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BioAssay: AID 656547

Inhibition of human recombinant Sky using poly-GT as substrate and [33P]ATP after 40 mins by beta counting

A series of aminopyrazines as inhibitors of Syk kinase activity and showing inhibition of LAD2 cells degranulation is described. Optimization of the carboxamide motif with aminomethylpiperidines provided high potency inhibiting Syk but low cellular activity. Amides of cis and trans adamantanol showed good inhibitory activity against Syk as well as remarkable activity in LAD2 cells degranulation assay. ..more
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 Tested Compounds
 Tested Compounds
All(37)
 
 
Active(36)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(42)
 
 
Active(41)
 
 
Unspecified(1)
 
 
AID: 656547
Data Source: ChEMBL (813619)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2013-05-16
Modify Date: 2014-08-25

Data Table ( Complete ):           View Active Data    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..
BioActive Compounds: 36
Description:
Title: Pyrazine-based Syk kinase inhibitors.

Abstract: A series of aminopyrazines as inhibitors of Syk kinase activity and showing inhibition of LAD2 cells degranulation is described. Optimization of the carboxamide motif with aminomethylpiperidines provided high potency inhibiting Syk but low cellular activity. Amides of cis and trans adamantanol showed good inhibitory activity against Syk as well as remarkable activity in LAD2 cells degranulation assay.
(PMID: 22425453)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

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
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50*IC50 PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6IC50 activity commentIC50 activity commentString
7IC50 standard flagIC50 standard flagInteger
8IC50 qualifierIC50 qualifierString
9IC50 published valueIC50 published valueFloatμM
10IC50 standard valueIC50 standard valueFloatnM
11IC50 binding domainsIC50 binding domainsString

* Activity Concentration.

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