A Perspective on the Kinetics of Covalent and Irreversible Inhibition.
Abstract
The clinical and commercial success of covalent drugs has prompted a renewed and more deliberate pursuit of covalent and irreversible mechanisms within drug discovery. A covalent mechanism can produce potent inhibition in a biochemical, cellular, or in vivo setting. In many cases, teams choose to focus on the consequences of the covalent event, defined by an IC50 value. In a biochemical assay, the IC50 may simply reflect the target protein...
Paper Details
Title
A Perspective on the Kinetics of Covalent and Irreversible Inhibition.
Published Date
Jan 1, 2017
Volume
22
Issue
1
Pages
3 - 20
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