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BioAssay: AID 241378

Inhibitory concentration required to inhibit Bcr-Abl tyrosine kinase

The constitutively active Abl kinase activity of the Bcr-Abl oncoprotein is causative for chronic myelogenous leukemia. Urea derivatives, structurally related to the therapeutic agent STI571, have been identified, which potently inhibit the tyrosine kinase activity of recombinant Abl. In particular a dimethylamino-aniline derivative (18) inhibited c-Abl transphosphorylation with an IC(50) value more ..
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 Tested Compounds
 Tested Compounds
All(12)
 
 
Inconclusive(12)
 
 
 Tested Substances
 Tested Substances
All(12)
 
 
Inconclusive(12)
 
 
 Related BioAssays
 Related BioAssays
AID: 241378
Data Source: ChEMBL (305472)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-05-24
Modify Date: 2014-05-20

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Breakpoint cluster region protein; AltName: Full=Renal carcinoma antigen NY-REN-26
Description ..   
Protein Family: RhoGAP_Bcr
Comment ..   

Gene:BCR     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Urea derivatives of STI571 as inhibitors of Bcr-Abl and PDGFR kinases.

Abstract: The constitutively active Abl kinase activity of the Bcr-Abl oncoprotein is causative for chronic myelogenous leukemia. Urea derivatives, structurally related to the therapeutic agent STI571, have been identified, which potently inhibit the tyrosine kinase activity of recombinant Abl. In particular a dimethylamino-aniline derivative (18) inhibited c-Abl transphosphorylation with an IC(50) value of 56 nM. Although this activity was not translated into cellular activity against the constitutively activated oncogenic Bcr-Abl, a number of compounds from this series potently inhibited cellular PDGFR autophosphorylation. It was also possible to differentiate between c-Abl and PDGFR kinase inhibition, with compound 22 being selective towards Abl and 23 selective for PDGFR.
(PMID: 15501042)
Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1IC50 activity commentIC50 activity commentString
2IC50 standard flagIC50 standard flagInteger
3IC50 qualifierIC50 qualifierString
4IC50 published valueIC50 published valueFloatnM
5IC50 standard valueIC50 standard valueFloat

Data Table (Concise)
Classification
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