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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
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Probe(1)
 
 
Active(1)
 
 
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 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 ):           View Active Data    View All Data
Target
BioActive Compound: Chemical Probe: 1    Active: 1
Related Experiments
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AIDNameTypeComment
488899MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_SinglePoint_HTS_ActivityScreeningdepositor-specified cross reference: 331578 hts compounds at singlepoint in TRPM-1 promoter activity assay measuring activity
493073MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_DoseNoFile_CherryPick_Activity_Set3Confirmatorydepositor-specified cross reference: 1241 cherrypick compounds at dose in TRPM-1 promoter activity assay measuring activity set 3
493102MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_DoseNoFile_CherryPick_Activity_Set4Confirmatorydepositor-specified cross reference: 1241 cherrypick compounds at dose in TRPM-1 promoter activity assay measuring activity set 4
493177MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_DoseNoFile_CherryPick_Activity_Set2Confirmatorydepositor-specified cross reference: 1242 cherrypick compounds at dose in TRPM-1 promoter activity assay measuring activity set 2
493191MITF Orthogonal Assay: MALME3 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-04_Inhibitor_Dose_CherryPick_ActivityConfirmatorydepositor-specified cross reference: 1280 cherrypick compounds at dose in MALME3 Cytotoxicity Assay measuring activity
493240MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_CherryPick_Activity_Set3Confirmatorydepositor-specified cross reference: 1280 cherrypick compounds at dose in SK-MEL-5 Cytotoxicity Assay measuring activity set 3##
540335MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_CherryPick_Activity_Set2Confirmatorydepositor-specified cross reference
540339MITF Orthogonal Assay: MALME3 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-04_Inhibitor_Dose_DryPowder_ActivityConfirmatorydepositor-specified cross reference
540346MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_ActivityConfirmatorydepositor-specified cross reference
540347MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_ActivityConfirmatorydepositor-specified cross reference
540348MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_ActivityConfirmatorydepositor-specified cross reference
624259MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set3Confirmatorydepositor-specified cross reference
624289MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set2Confirmatorydepositor-specified cross reference
624290MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set2Confirmatorydepositor-specified cross reference
624299MITF Orthogonal Assay: MALME3 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-04_Inhibitor_Dose_DryPowder_Activity_Set2Confirmatorydepositor-specified cross reference
624315MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set3Confirmatorydepositor-specified cross reference
624316MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set4Confirmatorydepositor-specified cross reference
624324MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set3Confirmatorydepositor-specified cross reference
624362MITF Orthogonal Assay: MALME3 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-04_Inhibitor_Dose_DryPowder_Activity_Set3Confirmatorydepositor-specified cross reference
624363MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set5Confirmatorydepositor-specified cross reference
624364MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set4Confirmatorydepositor-specified cross reference
624366MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set4Confirmatorydepositor-specified cross reference
624368MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set5Confirmatorydepositor-specified cross reference
624426MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set7Confirmatorydepositor-specified cross reference
624427MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set5Confirmatorydepositor-specified cross reference
624428MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set7Confirmatorydepositor-specified cross reference
624429MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set6Confirmatorydepositor-specified cross reference
624430MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set8Confirmatorydepositor-specified cross reference
624440MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set6Confirmatorydepositor-specified cross reference
624488MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set6Confirmatorydepositor-specified cross reference
624489MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set2Confirmatorydepositor-specified cross reference
624490MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set7Confirmatorydepositor-specified cross reference
624492MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set8Confirmatorydepositor-specified cross reference
651584MITF Orthogonal Assay: MALME3 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-04_Inhibitor_Dose_DryPowder_Activity_Set5Confirmatorydepositor-specified cross reference
651585MITF Orthogonal Assay: MALME3 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-04_Inhibitor_Dose_DryPowder_Activity_Set6Confirmatorydepositor-specified cross reference
651586MITF Orthogonal Assay: SK-MEL-5 CTG Assay Measured in Cell-Based System Using Plate Reader - 2084-02_Inhibitor_Dose_DryPowder_Activity_Set8Confirmatorydepositor-specified cross reference
651588MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set9Confirmatorydepositor-specified cross reference
651591MITF: Counter assay: A375 proliferation Measured in Cell-Based System Using Plate Reader - 2084-03_Inhibitor_Dose_DryPowder_Activity_Set9Confirmatorydepositor-specified cross reference
651753MITF Measured in Cell-Based System Using Plate Reader - 2084-01_Inhibitor_Dose_DryPowder_Activity_Set10Confirmatorydepositor-specified cross reference
651770qPCR Assay for TRPM1 Expression Measured in Cell-Based System Using RT-PCR - 2084-09_Inhibitor_Dose_DryPowder_ActivityConfirmatorydepositor-specified cross reference
651771qPCR Assay for DCT Expression Measured in Cell-Based System Using RT-PCR - 2084-12_Inhibitor_Dose_DryPowder_ActivityConfirmatorydepositor-specified cross reference
651772qPCR Assay for CDK2 Expression Measured in Cell-Based System Using RT-PCR - 2084-11_Inhibitor_Dose_DryPowder_ActivityConfirmatorydepositor-specified cross reference
651773qPCR Assay for MITF Expression Measured in Cell-Based System Using RT-PCR - 2084-05_Inhibitor_Dose_DryPowder_ActivityConfirmatorydepositor-specified cross reference
651795qPCR Assay for MLANA Expression Measured in Cell-Based System Using RT-PCR - 2084-13_Inhibitor_Dose_DryPowder_ActivityConfirmatorydepositor-specified cross reference
651920Primary human melanocyte cytotoxicity assay Measured in Cell-Based System Using Plate Reader - 2084-06_Inhibitor_Dose_DryPowder_ActivityConfirmatorydepositor-specified cross reference
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.
Categorized Comment - additional comments and annotations
From MLP Probe Report:
Probe count: 1
MLP Probe ML# for probe 1: ML329
PubChem Substance ID (SID) for probe 1: 144221520
PubChem Compound ID (CID) for probe 1: 12387471
Probe type for probe 1: Inhibitor
IC50/EC50 (nM) for probe 1: 1200
Target for probe 1: TRPM-1 promoter activity (gi: 40807040)
Disease relevance for probe 1: Cancer
Anti-target for probe 1: A375 cytotoxicity
Fold selectivity for probe 1: >30
NCBI Book chapter link for probe 1: http://www.ncbi.nlm.nih.gov/books/NBK154496/ (ID: 3050892)
Grant number for probe 1: DA031089-01
NCBI Book chapter title for probe 1: A Small Molecule Inhibitor of the MITF Molecular Pathway
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)
Data Table ( Complete ):     View Active Data    View All Data
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