Linking Ubiquitin Research to Drug Discovery

DUBprofiler-Cell™: DUB target engagement assay

Determination of DUB inhibitor in-cell target engagement

With the small molecule chemical tractability of DUBs demonstrated by a number of groups through the development of high affinity and selective inhibitors (supported by the DUBprofiler™ service) it is now becoming increasingly important to determine the in-cell DUB target engagement profile of these molecules as these drug discovery programmes progress towards the clinic.

We are now developing such a service with support from key collaborations such as CAST.

DUBprofiler-Cell will enable:

  • Determination of the DUB target engagement profile of your compound(s) in a live cell environment
    • Addressing; physiological protein folding, the cellular milieu for compound target engagement (pH, redox conditions etc), sub-cellular penetration (compound) and localisation (target), post-translational modifications and the presence of subunits, co-factors and substrates
  • Single point and EC50 determinations
  • Determination of DUB cellular target engagement in the presence and absence of stimuli
  • Determination of compound cell penetration
  • The capability to interrogate a cell lysate environment if your molecule is not cell penetrant
  • Profiling of any cell line and potentially tissues