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BioAssay: AID 666808

Modulation of human GAL4-fused PPARalpha LBD expressed in COS7 cells co-expressing pG5luc at 10 uM by luciferase reporter gene based transactivation assay

Selective peroxisome proliferator-activated receptor gamma (PPARgamma) modulators are expected to be a novel class of drugs improving plasma glucose levels without PPARgamma-related adverse effects. As a continuation of our studies for (-)-Cercosporamide derivatives as selective PPARgamma modulators, we synthesized substituted naphthalene type compounds and identified the most potent compound 15 more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Inactive(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Inactive(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 666808
Data Source: ChEMBL (823931)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-05-16
Modify Date: 2013-11-17

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Peroxisome proliferator-activated receptor alpha; Short=PPAR-alpha; AltName: Full=Nuclear receptor subfamily 1 group C member 1
Description ..   
Protein Family: The ligand binding domain of peroxisome proliferator-activated receptors
Comment ..   

Gene:PPARA     Related Protein 3D Structures     More BioActivity Data..
Tested Compound:
Description:
Title: Synthesis and biological evaluation of novel (-)-Cercosporamide derivatives as potent selective PPARgamma modulators.

Abstract: Selective peroxisome proliferator-activated receptor gamma (PPARgamma) modulators are expected to be a novel class of drugs improving plasma glucose levels without PPARgamma-related adverse effects. As a continuation of our studies for (-)-Cercosporamide derivatives as selective PPARgamma modulators, we synthesized substituted naphthalene type compounds and identified the most potent compound 15 (EC(50) = 0.94 nM, E(max) = 38%). Compound 15 selectively activated PPARgamma transcription and did not activate PPARalpha and PPARdelta. The potassium salt of compound 15 showed a high solubility and a good oral bioavailability (58%). Oral administration of the potassium salt remarkably improved the plasma glucose levels of female Zucker diabetic fatty rats at 1 mg/kg. Moreover, it did not cause a plasma volume increase or a cardiac enlargement in Wistar-Imamichi rats, even at 100 mg/kg.
(PMID: 22727448)
Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 163

ChEMBL Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat
5Activity standard valueActivity standard valueFloat

Data Table (Concise)
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