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BioAssay: AID 744878

Inhibition of Bcr-Abl kinase (unknown origin) after 30 mins by HTRF assay

A novel class of Nilotinib derivatives, B1-B20, were synthesized in high yields using various substituted anilines. All the title compounds were evaluated for their inhibitory activities against Bcr-Abl and antiproliferative effects on human leukemia cell (K562). The pharmacological results indicated that some compounds exhibited promising anticancer activity. In particular, compound B14 more ..
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 Tested Compounds
 Tested Compounds
All(21)
 
 
Active(16)
 
 
Inconclusive(5)
 
 
 Tested Substances
 Tested Substances
All(21)
 
 
Active(16)
 
 
Inconclusive(5)
 
 
AID: 744878
Data Source: ChEMBL (957284)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2014-05-03
Modify Date: 2014-08-23

Data Table ( Complete ):           View Active Data    View All Data
Targets
Sequence: RecName: Full=Tyrosine-protein kinase ABL1; AltName: Full=Abelson murine leukemia viral oncogene homolog 1; AltName: Full=Abelson tyrosine-protein kinase 1; AltName: Full=Proto-oncogene c-Abl; AltName: Full=p150
Description ..   
Protein Family: Catalytic domain of the Protein Tyrosine Kinase, Abelson kinase
Comment ..   

Gene:ABL1     Related Protein 3D Structures     More BioActivity Data..


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BioActive Compounds: 16
Description:
Title: Design, synthesis and biological activities of Nilotinib derivates as antitumor agents.

Abstract: A novel class of Nilotinib derivatives, B1-B20, were synthesized in high yields using various substituted anilines. All the title compounds were evaluated for their inhibitory activities against Bcr-Abl and antiproliferative effects on human leukemia cell (K562). The pharmacological results indicated that some compounds exhibited promising anticancer activity. In particular, compound B14 containing tertiary amine side chain exhibited Bcr-Abl inhibitory activity similar to that of Nilotinib. It was suggested that the introduction of the tertiary amine moiety could improve Bcr-Abl inhibitory activity and antitumor effects.
(PMID: 23538233)
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
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 valueFloatnM
10IC50 standard valueIC50 standard valueFloatnM

* Activity Concentration.

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