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Kinases are signalling proteins which have proven to be successful targets for the treatment of a variety of diseases, predominantly in cancers. However, only a small proportion of kinases (<20%) have been investigated for their therapeutic viability, likely due to the lack of available chemical tools across the kinome. In this work we describe initial efforts in the development of a selective chemical tool for protein kinase N2 (PKN2), a relatively unexplored kinase of interest in several types of cancer. The most successful compound, 5, has a measured IC50 of 0.064 μM against PKN2, with ca. 17-fold selectivity over close homologue, PKN1.

Original publication

DOI

10.1016/j.bmcl.2020.127040

Type

Journal article

Journal

Bioorganic & medicinal chemistry letters

Publication Date

17/02/2020

Addresses

Sussex Drug Discovery Centre, University of Sussex, Sussex House, Falmer, Brighton BN1 9RH, United Kingdom. Electronic address: f.scott@sussex.ac.uk.