Deep characterization of binding kinetics for 210 kinase inhibitors against 80+ kinases

Introduction

As a drug target class, kinases continue to provide a wealth of opportunities for addressing human disease, but often can be challenging to work with in vitro. Additionally, the ubiquitous nature of kinases across many critical pathways means therapeutic targeting of this class necessitates careful consideration regarding off-target profiles. Here we highlight the power of combining an extensive panel of active kinases with HT-SPR to generate a wealth of compound binding information. More than 80,000 binding interactions were measured during a three-day label-free screen. Detailed kinetics were then subsequently obtained for hits of interest. Beyond simple yes/no reporting, this approach allows for nuanced kinetic profiling for up to hundreds of binding events in parallel, thereby enabling thoughtful discovery of safe and efficacious drug candidates.

Posted by Noah T. Ditto and Rebecca L. Rich