PPARs are transcription factors that govern lipid and glucose homeostasis and play a central role in cardiovascular disease, obesity, and diabetes. Thus, there is significant interest in developing new agonists for these receptors. Given that the introduction of fluorine generally has a profound effect on the physical and/or biological properties of the target molecule, we synthesized a series of more ..
Target
Tested Compounds:
Description:
Title: Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptors ##/## dual agonists.
Abstract: PPARs are transcription factors that govern lipid and glucose homeostasis and play a central role in cardiovascular disease, obesity, and diabetes. Thus, there is significant interest in developing new agonists for these receptors. Given that the introduction of fluorine generally has a profound effect on the physical and/or biological properties of the target molecule, we synthesized a series of fluorinated analogs of the previously reported compound 2, some of which turned out to be remarkable PPAR## and PPAR## dual agonists. Docking experiments were also carried out to gain insight into the interactions of the most active derivatives with both receptors.
(PMID: 22341573)
Abstract: PPARs are transcription factors that govern lipid and glucose homeostasis and play a central role in cardiovascular disease, obesity, and diabetes. Thus, there is significant interest in developing new agonists for these receptors. Given that the introduction of fluorine generally has a profound effect on the physical and/or biological properties of the target molecule, we synthesized a series of fluorinated analogs of the previously reported compound 2, some of which turned out to be remarkable PPAR## and PPAR## dual agonists. Docking experiments were also carried out to gain insight into the interactions of the most active derivatives with both receptors.
(PMID: 22341573)
Categorized Comment
ChEMBL Assay Type: Binding
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 133
ChEMBL target type: Target is a single protein chain
ChEMBL Assay Data Source: Scientific Literature
ChEMBL Target ID: 133
ChEMBL target type: Target is a single protein chain
Result Definitions
| TID | Name | Description | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||
| 1 | Emax activity comment | Emax activity comment | String | |||
| 2 | Emax standard flag | Emax standard flag |  | Integer | ||
| 3 | Emax qualifier | Emax qualifier | String | |||
| 4 | Emax published value | Emax published value | | Float | % | |
| 5 | Emax standard value | Emax standard value | | Float | % |
Data Table (Concise)
Classification
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