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BioAssay: AID 641229

Inhibition of human PKR in HL-60 cells lysate assessed as reduction of labeling of acyl-phosphate ATP probe at 100 nM

We previously disclosed tricylic, 6-carboxylic acid-bearing 4-quinolones as GSK-3beta inhibitors. Herein we discuss the optimization of this series to yield a series of more potent 6-nitrile analogs with insignificant anti-microbial activity. Finally, kinase profiling indicated that members of this class were highly specific GSK-3 inhibitors. ..more
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 Tested Compounds
 Tested Compounds
All(4)
 
 
Unspecified(4)
 
 
 Tested Substances
 Tested Substances
All(4)
 
 
Unspecified(4)
 
 
 Related BioAssays
 Related BioAssays
AID: 641229
Data Source: ChEMBL (798677)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-08-24

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Interferon-induced, double-stranded RNA-activated protein kinase; AltName: Full=Eukaryotic translation initiation factor 2-alpha kinase 2; Short=eIF-2A protein kinase 2; AltName: Full=Interferon-inducible RNA-dependent protein kinase; AltName: Full=P1/eIF-2A protein kinase; AltName: Full=Protein kinase RNA-activated; Short=PKR; AltName: Full=Tyrosine-protein kinase EIF2AK2; AltName: Full=p68 kinase
Description ..   
Protein Family: Catalytic domain of the Serine/Threonine kinase, eukaryotic translation Initiation Factor 2-Alpha Kinase 2 or Protein Kinase regulated by RNA
Comment ..   

Gene:EIF2AK2     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: 6-Position optimization of tricyclic 4-quinolone-based inhibitors of glycogen synthase kinase-3beta: discovery of nitrile derivatives with picomolar potency.

Abstract: We previously disclosed tricylic, 6-carboxylic acid-bearing 4-quinolones as GSK-3beta inhibitors. Herein we discuss the optimization of this series to yield a series of more potent 6-nitrile analogs with insignificant anti-microbial activity. Finally, kinase profiling indicated that members of this class were highly specific GSK-3 inhibitors.
(PMID: 22202172)
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
BAO: Assay Format: cell-based format
Assay Cell Type: HL-60
Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Inhibition activity commentInhibition activity commentString
2Inhibition standard flagInhibition standard flagInteger
3Inhibition qualifierInhibition qualifierString
4Inhibition published valueInhibition published valueFloat%
5Inhibition standard valueInhibition standard valueFloat%

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