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BioAssay: AID 602479

qHTS Assay for Inhibitors of Bacillus subtilis Sfp phosphopantetheinyl transferase (PPTase): Mouse Liver Microsome Stability (Half Time)

PPTases are responsible for the activation of a variety of pathogen-associated virulence factors. Among these compounds are toxins such as mycolactone from Mycobacterium ulcerans, siderophores such as vibriobactin from Vibrio cholerae or mycobactin from Mycobacterium tuberculosis, as well as the mycolic acids which form the waxy cell wall of Mycobacteria. The biosyntheses of these natural more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Active(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 602479
Data Source: NCGC (PPTA909)
Depositor Category: NIH Molecular Libraries Probe Production Network
Deposit Date: 2012-03-22
Hold-until Date: 2013-03-21
Modify Date: 2013-03-21

Data Table ( Complete ):           Active    All
BioActive Compound: 1
Depositor Specified Assays
AIDNameTypeComment
1819Probe Development Summary of Inhibitors of Bacillus subtilis Sfp phosphopantetheinyl transferase (PPTase)summarySummary AID
Description:
PPTases are responsible for the activation of a variety of pathogen-associated virulence factors. Among these compounds are toxins such as mycolactone from Mycobacterium ulcerans, siderophores such as vibriobactin from Vibrio cholerae or mycobactin from Mycobacterium tuberculosis, as well as the mycolic acids which form the waxy cell wall of Mycobacteria. The biosyntheses of these natural products are considered attractive targets for drug design. After a large qHTS and several follow-up assays, a small molecule was identified and this in vitro ADME assay serves to better characterize its properties.

This bioassay provides profiling data on mouse liver microsome stability. Mouse liver microsomes contain many enzymes that are involved in Phase 1 drug metabolism and hence can provide valuable information on the compounds susceptibility to drug metabolizing enzymes.

NIH Chemical Genomics Center [NCGC]
NIH Molecular Libraries Probe Centers Network [MLPCN]

MLPCN Grant: MH083226
Assay Submitter (PI): Michale Burkart, University of California, San Diego
Protocol
1uM of compound in incubated in mouse liver microsome; the reference compound is ketanserin. Compounds are incubated at 37 degrees C for different time periods: 0, 5, 15, 30, 45, and 60 minutes. Samples are analyzed with LC-MS/MS.
Comment
Compounds are "active" if half time is more than 30 minutes; "inconclusive" if half time is between 15 and 30 minutes; "inactive" if half time is less than 15 minutes.

PUBCHEM_ACTIVITY_SCORE is the whole number in minutes of T1/2 of the compound.
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1Mouse Liver Microsome Half Time Floatmin
2Compound QCString
Additional Information
Grant Number: MH083226

Data Table (Concise)
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