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BioAssay: AID 757816

Transactivation of PPARdelta (unknown origin) relative to control

In this study we present the design, synthesis and biological evaluation of a small, first-generation library of small molecule aromatic amides based on the arylopeptoid skeleton. The compounds were efficiently synthesized using a highly convenient submonomer solid-phase methodology which potentially allows for access to great product diversity. The synthesized compounds were tested for their more ..
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 Tested Compounds
 Tested Compounds
All(3)
 
 
Unspecified(3)
 
 
 Tested Substances
 Tested Substances
All(3)
 
 
Unspecified(3)
 
 
 Related BioAssays
 Related BioAssays
AID: 757816
Data Source: ChEMBL (970841)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2014-05-03
Modify Date: 2014-08-24

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Peroxisome proliferator-activated receptor delta; Short=PPAR-delta; AltName: Full=NUCI; AltName: Full=Nuclear hormone receptor 1; Short=NUC1; AltName: Full=Nuclear receptor subfamily 1 group C member 2; AltName: Full=Peroxisome proliferator-activated receptor beta; Short=PPAR-beta
Description ..   
Protein Family: The ligand binding domain of peroxisome proliferator-activated receptors
Comment ..   

Gene:PPARD     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Discovery of new PPARgamma agonists based on arylopeptoids.

Abstract: In this study we present the design, synthesis and biological evaluation of a small, first-generation library of small molecule aromatic amides based on the arylopeptoid skeleton. The compounds were efficiently synthesized using a highly convenient submonomer solid-phase methodology which potentially allows for access to great product diversity. The synthesized compounds were tested for their ability to activate peroxisome proliferator-activated receptors (PPARs) and they all acted as PPARgamma agonists in the muM range spanning from 2.5- to 14.7-fold activation of the receptor. This is the first discovery of bioactive molecules based on the arylopeptoid architecture.
(PMID: 23731946)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1FC activity commentFC activity commentString
2FC standard flagFC standard flagInteger
3FC qualifierFC qualifierString
4FC published valueFC published valueFloat
5FC standard valueFC standard valueFloat

Data Table (Concise)
Data Table ( Complete ):     View All Data
Classification
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