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
Target
BioActive Compounds: 25
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
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
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
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 163
ChEMBL target type: Target is a single protein chain
Result Definitions
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| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | EC50* | EC50 PubChem standard value |  | Float | μM | |
| 2 | BEI | Binding Efficiency Index(nM) | | Float | ||
| 3 | SEI | Surface Efficiency Index(nM) | | Float | ||
| 4 | EC50 activity comment | EC50 activity comment | String | |||
| 5 | EC50 standard flag | EC50 standard flag | | Integer | ||
| 6 | EC50 qualifier | EC50 qualifier | String | |||
| 7 | EC50 published value | EC50 published value | | Float | nM | |
| 8 | EC50 standard value | EC50 standard value | | Float | nM | |
| 9 | EC50 binding domains | EC50 binding domains | String |
* Activity Concentration.
Data Table (Concise)
Classification
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