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BioAssay: AID 635193

Induction of [14C]oleic acid oxidation in a human myotubes after 4 days by beta liquid scintillation counting

(#)-2-Fluoro-2-(2-methyl-4-(((4-methyl-2-(4-(trifluoromethyl)phenyl)thiazol-5-yl)methyl)thio)phenoxy)acetic acid (2a) has been prepared and subjected to biological testing against all three subtypes of the PPARs. This compound exhibited agonist effects with EC(50) values of 560 and 55 nM against PPARalpha and PPARdelta, respectively, in a luciferase assay. Moreover, compound (#)-2a also exhibited more ..
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 Tested Compounds
 Tested Compounds
All(6)
 
 
Active(4)
 
 
Inconclusive(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(6)
 
 
Active(4)
 
 
Inconclusive(1)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 635193
Data Source: ChEMBL (792641)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-05-25

Data Table ( Complete ):           Active    All
BioActive Compounds: 4
Description:
Title: Synthesis, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.

Abstract: (#)-2-Fluoro-2-(2-methyl-4-(((4-methyl-2-(4-(trifluoromethyl)phenyl)thiazol-5-yl)methyl)thio)phenoxy)acetic acid (2a) has been prepared and subjected to biological testing against all three subtypes of the PPARs. This compound exhibited agonist effects with EC(50) values of 560 and 55 nM against PPARalpha and PPARdelta, respectively, in a luciferase assay. Moreover, compound (#)-2a also exhibited potent ability to induce oleic acid oxidation in a human myotube cell assay with EC(50)=3.7 nM. Compound (#)-2a can be classified as a dual PPARalpha/delta agonist with a 10-fold higher potency against the PPARdelta receptor than against the PPARalpha receptor. Molecular modeling studies revealed that both enantiomers of 2a bind to the PPARdelta receptor with similar binding energies.
(PMID: 22051054)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Putative Target:

ChEMBL Target ID: 22226
Target Type: UNCHECKED
Pref Name: Unchecked
Confidence: Default value - Target unknown or has yet to be assigned
Relationship Type: Default value - Target has yet to be curated
Categorized Comment
Assay Type: Functional

Assay Data Source: Scientific Literature

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
2EC50 activity commentEC50 activity commentString
3EC50 standard flagEC50 standard flagInteger
4EC50 qualifierEC50 qualifierString
5EC50 published valueEC50 published valueFloatnM
6EC50 standard valueEC50 standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
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