A series of novel cyclic amine-substituted benzoic acid derivatives were synthesized and evaluated for their PPAR## 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 PPAR## agonist. (S)-4f showed excellent PK profile and oral administration of (S)-4f to high-fat diet dogs effectively lowered triglycerides. ..more
Tested Compound:
Description:
Title: Discovery of cyclic amine-substituted benzoic acids as PPAR## agonists.
Abstract: A series of novel cyclic amine-substituted benzoic acid derivatives were synthesized and evaluated for their PPAR## 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 PPAR## agonist. (S)-4f showed excellent PK profile and oral administration of (S)-4f to high-fat diet dogs effectively lowered triglycerides.
(PMID: 22133631)
Abstract: A series of novel cyclic amine-substituted benzoic acid derivatives were synthesized and evaluated for their PPAR## 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 PPAR## 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
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
ChEMBL Assay Type: Functional
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Assay Data Source: Scientific Literature
Result Definitions
| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | Activity activity comment | Activity activity comment | String | |||
| 2 | Activity standard flag | Activity standard flag |  | Integer | ||
| 3 | Activity qualifier | Activity qualifier | String | |||
| 4 | Activity published value | Activity published value | | Float | mg/dl | |
| 5 | Activity standard value | Activity standard value | | Float | mg/dl |
Data Table (Concise)
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