Bookmark and Share
BioAssay: AID 639124

Transactivation of human PPARdelta expressed in CHO-K1 cells at 30 uM

A series of novel cyclic amine-substituted benzoic acid derivatives were synthesized and evaluated for their PPARalpha agonist activity. Strucure-activity relationship studies led to the identification of (S)-3-[3-[2-(4-chlorophenyl)-4-methylthyazole-5-carboxamido]piperidin-1-yl]benzoic acid (S)-4f (KRP-105) as a potent and high subtype-selective human PPARalpha agonist. (S)-4f showed excellent PK profile and oral administration of (S)-4f to high-fat diet dogs effectively lowered triglycerides. ..more
_
   
 Tested Compounds
 Tested Compounds
All(4)
 
 
Inactive(4)
 
 
 Tested Substances
 Tested Substances
All(4)
 
 
Inactive(4)
 
 
 Related BioAssays
 Related BioAssays
AID: 639124
Data Source: ChEMBL (796572)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-05-25

Data Table ( Complete ):           All
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 cyclic amine-substituted benzoic acids as PPARalpha agonists.

Abstract: A series of novel cyclic amine-substituted benzoic acid derivatives were synthesized and evaluated for their PPARalpha agonist activity. Strucure-activity relationship studies led to the identification of (S)-3-[3-[2-(4-chlorophenyl)-4-methylthyazole-5-carboxamido]piperidin-1-yl]benzoic acid (S)-4f (KRP-105) as a potent and high subtype-selective human PPARalpha agonist. (S)-4f showed excellent PK profile and oral administration of (S)-4f to high-fat diet dogs effectively lowered triglycerides.
(PMID: 22133631)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: cell-based format

Assay Cell Type: CHO-K1

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50 activity commentEC50 activity commentString
2EC50 standard flagEC50 standard flagInteger
3EC50 qualifierEC50 qualifierString
4EC50 published valueEC50 published valueFloat
5EC50 standard valueEC50 standard valueFloat

Data Table (Concise)
PageFrom: