◎ Sugi Atlas

Atlas / Gene / PPARG

PPARG

gene
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Also known as PPARG1PPARG2NR1C3PPARgamma

Summary

PPARG (peroxisome proliferator activated receptor gamma, HGNC:9236) is a protein-coding gene on chromosome 3p25.2, encoding Peroxisome proliferator-activated receptor gamma (P37231). Ligand-activated transcription factor that forms obligate heterodimers with the retinoic acid receptor and acts as a key regulator of biological processes, such as adipocyte differentiation, lipid metabolism, glucose homeostasis and beta-oxidation of fatty acids.

This gene encodes a member of the peroxisome proliferator-activated receptor (PPAR) subfamily of nuclear receptors. PPARs form heterodimers with retinoid X receptors (RXRs) and these heterodimers regulate transcription of various genes. Three subtypes of PPARs are known: PPAR-alpha, PPAR-delta, and PPAR-gamma. The protein encoded by this gene is PPAR-gamma and is a regulator of adipocyte differentiation. Additionally, PPAR-gamma has been implicated in the pathology of numerous diseases including obesity, diabetes, atherosclerosis and cancer. Alternatively spliced transcript variants that encode different isoforms have been described.

Source: NCBI Gene 5468 — RefSeq curated summary.

At a glance

  • Gene–disease (curated): lipodystrophy (Definitive, ClinGen) — +2 more curated relationships
  • GWAS associations: 231
  • Clinical variants (ClinVar): 257 total — 18 pathogenic, 17 likely-pathogenic
  • Phenotypes (HPO): 55
  • Druggable target: yes — 83 molecules with ChEMBL bioactivity
  • Transcription factor: yes — 385 downstream targets (CollecTRI)
  • MANE Select transcript: NM_138711

Identifiers

Gene identifiers

FieldValue
HGNC IDHGNC:9236
Approved symbolPPARG
Nameperoxisome proliferator activated receptor gamma
Location3p25.2
Locus typegene with protein product
StatusApproved
AliasesPPARG1, PPARG2, NR1C3, PPARgamma
Ensembl geneENSG00000132170
Ensembl biotypeprotein_coding
OMIM601487
Entrez5468

Gene structure

Transcript identifiers

Ensembl transcripts: 76 — 64 protein_coding, 6 retained_intron, 4 nonsense_mediated_decay, 2 protein_coding_CDS_not_defined

ENST00000287820, ENST00000309576, ENST00000396999, ENST00000397000, ENST00000397010, ENST00000397015, ENST00000397023, ENST00000397026, ENST00000397029, ENST00000438682, ENST00000455517, ENST00000477039, ENST00000497594, ENST00000643197, ENST00000643888, ENST00000644622, ENST00000651735, ENST00000652098, ENST00000652431, ENST00000652522, ENST00000681966, ENST00000681982, ENST00000682125, ENST00000682446, ENST00000682494, ENST00000682604, ENST00000683586, ENST00000683599, ENST00000683699, ENST00000683700, ENST00000683749, ENST00000684065, ENST00000684094, ENST00000684277, ENST00000892317, ENST00000892318, ENST00000892319, ENST00000892320, ENST00000892321, ENST00000892322, ENST00000892323, ENST00000892324, ENST00000892325, ENST00000892326, ENST00000892327, ENST00000892328, ENST00000892329, ENST00000892330, ENST00000892331, ENST00000942257, ENST00000942258, ENST00000942259, ENST00000942260, ENST00000942261, ENST00000942262, ENST00000942263, ENST00000942264, ENST00000942265, ENST00000942266, ENST00000942267, ENST00000942268, ENST00000942269, ENST00000942270, ENST00000942271, ENST00000942272, ENST00000942273, ENST00000942274, ENST00000942275, ENST00000942276, ENST00000942277, ENST00000942278, ENST00000942279, ENST00000942280, ENST00000942281, ENST00000942282, ENST00000942283

RefSeq mRNA: 16 — MANE Select: NM_138711 NM_001330615, NM_001354666, NM_001354667, NM_001354668, NM_001354669, NM_001354670, NM_001374261, NM_001374262, NM_001374263, NM_001374264, NM_001374265, NM_001374266, NM_005037, NM_015869, NM_138711, NM_138712

CCDS: CCDS2609, CCDS2610, CCDS87046, CCDS93212

Canonical transcript exons

ENST00000651735 — 8 exons

ExonStartEnd
ENSE000012094101231238012312453
ENSE000035777481240588212406081
ENSE000036011981243389812434344
ENSE000036331321241670412417154
ENSE000036635341237970412379931
ENSE000036937031239261412392752
ENSE000037910651238132212381491
ENSE000038418351228907012289134

Expression profiles

Bgee: expression breadth ubiquitous, 194 present calls, max score 97.11.

FANTOM5 (CAGE): breadth ubiquitous, TPM avg 15.9129 / max 545.1231, expressed in 1207 samples.

FANTOM5 promoters (12 alternative TSS)

Promoter IDTPM avgSamples expressed
353706.2732617
353674.0886911
353663.2180925
353750.5655116
353770.539899
353680.3282177
353690.2754158
353740.265876
353760.164751
353780.106340

Top tissues by expression

284 total, by Bgee expression score (0-100, higher = more expressed):

TissueAnatomy IDExpression scoreQuality
omental fat padUBERON:001041497.11gold quality
peritoneumUBERON:000235896.96gold quality
adipose tissue of abdominal regionUBERON:000780896.94gold quality
mucosa of transverse colonUBERON:000499196.47gold quality
adipose tissueUBERON:000101396.12gold quality
subcutaneous adipose tissueUBERON:000219095.96gold quality
connective tissueUBERON:000238494.73gold quality
rectumUBERON:000105294.09gold quality
colonic epitheliumUBERON:000039791.88gold quality
transverse colonUBERON:000115790.64gold quality
colonic mucosaUBERON:000031790.17gold quality
mucosa of sigmoid colonUBERON:000499388.86gold quality
right lungUBERON:000216788.67gold quality
male germ line stem cell (sensu Vertebrata) in testisCL:0000089 ∩ UBERON:000047387.89gold quality
urinary bladderUBERON:000125587.32gold quality
primordial germ cell in gonadCL:0000670 ∩ UBERON:000099187.25gold quality
calcaneal tendonUBERON:000370186.44gold quality
jejunal mucosaUBERON:000039986.11gold quality
large intestineUBERON:000005985.80gold quality
placentaUBERON:000198785.67gold quality
colonUBERON:000115585.66gold quality
upper lobe of left lungUBERON:000895285.50gold quality
body of stomachUBERON:000116185.22gold quality
upper lobe of lungUBERON:000894884.80gold quality
right lobe of thyroid glandUBERON:000111984.77gold quality
intestineUBERON:000016084.62gold quality
left lobe of thyroid glandUBERON:000112084.60gold quality
left ovaryUBERON:000211984.55gold quality
right ovaryUBERON:000211884.49gold quality
stomachUBERON:000094584.41gold quality

Single-cell (SCXA)

Detected in 4 experiment(s), a significant marker in 4.

ExperimentMarker?Max mean expression
E-ANND-2yes2954.88
E-ANND-3yes16.53
E-HCAD-10yes13.59
E-CURD-112yes11.13

Regulation

Is transcription factor: yes

Downstream targets (CollecTRI)

385 targets.

TargetRegulation
AACSUnknown
ABCA1Activation
ABCA12Activation
ABCG1Activation
ABCG2Activation
ACAT1Activation
ACEUnknown
ACSL1
ACTA2Repression
ACTG2Repression
ADAM2
ADAMTS4Repression
ADIPOQActivation
ADIPOR2Repression
ADSS2Activation
AGERRepression
AGTActivation
AGTR1Unknown
ALBRepression
ALOXE3Unknown
ANGPTL4Activation
AP1Repression
APMAPActivation
APOA1Unknown
APOA2Unknown
APOA4Activation
APOBRepression
APOBRRepression
APOC4Unknown
APOEActivation

JASPAR motifs

MotifNameFamily
MA0065.1PPARG::RXRAThyroid hormone receptor-related factors (NR1)::RXR-related receptors (NR2)
MA0066.1PPARGThyroid hormone receptor-related factors (NR1)
MA0066.2PPARGThyroid hormone receptor-related factors (NR1)

JASPAR matrix evidence (PMIDs): PMID:11139380

Upstream regulators (CollecTRI, top): AP1, ARID5B, ATF1, ATF2, BHLHE40, BMP2, BMP7, CDX1, CEBPA, CEBPB, CEBPD, CEBPG, CREB1, CREBL2, CTNNB1, DDIT3, DLX5, E2F1, E2F4, EBF1, EDN1, EGR1, ELF4, ESR1, ETV4, EWSR1, FGFR2, FOSL2, FOXA1, FOXO1, GATA2, GATA3, HES1, HES6, HIF1A, HIVEP2, HNF4A, IFI16, IFNG, INS

miRNA regulators (miRDB)

64 targeting PPARG, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):

miRNAMax scoreAvg scoremiRNA target_count
HSA-MIR-3163100.0077.238605
HSA-MIR-513A-5P100.0069.772465
HSA-MIR-340-5P100.0072.504437
HSA-MIR-548N99.9871.944170
HSA-MIR-27A-3P99.9872.132955
HSA-MIR-27B-3P99.9872.132955
HSA-MIR-998599.9872.112939
HSA-MIR-3617-3P99.9867.86918
HSA-MIR-477599.9875.006394
HSA-MIR-590-3P99.9674.346478
HSA-MIR-548AB99.9571.313488
HSA-MIR-55999.9572.283609
HSA-MIR-128-3P99.9571.172484
HSA-MIR-216A-3P99.9571.192505
HSA-MIR-548A-5P99.9471.273482
HSA-MIR-548AD-5P99.9471.233502
HSA-MIR-548AE-5P99.9471.233502
HSA-MIR-548AK99.9471.243488
HSA-MIR-548AM-5P99.9471.243488
HSA-MIR-548AP-5P99.9471.143489
HSA-MIR-548AQ-5P99.9471.343426
HSA-MIR-548AR-5P99.9471.283515
HSA-MIR-548AS-5P99.9471.223482
HSA-MIR-548AU-5P99.9471.243488
HSA-MIR-548AY-5P99.9471.233502
HSA-MIR-548B-5P99.9471.233502
HSA-MIR-548BB-5P99.9471.273509
HSA-MIR-548C-5P99.9471.243488
HSA-MIR-548D-5P99.9471.233502
HSA-MIR-548H-5P99.9471.243488

Literature-anchored findings (GeneRIF, showing 40)

  • The expression of the human PPARgamma gene is controlled by RORalpha1. (PMID:11554739)
  • PPAR-gamma induces pancreatic cancer cell apoptosis (PMID:11554760)
  • role in inducing cyclooxygenase-2 in monocytes (PMID:11809750)
  • Expression of peroxisome proliferator-activated receptor gamma and the growth inhibitory effect of its synthetic ligands in human salivary gland cancer cell lines. (PMID:11836575)
  • Reduced lipolysis as possible cause for greater weight gain in subjects with the Pro12Ala polymorphism in PPARgamma2 (PMID:11845236)
  • Peroxisome proliferator-activated receptor gamma agonists inhibit HIV-1 replication in macrophages by transcriptional and post-transcriptional effects. (PMID:11847231)
  • the role of peroxisome proliferator-activated receptor gamma (PPARgamma) in high-fat diet induced-obesity and insulin resistance by gene targeting and case-control study using the common PPARgamma2 polymorphism (PMID:11872365)
  • Pharmacologic activation of PPARgamma in vascular cells may provide a novel therapeutic approach to retard diabetes-associated vascular disease. (PMID:11872366)
  • the roles of PPARgamma and the actions of PPARgamma ligands in the cardiovascular system (PMID:11872377)
  • T0070907, a selective ligand for peroxisome proliferator-activated receptor gamma, functions as an antagonist of biochemical and cellular activities (PMID:11877444)
  • Activation of PPAR gamma by oxidized lipoproteins (oxLDL) promotes macrophage desensitization by reducing oxLDL-stimulated oxygen radical formation, an important determinant of the activation/deactivation balance in macrophages. (PMID:11884452)
  • The presence of PPAR gamma in bladder cancers having characteristics of low malignancy is associated with its role in modulating expression of those angiogenic factors (e.g., bFGF and PDECGF) that may be responsible for malignancy in bladder tumor cells. (PMID:11888683)
  • cPLA(2) plays a critical role in PPAR-mediated gene transcription in HepG2 cells (PMID:11897617)
  • Nuclear receptor corepressor-dependent repression of peroxisome-proliferator-activated receptor delta-mediated transactivation (PMID:11903058)
  • PPARgamma augments TNF-family induced apoptosis (PMID:11914642)
  • Lack of association between peroxisome proliferator-activated receptor-gamma-2 gene variants and the occurrence of coronary heart disease in patients with diabetes mellitus. (PMID:11916624)
  • Retinoid X receptor alpha is implicated in the nuclear reorganization of PPAR gamma and suggest that PPAR gamma colocalizes with RXR alpha at specific locations within the nucleus independent of added ligand. (PMID:11923467)
  • PPARgamma2 pro12Ala polymorphism and insulin resistance in Japanese hypertensive patients. (PMID:11924722)
  • Pro12Ala polymorphism of PPAR(gamma2) gene is not associated with diabetic retinopathy but is associated with dyslipidemia in male type 2 diabetic patients (PMID:11928067)
  • activation of PPARgamma in human CD4-positive T cells limits the expression of proinflammatory cytokines, such as IFNgamma (PMID:11934839)
  • Activation of peroxisome proliferator-activated receptor-gamma stimulates the growth arrest and DNA-damage inducible 153 gene in non-small cell lung carcinoma cells. (PMID:11948400)
  • PPAR-gamma is induced in prostate cancer; PPAR-gamma ligands may mediate its antiproliferative effect against prostate cancer cells through differentiation (PMID:11948965)
  • Inhibition of human chondrosarcoma cell growth via apoptosis by peroxisome proliferator-activated receptor-gamma. (PMID:11953889)
  • Frequent polymorphism of peroxisome proliferator activated receptor gamma gene in colorectal cancer containing wild-type K-ras gene. (PMID:11956653)
  • Pro12Ala polymorphism of the gene is associated with reduced type 2 diabetes risk and increased insulin sensitivity (PMID:11972302)
  • genes of C3, HSL, and PPARgamma may exert a modifying effect on lipid and glucose metabolism in familial combined hyperlipidemia (PMID:11979403)
  • differential regulation of vascular endothelial growth factor expression in bladder cancer cells (peroxisome proliferative activated receptor, beta) (PMID:11980898)
  • PPRE in intron 1 of the ACBP gene is a bona fide PPARgamma-response element. (PMID:12015306)
  • findings suggest an involvement of PPARgamma in trophoblast differentiation during normal placental development; down-regulation of PPARgamma may contribute to trophoblastic diseases such as hydatidufirm mole and choriocarcinoma (PMID:12029076)
  • PPAR activators inhibit endothelial cell migration by targeting Akt. (PMID:12054675)
  • adipose tissue peroxisome proliferator-activated receptor gamma1 mRNA concentration is positively regulated by eicosapentaenoic acid (PMID:12055328)
  • Activation of peroxisome proliferator-activated receptor gamma inhibits osteoprotegerin gene expression in human aortic smooth muscle cells (PMID:12056809)
  • Differential effect of variants in the development of type 2 diabetes between native Japanese and Japanese Americans. (PMID:12062858)
  • PPARgamma is a target for induction of apoptosis in rheumatoid synovial cells (PMID:12065695)
  • 85kD PLA2 mediates PPARG activation in lung epithelial cells (PMID:12077117)
  • reduces growth of esophageal cancer (PMID:12080321)
  • obesity is associated with an inverse relationship between PPARgamma and retinoic acid receptor alpha expressions in subcutaneous adipose tissue (PMID:12080444)
  • effect of polymorphism on insulin sensitivity and metabolism; interactions with birth size (PMID:12086968)
  • Activation of endothelial PPAR-gamma has a potent anti-inflammatory role. (PMID:12107164)
  • we describe a family in which five individuals with severe insulin resistance, but no unaffected family members, were compound heterozygous with respect to frameshift/premature stop mutations in two unlinked genes, PPARG and PPP1R3A (PMID:12118251)

Cross-species orthologs

187 orthologs

OrganismSymbolGene ID
mus_musculusPpargENSMUSG00000000440
rattus_norvegicusPpargENSRNOG00000008839
drosophila_melanogasterEcRFBGN0000546
drosophila_melanogasterHr96FBGN0015240
caenorhabditis_elegansWBGENE00001062
caenorhabditis_elegansnhr-2WBGENE00003601
caenorhabditis_elegansWBGENE00003608
caenorhabditis_elegansWBGENE00003611
caenorhabditis_elegansWBGENE00003614
caenorhabditis_elegansWBGENE00003615
caenorhabditis_elegansWBGENE00003617
caenorhabditis_elegansWBGENE00003618
caenorhabditis_elegansWBGENE00003620
caenorhabditis_elegansnhr-23WBGENE00003622
caenorhabditis_elegansWBGENE00003624
caenorhabditis_elegansWBGENE00003632
caenorhabditis_elegansWBGENE00003634
caenorhabditis_elegansWBGENE00003638
caenorhabditis_elegansWBGENE00003640
caenorhabditis_elegansWBGENE00003641
caenorhabditis_elegansWBGENE00003642
caenorhabditis_elegansWBGENE00003643
caenorhabditis_elegansWBGENE00003644
caenorhabditis_elegansWBGENE00003645
caenorhabditis_elegansWBGENE00003646
caenorhabditis_elegansWBGENE00003648
caenorhabditis_elegansWBGENE00003649
caenorhabditis_elegansWBGENE00003651
caenorhabditis_elegansWBGENE00003653
caenorhabditis_elegansWBGENE00003655
caenorhabditis_elegansWBGENE00003658
caenorhabditis_elegansWBGENE00003660
caenorhabditis_elegansWBGENE00003662
caenorhabditis_elegansnhr-73WBGENE00003663
caenorhabditis_elegansnhr-77WBGENE00003667
caenorhabditis_elegansWBGENE00003669
caenorhabditis_elegansnhr-81WBGENE00003671
caenorhabditis_elegansnhr-82WBGENE00003672
caenorhabditis_elegansWBGENE00003676
caenorhabditis_elegansWBGENE00003677
caenorhabditis_elegansWBGENE00003680
caenorhabditis_elegansWBGENE00003682
caenorhabditis_elegansWBGENE00003684
caenorhabditis_elegansWBGENE00003685
caenorhabditis_elegansWBGENE00003686
caenorhabditis_elegansWBGENE00003688
caenorhabditis_elegansWBGENE00003689
caenorhabditis_elegansWBGENE00003692
caenorhabditis_elegansWBGENE00003693
caenorhabditis_elegansWBGENE00003694
caenorhabditis_elegansWBGENE00003696
caenorhabditis_elegansWBGENE00003698
caenorhabditis_elegansWBGENE00003699
caenorhabditis_elegansWBGENE00003700
caenorhabditis_elegansWBGENE00003702
caenorhabditis_elegansWBGENE00003704
caenorhabditis_elegansWBGENE00003705
caenorhabditis_elegansWBGENE00003707
caenorhabditis_elegansWBGENE00003708
caenorhabditis_elegansWBGENE00003712
caenorhabditis_elegansWBGENE00003713
caenorhabditis_elegansWBGENE00003714
caenorhabditis_elegansWBGENE00003715
caenorhabditis_elegansWBGENE00003716
caenorhabditis_elegansWBGENE00003717
caenorhabditis_elegansWBGENE00003718
caenorhabditis_elegansWBGENE00003720
caenorhabditis_elegansWBGENE00003721
caenorhabditis_elegansWBGENE00003722
caenorhabditis_elegansWBGENE00003723
caenorhabditis_elegansWBGENE00003724
caenorhabditis_elegansWBGENE00003725
caenorhabditis_elegansWBGENE00003728
caenorhabditis_elegansWBGENE00004786
caenorhabditis_elegansWBGENE00006471
caenorhabditis_elegansunc-55WBGENE00006790
caenorhabditis_elegansWBGENE00007367
caenorhabditis_elegansWBGENE00008056
caenorhabditis_elegansnhr-165WBGENE00008158
caenorhabditis_elegansWBGENE00008208
caenorhabditis_elegansnhr-169WBGENE00008289
caenorhabditis_elegansWBGENE00008309
caenorhabditis_elegansnhr-174WBGENE00008474
caenorhabditis_elegansWBGENE00008619
caenorhabditis_elegansWBGENE00008630
caenorhabditis_elegansWBGENE00008778
caenorhabditis_elegansWBGENE00008830
caenorhabditis_elegansWBGENE00008884
caenorhabditis_elegansWBGENE00008901
caenorhabditis_elegansnhr-265WBGENE00009608
caenorhabditis_elegansWBGENE00010017
caenorhabditis_elegansWBGENE00010180
caenorhabditis_elegansWBGENE00010186
caenorhabditis_elegansWBGENE00010215
caenorhabditis_elegansWBGENE00010410
caenorhabditis_elegansWBGENE00010600
caenorhabditis_elegansWBGENE00010601
caenorhabditis_elegansWBGENE00010602
caenorhabditis_elegansWBGENE00010603
caenorhabditis_elegansWBGENE00010604
caenorhabditis_elegansWBGENE00011002
caenorhabditis_elegansWBGENE00011150
caenorhabditis_elegansWBGENE00011396
caenorhabditis_elegansWBGENE00011520
caenorhabditis_elegansWBGENE00011565
caenorhabditis_elegansWBGENE00011566
caenorhabditis_elegansWBGENE00011568
caenorhabditis_elegansnhr-217WBGENE00011651
caenorhabditis_elegansWBGENE00011750
caenorhabditis_elegansWBGENE00012050
caenorhabditis_elegansWBGENE00012056
caenorhabditis_elegansWBGENE00012446
caenorhabditis_elegansWBGENE00012449
caenorhabditis_elegansWBGENE00012596
caenorhabditis_elegansWBGENE00012703
caenorhabditis_elegansWBGENE00013067
caenorhabditis_elegansWBGENE00013483
caenorhabditis_elegansnhr-276WBGENE00013512
caenorhabditis_elegansWBGENE00013584
caenorhabditis_elegansWBGENE00013940
caenorhabditis_elegansWBGENE00014068
caenorhabditis_elegansnhr-245WBGENE00014189
caenorhabditis_elegansWBGENE00014193
caenorhabditis_elegansWBGENE00015497
caenorhabditis_elegansWBGENE00015758
caenorhabditis_elegansWBGENE00015897
caenorhabditis_elegansWBGENE00015900
caenorhabditis_elegansWBGENE00015901
caenorhabditis_elegansWBGENE00015902
caenorhabditis_elegansWBGENE00016091
caenorhabditis_elegansWBGENE00016233
caenorhabditis_elegansWBGENE00016364
caenorhabditis_elegansWBGENE00016365
caenorhabditis_elegansWBGENE00016366
caenorhabditis_elegansWBGENE00016367
caenorhabditis_elegansWBGENE00016368
caenorhabditis_elegansWBGENE00016517
caenorhabditis_elegansWBGENE00016772
caenorhabditis_elegansWBGENE00016926
caenorhabditis_elegansWBGENE00016927
caenorhabditis_elegansWBGENE00017503
caenorhabditis_elegansWBGENE00017512
caenorhabditis_elegansWBGENE00017961
caenorhabditis_elegansWBGENE00018189
caenorhabditis_elegansWBGENE00018265
caenorhabditis_elegansWBGENE00018266
caenorhabditis_elegansWBGENE00018404
caenorhabditis_elegansWBGENE00018412
caenorhabditis_elegansWBGENE00018415
caenorhabditis_elegansWBGENE00018539
caenorhabditis_elegansWBGENE00018541
caenorhabditis_elegansWBGENE00018542
caenorhabditis_elegansWBGENE00018544
caenorhabditis_elegansWBGENE00018545
caenorhabditis_elegansWBGENE00018622
caenorhabditis_elegansWBGENE00019115
caenorhabditis_elegansWBGENE00019116
caenorhabditis_elegansWBGENE00019741
caenorhabditis_elegansWBGENE00019742
caenorhabditis_elegansWBGENE00019743
caenorhabditis_elegansWBGENE00020015
caenorhabditis_elegansWBGENE00020062
caenorhabditis_elegansWBGENE00020152
caenorhabditis_elegansWBGENE00020153
caenorhabditis_elegansWBGENE00020385
caenorhabditis_elegansWBGENE00020460
caenorhabditis_elegansWBGENE00020555
caenorhabditis_elegansWBGENE00020750
caenorhabditis_elegansWBGENE00020849
caenorhabditis_elegansWBGENE00020850
caenorhabditis_elegansWBGENE00020851
caenorhabditis_elegansWBGENE00020852
caenorhabditis_elegansWBGENE00021163
caenorhabditis_elegansWBGENE00021522
caenorhabditis_elegansWBGENE00021610
caenorhabditis_elegansWBGENE00021611
caenorhabditis_elegansWBGENE00021617
caenorhabditis_elegansWBGENE00022097
caenorhabditis_elegansWBGENE00022637
caenorhabditis_elegansWBGENE00022639
caenorhabditis_elegansWBGENE00022640
caenorhabditis_elegansWBGENE00022726
caenorhabditis_elegansWBGENE00022756
caenorhabditis_elegansWBGENE00022805
caenorhabditis_elegansWBGENE00044353
caenorhabditis_elegansWBGENE00044699
caenorhabditis_elegansWBGENE00045515

Paralogs (18): NR1H4 (ENSG00000012504), NR1H3 (ENSG00000025434), RORA (ENSG00000069667), RARB (ENSG00000077092), VDR (ENSG00000111424), PPARD (ENSG00000112033), THRA (ENSG00000126351), NR1D1 (ENSG00000126368), NR1H2 (ENSG00000131408), RARA (ENSG00000131759), NR1I3 (ENSG00000143257), RORC (ENSG00000143365), NR1I2 (ENSG00000144852), THRB (ENSG00000151090), RARG (ENSG00000172819), NR1D2 (ENSG00000174738), PPARA (ENSG00000186951), RORB (ENSG00000198963)

Protein

Protein identifiers

Peroxisome proliferator-activated receptor gamma — P37231 (reviewed: P37231)

Alternative names: Nuclear receptor subfamily 1 group C member 3

All UniProt accessions (16): P37231, A0A3P3ZKM0, A0A494C012, A0A494C0D9, A0A494C0T3, A0A499FIV4, A0A804HIG1, A0A804HJN2, A0A804HL89, A0A804HLH1, E7EU07, E7EUD1, E9PFV2, E9PFV3, E9PFX5, Q6L9M1

UniProt curated annotations — full annotation on UniProt →

Function. Ligand-activated transcription factor that forms obligate heterodimers with the retinoic acid receptor and acts as a key regulator of biological processes, such as adipocyte differentiation, lipid metabolism, glucose homeostasis and beta-oxidation of fatty acids. Activated by lipid ligands: binds peroxisome proliferators, such as hypolipidemic drugs, and fatty acids, such as prostaglandin J2 metabolites. Ligand-binding results in a conformational change in the receptor, promoting dissociation of repressors and recruitment of coactivators, and subsequent activation of target gene expression. Specifically binds to DNA specific PPAR response elements (PPRE) and modulates the transcription of its target genes, such as acyl-CoA oxidase. Acts as a critical regulator of gut homeostasis by suppressing NF-kappa-B-mediated pro-inflammatory responses. Plays a role in the regulation of cardiovascular circadian rhythms by regulating the transcription of BMAL1 in the blood vessels. Nuclear receptor that acts as the key factor controlling the development of adipocytes. Specifically activated by 15-deoxy-delta12,14-prostaglandin J2 ligand during early adipogenesis, driving differentiation of all types of adipocytes (white, beige and brown). Acts together with retinoic acid receptor RXRA, forming the ARF6 complex, which acts as a key regulator of the tissue-specific adipocyte P2 (aP2) enhancer. Following recruitment of TLE3, promotes differentiation of white adipocytes. Following recruitment of PRDM16, promotes differentiation of myoblastic precursors into brown adipose cells (BAT), which are specialized in dissipating energy in the form of heat in response to cold or excess feeding. Also mediates diffentiation of white adipocytes into beige adipocytes by mediating recruitment of PRDM16. (Microbial infection) Upon treatment with M.tuberculosis or its lipoprotein LpqH, phosphorylation of MAPK p38 and IL-6 production are modulated, probably via this protein.

Subunit / interactions. Heterodimer with retinoic acid receptor, such as RXRA. The heterodimer with the retinoic acid receptor RXRA is called adipocyte-specific transcription factor ARF6. Interacts with NCOA6 coactivator, leading to a strong increase in transcription of target genes. Interacts with coactivator PPARBP, leading to a mild increase in transcription of target genes. Interacts with NCOA7 in a ligand-inducible manner. Interacts with NCOA1 and NCOA2 LXXLL motifs. Interacts with ASXL1, ASXL2, DNTTIP2, FAM120B, MAP2K1/MEK1, NR0B2, PDPK1, PRMT2 and TGFB1I1. Interacts (when activated by agonist) with PPP5C. Interacts with HELZ2 and THRAP3; the interaction stimulates the transcriptional activity of PPARG. Interacts with PER2, the interaction is ligand dependent and blocks PPARG recruitment to target promoters. Interacts with NOCT. Interacts with FOXO1 (acetylated form). Interacts with ACTN4. Interacts (when in the liganded conformation) with GPS2. Interacts with CRY1 and CRY2 in a ligand-dependent manner. In the absence of hormonal ligand, interacts with TACC1. In macrophages, interacts with PAQR3 and STUB1; these interactions promote PPARG poylubiquitination and STUB1-mediated degradation. Interacts with YTDC1 (via its intrinsically disordered region); the interaction prevents the ubiquitin-mediated proteasomal degradation of PPARG. Interacts with CEBPA; promoting activation of the adipogenic program. Interacts with PRDM16; promoting activation of brown and beige adipocytes.

Subcellular location. Nucleus. Cytoplasm Nucleus.

Tissue specificity. Highest expression in adipose tissue. Lower in skeletal muscle, spleen, heart and liver. Also detectable in placenta, lung and ovary.

Post-translational modifications. O-GlcNAcylation at Thr-84 reduces transcriptional activity in adipocytes. Phosphorylated in basal conditions and dephosphorylated when treated with the ligand. May be dephosphorylated by PPP5C. The phosphorylated form may be inactive and dephosphorylation at Ser-112 induces adipogenic activity. Ubiquitinated by E3 ubiquitin-protein ligase complex containing FBXO9; leading to proteasomal degradation. Ubiquitinated at Lys-252 by TRIM55 leading to proteasomal degradation. Ubiquitinated by E3 ubiquitin-protein ligase STUB1/CHIP; leading to proteasomal degradation. Ubiquitinated by E3 ubiquitin-protein ligase ARIH2; leading to proteasomal degradation.

Disease relevance. Defects in PPARG can lead to type 2 insulin-resistant diabetes and hyptertension. PPARG mutations may be associated with colon cancer. Obesity (OBESITY) [MIM:601665] A condition characterized by an increase of body weight beyond the limitation of skeletal and physical requirements, as the result of excessive accumulation of body fat. Disease susceptibility may be associated with variants affecting the gene represented in this entry. Lipodystrophy, familial partial, 3 (FPLD3) [MIM:604367] An autosomal dominant form of lipodystrophy characterized by marked loss of subcutaneous fat from the extremities. Facial adipose tissue may be increased, decreased or normal. Affected individuals show an increased preponderance of insulin resistance, diabetes mellitus and dyslipidemia. The disease is caused by variants affecting the gene represented in this entry. Glioma 1 (GLM1) [MIM:137800] Gliomas are benign or malignant central nervous system neoplasms derived from glial cells. They comprise astrocytomas and glioblastoma multiforme that are derived from astrocytes, oligodendrogliomas derived from oligodendrocytes and ependymomas derived from ependymocytes. Disease susceptibility may be associated with variants affecting the gene represented in this entry. Polymorphic PPARG alleles have been found to be significantly over-represented among a cohort of American patients with sporadic glioblastoma multiforme suggesting a possible contribution to disease susceptibility.

Activity regulation. PDPK1 activates its transcriptional activity independently of its kinase activity.

Domain organisation. The 9aaTAD motif is a transactivation domain present in a large number of yeast and animal transcription factors.

Induction. (Microbial infection) Expression increases when incubated with M.tuberculosis or its lipoprotein LpqH; induction is TLR2-dependent (at protein level).

Polymorphism. Genetic variations in PPARG define the body mass index quantitative trait locus 1 (BMIQ1) [MIM:606641]. The body max index (BMI) reflects the amount of fat, lean mass, and body build.

Miscellaneous. Exhibits dominant negative activity over isoform 1.

Similarity. Belongs to the nuclear hormone receptor family. NR1 subfamily.

Isoforms (3)

UniProt IDNamesCanonical?
P37231-12, PPARgamma2, PPARgamma-2yes
P37231-21, PPARgamma1(wt)
P37231-33, PPARgamma1(tr)

RefSeq proteins (16): NP_001317544, NP_001341595, NP_001341596, NP_001341597, NP_001341598, NP_001341599, NP_001361190, NP_001361191, NP_001361192, NP_001361193, NP_001361194, NP_001361195, NP_005028, NP_056953, NP_619725, NP_619726 (=MANE)

Domains & families (InterPro)

IDNameType
IPR000536Nucl_hrmn_rcpt_lig-bdDomain
IPR001628Znf_hrmn_rcptDomain
IPR001723Nuclear_hrmn_rcptFamily
IPR0030741Cnucl_rcptFamily
IPR003077PPAR-gammaFamily
IPR013088Znf_NHR/GATAHomologous_superfamily
IPR022590PPARgamma_NDomain
IPR035500NHR-like_dom_sfHomologous_superfamily
IPR050234Nuclear_hormone_rcpt_NR1Family

Pfam: PF00104, PF00105, PF12577

UniProt features (71 total): helix 20, strand 14, sequence variant 9, turn 7, binding site 4, splice variant 3, sequence conflict 3, zinc finger region 2, chain 1, domain 1, modified residue 1, glycosylation site 1, cross-link 1, DNA-binding region 1, mutagenesis site 1, region of interest 1, short sequence motif 1

Structure

Experimental structures (PDB)

380 structures, top 30 by resolution.

PDBMethodResolution (Å)
9F7WX-RAY DIFFRACTION1.25
8BF1X-RAY DIFFRACTION1.36
9V8GX-RAY DIFFRACTION1.39
9V8HX-RAY DIFFRACTION1.39
8FKCX-RAY DIFFRACTION1.42
6MS7X-RAY DIFFRACTION1.43
9V8DX-RAY DIFFRACTION1.44
3U9QX-RAY DIFFRACTION1.52
8B94X-RAY DIFFRACTION1.55
8DKVX-RAY DIFFRACTION1.59
3B1MX-RAY DIFFRACTION1.6
3V9VX-RAY DIFFRACTION1.6
9F7XX-RAY DIFFRACTION1.63
3V9TX-RAY DIFFRACTION1.65
6T1SX-RAY DIFFRACTION1.65
8B92X-RAY DIFFRACTION1.66
5Y2TX-RAY DIFFRACTION1.7
9R6IX-RAY DIFFRACTION1.7
9V8EX-RAY DIFFRACTION1.7
8B95X-RAY DIFFRACTION1.72
7AWCX-RAY DIFFRACTION1.74
6IZNX-RAY DIFFRACTION1.75
9V8FX-RAY DIFFRACTION1.75
4CI5X-RAY DIFFRACTION1.77
7E0AX-RAY DIFFRACTION1.77
8B8XX-RAY DIFFRACTION1.78
6ZLYX-RAY DIFFRACTION1.79
1ZGYX-RAY DIFFRACTION1.8
5Z5SX-RAY DIFFRACTION1.8
5Z6SX-RAY DIFFRACTION1.8

Predicted structure (AlphaFold)

ModelpLDDTFraction very-high
AF-P37231-F176.110.55

Functional residue map

Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.

Ligand- & substrate-binding residues (4): 501; 314–317; 351; 477

Post-translational modifications (2): 112, 252

Glycosylation sites (1): 84

Mutagenesis-validated functional residues (1):

PositionPhenotype
252more than 50% loss of ubiquitination.

Function

Pathways and Gene Ontology

Reactome pathways

8 pathways

IDPathway
R-HSA-1989781PPARA activates gene expression
R-HSA-381340Transcriptional regulation of white adipocyte differentiation
R-HSA-383280Nuclear Receptor transcription pathway
R-HSA-4090294SUMOylation of intracellular receptors
R-HSA-8943724Regulation of PTEN gene transcription
R-HSA-9022707MECP2 regulates transcription factors
R-HSA-9844594Transcriptional regulation of brown and beige adipocyte differentiation by EBF2
R-HSA-9841922MLL4 and MLL3 complexes regulate expression of PPARG target genes in adipogenesis and hepatic steatosis

MSigDB gene sets: 782 (showing top): GOBP_MYELOID_CELL_DIFFERENTIATION, GSE18804_SPLEEN_MACROPHAGE_VS_TUMORAL_MACROPHAGE_DN, GOBP_CIRCADIAN_RHYTHM, GOBP_CELLULAR_RESPONSE_TO_LIPOPROTEIN_PARTICLE_STIMULUS, GOBP_NEGATIVE_REGULATION_OF_EPITHELIAL_CELL_PROLIFERATION, REACTOME_TRANSCRIPTIONAL_REGULATION_OF_WHITE_ADIPOCYTE_DIFFERENTIATION, GOBP_SMAD_PROTEIN_SIGNAL_TRANSDUCTION, PID_HDAC_CLASSI_PATHWAY, GOBP_RESPONSE_TO_NITROGEN_COMPOUND, GOBP_REGULATION_OF_LIPID_STORAGE, GOBP_REGULATION_OF_CELLULAR_RESPONSE_TO_GROWTH_FACTOR_STIMULUS, GOBP_EPITHELIUM_DEVELOPMENT, GOBP_REGULATION_OF_FAT_CELL_DIFFERENTIATION, GOBP_REGULATION_OF_BLOOD_PRESSURE, GOBP_NEGATIVE_REGULATION_OF_SMOOTH_MUSCLE_CELL_PROLIFERATION

GO Biological Process (104): negative regulation of transcription by RNA polymerase II (GO:0000122), placenta development (GO:0001890), regulation of transcription by RNA polymerase II (GO:0006357), fatty acid metabolic process (GO:0006631), response to nutrient (GO:0007584), regulation of blood pressure (GO:0008217), hormone-mediated signaling pathway (GO:0009755), positive regulation of gene expression (GO:0010628), negative regulation of gene expression (GO:0010629), negative regulation of macrophage derived foam cell differentiation (GO:0010745), positive regulation of cholesterol efflux (GO:0010875), negative regulation of cholesterol storage (GO:0010887), negative regulation of lipid storage (GO:0010888), long-chain fatty acid transport (GO:0015909), negative regulation of angiogenesis (GO:0016525), cell differentiation (GO:0030154), monocyte differentiation (GO:0030224), BMP signaling pathway (GO:0030509), negative regulation of transforming growth factor beta receptor signaling pathway (GO:0030512), negative regulation of BMP signaling pathway (GO:0030514), intracellular receptor signaling pathway (GO:0030522), epithelial cell differentiation (GO:0030855), positive regulation of cholesterol transport (GO:0032376), cellular response to insulin stimulus (GO:0032869), response to lipid (GO:0033993), peroxisome proliferator activated receptor signaling pathway (GO:0035357), glucose homeostasis (GO:0042593), regulation of circadian rhythm (GO:0042752), mRNA transcription by RNA polymerase II (GO:0042789), negative regulation of MAPK cascade (GO:0043409), negative regulation of blood vessel endothelial cell migration (GO:0043537), innate immune response (GO:0045087), cell fate commitment (GO:0045165), fat cell differentiation (GO:0045444), positive regulation of fat cell differentiation (GO:0045600), negative regulation of osteoblast differentiation (GO:0045668), positive regulation of lipid metabolic process (GO:0045834), negative regulation of DNA-templated transcription (GO:0045892), positive regulation of DNA-templated transcription (GO:0045893), positive regulation of fatty acid metabolic process (GO:0045923)

GO Molecular Function (33): transcription cis-regulatory region binding (GO:0000976), RNA polymerase II cis-regulatory region sequence-specific DNA binding (GO:0000978), DNA-binding transcription factor activity, RNA polymerase II-specific (GO:0000981), transcription coregulator binding (GO:0001221), DNA-binding transcription repressor activity, RNA polymerase II-specific (GO:0001227), DNA-binding transcription activator activity, RNA polymerase II-specific (GO:0001228), nucleic acid binding (GO:0003676), DNA binding (GO:0003677), chromatin binding (GO:0003682), double-stranded DNA binding (GO:0003690), DNA-binding transcription factor activity (GO:0003700), nuclear receptor activity (GO:0004879), prostaglandin receptor activity (GO:0004955), zinc ion binding (GO:0008270), enzyme binding (GO:0019899), peptide binding (GO:0042277), identical protein binding (GO:0042802), sequence-specific DNA binding (GO:0043565), nuclear retinoid X receptor binding (GO:0046965), arachidonate binding (GO:0050544), DNA binding domain binding (GO:0050692), LBD domain binding (GO:0050693), WW domain binding (GO:0050699), alpha-actinin binding (GO:0051393), R-SMAD binding (GO:0070412), E-box binding (GO:0070888), STAT family protein binding (GO:0097677), DNA-binding transcription factor binding (GO:0140297), transcription coactivator binding (GO:0001223), protein binding (GO:0005515), protein phosphatase binding (GO:0019903), nuclear estrogen receptor binding (GO:0030331), metal ion binding (GO:0046872)

GO Cellular Component (8): chromatin (GO:0000785), nucleus (GO:0005634), nucleoplasm (GO:0005654), cytosol (GO:0005829), signaling receptor complex (GO:0043235), RNA polymerase II transcription regulator complex (GO:0090575), cytoplasm (GO:0005737), perinuclear region of cytoplasm (GO:0048471)

Reactome top-level categories

Rollup of top-8 pathways:

CategoryPathways
Regulation of lipid metabolism by PPARalpha1
Adipogenesis1
Generic Transcription Pathway1
SUMO E3 ligases SUMOylate target proteins1
PTEN Regulation1
Transcriptional Regulation by MECP21
Transcriptional regulation of brown and beige adipocyte differentiation1
Epigenetic regulation of adipogenesis genes by MLL3 and MLL4 complexes1

GO top-level categories

Rollup of top GO terms by namespace:

CategoryTerms
cellular anatomical structure5
RNA polymerase II transcription regulatory region sequence-specific DNA binding4
DNA-binding transcription factor activity, RNA polymerase II-specific3
binding3
regulation of transcription by RNA polymerase II2
transcription by RNA polymerase II2
regulation of DNA-templated transcription2
gene expression2
regulation of gene expression2
negative regulation of transmembrane receptor protein serine/threonine kinase signaling pathway2
DNA binding2
protein binding2
cytoplasm2
negative regulation of DNA-templated transcription1
animal organ development1
lipid metabolic process1
monocarboxylic acid metabolic process1
response to nutrient levels1
response to chemical1
blood circulation1
regulation of biological quality1
signal transduction1
cellular response to hormone stimulus1
positive regulation of macromolecule biosynthetic process1
negative regulation of macromolecule biosynthetic process1
macrophage derived foam cell differentiation1
regulation of macrophage derived foam cell differentiation1
negative regulation of cell differentiation1
regulation of cholesterol efflux1
positive regulation of cholesterol transport1
cholesterol efflux1
cholesterol storage1
regulation of cholesterol storage1
negative regulation of lipid storage1
regulation of lipid storage1
lipid storage1
negative regulation of cellular process1
negative regulation of lipid localization1
fatty acid transport1
angiogenesis1

Protein interactions and networks

STRING

6959 interactions, top by confidence (×1000):

Protein AProtein BPartner UniProtScore
PPARGPPARGC1AQ9UBK2999
PPARGPRDM16Q9HAZ2996
PPARGXPR1Q9UBH6996
PPARGRXRAP19793987
PPARGNCOR1O75376986
PPARGFABP4P15090983
PPARGSIRT1Q96EB6981
PPARGCTNNB1P35222980
PPARGRELAQ04206976
PPARGCEBPAP49715964
PPARGEP300Q09472963
PPARGMED1Q15648961
PPARGPAX8Q06710946
PPARGINSP01308944
PPARGSREBF1P36956934

IntAct

122 interactions, top by confidence:

ABTypeScore
PPARGHTTpsi-mi:“MI:0915”(physical association)0.670
HTTPPARGpsi-mi:“MI:0915”(physical association)0.670
PPARGRXRApsi-mi:“MI:0914”(association)0.640
PPARGRXRApsi-mi:“MI:0915”(physical association)0.640
PPARGRXRBpsi-mi:“MI:0915”(physical association)0.630
RXRBPPARGpsi-mi:“MI:0915”(physical association)0.630
PPARGPPARGC1Apsi-mi:“MI:0915”(physical association)0.590
PPARGC1APPARGpsi-mi:“MI:0407”(direct interaction)0.590
SIRT1PPARGpsi-mi:“MI:0915”(physical association)0.580
EDF1PPARGpsi-mi:“MI:0915”(physical association)0.580

BioGRID (666): PRKAA1 (Affinity Capture-Western), PRKAA2 (Affinity Capture-Western), PPARG (Affinity Capture-Western), PPARG (Reconstituted Complex), CDC34 (Reconstituted Complex), HDAC3 (Affinity Capture-Western), PPARG (Affinity Capture-Western), PPARG (Biochemical Activity), PPARG (Affinity Capture-Western), RXRA (Reconstituted Complex), PPARG (Affinity Capture-Western), SP1 (Affinity Capture-Western), PPARG (Affinity Capture-Western), CTNNB1 (Affinity Capture-Western), PPARG (Reconstituted Complex)

ESM2 similar proteins: A8XNK6, G5ED47, G5EEM0, G5EGN8, O01929, O01930, O01931, O02235, O02305, O02316, O16391, O17573, O17611, O17657, O17683, O17706, O17748, O17898, O17927, O18086, O18141, O18924, O18971, O19052, O45365, O45436, O45449, O45460, O62389, O62807, O88275, P23204, P37230, P37231, P37238, P57797, Q09565, Q18299, Q21701, Q21806

Diamond homologs: A0JNE3, A0P8Z4, A2T928, A4IIG7, F1QJF4, F1QLY4, O01639, O09018, O18924, O18971, O35507, O62807, O77245, O88275, P10276, P10589, P10826, P11416, P13055, P13056, P13631, P16375, P16376, P17671, P18514, P18515, P18516, P18911, P22448, P22605, P24468, P28699, P31396, P33244, P35398, P37231, P37233, P37238, P41828, P41829

SIGNOR signaling

129 interactions.

AEffectBMechanism
RXRAup-regulatesPPARGbinding
RXRBup-regulatesPPARGbinding
dexamethasoneup-regulatesPPARG
3-isobutyl-1-methylxanthineup-regulatesPPARG
MAPK1“down-regulates quantity by destabilization”PPARGphosphorylation
GATA2“down-regulates activity”PPARG
ESR1“down-regulates quantity by repression”PPARG“transcriptional regulation”
PPARGdown-regulatesHDAC1relocalization
PPARG“down-regulates quantity by repression”CTNNB1“transcriptional regulation”
NCOA2up-regulatesPPARGbinding
MAP2K2up-regulatesPPARGbinding
MAPK1down-regulatesPPARGrelocalization
MAPK3“down-regulates quantity by destabilization”PPARGphosphorylation
MAPK3“down-regulates activity”PPARGrelocalization
PRDM16up-regulatesPPARGbinding
WNT5Bup-regulatesPPARG
WWTR1down-regulatesPPARGbinding
3-isobutyl-1-methyl-7H-xanthineup-regulatesPPARG
KLF2down-regulatesPPARG“transcriptional regulation”
GATA3down-regulatesPPARG“transcriptional regulation”
E2F1up-regulatesPPARG“transcriptional regulation”
E2F4down-regulatesPPARG“transcriptional regulation”
MAPK14up-regulatesPPARG
MAPK1down-regulatesPPARGphosphorylation
ERK1/2“up-regulates activity”PPARGphosphorylation
FGFR2“up-regulates quantity by expression”PPARG“transcriptional regulation”
SMAD1/4“up-regulates quantity by expression”PPARG“transcriptional regulation”
MEK1/2up-regulatesPPARGbinding
STAT6“up-regulates quantity by expression”PPARG“transcriptional regulation”
PPARGup-regulatesM2_polarization

Enriched among interaction partners

Reactome pathways and GO biological processes over-represented among this gene’s 55 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.

Reactome pathways:

PathwayPartnersFoldFDR
RORA,B,C and NR1D1 (REV-ERBA) regulate gene expression654.4×8e-08
Expression of BMAL (ARNTL), CLOCK, and NPAS2745.5×2e-08
NR1H3 & NR1H2 regulate gene expression linked to cholesterol transport and efflux641.1×4e-07
Nuclear Receptor transcription pathway940.1×4e-10
R-HSA-400253538.5×8e-06
Heme signaling733.5×9e-08
Epigenetic regulation of adipogenesis genes by MLL3 and MLL4 complexes523.9×6e-05
Transcriptional activation of mitochondrial biogenesis522.7×8e-05

GO biological processes:

GO termPartnersFoldFDR
retinoic acid receptor signaling pathway672.0×1e-07
mRNA transcription by RNA polymerase II636.7×2e-06
regulation of circadian rhythm524.0×2e-04
protein stabilization67.4×5e-03
positive regulation of gene expression107.2×1e-04
proteasome-mediated ubiquitin-dependent protein catabolic process76.8×3e-03
negative regulation of apoptotic process106.4×2e-04
nervous system development76.0×6e-03

Disease & clinical

Clinical variants and AI predictions

ClinVar

257 variants total. Per-class counts are floors (≥ shown; pagination cap):

ClassificationCount (floor)
Pathogenic18
Likely pathogenic17
Uncertain significance111
Likely benign66
Benign14

Top pathogenic / likely-pathogenic (30)

Variant IDHGVSClassification
1285541NM_138711.6(PPARG):c.530-1G>APathogenic
1686090NM_138711.6(PPARG):c.1181-2A>TPathogenic
1686091NM_138711.6(PPARG):c.1184G>A (p.Arg395His)Pathogenic
2412803NM_138711.6(PPARG):c.258T>G (p.Tyr86Ter)Pathogenic
3024550NM_138711.6(PPARG):c.443T>C (p.Leu148Pro)Pathogenic
3358997NM_138711.6(PPARG):c.221-1G>CPathogenic
3691790NM_138711.6(PPARG):c.1245_1246delinsCT (p.Glu416Ter)Pathogenic
436400NM_138711.6(PPARG):c.924_928del (p.Asp308fs)Pathogenic
436405NM_138711.6(PPARG):c.1271del (p.Pro424fs)Pathogenic
4536742NC_000003.11:g.(12458654_12475396)(12475844?)delPathogenic
8132NM_138711.6(PPARG):c.466del (p.Ser156fs)Pathogenic
8133NM_138711.6(PPARG):c.851A>C (p.Gln284Pro)Pathogenic
8134NM_138711.6(PPARG):c.949A>T (p.Lys317Ter)Pathogenic
8137NM_138711.6(PPARG):c.862G>A (p.Val288Met)Pathogenic
8140NM_138711.6(PPARG):c.464_466delinsT (p.Lys155fs)Pathogenic
8141NM_138711.6(PPARG):c.1074T>A (p.Phe358Leu)Pathogenic
8143NM_138711.6(PPARG):c.478T>A (p.Cys160Ser)Pathogenic
8144NM_138711.6(PPARG):c.490C>T (p.Arg164Trp)Pathogenic
1098721NM_138711.6(PPARG):c.353G>A (p.Gly118Glu)Likely pathogenic
1337735NM_138711.6(PPARG):c.920T>C (p.Leu307Pro)Likely pathogenic
1341578NM_138711.6(PPARG):c.1124T>C (p.Leu375Pro)Likely pathogenic
1675904NM_138711.6(PPARG):c.1063C>T (p.Arg355Ter)Likely pathogenic
1676242NM_138711.6(PPARG):c.841C>T (p.Gln281Ter)Likely pathogenic
1804804NM_138711.6(PPARG):c.-8-28082delLikely pathogenic
3340491NM_138711.6(PPARG):c.346dup (p.Ala116fs)Likely pathogenic
3660512NM_138711.6(PPARG):c.390+1G>ALikely pathogenic
3901178NM_138711.6(PPARG):c.380A>C (p.Glu127Ala)Likely pathogenic
436397NM_138711.6(PPARG):c.491G>A (p.Arg164Gln)Likely pathogenic
436398NM_138711.6(PPARG):c.545G>A (p.Arg182Gln)Likely pathogenic
436399NM_138711.6(PPARG):c.881T>C (p.Ile294Thr)Likely pathogenic

SpliceAI

1864 predictions. Top by Δscore:

VariantEffectΔscore
3:12379699:TTCA:Tacceptor_loss1.0000
3:12379700:TCAG:Tacceptor_loss1.0000
3:12379701:CAGA:Cacceptor_loss1.0000
3:12379702:A:AGacceptor_gain1.0000
3:12379702:A:Cacceptor_loss1.0000
3:12379703:G:Aacceptor_loss1.0000
3:12379703:G:GCacceptor_gain1.0000
3:12379703:GA:Gacceptor_gain1.0000
3:12379703:GAA:Gacceptor_gain1.0000
3:12379703:GAAA:Gacceptor_gain1.0000
3:12379703:GAAAT:Gacceptor_gain1.0000
3:12379903:G:GGdonor_gain1.0000
3:12379932:G:GGdonor_gain1.0000
3:12381317:C:Gacceptor_gain1.0000
3:12381318:A:AGacceptor_gain1.0000
3:12381318:ACAG:Aacceptor_gain1.0000
3:12381320:A:AGacceptor_gain1.0000
3:12381320:AGG:Aacceptor_loss1.0000
3:12381321:G:GGacceptor_gain1.0000
3:12381321:GGT:Gacceptor_gain1.0000
3:12381488:CAAG:Cdonor_loss1.0000
3:12381489:AAGGT:Adonor_loss1.0000
3:12381490:AGGTA:Adonor_loss1.0000
3:12381492:G:GCdonor_loss1.0000
3:12381493:T:Gdonor_loss1.0000
3:12392608:TTGCA:Tacceptor_loss1.0000
3:12392609:TGCA:Tacceptor_loss1.0000
3:12392610:GCA:Gacceptor_loss1.0000
3:12392611:CA:Cacceptor_loss1.0000
3:12392612:A:AGacceptor_gain1.0000

AlphaMissense

0 scored. Top likely-pathogenic:

dbSNP variants (sampled 300 via entrez): RS1000005493 (3:12394077 T>G), RS1000014932 (3:12299368 C>A,T), RS1000050070 (3:12392602 A>G), RS1000072937 (3:12293300 A>T), RS1000101657 (3:12430077 A>G), RS1000110322 (3:12357030 G>A,T), RS1000118469 (3:12342727 T>C), RS1000156529 (3:12385842 G>A), RS1000205914 (3:12369523 A>G), RS1000206701 (3:12405646 C>T), RS1000207210 (3:12325158 C>G), RS1000213685 (3:12387277 T>A), RS1000226053 (3:12367871 C>T), RS1000227753 (3:12394485 C>G), RS1000290570 (3:12412501 A>T)

Disease associations

OMIM: gene MIM:601487 | disease phenotypes: MIM:604367, MIM:151660, MIM:125853, MIM:601665, MIM:137800

GenCC curated gene-disease

DiseaseClassificationInheritance
PPARG-related familial partial lipodystrophyDefinitiveAutosomal dominant
Berardinelli-Seip congenital lipodystrophySupportiveAutosomal recessive

ClinGen Gene-Disease Validity (1)

Expert-panel classifications — Definitive > Strong > Moderate > Limited > Disputed > Refuted.

DiseaseClassificationInheritance
lipodystrophyDefinitiveSD

Mondo (11): PPARG-related familial partial lipodystrophy (MONDO:0011448), familial partial lipodystrophy (MONDO:0020088), obesity disorder (MONDO:0011122), type 2 diabetes mellitus (MONDO:0005148), lipodystrophy (MONDO:0006573), inherited obesity (MONDO:0019182), monogenic diabetes (MONDO:0015967), morbid obesity (MONDO:0005139), colon carcinoma (MONDO:0002032), glioma susceptibility 1 (MONDO:0024498), Berardinelli-Seip congenital lipodystrophy (MONDO:0018883)

Orphanet (6): PPARG-related familial partial lipodystrophy (Orphanet:79083), Familial partial lipodystrophy (Orphanet:98306), Obesity due to melanocortin 4 receptor deficiency (Orphanet:71529), Genetic obesity (Orphanet:77828), Rare genetic diabetes mellitus (Orphanet:183625), NON RARE IN EUROPE: Non rare obesity (Orphanet:521399)

HPO phenotypes

55 total (30 of 55 shown, HPO-id order):

HPOTerm
HP:0000006Autosomal dominant inheritance
HP:0000007Autosomal recessive inheritance
HP:0000147Polycystic ovaries
HP:0000292Loss of facial adipose tissue
HP:0000786Primary amenorrhea
HP:0000819Diabetes mellitus
HP:0000822Hypertension
HP:0000831Insulin-resistant diabetes mellitus
HP:0000842Hyperinsulinemia
HP:0000855Insulin resistance
HP:0000869Secondary amenorrhea
HP:0000876Oligomenorrhea
HP:0000956Acanthosis nigricans
HP:0000963Thin skin
HP:0000991Xanthomatosis
HP:0001007Hirsutism
HP:0001015Prominent superficial veins
HP:0001394Cirrhosis
HP:0001397Hepatic steatosis
HP:0001513Obesity
HP:0001635Congestive heart failure
HP:0001639Hypertrophic cardiomyopathy
HP:0001677Coronary artery atherosclerosis
HP:0001733Pancreatitis
HP:0001744Splenomegaly
HP:0002149Hyperuricemia
HP:0002155Hypertriglyceridemia
HP:0002230Generalized hirsutism
HP:0002240Hepatomegaly
HP:0002621Atherosclerosis

GWAS associations

231 associations (top):

StudyTraitp-value
GCST000024_5Type 2 diabetes2.000000e-06
GCST000025_7Type 2 diabetes2.000000e-06
GCST000028_5Type 2 diabetes2.000000e-06
GCST000167_10Type 2 diabetes2.000000e-07
GCST000712_22Type 2 diabetes2.000000e-07
GCST001526_3Fasting blood insulin (BMI interaction)2.000000e-07
GCST001673_1Drug-induced liver injury2.000000e-08
GCST001684_1Plasminogen activator inhibitor type 1 levels (PAI-1)9.000000e-08
GCST002063_7Sexual dimorphism in anthropometric traits4.000000e-06
GCST002352_25Type 2 diabetes6.000000e-10
GCST002782_248Waist-to-hip ratio adjusted for body mass index5.000000e-14
GCST002782_249Waist-to-hip ratio adjusted for body mass index2.000000e-09
GCST002782_250Waist-to-hip ratio adjusted for body mass index4.000000e-14
GCST002782_251Waist-to-hip ratio adjusted for body mass index6.000000e-10
GCST002783_452Body mass index1.000000e-07
GCST002783_488Body mass index2.000000e-07
GCST002896_17Cholesterol, total9.000000e-12
GCST002898_22LDL cholesterol3.000000e-10
GCST003658_1Modified Stumvoll Insulin Sensitivity Index (model adjusted for BMI)1.000000e-06
GCST003854_55Gut microbiota (functional units)5.000000e-06
GCST004064_23Waist-hip ratio2.000000e-12
GCST004064_72Waist-hip ratio2.000000e-06
GCST004067_185Hip circumference adjusted for BMI2.000000e-10
GCST004067_68Hip circumference adjusted for BMI9.000000e-10
GCST004505_94Waist-to-hip ratio adjusted for BMI (adjusted for smoking behaviour)9.000000e-10
GCST004505_95Waist-to-hip ratio adjusted for BMI (adjusted for smoking behaviour)6.000000e-07
GCST004507_27Waist-to-hip ratio adjusted for BMI (joint analysis main effects and smoking interaction)6.000000e-06
GCST004508_21Waist-to-hip ratio adjusted for BMI in non-smokers2.000000e-06
GCST004567_140Waist-to-hip ratio adjusted for BMI (joint analysis for main effect and physical activity interaction)6.000000e-06
GCST004567_41Waist-to-hip ratio adjusted for BMI (joint analysis for main effect and physical activity interaction)6.000000e-07

EFO canonical traits (44, from GWAS)

EFO IDTrait name
EFO:0004340body mass index
EFO:0004792plasminogen activator inhibitor 1 measurement
EFO:0004343waist-hip ratio
EFO:0005951sexual dimorphism
EFO:0007788BMI-adjusted waist-hip ratio
EFO:0004574total cholesterol measurement
EFO:0004611low density lipoprotein cholesterol measurement
EFO:0004471insulin sensitivity measurement
EFO:0007874gut microbiome measurement
EFO:0008039BMI-adjusted hip circumference
EFO:0004318smoking behavior
EFO:0008002physical activity measurement
EFO:0007991eosinophil percentage of leukocytes
EFO:0004348hematocrit
EFO:0004842eosinophil count
EFO:0004509hemoglobin measurement
EFO:0007996eosinophil percentage of granulocytes
EFO:0007994neutrophil percentage of granulocytes
EFO:0008007age at assessment
EFO:0008343sex interaction measurement
EFO:0004309platelet count
EFO:0004612high density lipoprotein cholesterol measurement
EFO:0009283potassium measurement
EFO:0009270heel bone mineral density
EFO:0009924Drugs used in diabetes use measurement
EFO:0009932HMG CoA reductase inhibitor use measurement
EFO:0009933Thyroid preparation use measurement
EFO:0004329alcohol drinking
EFO:0004517arterial stiffness measurement
EFO:1001930idiopathic osteonecrosis of the femoral head

MeSH disease descriptors (4)

DescriptorNameTree numbers
D003924Diabetes Mellitus, Type 2C18.452.394.750.149; C19.246.300
D008060LipodystrophyC17.800.849.391; C18.452.584.625; C18.452.880.391
D052496Lipodystrophy, Familial PartialC16.320.488.813; C17.800.849.391.700; C18.452.584.563.798; C18.452.584.625.700; C18.452.880.391.700
D009767Obesity, MorbidC18.654.726.750.500.700; C23.888.144.699.500.500

Drugs & pharmacology

Drug and pharmacology data

Is drug target: yes

ChEMBL targets (9): CHEMBL2095161 (PROTEIN-PROTEIN INTERACTION), CHEMBL2095162 (PROTEIN-PROTEIN INTERACTION), CHEMBL2095163 (PROTEIN-PROTEIN INTERACTION), CHEMBL2096976 (PROTEIN-PROTEIN INTERACTION), CHEMBL2111325 (SELECTIVITY GROUP), CHEMBL2111371 (SELECTIVITY GROUP), CHEMBL2111394 (PROTEIN COMPLEX), CHEMBL235 (SINGLE PROTEIN), CHEMBL3559683 (PROTEIN FAMILY)

Molecules with ChEMBL bioactivity

83 molecules (phase ≥1), by development phase (incl. off-target/promiscuous compounds). Patent mentions across the top 20 by phase: 756,003 (via chembl_molecule»patent_compound — counts attach to the compound, not the gene–compound relationship, so off-target/promiscuous molecules can dominate).

MoleculeNamePhasePatents
CHEMBL405110METHYLENE BLUE ANHYDROUS4113,934
CHEMBL388590BENZBROMARONE48,245
CHEMBL1023BEXAROTENE440,951
CHEMBL1715PIOGLITAZONE HYDROCHLORIDE410,091
CHEMBL843ROSIGLITAZONE MALEATE422,589
CHEMBL1014CANDESARTAN CILEXETIL411,194
CHEMBL1017TELMISARTAN427,457
CHEMBL111RIMONABANT415,726
CHEMBL1146CEFAMANDOLE421,886
CHEMBL1159650CLOBETASOL PROPIONATE430,865
CHEMBL121ROSIGLITAZONE458,849
CHEMBL1358FULVESTRANT456,655
CHEMBL1544LIOTHYRONINE423,700
CHEMBL15770SULINDAC480,712
CHEMBL161CEFTRIAXONE471,135
CHEMBL1624LEVOTHYROXINE481,643
CHEMBL1730CEFOTAXIME4480
CHEMBL190461CANNABIDIOL426,379
CHEMBL222559TIPRANAVIR417,513
CHEMBL223228EFAVIRENZ435,999
CHEMBL247951PEMAFIBRATE4
CHEMBL313972MASOPROCOL4
CHEMBL328190LASOFOXIFENE4
CHEMBL3707395ELAFIBRANOR4
CHEMBL404108LUMIRACOXIB4
CHEMBL408TROGLITAZONE4
CHEMBL44354CEFTAZIDIME4
CHEMBL457GEMFIBROZIL4
CHEMBL472GLYBURIDE4
CHEMBL502835NINTEDANIB4

PharmGKB: 1 entry (VIP=true, CPIC=false)

PharmGKB clinical annotations

3 annotations.

VariantTypeLevelDrugsPhenotypes
rs1801282Toxicity3olanzapineSchizophrenia
rs1801282Efficacy3pioglitazoneDiabetes Mellitus;Type 2
rs3856806Toxicity3aspirinAsthma

PharmGKB variants

23 variants.

VariantGenesLevelScore#Clin annotsDrugs
rs709149PPARG0.000
rs1175542PPARG0.000
rs1177809PPARG0.000
rs1797912PPARG0.000
rs1801282PPARG31.252pioglitazone;olanzapine
rs2120825PPARG0.000
rs3856806PPARG35.501aspirin
rs4135247PPARG0.000
rs4135256PPARG0.000
rs4135258PPARG0.000
rs4135268PPARG0.000
rs4135275PPARG0.000
rs6782475PPARG0.000
rs7620165PPARG0.000
rs7645903PPARG0.000
rs7650895PPARG0.000
rs10865710PPARG0.000
rs12629751PPARG0.000
rs17036160PPARG0.000
rs17793693PPARG0.000
rs17036170PPARG0.000
rs2972164PPARG0.000
rs880663PPARG0.000

GtoPdb / IUPHAR curated pharmacology

(IUPHAR/BPS Guide to Pharmacology — expert-curated)

Target class: nhr — 1C. Peroxisome proliferator-activated receptors

Most potent curated ligand interactions (60 total), top 25:

LigandActionAffinityParameter
GW409544Full agonist9.55pEC50
T0070907Antagonist9.0pKi
MRL24Partial agonist9.0pIC50
(R)-16 [PMID: 32267688]Agonist8.8pEC50
GW1929Full agonist8.8pKi
L-796449Full agonist8.7pKi
MRL20Partial agonist8.7pIC50
SB-219994Full agonist8.68pIC50
saroglitazarAgonist8.52pEC50
GW7845Full agonist8.43pKi
GW9662Irreversible inhibition8.1pIC50
LY-510929Full agonist8.0pIC50
bardoxolonePartial agonist8.0pKi
L-783483Full agonist7.85pKi
L-165461Full agonist7.8pKi
AD-5061Full agonist7.7pIC50
AD5075Full agonist7.66pKi
[3H]AD5075Full agonist7.66pKi
compound 10 [O’Mahony et al., 2022]Binding7.62pIC50
farglitazarPartial agonist7.47pKd
edaglitazoneAgonist7.45pEC50
indomethacinPartial agonist7.38pKd
elafibranorAgonist7.33pEC50
TZD18Full agonist7.24pIC50
L-764406Partial agonist7.15pIC50

Binding affinities (BindingDB)

601 measured of 700 human assays (701 total across all organisms); most potent 50 below. Values come from heterogeneous assays and are not directly comparable.

LigandMeasureValuePatent
(2S)-2-[4-chloro-3-[[2,3-dimethyl-5-[[(1S)-1-(3-propan-2-ylphenyl)ethyl]carbamoyl]indol-1-yl]methyl]phenoxy]propanoic acidIC500.06 nMUS-9051265: N-benzylindole modulators of PPARG
2-[4-[[2,3-dimethyl-5-[[(1R)-1-phenylpropyl]carbamoyl]indol-1-yl]methyl]phenyl]benzoic acidIC500.1 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
CHEMBL3317867KD0.11 nM
(2S)-2-[5-[[5-[[(1S)-1-(4-tert-butylphenyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]-2-chlorophenoxy]propanoic acidIC500.2 nMUS-9051265: N-benzylindole modulators of PPARG
(2S)-2-[3-[[5-[[(1S)-1-(4-tert-butylphenyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]-4-chlorophenoxy]propanoic acidIC500.2 nMUS-9051265: N-benzylindole modulators of PPARG
(2S)-2-[3-[[5-[[(1S)-1-(4-bromophenyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]-4-chlorophenoxy]propanoic acidIC500.3 nMUS-9051265: N-benzylindole modulators of PPARG
2-[4-[[5-[[(1R)-1-(4-methoxyphenyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC500.5 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[2,3-dimethyl-5-(2-phenylpropan-2-ylcarbamoyl)indol-1-yl]methyl]phenyl]benzoic acidIC500.5 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
1-[[4-(2-cyanophenyl)phenyl]methyl]-2,3-dimethyl-N-(1-phenylpropyl)indole-5-carboxamideIC500.54 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
(2S)-2-[2-chloro-5-[[2,3-dimethyl-5-[[(1S)-1-(3-propan-2-ylphenyl)ethyl]carbamoyl]indol-1-yl]methyl]phenoxy]propanoic acidIC500.6 nMUS-9051265: N-benzylindole modulators of PPARG
(2S)-2-[2-chloro-5-[[5-[[(1S)-1-(3-cyclopropylphenyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]phenoxy]propanoic acidIC500.6 nMUS-9051265: N-benzylindole modulators of PPARG
(2S)-2-[4-chloro-3-[[5-[[(1S)-1-(3-cyclopropylphenyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]phenoxy]propanoic acidIC500.6 nMUS-9051265: N-benzylindole modulators of PPARG
2-[4-[[5-[[(1R)-1-(4-bromophenyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC500.7 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
(2S)-2-[5-[[5-[[(1S)-1-(4-bromophenyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]-2-chlorophenoxy]propanoic acidIC500.7 nMUS-9051265: N-benzylindole modulators of PPARG
2-[4-[[5-[[(1R)-1-(4-fluorophenyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC500.8 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[2,3-dimethyl-5-[[(1S)-1-phenylbutyl]carbamoyl]indol-1-yl]methyl]phenyl]benzoic acidIC500.8 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[5-[[(1S)-1-(4-methoxyphenyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC500.9 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[2,3-dimethyl-5-(thiophen-2-ylmethylcarbamoyl)indol-1-yl]methyl]phenyl]benzoic acidIC501 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
N-[2-(4-bromophenyl)propan-2-yl]-2,3-dimethyl-1-[(4-phenylphenyl)methyl]indole-5-carboxamideIC501 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[2,3-dimethyl-5-[[(1R)-1-[2-(trifluoromethyl)phenyl]ethyl]carbamoyl]indol-1-yl]methyl]phenyl]benzoic acidIC501 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[5-[[(1S)-1-(2-bromophenyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC501 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
1-[(2,4-difluorophenyl)methyl]-N-(1-phenylpropyl)indole-5-carboxamideIC501 nMUS-9051265: N-benzylindole modulators of PPARG
4’-((5-(benzylcarbamoyl)-2,3-dimethyl-1H-indol-1-yl)methyl)biphenyl-2-carboxylic acidIC501 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
(2S)-2-[5-[[5-[[(1S)-1-(3-tert-butylphenyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]-2-chlorophenoxy]propanoic acidIC501.6 nMUS-9051265: N-benzylindole modulators of PPARG
(2S)-2-[3-[[5-[[(1S)-1-(3-tert-butylphenyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]-4-chlorophenoxy]propanoic acidIC501.6 nMUS-9051265: N-benzylindole modulators of PPARG
2-[4-[[5-[(4-methoxycarbonylphenyl)methylcarbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
4-[3-[[5-(1-phenylpropylcarbamoyl)indol-1-yl]methyl]phenyl]benzoic acidIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[2,3-dimethyl-5-[[(1R)-1-(4-nitrophenyl)ethyl]carbamoyl]indol-1-yl]methyl]phenyl]benzoic acidIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[5-[(3-chlorophenyl)methylcarbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[2,3-dimethyl-5-(1-naphthalen-1-ylethylcarbamoyl)indol-1-yl]methyl]phenyl]benzoic acidIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[3-methyl-5-(1-phenylpropylcarbamoyl)indol-1-yl]methyl]phenyl]benzoic acidIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2,3-dimethyl-1-[(4-phenylphenyl)methyl]-N-[(1S)-1-pyridin-2-ylethyl]indole-5-carboxamideIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
N-[(1R)-1-(3-methoxyphenyl)ethyl]-2,3-dimethyl-1-[(4-phenylphenyl)methyl]indole-5-carboxamideIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
N-[[4-chloro-2-(trifluoromethyl)phenyl]methyl]-2,3-dimethyl-1-[(4-phenylphenyl)methyl]indole-5-carboxamideIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[5-[[(1R)-1-[2-methoxy-4-(trifluoromethyl)phenyl]ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
N-[(1R)-1-[2-chloro-3-(trifluoromethyl)phenyl]ethyl]-2,3-dimethyl-1-[(4-phenylphenyl)methyl]indole-5-carboxamideIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[5-[[(1S)-1-(5-bromo-2-pyridinyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[5-[[(1R)-1-(6-bromo-2-pyridinyl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
4’-((2-methyl-5-(1-phenylpropylcarbamoyl)-1H-indol-1-yl)methyl)biphenyl-2-carboxylic acidIC502 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[2,3-dimethyl-5-[[(1S)-1-phenylpropyl]carbamoyl]indol-1-yl]methyl]phenyl]benzoic acidIC503 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[2,3-dimethyl-5-(4-phenylbutan-2-ylcarbamoyl)indol-1-yl]methyl]phenyl]benzoic acidIC503 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
N-[(1S)-1-(3-chlorophenyl)ethyl]-2,3-dimethyl-1-[(4-phenylphenyl)methyl]indole-5-carboxamideIC503 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[5-[[(1R)-1-(2,3-dihydro-1,4-benzodioxin-3-yl)ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC503 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2,3-dimethyl-1-[(4-phenylphenyl)methyl]-N-[(1R)-1-(2,3,6-trifluorophenyl)ethyl]indole-5-carboxamideIC503 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[2,3-dimethyl-5-[[(1S)-1-(2-methylphenyl)ethyl]carbamoyl]indol-1-yl]methyl]phenyl]benzoic acidIC503 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[5-[[(1S)-1-[2-chloro-5-(trifluoromethyl)phenyl]ethyl]carbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC503 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
1-[(6-chloro-3-pyridinyl)methyl]-N-(1-phenylpropyl)indole-5-carboxamideIC503 nMUS-9051265: N-benzylindole modulators of PPARG
(R)-2-Benzyl-3-(3-(((4-adamantan-1-yl)benzamido)-methyl)-4-propoxyphenyl)propanoic AcidEC503.6 nM
2-[4-[[5-[(4-iodophenyl)methylcarbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC504 nMUS-8957093: N-biphenylmethylindole modulators of PPARG
2-[4-[[5-[(4-chlorophenyl)methylcarbamoyl]-2,3-dimethylindol-1-yl]methyl]phenyl]benzoic acidIC504 nMUS-8957093: N-biphenylmethylindole modulators of PPARG

ChEMBL bioactivities

6100 potent at pChembl≥5 of 6100 total, top 50 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).

pChemblTypeValueUnitMolecule
10.89EC500.01288nMCHEMBL315048
10.83EC500.01479nMCHEMBL86657
10.76EC500.01738nMCHEMBL314483
10.74EC500.018nMCHEMBL1813011
10.42EC500.038nMEFATUTAZONE
10.35EC500.04467nMCHEMBL327481
10.30Ki0.0497nMCHEMBL434063
10.30EC500.05nMCHEMBL1813008
10.22IC500.06nMCHEMBL3678131
10.00EC500.1nMCHEMBL358379
10.00EC500.1nMCHEMBL2282517
10.00Kd0.1nMCHEMBL3317860
10.00IC500.1nMCHEMBL3695832
10.00EC500.1nMCHEMBL230814
9.96Kd0.11nMCHEMBL3317867
9.90EC500.1259nMCHEMBL147384
9.89IC500.13nMCHEMBL3695832
9.80IC500.16nMCHEMBL5191837
9.77Ki0.17nMCHEMBL594625
9.77IC500.17nMCHEMBL5207130
9.72EC500.19nMCHEMBL230705
9.70EC500.2nMCHEMBL410478
9.70IC500.2nMCHEMBL3678128
9.70IC500.2nMCHEMBL3678134
9.66IC500.22nMCHEMBL5187164
9.64IC500.23nMCHEMBL5179281
9.61EC500.2455nMCHEMBL147095
9.60IC500.25nMCHEMBL5206512
9.55EC500.28nMCHEMBL410478
9.55EC500.2818nMCHEMBL2112870
9.54IC500.29nMCHEMBL5207464
9.52IC500.3nMCHEMBL3678133
9.52EC500.3nMCHEMBL388645
9.52EC500.302nMCHEMBL147770
9.51EC500.31nMCHEMBL230707
9.49IC500.32nMCHEMBL5204936
9.47EC500.3388nMFARGLITAZAR
9.47EC500.3388nMCHEMBL2282523
9.47EC500.34nMCHEMBL2282523
9.47EC500.34nMFARGLITAZAR
9.44EC500.36nMCHEMBL230706
9.43IC500.37nMCHEMBL602468
9.42EC500.38nMCHEMBL3585575
9.40Kd0.4nMCHEMBL3317863
9.40IC500.4nMCHEMBL5207130
9.40EC500.4nMCHEMBL422088
9.40Ki0.4nMCHEMBL65805
9.39Kd0.41nMCHEMBL3317865
9.39EC500.41nMCHEMBL4776913
9.37Ki0.43nMCHEMBL4752243

PubChem BioAssay actives

2321 with measured affinity, of 6100 total; 50 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.

CompoundAssayTypeValueUnit
(2R)-2-[[3-[[[4-(azocan-1-yl)benzoyl]amino]methyl]-4-propoxyphenyl]methyl]-3-phenylpropanoic acid1183474: Binding affinity to human His-tagged PPARgamma LBD by SPR methodkd0.0001uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-(5-methyl-2-phenyl-1,3-thiazol-4-yl)ethoxy]phenyl]propanoic acid157126: Tested functionally in vitro for inducing 50% of the maximum alkaline phosphate activity (Transactivation) against Peroxisome proliferator activated receptor gammaec500.0001uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-[2-(4-fluorophenyl)-5-methyl-1,3-oxazol-4-yl]ethoxy]phenyl]propanoic acid157126: Tested functionally in vitro for inducing 50% of the maximum alkaline phosphate activity (Transactivation) against Peroxisome proliferator activated receptor gammaec500.0001uM
(2R)-2-[[3-[[[4-(2-azatricyclo[3.3.1.13,7]decan-2-yl)benzoyl]amino]methyl]-4-propoxyphenyl]methyl]-3-phenylpropanoic acid1183474: Binding affinity to human His-tagged PPARgamma LBD by SPR methodkd0.0001uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-[5-methyl-2-(5-methylthiophen-2-yl)-1,3-oxazol-4-yl]ethoxy]phenyl]propanoic acid157126: Tested functionally in vitro for inducing 50% of the maximum alkaline phosphate activity (Transactivation) against Peroxisome proliferator activated receptor gammaec500.0002uM
2-chloro-N-[2-(4-ethylphenyl)-1,3-benzoxazol-5-yl]-5-nitrobenzamide1858185: Inverse agonist activity at PPARgamma in human RT112/84-FABP4 cells assessed as reduction in PPARgamma transactivation measured by Nanoluciferase reporter gene assayic500.0002uM
2-chloro-N-[2-(3-fluoro-4-methoxyphenyl)-1,3-benzoxazol-5-yl]-5-nitrobenzamide1858185: Inverse agonist activity at PPARgamma in human RT112/84-FABP4 cells assessed as reduction in PPARgamma transactivation measured by Nanoluciferase reporter gene assayic500.0002uM
2-chloro-N-[2-(5-methyl-3-pyridinyl)-1,3-benzoxazol-5-yl]-5-nitrobenzamide1858185: Inverse agonist activity at PPARgamma in human RT112/84-FABP4 cells assessed as reduction in PPARgamma transactivation measured by Nanoluciferase reporter gene assayic500.0002uM
(2S)-2-[2-(cyclohexanecarbonyl)anilino]-3-[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]phenyl]propanoic acid157123: in vitro agonist activity against peroxisome proliferator activated receptor-gamma (PPAR-gamma), using alkaline phosphatase activity transactivator assayec500.0003uM
2-chloro-N-[2-(4-methylphenyl)benzotriazol-5-yl]-5-nitrobenzamide1858185: Inverse agonist activity at PPARgamma in human RT112/84-FABP4 cells assessed as reduction in PPARgamma transactivation measured by Nanoluciferase reporter gene assayic500.0003uM
2-chloro-N-[2-(6-ethyl-3-pyridinyl)-1,3-benzoxazol-5-yl]-5-nitrobenzamide1858185: Inverse agonist activity at PPARgamma in human RT112/84-FABP4 cells assessed as reduction in PPARgamma transactivation measured by Nanoluciferase reporter gene assayic500.0003uM
N-[2-(4-ethylphenyl)-1,3-benzoxazol-5-yl]-2-iodo-5-nitrobenzamide1858185: Inverse agonist activity at PPARgamma in human RT112/84-FABP4 cells assessed as reduction in PPARgamma transactivation measured by Nanoluciferase reporter gene assayic500.0003uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]phenyl]propanoic acid156931: Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay.ec500.0003uM
(2E,4E,6Z)-7-[2-(2,2-difluoroethoxy)-5-(2-fluorophenyl)-3-propan-2-ylphenyl]-3-methylocta-2,4,6-trienoic acid47377: In vitro agonistic activity against PPAR gamma along with 100 nM BRL-49653ec500.0004uM
(2R)-2-benzyl-3-[4-propoxy-3-[[[4-(3,3,5,5-tetramethylpiperidin-1-yl)benzoyl]amino]methyl]phenyl]propanoic acid1183474: Binding affinity to human His-tagged PPARgamma LBD by SPR methodkd0.0004uM
(2R)-2-[[3-[[[4-(9-azabicyclo[3.3.1]nonan-9-yl)benzoyl]amino]methyl]-4-propoxyphenyl]methyl]-3-phenylpropanoic acid1183474: Binding affinity to human His-tagged PPARgamma LBD by SPR methodkd0.0004uM
(2R)-2-[[3-[[[4-(8-azabicyclo[3.2.1]octan-8-yl)benzoyl]amino]methyl]-4-propoxyphenyl]methyl]-3-phenylpropanoic acid1183474: Binding affinity to human His-tagged PPARgamma LBD by SPR methodkd0.0006uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-[2-(4-methoxyphenyl)-5-methyl-1,3-oxazol-4-yl]ethoxy]phenyl]propanoic acid157126: Tested functionally in vitro for inducing 50% of the maximum alkaline phosphate activity (Transactivation) against Peroxisome proliferator activated receptor gammaec500.0006uM
(3E)-2-[[4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]phenyl]methyl]-3-propoxyiminobutanoic acid289933: Agonist activity at human PPARgamma in HepG2 cells by PPAR-GAL4 transactivation assayec500.0006uM
2-chloro-5-nitro-N-(2-phenylimidazo[1,2-a]pyridin-6-yl)benzamide1858185: Inverse agonist activity at PPARgamma in human RT112/84-FABP4 cells assessed as reduction in PPARgamma transactivation measured by Nanoluciferase reporter gene assayic500.0006uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-(1-methyl-4-phenylimidazol-2-yl)ethoxy]phenyl]propanoic acid157270: Inhibition by 50% of in vitro binding to Peroxisome proliferator activated receptor gammaki0.0007uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-(5-methyl-2-morpholin-4-yl-1,3-thiazol-4-yl)ethoxy]phenyl]propanoic acid157270: Inhibition by 50% of in vitro binding to Peroxisome proliferator activated receptor gammaki0.0008uM
(2R)-2-[[3-[[[4-(3-azabicyclo[3.2.1]octan-3-yl)benzoyl]amino]methyl]-4-propoxyphenyl]methyl]-3-phenylpropanoic acid1183474: Binding affinity to human His-tagged PPARgamma LBD by SPR methodkd0.0008uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-[5-methyl-2-(5-methyl-1,2-oxazol-3-yl)-1,3-thiazol-4-yl]ethoxy]phenyl]propanoic acid157270: Inhibition by 50% of in vitro binding to Peroxisome proliferator activated receptor gammaki0.0009uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-(5-methyl-2-pyridin-4-yl-1,3-thiazol-4-yl)ethoxy]phenyl]propanoic acid157270: Inhibition by 50% of in vitro binding to Peroxisome proliferator activated receptor gammaki0.0009uM
(9aS)-8-acetyl-N-[(2-ethyl-4-fluoronaphthalen-1-yl)methyl]-1,7-dihydroxy-3-methoxy-9a-methyl-9-oxodibenzofuran-4-carboxamide666690: Modulation of full-length human pSG5-fused PPARgamma expressed in MG-63 cells co-expressing pGV-P2-PPRE after 24 hrs by luciferase reporter gene based transactivation assayec500.0009uM
2-[2-[[1-(4-methoxybenzoyl)-2-methyl-5-(trifluoromethoxy)indol-3-yl]methyl]phenoxy]propanoic acid241613: In vitro inhibition of human Peroxisome proliferator activated receptor gammaic500.0010uM
2-[5-[2-[2-(3-methoxyphenyl)-5-methyl-1,3-oxazol-4-yl]ethoxy]-2,3-dihydro-1H-inden-1-yl]butanoic acid258092: Activity against PPAR gamma in human by FRET assayec500.0010uM
2-[2-[[1-(4-methoxybenzoyl)-2-methyl-5-(trifluoromethoxy)indol-3-yl]methyl]phenoxy]-2-methylpropanoic acid241613: In vitro inhibition of human Peroxisome proliferator activated receptor gammaic500.0010uM
2-[3-[[1-(4-methoxybenzoyl)-2-methyl-5-(trifluoromethoxy)indol-3-yl]methyl]phenoxy]propanoic acid241613: In vitro inhibition of human Peroxisome proliferator activated receptor gammaic500.0010uM
(2S)-2-[2-chloro-5-[1-(6-chloro-1,2-benzoxazol-3-yl)-2-methyl-5-(trifluoromethoxy)indol-3-yl]oxyphenoxy]propanoic acid242602: Inhibition of human peroxisome proliferator activated receptor gamma bindingic500.0010uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-[5-methyl-2-(3-methylthiophen-2-yl)-1,3-oxazol-4-yl]ethoxy]phenyl]propanoic acid157126: Tested functionally in vitro for inducing 50% of the maximum alkaline phosphate activity (Transactivation) against Peroxisome proliferator activated receptor gammaec500.0010uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-[5-methyl-2-[4-[(2-methylpropan-2-yl)oxycarbonyl]piperazin-1-yl]-1,3-thiazol-4-yl]ethoxy]phenyl]propanoic acid157270: Inhibition by 50% of in vitro binding to Peroxisome proliferator activated receptor gammaki0.0010uM
(2E,4E,6Z)-7-[2-ethoxy-3,5-di(propan-2-yl)phenyl]-3-methylocta-2,4,6-trienoic acid47191: Transcriptional activity against RXR:PPAR-gamma synergy was determined in vitroec500.0010uM
(2S)-3-[4-[2-(2-cyclohexyl-5-methyl-1,3-oxazol-4-yl)ethoxy]phenyl]-2-methyl-2-phenoxypropanoic acid156361: Transcriptional activation of reporter assay by PPAR gamma receptor in CV-1 cellsec500.0010uM
2-[[6-[2-[2-(3-chlorophenyl)-5-methyl-1,3-oxazol-4-yl]ethoxy]-3-pyridinyl]methyl]oxolane-2-carboxylic acid276590: Agonist activity at human PPAR gamma in a HepG2 cells by PPAR-GAL4 transactivation assayec500.0010uM
3-[(1E)-1-[3-fluoro-8-[(2-propylbenzimidazol-1-yl)methyl]-6H-benzo[c][1]benzoxepin-11-ylidene]ethyl]-4H-1,2,4-oxadiazol-5-one1512622: Agonist activity at PPARgamma in human MKN45 cells assessed as induction of cell aggregation incubated for 5 days by Hoechst 33342 staining based IN cell analyzer methodec500.0010uM
3-[(1E)-1-[8-[[7-chloro-2-(methoxymethyl)imidazo[1,2-a]pyridin-3-yl]methyl]-3-fluoro-6H-benzo[c][1]benzoxepin-11-ylidene]ethyl]-4H-1,2,4-oxadiazol-5-one1512622: Agonist activity at PPARgamma in human MKN45 cells assessed as induction of cell aggregation incubated for 5 days by Hoechst 33342 staining based IN cell analyzer methodec500.0010uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-(5-methyl-3-phenylpyrazol-1-yl)ethoxy]phenyl]propanoic acid157126: Tested functionally in vitro for inducing 50% of the maximum alkaline phosphate activity (Transactivation) against Peroxisome proliferator activated receptor gammaec500.0011uM
3-[2-[[3-chloro-5-(trifluoromethyl)-2-pyridinyl]oxy]-4-(2-methoxyethoxy)phenyl]-N-(pentylsulfamoyl)propanamide658316: Transactivation of human PPARgamma1 expressed in CHO-K1 cells co-expressing RXRalpha and PPRE after 1 day by luciferase reporter gene assayec500.0011uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-[5-methyl-2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]ethoxy]phenyl]propanoic acid157126: Tested functionally in vitro for inducing 50% of the maximum alkaline phosphate activity (Transactivation) against Peroxisome proliferator activated receptor gammaec500.0013uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-(5-methyl-1-phenylpyrazol-3-yl)ethoxy]phenyl]propanoic acid157270: Inhibition by 50% of in vitro binding to Peroxisome proliferator activated receptor gammaki0.0013uM
(2S)-2-(2-benzoylanilino)-3-[4-[2-(5-methyl-2-pyridin-4-yl-1,3-oxazol-4-yl)ethoxy]phenyl]propanoic acid157270: Inhibition by 50% of in vitro binding to Peroxisome proliferator activated receptor gammaki0.0014uM
3-[4-[2-[1,3-benzoxazol-2-yl(methyl)amino]ethoxy]phenyl]-2-[(4-benzoylthiophen-3-yl)amino]propanoic acid157119: -log concentration required to induce 50% maximum lipogenic activity against Peroxisome proliferator activated receptor gammaec500.0014uM
3-[(1E)-1-[8-[(7-chloro-2-cyclopropylimidazo[1,2-a]pyridin-3-yl)methyl]-3-fluoro-6H-benzo[c][1]benzoxepin-11-ylidene]ethyl]-4H-1,2,4-oxadiazol-5-one1512622: Agonist activity at PPARgamma in human MKN45 cells assessed as induction of cell aggregation incubated for 5 days by Hoechst 33342 staining based IN cell analyzer methodec500.0014uM
(2S)-3-[4-[2-[1,3-benzoxazol-2-yl(methyl)amino]ethoxy]phenyl]-2-(2-benzoylanilino)propanoic acid157275: In vitro binding to peroxisome proliferator activated receptor gamma (PPAR gamma) using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA)ki0.0015uM
2-chloro-N-[4-(5,6-dimethyl-1,3-benzoxazol-2-yl)phenyl]-5-nitrobenzamide1858185: Inverse agonist activity at PPARgamma in human RT112/84-FABP4 cells assessed as reduction in PPARgamma transactivation measured by Nanoluciferase reporter gene assayic500.0016uM
(2R)-2-[[6-[(2,4-dichlorophenyl)sulfonylamino]-1,3-benzothiazol-2-yl]sulfanyl]octanoic acid1561651: Partial agonist activity at Gal4-fused PPARgamma LBD (unknown origin) expressed in HEK293T cells after 14 to 16 hrs by dual-Glo luciferase assayec500.0016uM
3-[4-[2-[1,3-benzoxazol-2-yl(methyl)amino]ethoxy]phenyl]-2-[2-(2-methoxybenzoyl)anilino]propanoic acid157271: Binding affinity against peroxisome proliferator activated receptor gamma (PPAR-gamma)ki0.0017uM
3-[(1E)-1-[8-[(2-cyclopropyl-7-fluoroimidazo[1,2-a]pyridin-3-yl)methyl]-3-fluoro-6H-benzo[c][1]benzoxepin-11-ylidene]ethyl]-4H-1,2,4-oxadiazol-5-one1512622: Agonist activity at PPARgamma in human MKN45 cells assessed as induction of cell aggregation incubated for 5 days by Hoechst 33342 staining based IN cell analyzer methodec500.0017uM

CTD chemical–gene interactions

630 total (human), top 30 by PubMed support.

ChemicalActions (top 5)PubMed papers
Rosiglitazoneaffects reaction, affects activity, affects expression, affects localization, affects binding (+11 more)110
Troglitazoneaffects reaction, affects cotreatment, increases expression, affects binding, increases abundance (+12 more)59
2-chloro-5-nitrobenzanilidedecreases abundance, affects cotreatment, affects reaction, decreases activity, increases expression (+10 more)32
bisphenol Aincreases activity, affects cotreatment, affects reaction, affects binding, decreases activity (+8 more)30
Pioglitazoneaffects binding, decreases expression, affects reaction, increases expression, decreases reaction (+4 more)29
ciglitazoneaffects binding, increases activity, decreases reaction, increases reaction, increases localization (+4 more)23
Dexamethasonedecreases expression, affects expression, decreases reaction, affects cotreatment, increases expression (+3 more)21
15-deoxy-delta(12,14)-prostaglandin J2decreases expression, increases expression, increases activity, increases localization, increases reaction (+7 more)20
mono-(2-ethylhexyl)phthalateaffects activity, affects binding, decreases expression, increases expression, decreases reaction (+6 more)19
1-Methyl-3-isobutylxanthinedecreases expression, affects expression, decreases response to substance, affects cotreatment, increases expression (+3 more)17
Indomethacindecreases expression, decreases reaction, increases activity, increases expression, affects localization (+4 more)15
Resveratrolaffects binding, decreases activity, decreases reaction, decreases response to substance, increases reaction (+5 more)14
tributyltindecreases reaction, increases expression, affects expression, affects binding, increases activity13
Oleic Acidaffects cotreatment, decreases expression, affects binding, increases activity, increases reaction (+2 more)12
bisphenol A diglycidyl etherdecreases activity, decreases reaction, increases expression, affects binding, increases activity (+4 more)11
perfluorooctanoic acidaffects binding, decreases activity, decreases response to substance, increases activity, affects cotreatment (+2 more)11
Diethylhexyl Phthalateincreases reaction, increases expression, affects binding, decreases activity, increases activity (+4 more)11
tetrabromobisphenol Adecreases reaction, increases response to substance, decreases expression, increases expression, affects binding (+1 more)10
perfluorooctane sulfonic acidaffects expression, affects binding, increases activity, decreases expression, increases expression10
bisphenol Sdecreases reaction, increases expression, increases activity, affects reaction, affects cotreatment (+3 more)10
triphenyl phosphateaffects reaction, affects binding, decreases expression, increases activity, affects cotreatment (+1 more)9
pirinixic aciddecreases reaction, increases expression, increases reaction, affects activity, affects binding (+2 more)9
15-deoxyprostaglandin J2increases reaction, decreases expression, increases response to substance, affects binding, increases abundance (+4 more)9
tetrachlorodianincreases activity, affects binding, decreases reaction8
Estradiolincreases expression, affects binding, decreases activity, affects cotreatment, decreases expression (+3 more)8
butylbenzyl phthalatedecreases reaction, decreases expression, affects binding, increases activity7
Dibutyl Phthalateaffects binding, increases activity, increases expression, affects response to substance7
sodium arseniteaffects cotreatment, increases abundance, decreases expression, increases reaction6
9-deoxy-delta-9-prostaglandin D2decreases activity, decreases reaction, increases expression, affects binding, increases activity (+2 more)6
GW 1929affects binding, decreases reaction, decreases response to substance, increases activity, increases reaction (+1 more)6

ChEMBL screening assays

2033 unique, capped per target: 1593 binding, 380 functional, 56 admet, 3 toxicity, 1 unclassified

Representative assays (with source publication via chembl_document):

Assay IDTypeDescriptionSource paper
CHEMBL1614001FunctionalPUBCHEM_BIOASSAY: Dose response biochemical High Throughput Screening assay for agonists of the steroid receptor coactivator 3 (SRC-3) recruitment by the peroxisome proliferator-activated receptor gamma (PPARgamma). (Class of assay: confirmPubChem BioAssay data set
CHEMBL1613929BindingPUBCHEM_BIOASSAY: TR-FRET dose response biochemical High Throughput Screening assay for agonists of the steroid receptor coactivator 1 (SRC-1) recruitment by the peroxisome proliferator-activated receptor gamma (PPAR gamma): non-selective aPubChem BioAssay data set
CHEMBL4184538ADMETModulatory activity at PPARalpha/PPARgamma in human primary muscle cells assessed as effect on AKR1B1 gene expression at EC50 measured after 24 hrsHighly selective peroxisome proliferator-activated receptor δ (PPARδ) modulator demonstrates improved safety profile compared to GW501516. — Bioorg Med Chem Lett

Cellosaurus cell lines

17 cell lines: 10 cancer cell line, 4 embryonic stem cell, 2 transformed cell line, 1 spontaneously immortalized cell line

First 10 cell lines (id-ordered, not curated):

CellosaurusNameCategorySex
CVCL_A5P0SEES3-1V human PPARG, clone1Embryonic stem cellMale
CVCL_A5P1SEES3-1V human PPARG, clone2Embryonic stem cellMale
CVCL_A5P2SEES3-1V human PPARG, clone3Embryonic stem cellMale
CVCL_B8MXAbcam HCT 116 PPARG KOCancer cell lineMale
CVCL_B9AIAbcam MCF-7 PPARG KOCancer cell lineFemale
CVCL_B9Q6Abcam A-549 PPARG KOCancer cell lineMale
CVCL_BW93ES-R1 CAG-S-hPPARgamma2Embryonic stem cellMale
CVCL_D7Y3Ubigene A-549 PPARG KOCancer cell lineMale
CVCL_D8TJUbigene HCT 116 PPARG KOCancer cell lineMale
CVCL_D9P3Ubigene HEK293 PPARG KOTransformed cell lineFemale

Clinical trials (associated diseases)

300 trials via MONDO — disease-level, not drug-specific.

TrialPhaseStatusTitle
NCT00076362PHASE4COMPLETEDPediatric Hypothalamic Obesity
NCT00079547PHASE4COMPLETEDThe Safety and Effectiveness of Low and High Carbohydrate Diets
NCT00115063PHASE4TERMINATEDLOSS- Louisiana Obese Subjects Study
NCT00134303PHASE4COMPLETEDTrial Comparing Metformin Versus Placebo in Non Alcoholic Steatohepatitis (NASH) Patients Receiving Bariatric Surgery for Obesity
NCT00143936PHASE4COMPLETEDThe Safety and Efficacy of Low and High Carbohydrate Diets
NCT00143962PHASE4COMPLETEDComparison of Two Approaches to Weight Loss Follow-Up Study
NCT00152360PHASE4COMPLETEDThe Effect of Xenical on Weight and Risk Factors
NCT00176306PHASE4COMPLETEDLevofloxacin Pharmacokinetics (PK) in the Severely Obese
NCT00203450PHASE4COMPLETEDZonegran for the Treatment of Weight Gain Associated With Psychotropic Medication Use: A Placebo-Controlled Trial
NCT00205504PHASE4COMPLETEDOral Contraceptives in the Metabolic Syndrome
NCT00229229PHASE4TERMINATEDComparison of 4 Diets in the Management of Overweight Patients With Vascular Disease
NCT00234988PHASE4COMPLETEDA Phase IV, Multi-Center, Open-Label Trial of Sibutramine in Combination With a Hypocaloric Diet in Obese and Overweight Thai Subjects.
NCT00264589PHASE4COMPLETEDExercise Training and Cardiovascular Function in Obesity and in Type 2 Diabetes
NCT00288873PHASE4COMPLETEDCharacterization of Hyperparathyroidism and Vitamin D Deficiency in Obesity
NCT00298857PHASE4TERMINATEDA Pharmacokinetic Study to Compare the Dosing of Valproic Acid in Subjects With Different Body Weights
NCT00315146PHASE4COMPLETEDOptimizing Body Composition for Function in Older Adults
NCT00319202PHASE4TERMINATEDClinical Trial to Assess the Effects of Candesartan on the Carbohydrate Metabolism of Obese Subjects
NCT00327912PHASE4UNKNOWNLaparoscopic Roux-en-Y Gastric Bypass Versus Laparoscopic Biliopancreatic Diversion (BPD)- Duodenal Switch for Superobesity
NCT00352287PHASE4COMPLETEDStudy to Determine the Effects of Human Growth Hormone and Pioglitazone in Overweight, Prediabetic Adults
NCT00353054PHASE4COMPLETEDEffect of Calcium/Vitamin D Supplementation on Body Weight and Fat Loss.
NCT00390637PHASE4COMPLETEDDiet, Obesity and Genes (DiOGenes)
NCT00415688PHASE4COMPLETEDLifestyle Modification for Obesity-Related Type 2 Diabetes
NCT00433641PHASE4COMPLETEDWeight Loss in Response to Sibutramine (MERIDIA) is Influenced by the Inherited Genes
NCT00440375PHASE4COMPLETEDEffects of Rosiglitazone on Bone in Postmenopausal Diabetic Women
NCT00453557PHASE4COMPLETEDMechanism of Growth Hormone Effects on Adipose Tissue
NCT00456885PHASE4COMPLETEDThe Effect of Exenatide on Weight and Hunger in Obese, Healthy Women
NCT00463112PHASE4COMPLETEDEffect of Diet Plus Sibutramine on Hormonal and Metabolic Features in Overweight and Obese Women With PCOS
NCT00512187PHASE4COMPLETEDModerate Weight Loss Makes Obese Patients With Severe Chronic Plaque Psoriasis Responsive to Sub-Optimal Dose of Cyclosporine: an Investigator Blinded, Controlled, Randomized Clinical Trial
NCT00516919PHASE4COMPLETEDStudy of Behavioral Weight Loss Therapy for Obesity and Binge Eating in Monolingual Hispanic Persons
NCT00522470PHASE4COMPLETEDEffects of Rosiglitazone on Serum Ghrelin and Peptide YY Levels
NCT00537810PHASE4COMPLETEDTreatment of Binge Eating in Obese Patients in Primary Care
NCT00538486PHASE4COMPLETEDA Randomized, Double-Blind, Active Control Trial Comparing Effects of Telmisartan, Candesartan and Amlodipine, Alone or Plus Metformin, on Non-Diabetic, Obese Hypertensive Patients
NCT00584389PHASE4TERMINATEDThe Effect of Rimonabant on Energy Expenditure, Fat Metabolism and Body Composition
NCT00585182PHASE4COMPLETEDStudy to Evaluate Weight-based Enoxaparin Dosing in Obese Medical Patients at Risk for DVT
NCT00632840PHASE4COMPLETEDPharmacological Regulation of Fat Transport in Metabolic Syndrome
NCT00636142PHASE4COMPLETEDEffects of Infliximab on Insulin Sensitivity and Beta Cell Function in Insulin Resistant Human Obesity
NCT00675987PHASE4COMPLETEDA Randomized Clinical Trial To Study Losartan On Endothelial Dysfunction and Insulin Resistance In Obese Patients
NCT00694811PHASE4COMPLETEDEffects of Re-Feeding Duration on Weight Maintenance After Weight Loss With Very-Low-Energy Diets (VLEDs)
NCT00699413PHASE4TERMINATEDSupplements for Controlling Resistance to Insulin
NCT00729963PHASE4COMPLETEDSibutramine Versus Continuous Positive Airway Pressure (CPAP)in Obstructive Sleep Apnea (OSA) Patients

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

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Sources 81

This page pulls from 81 datasets indexed by BioBTree:

alphafoldalphamissenseantibodybgeebgee_evidencebindingdbbiogrid_interactionbrendabrenda_kineticsccdscellosauruschembl_activitychembl_assaychembl_documentchembl_moleculechembl_targetciviccivic_evidenceclingen_dosageclingen_gene_validityclinical_trialsclinvarcollectrictd_gene_interactiondbsnpdepmapdiamond_similarityefoensemblentrezesm2_similarityexonfantom5_genefantom5_promotergenccgenerifgogoparentgtopdbgtopdb_interactiongwasgwas_studyhgnchpointactinterprointogenjasparmeshmimmirdbmondomsigdborphanetorthologparalogpatentpatent_compoundpdbpfampharmgkb_clinicalpharmgkb_genepharmgkb_guidelinepharmgkb_variantpubchempubchem_activitypubchem_assaypubmedreactomereactomeparentrefseqrhearnacentralscxa_expressionscxa_gene_experimentsignorspliceaistring_interactiontranscriptufeatureuniprot