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BioAssay: AID 639118

Toxicity in high-fat diet fed dog assessed as change in body weight at 0.003 mg/kg, po administered QD for 1 week (Rvb = 14.8 +/- 0.7 kg)

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
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 639118
Data Source: ChEMBL (796566)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-05-25

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Tested Compound:
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)
Comment
Putative Target:

ChEMBL Target ID: 50588
Target Type: ORGANISM
Pref Name: Canis familiaris
Organism: Canis lupus familiaris
Tax ID: 9615
Confidence: Target assigned is non-molecular
Relationship Type: Non-molecular target assigned
Categorized Comment
Assay Type: ADME

Assay Data Source: Scientific Literature

BAO: Assay Format: organism-based format

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

Data Table (Concise)
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