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BioAssay: AID 743199

qHTS assay to identify small molecule antagonists of the peroxisome proliferator-activated receptor gamma (PPARg) signaling pathway: Summary

The peroxisome proliferator-activated receptors (PPARs) are lipid-activated transcription factors of the nuclear receptor superfamily with three distinct subtypes namely PPAR alpha, PPAR delta (also called PPAR beta) and PPAR gamma (PPARg). All these subtypes heterodimerize with Retinoid X receptor (RXR) and these heterodimers regulate transcription of various genes. PPAR-gamma receptor more ..
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 Tested Compounds
 Tested Compounds
All(7343)
 
 
Active(384)
 
 
Inactive(5890)
 
 
Inconclusive(1370)
 
 
 Tested Substances
 Tested Substances
All(9315)
 
 
Active(430)
 
 
Inactive(7317)
 
 
Inconclusive(1568)
 
 
AID: 743199
Data Source: Tox21 (PPARGN781)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: Other
Deposit Date: 2013-12-09

Data Table ( Complete ):           Active    All
Target
BioActive Compounds: 384
Depositor Specified Assays
AIDNameTypeComment
743191qHTS assay to identify small molecule antagonists of the peroxisome proliferator-activated receptor gamma (PPARg) signaling pathwayconfirmatoryPPARg antagonist mode screen
743194qHTS assay to identify small molecule antagonists of the peroxisome proliferator-activated receptor gamma (PPARg) signaling pathway - cell viability counter screenconfirmatoryCell viability counter screen
Description:
U.S. Tox21 Program

National Center for Advancing Translational Sciences [NCATS]
NIH Chemical Genomics Center [NCGC]
U.S. Environmental Protection Agency [EPA]
National Institutes of Environmental Health Sciences [NIEHS]
National Toxicology Program [NTP]
U.S. Food and Drug Administration [FDA]

Tox21 Assay Overview:

The peroxisome proliferator-activated receptors (PPARs) are lipid-activated transcription factors of the nuclear receptor superfamily with three distinct subtypes namely PPAR alpha, PPAR delta (also called PPAR beta) and PPAR gamma (PPARg). All these subtypes heterodimerize with Retinoid X receptor (RXR) and these heterodimers regulate transcription of various genes. PPAR-gamma receptor (glitazone receptor) is involved in the regulation of glucose and lipid metabolism. To identify the compounds that activate PPAR-gamma signaling, GeneBLAzer PPAR gamma UAS-bla HEK293H cell line (Invitrogen, Carlsbad, CA, USA) containing a beta-lactamase reporter gene under the control of an Upstream Activator Sequence (UAS) was used to screen the Tox21 compound library. The cytotoxicity of the Tox21 compound library against the PPARg-bla cell line was tested in parallel by measuring the cell viability using CellTiter-Glo assay in the same wells.
Protocol
Please refer to other AIDs, 743191 and 743194, for detailed assay protocols.
Comment
This summary is written for the purposes of summarizing the compound activities from the project combining the results from both the PPARg antagonist mode assay (AID 743191) and cell viability counter screen (AID 743194). For all inactive compounds, PUBCHEM_ACTIVITY_SCORE is 0. Active compounds have PUBCHEM_ACTIVITY_SCORE between 40 and 100. Potency and efficacy were used for determining relative score. Inconclusive compounds have PUBCHEM_ACTIVITY_SCORE between 5 and 30 determined by phenotype.

Disclaimer:

Although all reasonable efforts have been made to ensure the accuracy and reliability of the data, caution should be exercised when interpreting the results as artifacts are possible from nonspecific effects such as assay signal interference. The curve fitting and activity calls presented here are based on the NCATS analysis methods. Alternative analysis methods and interpretations of the data are available at EPA (http://actor.epa.gov) and NTP (http://tools.niehs.nih.gov/cebs3/ui/).
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1Activity SummaryType of compound activity based on both the PPARg antagonist mode screen and the cell viability counter screens.String
2Ratio ActivityType of compound activity in the ratio readout of the PPARg antagonist mode screen.String
3Ratio Potency (uM)The concentration of sample yielding half-maximal inhibition in the ratio readout of the PPARg antagonist mode screen.FloatμM
4Ratio Efficacy (%)Percent inhibition in the ratio readout of the PPARg antagonist mode screen.Float%
5530 nm ActivityType of compound activity in the 530 nm readout of the PPARg antagonist mode screen.String
6530 nm Potency (uM)The concentration of sample yielding half-maximal inhibition in the 530 nm readout of the PPARg antagonist mode screen.FloatμM
7530 nm Efficacy (%)Percent inhibition in the 530 nm readout of the PPARg antagonist mode screen.Float%
8460 nm ActivityType of compound activity in the 460 nm readout of the PPARg antagonist mode screen.String
9460 nm Potency (uM)The concentration of sample yielding half-maximal inhibition in the 460 nm readout of the PPARg antagonist mode screen.FloatμM
10460 nm Efficacy (%)Percent inhibition in the 460 nm readout of the PPARg antagonist mode screen.Float%
11Viability ActivityType of compound activity in the cell viability counter screens.String
12Viability Potency (uM)The concentration of sample yielding half-maximal inhibition in the cell viability counter screen.FloatμM
13Viability Efficacy (%)Percent inhibition in the cell viability counter screen.Float%
14Sample SourceWhere sample was obtained.String

Data Table (Concise)
Classification
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