Easy Kinome Profiling: Synergy of Carna Bioscience’s® Biotinylated Kinases and Carterra’s® HT-SPR™

Kinases are an attractive target class across many therapeutic areas. To dig deeper into this target class, mechanisms beyond ATP-competition are actively under investigation including allosteric inhibition, degradation, or as partners in molecular glues.

For these approaches, standard activity assays and even advanced enzymology can only go so far in providing sufficient detail to inform chemistry decisions. Direct label-free approaches, such as SPR binding, provide the intrinsic kinetics of interactions which allow differentiation of compounds and compound series that, although potentially similar in activity assays, ultimately show distinct kinetics. Critically these different mechanisms can have an impact on efficacy in humans.

In this talk we will present the benefits of kinase profiling via HT-SPR technology. Straightforward assay development, enabled by high quality biotinylated kinases, supported rapid screening of a library of small molecule compounds against 87 different kinases. By measuring 384 binding events per cycle, over 80,000 interactions were characterized in a 3-day run. Initial screening data combined with more detailed follow up assays provided a wealth of deep kinetic data which correlated well to activity data thus validating the accuracy of Carterra’s LSA-XT platform as well as the quality, activity, and stability of Carna’s biotinylated kinases.