Inhibition of human recombinant PI3K p110alpha after 1 hr by radiometric scintillation proximity assay - BioAssay Summary
Two classes of trisubstituted pyrimidines related to PI-103 1 have been prepared and their inhibitory activities against phosphatidylinositol 3-kinase (PI3K) p110## were determined. From those with direct 6-aryl substitution compound 11a was the most potent inhibitor with an IC# ..more
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 Tested Compounds
 Tested Compounds
All(48)
 
 
Active(32)
 
 
Unspecified(16)
 
 
 Tested Substances
 Tested Substances
All(48)
 
 
Active(32)
 
 
Unspecified(16)
 
 
 Related BioAssays
 Related BioAssays
Table of Contents
AID: 552454
Data Source: ChEMBL (700982)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2011-09-18
Modify Date: 2013-05-13

Data Table (Complete):           Active    All
Target
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Sequence: RecName: Full=Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform; Short=PI3-kinase subunit alpha; Short=PI3K-alpha; Short=PI3Kalpha; Short=PtdIns-3-kinase subunit alpha; AltName: Full=Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha; Short=PtdIns-3-kinase subunit p110-alpha; Short=p110alpha; AltName: Full=Phosphoinositide-3-kinase catalytic alpha polypeptide; AltName: Full=Serine/threonine protein kinase PIK3CA
Description ..   
Protein Family: PI3Kc_IA_alpha
Comment ..   

Gene:PIK3CA     Related Protein 3D Structures
BioActive Compounds: 32
Description:
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Title: Preparation and evaluation of trisubstituted pyrimidines as phosphatidylinositol 3-kinase inhibitors. 3-Hydroxyphenol analogues and bioisosteric replacements.

Abstract: Two classes of trisubstituted pyrimidines related to PI-103 1 have been prepared and their inhibitory activities against phosphatidylinositol 3-kinase (PI3K) p110## were determined. From those with direct 6-aryl substitution compound 11a was the most potent inhibitor with an IC#
(PMID: 21216151)
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: 11362

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
* Activity Concentration.

Data Table (Concise)
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Classification
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