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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




Journal article


Bioorganic & medicinal chemistry letters

Publication Date





Sussex Drug Discovery Centre, University of Sussex, Sussex House, Falmer, Brighton BN1 9RH, United Kingdom. Electronic address:


Humans, Neoplasms, Benzimidazoles, Protein Kinase C, Antineoplastic Agents, Protein Kinase Inhibitors, Crystallography, X-Ray, Molecular Structure, Structure-Activity Relationship, Dose-Response Relationship, Drug, Models, Molecular, Drug Development