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BioAssay: AID 488944

Summary of Broad Institute MLPCN Identification of MITF Inhibitors Project

This project aims to execute a robust and sensitive primary screen to identify suppressors of MITF activity. The short-term goals of these experiments are to identify MITF inhibitors that recapitulate genetic manipulation of MITF. The longer term goal is to use these probes to elucidate molecular pathways regulating MITF activity with the goal of translating this knowledge and these leads into therapeutic opportunities. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Probe(1)
 
 
Active(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Probe(1)
 
 
Active(1)
 
 
AID: 488944
Data Source: Broad Institute (2084-01_Inhibitors)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: NIH Molecular Libraries Probe Production Network
BioAssay Version:
Deposit Date: 2010-10-27
Modify Date: 2013-07-09

Data Table ( Complete ):           Active    All
Target
BioActive Compound: Chemical Probe: 1    Active: 1
Depositor Specified Assays
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AIDNameTypeComment
488899MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_SinglePoint_HTS_Activityscreening331578 hts compounds at singlepoint in TRPM-1 promoter activity assay measuring activity
493102MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_DoseNoFile_CherryPick_Activity_Set4confirmatory1241 cherrypick compounds at dose in TRPM-1 promoter activity assay measuring activity set 4
493191MITF Orthogonal Assay: MALME3 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-04_Inhibitor_Dose_CherryPick_Activityconfirmatory1280 cherrypick compounds at dose in MALME3 Cytotoxicity Assay measuring activity
493177MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_DoseNoFile_CherryPick_Activity_Set2confirmatory1242 cherrypick compounds at dose in TRPM-1 promoter activity assay measuring activity set 2
493073MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_DoseNoFile_CherryPick_Activity_Set3confirmatory1241 cherrypick compounds at dose in TRPM-1 promoter activity assay measuring activity set 3
493240MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_CherryPick_Activity_Set3confirmatory1280 cherrypick compounds at dose in SK-MEL-5 Cytotoxicity Assay measuring activity set 3##
624363MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set5confirmatory
624366MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set4confirmatory
624426MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set7confirmatory
624429MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set6confirmatory
624490MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set7confirmatory
540347MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activityconfirmatory
651586MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set8confirmatory
651795qPCR Assay for MLANA Expression Measured in Cell-Based System Using RT-PCR - 2084-13_Inhibitor_Dose_DryPowder_Activityconfirmatory
540339MITF Orthogonal Assay: MALME3 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-04_Inhibitor_Dose_DryPowder_Activityconfirmatory
651753MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set10confirmatory
624315MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set3confirmatory
624427MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set5confirmatory
624430MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set8confirmatory
624488MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set6confirmatory
651584MITF Orthogonal Assay: MALME3 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-04_Inhibitor_Dose_DryPowder_Activity_Set5confirmatory
651770qPCR Assay for TRPM1 Expression Measured in Cell-Based System Using RT-PCR - 2084-09_Inhibitor_Dose_DryPowder_Activityconfirmatory
624289MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set2confirmatory
624324MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set3confirmatory
651773qPCR Assay for MITF Expression Measured in Cell-Based System Using RT-PCR - 2084-05_Inhibitor_Dose_DryPowder_Activityconfirmatory
624290MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set2confirmatory
624299MITF Orthogonal Assay: MALME3 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-04_Inhibitor_Dose_DryPowder_Activity_Set2confirmatory
624440MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set6confirmatory
540346MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activityconfirmatory
624362MITF Orthogonal Assay: MALME3 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-04_Inhibitor_Dose_DryPowder_Activity_Set3confirmatory
624364MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set4confirmatory
624368MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set5confirmatory
540348MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activityconfirmatory
624316MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set4confirmatory
624428MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set7confirmatory
624489MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set2confirmatory
624492MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set8confirmatory
651585MITF Orthogonal Assay: MALME3 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-04_Inhibitor_Dose_DryPowder_Activity_Set6confirmatory
651588MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set9confirmatory
651591MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set9confirmatory
651771qPCR Assay for DCT Expression Measured in Cell-Based System Using RT-PCR - 2084-12_Inhibitor_Dose_DryPowder_Activityconfirmatory
624259MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set3confirmatory
540335MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_CherryPick_Activity_Set2confirmatory
651772qPCR Assay for CDK2 Expression Measured in Cell-Based System Using RT-PCR - 2084-11_Inhibitor_Dose_DryPowder_Activityconfirmatory
651920Primary human melanocyte cytotoxicity assay Measured in Cell-Based System Using Plate Reader - 2084-06_Inhibitor_Dose_DryPowder_Activityconfirmatory
Description:
Primary Collaborators:
David Fisher,MGH,Dfisher3@partners.org

Project Goal:
This project aims to execute a robust and sensitive primary screen to identify suppressors of MITF activity. The short-term goals of these experiments are to identify MITF inhibitors that recapitulate genetic manipulation of MITF. The longer term goal is to use these probes to elucidate molecular pathways regulating MITF activity with the goal of translating this knowledge and these leads into therapeutic opportunities.

melanoma, MITF, TRPM1Biological Relevance:
Micropthalmia-associated transcription factor (MITF) is a tissue-restricted basic helix-loop-helix leucine zipper (bHLH-Zip) transcription factor that is essential for melanocyte differentiation, function and survival. In approximately 15% of melanomas, amplification of MITF is oncogenic, as their survival and growth is dependent on MITF expression. In nearly all other melanomas, MITF remains essential for cell survival, making MITF an attractive lineage-specific target for melanoma therapy.
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1ML_NUMML number of probeString
Additional Information
Grant Number: 1 R03 DA031089-01

Data Table (Concise)
Classification
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