Compounds > ly 518674
Page last updated: 2024-10-15

ly 518674

Description

LY 518674: a peroxisome proliferator-activated receptor alpha agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID135449333
CHEMBL ID424133
SCHEMBL ID2669568
MeSH IDM0457997

Synonyms (32)

Synonym
gtpl2658
2-methyl-2-[4-[3-[1-[(4-methylphenyl)methyl]-5-oxo-2h-1,2,4-triazol-3-yl]propyl]phenoxy]propanoic acid
ly-674
ly-518674
ly 518674
2-methyl-2-(4-{3-[1-(4-methyl-benzyl)-5-oxo-4,5-dihydro-1h-[1,2,4]triazol-3-yl]-propyl}-phenoxy)-propionic acid
bdbm50135780
kb-68984
CHEMBL424133 ,
ly518674
2-methyl-2-(4-{3-(1-(4-methylbenzyl)-5-oxo-4,5-dihydro-1h-1,2,4-triazol-3-yl)propyl}phenoxy)propanoic acid
propanoic acid, 2-(4-(3-(2,5-dihydro-1-((4-methylphenyl)methyl)-5-oxo-1h-1,2,4-triazol-3-yl)propyl)phenoxy)-2-methyl-
u8i57rc739 ,
unii-u8i57rc739
425671-29-0
PNHFDVSKDSLUFH-UHFFFAOYSA-N ,
2-[4-[3-[2,5-dihydro-1-[(4-methylphenyl)methyl]-5-oxo-1h-1,2,4-triazol-3-yl]propyl]phenoxy]-2-methyl-propanoic acid
SCHEMBL2669568
DB12988
AKOS032947316
2-methyl-2-[4-[3-[1-(4-methylbenzyl)-5-oxo-4,5-dihydro-1h-1,2,4-triazol-3-yl]propyl]phenoxy]propanoic acid
CS-0004237
HY-50665
Q27083211
2-methyl-2-(4-(3-(1-(4-methylbenzyl)-5-oxo-4,5-dihydro-1h-1,2,4-triazol-3-yl)propyl)phenoxy)propanoic acid
cid 9909438
2-methyl-2-[4-[3-[2-[(4-methylphenyl)methyl]-3-oxo-1h-1,2,4-triazol-5-yl]propyl]phenoxy]propanoic acid
2-methyl-2-[4-[3-[1-[(4-methylphenyl)methyl]-5-oxo-4h-1,2,4-triazol-3-yl]propyl]phenoxy]propanoic acid
MS-27052
2-methyl-2-[4-(3-{1-[(4-methylphenyl)methyl]-5-oxo-2,5-dihydro-1h-1,2,4-triazol-3-yl}propyl)phenoxy]propanoic acid
DTXSID10962564
EX-A5645

Bioavailability

ExcerptReference
" After testing for selective and dual potency, off-target counter screening, metabolic stability, oral bioavailability and associated toxicity, compound 11, the first reported PPARα/δ dual antagonist was chosen for more advanced preclinical evaluation."( Discovery of potent and selective PPARα/δ dual antagonists and initial biological studies.
Baccei, CS; Bravo, Y; Broadhead, A; Chen, A; Correa, L; Fischer, K; Jacintho, JD; Laffitte, B; Lee, C; Lorrain, DS; Messmer, D; Prasit, P; Stebbins, KJ; Stock, NS, 2019)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Peroxisome proliferator-activated receptor gammaHomo sapiens (human)IC50 (µMol)6.50060.00501.205110.0000AID156956; AID665205
Peroxisome proliferator-activated receptor deltaHomo sapiens (human)IC50 (µMol)3.80090.00100.85056.3100AID156773; AID665204
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)IC50 (µMol)0.02400.00050.82696.3100AID156283; AID665203
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Peroxisome proliferator-activated receptor alphaHomo sapiens (human)EC50 (µMol)0.04200.00061.607410.0000AID1140788; AID1535336; AID156131
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (135)

Processvia Protein(s)Taxonomy
negative regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of cholesterol effluxPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
long-chain fatty acid transportPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of osteoblast differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of smooth muscle cell proliferationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of receptor signaling pathway via STATPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of low-density lipoprotein receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of signaling receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of BMP signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of MAP kinase activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of adiponectin secretionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of miRNA transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of cardiac muscle hypertrophy in response to stressPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of connective tissue replacement involved in inflammatory response wound healingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
placenta developmentPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
lipid metabolic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
signal transductionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
G protein-coupled receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
response to nutrientPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of blood pressurePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of gene expressionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
macrophage derived foam cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of macrophage derived foam cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of cholesterol storagePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of lipid storagePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of sequestering of triglyceridePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of angiogenesisPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
monocyte differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
BMP signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
epithelial cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cellular response to insulin stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
response to lipidPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
peroxisome proliferator activated receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
glucose homeostasisPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of circadian rhythmPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
mRNA transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
lipoprotein transportPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of blood vessel endothelial cell migrationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
innate immune responsePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cell fate commitmentPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of fat cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of DNA-templated transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of DNA-templated transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
retinoic acid receptor signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cell maturationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
rhythmic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
white fat cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of DNA-binding transcription factor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
lipid homeostasisPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of type II interferon-mediated signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of SMAD protein signal transductionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of cholesterol transporter activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cellular response to low-density lipoprotein particle stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cellular response to hypoxiaPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of mitochondrial fissionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
regulation of cellular response to insulin stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of extracellular matrix assemblyPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of miRNA transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of miRNA transcriptionPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of cellular response to transforming growth factor beta stimulusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of adipose tissue developmentPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of vascular associated smooth muscle cell proliferationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of vascular associated smooth muscle cell apoptotic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of vascular endothelial cell proliferationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
positive regulation of fatty acid metabolic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
fatty acid metabolic processPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of inflammatory responsePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cell differentiationPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
hormone-mediated signaling pathwayPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
glucose metabolic processPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
generation of precursor metabolites and energyPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
lipid metabolic processPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
fatty acid beta-oxidationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
apoptotic processPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
embryo implantationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
cholesterol metabolic processPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
cell population proliferationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
axon ensheathmentPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
fatty acid catabolic processPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
positive regulation of gene expressionPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
regulation of skeletal muscle satellite cell proliferationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
fatty acid transportPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
intracellular receptor signaling pathwayPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
cell-substrate adhesionPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
cellular response to nutrient levelsPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
wound healingPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
steroid hormone mediated signaling pathwayPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
positive regulation of skeletal muscle tissue regenerationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
phosphatidylinositol 3-kinase/protein kinase B signal transductionPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
keratinocyte proliferationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
positive regulation of fat cell differentiationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
negative regulation of myoblast differentiationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
negative regulation of DNA-templated transcriptionPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
positive regulation of DNA-templated transcriptionPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
decidualizationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
negative regulation of epithelial cell proliferationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
keratinocyte migrationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
adipose tissue developmentPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
fat cell proliferationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
positive regulation of fat cell proliferationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
cellular response to hypoxiaPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
energy homeostasisPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
apoptotic signaling pathwayPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
negative regulation of miRNA transcriptionPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
glucose transmembrane transportPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
positive regulation of myoblast proliferationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
positive regulation of fatty acid metabolic processPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
fatty acid metabolic processPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
negative regulation of cholesterol storagePeroxisome proliferator-activated receptor deltaHomo sapiens (human)
cell differentiationPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
negative regulation of inflammatory responsePeroxisome proliferator-activated receptor deltaHomo sapiens (human)
hormone-mediated signaling pathwayPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
negative regulation of cytokine production involved in inflammatory responsePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of reactive oxygen species biosynthetic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of hepatocyte apoptotic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of signaling receptor activityPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of ATP biosynthetic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of transformation of host cell by virusPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
response to hypoxiaPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
gluconeogenesisPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
heart developmentPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
response to nutrientPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
epidermis developmentPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
cellular response to starvationPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
regulation of cellular ketone metabolic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of macrophage derived foam cell differentiationPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of cholesterol storagePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of sequestering of triglyceridePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
regulation of fatty acid metabolic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
intracellular receptor signaling pathwayPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of fatty acid beta-oxidationPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of appetitePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
response to insulinPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
circadian regulation of gene expressionPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
behavioral response to nicotinePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
wound healingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
lipoprotein metabolic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
regulation of circadian rhythmPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
steroid hormone mediated signaling pathwayPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
response to ethanolPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of gluconeogenesisPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of blood pressurePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of glycolytic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of DNA-templated transcriptionPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
nitric oxide metabolic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of fatty acid oxidationPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of lipid biosynthetic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of inflammatory responsePeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of cell growth involved in cardiac muscle cell developmentPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
enamel mineralizationPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
cellular response to fructose stimulusPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of miRNA transcriptionPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
negative regulation of leukocyte cell-cell adhesionPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
regulation of fatty acid transportPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
hormone-mediated signaling pathwayPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
fatty acid metabolic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
positive regulation of fatty acid metabolic processPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
cell differentiationPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (42)

Processvia Protein(s)Taxonomy
transcription cis-regulatory region bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
transcription coregulator bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleic acid bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
chromatin bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
double-stranded DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription factor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nuclear receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
prostaglandin receptor activityPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
protein bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
zinc ion bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
enzyme bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
peptide bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
identical protein bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
sequence-specific DNA bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nuclear retinoid X receptor bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
arachidonic acid bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA binding domain bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
LBD domain bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
alpha-actinin bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
R-SMAD bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
E-box bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
STAT family protein bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription factor bindingPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
transcription coactivator bindingPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
DNA bindingPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
DNA-binding transcription factor activityPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
nuclear steroid receptor activityPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
nuclear receptor activityPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
protein bindingPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
zinc ion bindingPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
lipid bindingPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
linoleic acid bindingPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
DNA-binding transcription factor bindingPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
sequence-specific double-stranded DNA bindingPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA-binding transcription activator activityPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
transcription coactivator bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA-binding transcription factor activityPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
nuclear steroid receptor activityPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
nuclear receptor activityPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
protein bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
zinc ion bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
lipid bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
phosphatase bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
protein domain specific bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
mitogen-activated protein kinase kinase kinase bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
ubiquitin conjugating enzyme bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
sequence-specific DNA bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
protein-containing complex bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
NFAT protein bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
MDM2/MDM4 family protein bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
DNA-binding transcription factor bindingPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (7)

Processvia Protein(s)Taxonomy
nucleusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleusPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleoplasmPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
cytosolPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
intracellular membrane-bounded organellePeroxisome proliferator-activated receptor gammaHomo sapiens (human)
RNA polymerase II transcription regulator complexPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
chromatinPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
receptor complexPeroxisome proliferator-activated receptor gammaHomo sapiens (human)
nucleusPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
nucleusPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
nucleoplasmPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
chromatinPeroxisome proliferator-activated receptor deltaHomo sapiens (human)
nucleusPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
nucleoplasmPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
chromatinPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
nucleusPeroxisome proliferator-activated receptor alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (15)

Assay IDTitleYearJournalArticle
AID1535336Agonist activity at human PPARalpha2019Bioorganic & medicinal chemistry letters, 02-01, Volume: 29, Issue:3
Discovery of potent and selective PPARα/δ dual antagonists and initial biological studies.
AID665205Agonist activity at PPARgamma2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Activity landscape modeling of PPAR ligands with dual-activity difference maps.
AID115859Compound was evaluated in human apoA-I transgenic mice for maximal percent increase in HDL-cholesterol2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
AID665203Agonist activity at PPARalpha2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Activity landscape modeling of PPAR ligands with dual-activity difference maps.
AID156131Cotransfection activity against human Peroxisome proliferator activated receptor alpha2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
AID114821Compound was evaluated in human apoA-I transgenic mice for its ability to alter serum triglyceride2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
AID156948Cotransfection activity of compound against human Peroxisome proliferator activated receptor gamma was determined at 10 uM2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
AID665204Agonist activity at PPARdelta2012Bioorganic & medicinal chemistry, Jun-01, Volume: 20, Issue:11
Activity landscape modeling of PPAR ligands with dual-activity difference maps.
AID1140788Agonist activity at human PPAR-alpha2014Bioorganic & medicinal chemistry letters, May-15, Volume: 24, Issue:10
Identification of the first potent, selective and bioavailable PPARα antagonist.
AID156773Inhibitory activity of compound against the binding of human Peroxisome proliferator activated receptor delta was determined2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
AID156618Cotransfection activity of compound against human Peroxisome proliferator activated receptor delta was determined at 10 uM2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
AID156956Inhibitory activity of compound against the binding of human Peroxisome proliferator activated receptor gamma was determined2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
AID156283Inhibitory activity against human Peroxisome proliferator activated receptor alpha2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
AID114820Compound was evaluated in human apoA-I transgenic mice for its ability to alter HDL-cholesterol levels2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
AID1346733Human Peroxisome proliferator-activated receptor-alpha (1C. Peroxisome proliferator-activated receptors)2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (12)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's7 (58.33)29.6817
2010's5 (41.67)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials3 (25.00%)5.53%
Reviews1 (8.33%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other8 (66.67%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
niacin
Niacin: A water-soluble vitamin of the B complex occurring in various animal and plant tissues. It is required by the body for the formation of coenzymes NAD and NADP. It has PELLAGRA-curative, vasodilating, and antilipemic properties.. vitamin B3 : Any member of a group of vitamers that belong to the chemical structural class called pyridines that exhibit biological activity against vitamin B3 deficiency. Vitamin B3 deficiency causes a condition known as pellagra whose symptoms include depression, dermatitis and diarrhea. The vitamers include nicotinic acid and nicotinamide (and their ionized and salt forms).. nicotinic acid : A pyridinemonocarboxylic acid that is pyridine in which the hydrogen at position 3 is replaced by a carboxy group.		2.0510pyridine alkaloid;
pyridinemonocarboxylic acid;
vitamin B3		antidote;
antilipemic drug;
EC 3.5.1.19 (nicotinamidase) inhibitor;
Escherichia coli metabolite;
human urinary metabolite;
metabolite;
mouse metabolite;
plant metabolite;
vasodilator agent
fenofibrate
Pharmavit: a polyvitamin product, comprising vitamins A, D2, B1, B2, B6, C, E, nicotinamide, & calcium pantothene; may be a promising agent for application to human populations exposed to carcinogenic and genetic hazards of ionizing radiation; RN from CHEMLINE		6.4652aromatic ether;
chlorobenzophenone;
isopropyl ester;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
gemfibrozil
[no description available]		2.4520aromatic etherantilipemic drug
pioglitazone
Pioglitazone: A thiazolidinedione and PPAR GAMMA agonist that is used in the treatment of TYPE 2 DIABETES MELLITUS.. pioglitazone : A member of the class of thiazolidenediones that is 1,3-thiazolidine-2,4-dione substituted by a benzyl group at position 5 which in turn is substituted by a 2-(5-ethylpyridin-2-yl)ethoxy group at position 4 of the phenyl ring. It exhibits hypoglycemic activity.		2.0510aromatic ether;
pyridines;
thiazolidinediones		antidepressant;
cardioprotective agent;
EC 2.7.1.33 (pantothenate kinase) inhibitor;
EC 6.2.1.3 (long-chain-fatty-acid--CoA ligase) inhibitor;
ferroptosis inhibitor;
geroprotector;
hypoglycemic agent;
insulin-sensitizing drug;
PPARgamma agonist;
xenobiotic
tyrosine
Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.		2.110amino acid zwitterion;
erythrose 4-phosphate/phosphoenolpyruvate family amino acid;
L-alpha-amino acid;
proteinogenic amino acid;
tyrosine		EC 1.3.1.43 (arogenate dehydrogenase) inhibitor;
fundamental metabolite;
micronutrient;
nutraceutical
pyrroles
1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.		5.7722pyrrole;
secondary amine
oxazoles
Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom.		2.1101,3-oxazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
thiazoles
[no description available]		2.05101,3-thiazoles;
mancude organic heteromonocyclic parent;
monocyclic heteroarene
deuterium
Deuterium: The stable isotope of hydrogen. It has one neutron and one proton in the nucleus.		3.4311dihydrogen
bezafibrate
[no description available]		2.4520aromatic ether;
monocarboxylic acid amide;
monocarboxylic acid;
monochlorobenzenes		antilipemic drug;
environmental contaminant;
geroprotector;
xenobiotic
atorvastatin
[no description available]		5.7722aromatic amide;
dihydroxy monocarboxylic acid;
monofluorobenzenes;
pyrroles;
statin (synthetic)		environmental contaminant;
xenobiotic
fenofibric acid
fenofibric acid: RN given refers to parent cpd without isomeric designation; structure. fenofibric acid : A monocarboxylic acid that is 2-methylpropanoic acid substituted by a 4-(4-chlorobenzoyl)phenoxy group at position 2. It is a metabolite of the drug fenofibrate.		2.0110aromatic ketone;
chlorobenzophenone;
monocarboxylic acid		drug metabolite;
marine xenobiotic metabolite
triazoles
Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.		8.891141,2,3-triazole
gw 409544
GW 409544: a PPARalpha agonist; structure in first source		2.110monocarboxylic acid
gw 7647
GW 7647: a PPAR-alpha agonist; structure in first source. GW 7647 : A monocarboxylic acid that is 2-(phenylsulfanyl)isobutyric acid in which the phenyl group is substituted at the para- position by a 3-aza-7-cyclohexylhept-1-yl group in which the nitrogen is acylated by a (cyclohexylamino)carbonyl group.		2.110aryl sulfide;
monocarboxylic acid;
ureas		PPARalpha agonist
gw 501516
GW 501516: a selective PPARdelta agonist; structure in first source. GW 501516 : An aromatic ether that is phenoxyacetic acid in which the phenyl group is substituted at position 2 by a methyl group and at position 4 by a (1,3-thiazol-5-ylmethyl)sulfanediyl group, and in which the 1,3-thiazolyl group is substituted at positions 2 and 4 by p-trifluoromethylphenyl and methyl groups, respectively.		2.46201,3-thiazoles;
aromatic ether;
aryl sulfide;
monocarboxylic acid;
organofluorine compound		carcinogenic agent;
PPARbeta/delta agonist
bms201038
BMS201038: an anticholesteremic agent and microsomal triglycide transfer protein inhibitor. lomitapide : A member of the class of benzamides obtained by formal condensation of the carboxy group of 4'-(trifluoromethyl)biphenyl-2-carboxylic acid with the primary amino group of 9-[4-(4-aminopiperidin-1-yl)butyl]-N-(2,2,2-trifluoroethyl)-9H-fluorene-9-carboxamide. Used (as its mesylate salt) as a complement to a low-fat diet and other lipid-lowering treatments in patients with homozygous familial hypercholesterolemia.		2.0510(trifluoromethyl)benzenes;
benzamides;
fluorenes;
piperidines		anticholesteremic drug;
MTP inhibitor
gw 9578
GW 9578: a peroxisome proliferator-activated receptor alpha agonist; structure in first source		2.0110
naveglitazar
naveglitazar: LY-519818 is the (alpha-S)-isomer; an antidiabetic agent; structure in first source		2.0710aromatic ether
l 796449
L 796449: a peroxisomal proliferator-activated receptor-gamma agonist; structure in first source		2.0710
3-chloro-4-(3-(7-propyl-3-trifluoromethyl-6-benzisoxazolyl)propylthio)phenylacetic acid
[no description available]		2.0710
ConditionIndicatedRelationship StrengthStudiesTrials
Experimental Neoplasms
[description not available]		02.2110
Cancer of Ovary
[description not available]		02.2110
Ovarian Neoplasms
Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.		02.2110
Cardiometabolic Syndrome
A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components not only include metabolic dysfunctions of METABOLIC SYNDROME but also HYPERTENSION, and ABDOMINAL OBESITY.		04.4222
Metabolic Syndrome
A cluster of symptoms that are risk factors for CARDIOVASCULAR DISEASES and TYPE 2 DIABETES MELLITUS. The major components of metabolic syndrome include ABDOMINAL OBESITY; atherogenic DYSLIPIDEMIA; HYPERTENSION; HYPERGLYCEMIA; INSULIN RESISTANCE; a proinflammatory state; and a prothrombotic (THROMBOSIS) state.		16.4222
Dyslipidemia
[description not available]		07.6454
Cardiovascular Diseases
Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.		02.0510
Dyslipidemias
Abnormalities in the serum levels of LIPIDS, including overproduction or deficiency. Abnormal serum lipid profiles may include high total CHOLESTEROL, high TRIGLYCERIDES, low HIGH DENSITY LIPOPROTEIN CHOLESTEROL, and elevated LOW DENSITY LIPOPROTEIN CHOLESTEROL.		07.6454
Elevated Cholesterol
[description not available]		07.4644
Hypercholesterolemia
A condition with abnormally high levels of CHOLESTEROL in the blood. It is defined as a cholesterol value exceeding the 95th percentile for the population.		19.4644
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