Unleash the undrugged

WITH CETSA® NAVIGATE MS

Target engagement assessment for diffcult-to-drug targets with standard CETSA® followed by direct MS detection. No antibodies needed.

Did you know only 1-2% of disease-modifying proteins are traditionally considered druggable? Developing therapeutics for di  cult-to-drug targets is one of the key challenges of modern drug discovery and development. The problem has been that conventional methods often lack tools, such as antibodies, that would allow us to investigate and design ligands that target them.

That’s why we developed CETSA® Navigate MS. Reliable assessment of true target engagement – inside the cell, under actual physiological conditions – followed by direct MS read-out without the need for target detection antibodies. The leading target engagement platform CETSA® just got even better, with a new addition that allows you to pursue target proteins where no antibodies are available for detection. It’s time to unleash the undrugged.

A new tool for difficult-to-drug targets

In a proof-of-concept study of the CETSA® Navigate MS, we focused on cyclin-dependent kinase 6, CDK6, a well-established onco-target protein. A previously established CDK6 CETSA® Navigate assay, based on western blot detection, was used for benchmarking of the CETSA® Navigate MS assay. Pelago Bioscience profiled the cellular target engagement of CDK6 by the kinase inhibitor Palbociclib (Ibrance®) in K562 cells using the two formats in parallel to demonstrate that both assays reliably and efficiently can be used for evaluating cellular target engagement. Below you can download our Application Note to learn more about this study.

Downloads

Read more about CETSA® Navigate MS in our Application Note.

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Contact us to learn more about CETSA® Navigate MS