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BioAssay: AID 156234

In vitro transcription activation on human peroxisome proliferator activated receptor-delta (PPAR delta)

Lipid accumulation in nonadipose tissues is increasingly linked to the development of type 2 diabetes in obese individuals. We report here the design, synthesis, and evaluation of a series of novel PPARalpha selective activators containing 1,3-dicarbonyl moieties. Structure-activity relationship studies led to the identification of PPARalpha selective activators (compounds 10, 14, 17, 18, and 21) more ..
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 Tested Compounds
 Tested Compounds
All(12)
 
 
Active(12)
 
 
 Tested Substances
 Tested Substances
All(12)
 
 
Active(12)
 
 
 Related BioAssays
 Related BioAssays
AID: 156234
Data Source: ChEMBL (153488)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-20
Modify Date: 2013-11-12

Data Table ( Complete ):           Active    All
BioActive Compounds: 12
Description:
Title: Design, synthesis, and evaluation of a new class of noncyclic 1,3-dicarbonyl compounds as PPARalpha selective activators.

Abstract: Lipid accumulation in nonadipose tissues is increasingly linked to the development of type 2 diabetes in obese individuals. We report here the design, synthesis, and evaluation of a series of novel PPARalpha selective activators containing 1,3-dicarbonyl moieties. Structure-activity relationship studies led to the identification of PPARalpha selective activators (compounds 10, 14, 17, 18, and 21) with stronger potency and efficacy to activate PPARalpha over PPARgamma and PPARdelta. Experiments in vivo showed that compounds 10, 14, and 17 had blood glucose lowering effect in diabetic db/db mouse model after two weeks oral dosing. The data strongly support further testing of these lead compounds in other relevant disease animal models to evaluate their potential therapeutic benefits.
(PMID: 15177462)
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: 12227
Target Type: SINGLE PROTEIN
Pref Name: Peroxisome proliferator-activated receptor delta
Synonyms: NUC1;NUCI;Nuclear hormone receptor 1;Nuclear receptor subfamily 1 group C member 2;Peroxisome proliferator-activated receptor beta;Peroxisome proliferator-activated receptor delta;PPAR-beta;PPAR-delta;
Gene Name: NR1C2 ;PPARB;PPARD;
Protein Accession: Q03181;
Protein GI: 417522;
Organism: Homo sapiens
Tax ID: 9606
Target Classification: transcription factor nuclear receptor nr1 nr1c nr1c2
Confidence: Homologous single protein target assigned
Relationship Type: Homologous protein target assigned
Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1EC50*EC50 PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface 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 valueFloatμM
10EC50 standard valueEC50 standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
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