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BioAssay: AID 504738

Inhibitors of Bloom's syndrome helicase: Aqueous Profiling Assay

Survival of cells and the faithful propagation of the genome depend on elaborate mechanisms of detecting and repairing DNA damage. Treatment of advanced cancer relies on radiation therapy or chemotherapy, which kill cancer cells by causing extensive DNA damage. It is often found, that cancer cells develop resistance to therapy through enhanced activity of DNA repair functions; this has led to an more ..
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Inactive(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Inactive(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 504738
Data Source: NCGC (BLMA600)
Depositor Category: NIH Molecular Libraries Probe Production Network
Deposit Date: 2011-05-09
Hold-until Date: 2012-05-06
Modify Date: 2012-05-08

Data Table ( Complete ):           View All Data
Tested Compound:
Related Experiments
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AIDNameTypeComment
2386Probe Development Summary for Inhibitors of Bloom's syndrome helicase (BLM)Summarydepositor-specified cross reference: Summary AIS
2364qHTS Validation Assay for Inhibitors of Bloom's syndrome helicase (BLM)Confirmatorysame project related to Summary assay
2528qHTS Assay for Inhibitors of Bloom's syndrome helicase (BLM)Confirmatorysame project related to Summary assay
2585qHTS Confirmation Assay for Inhibitors of Bloom's syndrome helicase (BLM)Confirmatorysame project related to Summary assay
2712Counterscreen for BLMA Inhibitors: ADP Fluorescence Polarization Displacement AssayConfirmatorysame project related to Summary assay
504662Inhibitors of BLM Helicase: DNA Unwinding Measured by Gel Electrophoresis - BLM Helicase ActivityConfirmatorysame project related to Summary assay
504663Inhibitors of BLM Helicase: DNA Unwinding Measured by Gel Electrophoresis - RecQL1 Helicase CounterscreenConfirmatorysame project related to Summary assay
504736Inhibitors of Bloom's syndrome helicase: Efflux Ratio Profiling AssayOthersame project related to Summary assay
504737Inhibitors of Bloom's syndrome helicase: Caco-2 Permeability Profiling AssayOthersame project related to Summary assay
504739Inhibitors of Bloom's syndrome helicase: Metabolic Stability ProfilingOthersame project related to Summary assay
504740Inhibitors of Bloom's syndrome helicase: Mouse Plasma Stability ProfilingOthersame project related to Summary assay
504741Inhibitors of Bloom's syndrome helicase: PBS Stability Profiling AssayOthersame project related to Summary assay
720549qHTS for Inhibitors of Bloom's syndrome helicase (BLM): Helicase ATPase Orthogonal Confirmatory Assay for SAROthersame project related to Summary assay
720550qHTS for Inhibitors of Bloom's syndrome helicase (BLM): Thiazole Orange DNA Binding Counterscreen for SAR.Othersame project related to Summary assay
720555qHTS for Inhibitors of Bloom's syndrome helicase (BLM): Helicase DNA unwinding fluorescent orthogonal confirmatory assay for SAROthersame project related to Summary assay
Description:
Survival of cells and the faithful propagation of the genome depend on elaborate mechanisms of detecting and repairing DNA damage. Treatment of advanced cancer relies on radiation therapy or chemotherapy, which kill cancer cells by causing extensive DNA damage. It is often found, that cancer cells develop resistance to therapy through enhanced activity of DNA repair functions; this has led to an increased interest in developing drugs that interfere with DNA repair, which could sensitize cancer cells to conventional therapy. Bloom syndrome helicase (BLM), is important in resolving abnormal DNA structures formed during replication or homologous recombination. Shutting down the expression of BLM leads to chromosomal instability and higher radiation sensitivity in cultured cells.


This bioassay provides profiling data on aqueous kinetic solubility (PBS @ pH 7.4) of one of the lead compounds developed in the APE1 inhibitors project.

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

MLSCN Grant: MH087284
PI Name: Dr. Opher Gileadi, Structural Genomics Consortium, University of Oxford, UK
Protocol
1. 8ul of reference and test compound stock solution were added to 392ul 100mM phosphate buffer (pH 7.4)
2. Sample tubes were shaken for 1 hr (1000 rpm) at room temperature
3. Samples were centrifuged (10 min at 12000 rpm) to precipitate un-dissolved particles
4. Supernatants were transferred to new tubes
5. Concentration of the supernatant was determined by LC-UV or LC-MS/MS
Comment
Compounds are "active" if solubility is greater than 20; "inconclusive" if solubility is between 10 and 20; "inactive" if solubility is less than 10.
PUBCHEM_ACTIVITY_SCORE is the solubility rounded to the closet whole number.
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1SolubilityKinetic aqueous solubility (PBS at pH 7.4)FloatμM
2Compound QCSource of compound QCString
Additional Information
Grant Number: MH087284

Data Table (Concise)
Data Table ( Complete ):     View All Data
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