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BioAssay: AID 663627

Transactivation activity at human PPARalpha expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay

We have discovered and demonstrated the in#vitro and in#vivo PPARdelta-selective activity of novel Y-shaped agonists. These compounds activated hPPARdelta with EC(50) values between 1 and 523#nM. Surprisingly, compounds 10a, 11d, 11e and 11f were the most potent and most selective hPPARdelta agonists with 10(4)-fold selectivity over the other two subtypes, namely, hPPARalpha and hPPARgamma. The PPARdelta ligands 10a, 11e and 11f showed good bioavailability and in#vivo efficacy. ..more
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 Tested Compounds
 Tested Compounds
All(28)
 
 
Active(6)
 
 
Unspecified(22)
 
 
 Tested Substances
 Tested Substances
All(28)
 
 
Active(6)
 
 
Unspecified(22)
 
 
AID: 663627
Data Source: ChEMBL (820716)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-05-16
Modify Date: 2014-05-26

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Peroxisome proliferator-activated receptor alpha; Short=PPAR-alpha; AltName: Full=Nuclear receptor subfamily 1 group C member 1
Description ..   
Protein Family: The ligand binding domain of peroxisome proliferator-activated receptors
Comment ..   

Gene:PPARA     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 6
Description:
Title: Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor delta agonists as potent anti-obesity agents in vivo.

Abstract: We have discovered and demonstrated the in#vitro and in#vivo PPARdelta-selective activity of novel Y-shaped agonists. These compounds activated hPPARdelta with EC(50) values between 1 and 523#nM. Surprisingly, compounds 10a, 11d, 11e and 11f were the most potent and most selective hPPARdelta agonists with 10(4)-fold selectivity over the other two subtypes, namely, hPPARalpha and hPPARgamma. The PPARdelta ligands 10a, 11e and 11f showed good bioavailability and in#vivo efficacy.
(PMID: 22534184)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Assay Test Type: In vitro

BAO: Assay Format: cell-based format

Target Type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6EC50 activity commentEC50 activity commentString
7EC50 standard flagEC50 standard flagInteger
8EC50 qualifierEC50 qualifierString
9EC50 published valueEC50 published valueFloatnM
10EC50 standard valueEC50 standard valueFloatnM
11EC50 binding domainsEC50 binding domainsString
12EC50 activity commentEC50 activity commentString
13EC50 standard flagEC50 standard flagInteger
14EC50 qualifierEC50 qualifierString
15EC50 published valueEC50 published valueFloatμM
16EC50 standard valueEC50 standard valueFloatnM
17EC50 binding domainsEC50 binding domainsString

* Activity Concentration.

Data Table (Concise)
Classification
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