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BioAssay: AID 621629

Inhibition of human PIP5K2alpha in HL60 cells lysate at 10 uM using post probe-labeling by LC-MS/MS analysis relative to control

The synthesis, GSK-3beta inhibitory activity, and anti-microbial activity of bicyclic and tricyclic derivatives of the 5,7-diamino-6-fluoro-4-quinolone-3-carboxylic acid scaffold were studied. Kinase selectivity profiling indicated that members of this class were potent and highly selective GSK-3 inhibitors. ..more
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 Tested Compounds
 Tested Compounds
All(5)
 
 
Unspecified(5)
 
 
 Tested Substances
 Tested Substances
All(5)
 
 
Unspecified(5)
 
 
 Related BioAssays
 Related BioAssays
AID: 621629
Data Source: ChEMBL (771640)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-04-30
Modify Date: 2014-08-24

Data Table ( Complete ):           View All Data
Target
Sequence: RecName: Full=Phosphatidylinositol 5-phosphate 4-kinase type-2 alpha; AltName: Full=1-phosphatidylinositol 5-phosphate 4-kinase 2-alpha; AltName: Full=Diphosphoinositide kinase 2-alpha; AltName: Full=PIP5KIII; AltName: Full=Phosphatidylinositol 5-phosphate 4-kinase type II alpha; Short=PI(5)P 4-kinase type II alpha; Short=PIP4KII-alpha; AltName: Full=PtdIns(4)P-5-kinase B isoform; AltName: Full=PtdIns(4)P-5-kinase C isoform; AltName: Full=PtdIns(5)P-4-kinase isoform 2-alpha
Description ..   
Protein Family: Phosphatidylinositol phosphate kinases
Comment ..   

Gene:PIP4K2A     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Synthesis and structure-activity relationship of 4-quinolone-3-carboxylic acid based inhibitors of glycogen synthase kinase-3beta.

Abstract: The synthesis, GSK-3beta inhibitory activity, and anti-microbial activity of bicyclic and tricyclic derivatives of the 5,7-diamino-6-fluoro-4-quinolone-3-carboxylic acid scaffold were studied. Kinase selectivity profiling indicated that members of this class were potent and highly selective GSK-3 inhibitors.
(PMID: 21873061)
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
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
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