Kinase inhibitor library
The NCL includes most of the preclinically and clinically relevant published kinase inhibitors and a large series of previously patented compounds what we have developed.
We use or provide our Chemical Validation Library for in vitro or in vivo target validation.
Given the discrepancy of employing molecular biological tools for target validation, which affect an entire protein rather than just its activity, and the subsequent generation of pharmacological agents, which modulate the activity of kinase rather than affecting the whole kinase protein, we have chosen a strategy to validate potentially novel kinase targets with tools which are as close as possible to the final product, a pharmacologically active agent.
This strategy is called chemical validation and relies on a representative collection of proven kinase inhibitors, i.e. a kinase-biased compound library.
In that setting, a novel kinase target of interest is screened against this collection and the hits from one or more chemical series are determined.
Subsequently, these hits are employed in a cellular model combined with a direct cellular kinase assay. Provided that the hits show activity in the cell-free and in both cellular assays, the kinase of interest is considered validated and the tool inhibitors have already proven its druggability.