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BioAssay: AID 738225

Binding affinity to TYRO3 (unknown origin) at 1 uM after 1 hr relative to control

The TAM subfamily of Receptor Tyrosine Kinases (RTKs) contains three human proteins of therapeutical interest, Axl, Mer, and Tyro3. Our goal was to design a type II inhibitor specific for this family, i.e. able to interact with the allosteric pocket and with the hinge region of the kinase. We report the synthesis of several series of purine analogues of BMS-777607. The structural diversity of the more ..
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 Tested Compounds
 Tested Compounds
All(43)
 
 
Unspecified(43)
 
 
 Tested Substances
 Tested Substances
All(43)
 
 
Unspecified(43)
 
 
 Related BioAssays
 Related BioAssays
AID: 738225
Data Source: ChEMBL (950793)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-11-07
Modify Date: 2014-08-27

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Tyrosine-protein kinase receptor TYRO3; AltName: Full=Tyrosine-protein kinase BYK; AltName: Full=Tyrosine-protein kinase DTK; AltName: Full=Tyrosine-protein kinase RSE; AltName: Full=Tyrosine-protein kinase SKY; AltName: Full=Tyrosine-protein kinase TIF; Flags: Precursor
Description ..   
Protein Family: Catalytic domain of the Protein Tyrosine Kinase, Tyro3
Comment ..   

Gene:TYRO3     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Inhibitors of the TAM subfamily of tyrosine kinases: synthesis and biological evaluation.

Abstract: The TAM subfamily of Receptor Tyrosine Kinases (RTKs) contains three human proteins of therapeutical interest, Axl, Mer, and Tyro3. Our goal was to design a type II inhibitor specific for this family, i.e. able to interact with the allosteric pocket and with the hinge region of the kinase. We report the synthesis of several series of purine analogues of BMS-777607. The structural diversity of the designed inhibitors was expected to modify the interactions formed in the binding site and consequently to modulate their selectivity profiles. The most potent inhibitor 6g exhibits Kds of 39, 42, 65 and 200#nM against Axl, Mer, Met and Tyro3 respectively. Analysis of the affinity of 6g for active and inactive forms of Abl1, an RTK protein that does not belong to the TAM subfamily, together with the binding modes of 6g predicted by docking studies, indicates that 6g displays some selectivity for the TAM family and may act as a type II inhibitor.
(PMID: 22749189)
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Activity activity commentActivity activity commentString
2Activity standard flagActivity standard flagInteger
3Activity qualifierActivity qualifierString
4Activity published valueActivity published valueFloat%
5Activity standard valueActivity standard valueFloat%

Data Table (Concise)
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Classification
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