Inhibition of human FLT3 - BioAssay Summary
A series of inhibitors for the 90 kDa ribosomal S6 kinase (RSK) based on an 1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide scaffold were optimized for cellular potency and kinase selectivity. This led to the identification of compound 24, BIX 02565, an attractive candidate for use in vitro and in vivo to explore the role of RSK as a target for the treatment heart failure. ..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
Table of Contents
AID: 638375
Data Source: ChEMBL (795823)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2013-05-15

Data Table (Complete):           Active    All
Target
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Sequence: RecName: Full=Receptor-type tyrosine-protein kinase FLT3; AltName: Full=FL cytokine receptor; AltName: Full=Fetal liver kinase-2; Short=FLK-2; AltName: Full=Fms-like tyrosine kinase 3; Short=FLT-3; AltName: Full=Stem cell tyrosine kinase 1; Short=STK-1; AltName: CD_antigen=CD135; Flags: Precursor
Description ..   
Protein Family: Immunoglobulin domain
Comment ..   

Gene:FLT3     Related Protein 3D Structures
BioActive Compound: 1
Description:
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Title: Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity.

Abstract: A series of inhibitors for the 90 kDa ribosomal S6 kinase (RSK) based on an 1-oxo-2,3,4,5-tetrahydro-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide scaffold were optimized for cellular potency and kinase selectivity. This led to the identification of compound 24, BIX 02565, an attractive candidate for use in vitro and in vivo to explore the role of RSK as a target for the treatment heart failure.
(PMID: 22056746)
Comment
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Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
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ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 12670

ChEMBL target type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface Efficiency Index(nM)Float
4IC50 activity commentIC50 activity commentString
5IC50 standard flagIC50 standard flagInteger
6IC50 qualifierIC50 qualifierString
7IC50 published valueIC50 published valueFloatnM
8IC50 standard valueIC50 standard valueFloatnM
9IC50 binding domainsIC50 binding domainsString
* Activity Concentration.

Data Table (Concise)
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Classification
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