biosynthetic process)
GO:0045892 (negative regulation of transcription, DNA-templated)
GO:0045893 (positive regulation of transcription, DNA-templated)
GO:0045944 (positive regulation of transcription from RNA polymerase II promoter)
GO:0046321 (positive regulation of fatty acid oxidation)
GO:0048469 (cell maturation)
GO:0048511 (rhythmic process)
GO:0048662 (negative regulation of smooth muscle cell proliferation)
GO:0048714 (positive regulation of oligodendrocyte differentiation)
GO:0050872 (white fat cell differentiation)
GO:0051091 (positive regulation of sequence-specific DNA binding transcription factor activity)
GO:0051974 (negative regulation of telomerase activity)
GO:0055088 (lipid homeostasis)
GO:0055098 (response to low-density lipoprotein particle)
GO:0060100 (positive regulation of phagocytosis, engulfment)
GO:0060336 (negative regulation of interferon-gamma-mediated signaling pathway)
GO:0060694 (regulation of cholesterol transporter activity)
GO:0060850 (regulation of transcription involved in cell fate commitment)
GO:0071300 (cellular response to retinoic acid)
GO:0071306 (cellular response to vitamin E)
GO:0071379 (cellular response to prostaglandin stimulus)
GO:0071380 (cellular response to prostaglandin E stimulus)
GO:0071455 (cellular response to hyperoxia)
GO:1901558 (response to metformin)
GO:2000230 (negative regulation of pancreatic stellate cell proliferation)
Wikipedia Peroxisome_proliferator-activated_receptor_gamma

Target Cross References - Protein

canSAR P37231
CGD Lipodystrophy, familial, partial, type 3; Insulin resistance, severe, digenic
Human Protein Atlas ENSG00000132170
IntAct P37231
Guide to Pharmacology 595
Open Targets ENSG00000132170
PharmGKB PA281
Pharos P37231 (Tclin)
Reactome R-HSA-1989781 (PPARA activates gene expression.)
R-HSA-381340 (Transcriptional regulation of white adipocyte differentiation.)
R-HSA-383280 (Nuclear Receptor transcription pathway.)
TIMBAL PPAR-gamma
UniProt A8K3G6 B5BUA1 O00684 O00710 O14515 P37231 Q0QJH8 Q15178 Q15179 Q15180 Q15832 Q86U60 Q96J12

Target Cross References - Domain

InterPro IPR000536 (Nucl_hrmn_rcpt_lig-bd.)
IPR001628 (Znf_hrmn_rcpt.)
IPR001723 (Nuclear_hrmn_rcpt.)
IPR003074 (1Cnucl_rcpt.)
IPR003077 (1Cnucl_rcpt_G.)
IPR013088 (Znf_NHR/GATA.)
IPR022590 (PPARgamma_N.)
Pfam PF00104 (Hormone_recep)
PF00105 (zf-C4)
PF12577 (PPARgamma_N)

Target Cross References - Structure

PDBe 1FM6 1FM9 1I7I 1K74 1KNU 1NYX 1PRG 1RDT 1WM0 1ZEO 1ZGY 2ATH 2F4B 2FVJ 2G0G 2G0H 2GTK 2HFP 2HWQ 2HWR 2I4J 2I4P 2I4Z 2OM9 More...
CREDO 1FM6 1FM9 1I7I 1K74 1KNU 1NYX 1PRG 1RDT 1WM0 1ZEO 1ZGY 2ATH 2F4B 2FVJ 2G0G 2G0H 2GTK 2HFP 2HWQ 2HWR 2I4J 2I4P 2I4Z 2OM9 More...
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