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BioAssay: AID 262019

Inhibition of E255K Bcr-Abl

A series of 3-substituted benzamide derivatives structurally related to STI-571 (imatinib mesylate), a Bcr-Abl tyrosine kinase inhibitor used to treat chronic myeloid leukemia (CML), was prepared and evaluated for antiproliferative activity against the Bcr-Abl-positive leukemia cell line K562. About ten 3-halogenated and 3-trifluoromethylated benzamide derivatives were identified as highly potent Bcr-Abl kinase inhibitors. One of these, NS-187 (9b), is a promising new candidate Bcr-Abl inhibitor for the therapy of STI-571-resistant chronic myeloid leukemia. ..more
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 Tested Compounds
 Tested Compounds
All(1)
 
 
Inconclusive(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Inconclusive(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 262019
Data Source: ChEMBL (339753)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-24
Modify Date: 2013-11-18

Data Table ( Complete ):           All
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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Tested Compound:
Description:
Title: Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors.

Abstract: A series of 3-substituted benzamide derivatives structurally related to STI-571 (imatinib mesylate), a Bcr-Abl tyrosine kinase inhibitor used to treat chronic myeloid leukemia (CML), was prepared and evaluated for antiproliferative activity against the Bcr-Abl-positive leukemia cell line K562. About ten 3-halogenated and 3-trifluoromethylated benzamide derivatives were identified as highly potent Bcr-Abl kinase inhibitors. One of these, NS-187 (9b), is a promising new candidate Bcr-Abl inhibitor for the therapy of STI-571-resistant chronic myeloid leukemia.
(PMID: 16332440)
Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 104811

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)
Classification
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