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Assessment and Optimisation of Kinase Inhibitor Selectivity to Achieve Candidates with an Appropriate Safety Profile

Kinases make intriguing and attractive drug targets. Many are key players in disease-relevant pathways, and it is often relatively straightforward to develop screening assays and identify suitable chemical equity. While a large number of kinase inhibitors have entered the market in the past decade, it can be challenging to design kinase inhibitors with the right safety profile. Both on-target and off-target liabilities may be of concern, especially for non-directly life threatening diseases. This book chapter aims to discuss how to measure, assess, interpret and optimize the selectivity profile of kinase inhibitors, as part of a pro-active safety strategy to design and select drug candidates with an appropriate safety profile.

Publication details

Print publication date
06 Nov 2018
Copyright year
Print ISBN
ePub eISBN
From the book series:
Drug Discovery