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Taking quinazoline as a general support-Nog to design potent and selective kinase inhibitors: application to FMS-like tyrosine kinase 3.

CHEMMEDCHEM(2010)

Cited 21|Views49
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Abstract
Molecular joinery: Herein we propose a concept for the design of selective kinase inhibitors. This de novo design method involves restricted fragment growth by using quinazoline as a general molecular support-nog. Application of this concept to the design of FMS-like tyrosine kinase 3 (FLT3) inhibitors led to a potent (IC50=7 nM) and selective FLT3 inhibitor. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.
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Key words
de novo design,FMS-like tyrosine kinase 3,inhibitors,kinases,selectivity
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