Jump to main content
Jump to site search
SCHEDULED MAINTENANCE Close the message box

Maintenance work is planned for Monday 16 August 2021 from 07:00 to 23:59 (BST).

Website performance may be temporarily affected and you may not be able to access some PDFs or images. If this does happen, refreshing your web browser should resolve the issue. We apologise for any inconvenience this might cause and thank you for your patience.

All chapters


The Design of Brain Penetrant Kinase Inhibitors

The desire for brain penetrant kinase inhibitors has increased in recent years to enable the treatment of both primary and secondary brain tumours but also for the potential management of degenerative CNS diseases such as Alzheimer's and Parkinson's diseases. However, the design of compounds that are able to access the brain is a formidable challenge, exacerbated by the fact that traditional kinase inhibitor design space does not overlap well with the physicochemical properties of established CNS compounds. This chapter overviews the challenges facing kinase medicinal chemists and highlights progress to date, illustrating with a growing number of successful kinase inhibitor case histories where brain penetration has now been obtained and shown to drive in vivo CNS efficacy.

Publication details

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