Understanding your compounds target engagement in living cells beyond kinases!

It does not always need to be kinases – we also offer to determine the cellular target engagement of your compound with targets from the Ubiquitinylation field like E3-ligases that have been identified as great tools for the utilization of PROTAC molecules. Also, we have targets from the epigenetics field such as histone deacetylases (HDACs) and Bromodomain readers (BRDs).

Fig. 1: PROTACS are bifunctional molecules that bind both an E3-ligase and their intended target to create proximity. The E3-ligase will then poly-ubiquitinylate the target of interest which will then be degraded via the proteasome.
Fig. 2: HDACs can erase epigenetic acetylation marks from histones while BRDs can read certain epigenetic acetylation marks.

Please find a table including our emerging targets below:

Please select from our emerging targets!

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Test Molecule requirements

  • 100 µL of a 10 mM stock in 100% DMSO
  • Test molecule needs to be soluble – we will not attempt to solubilize your molecule but test the stock as is
  • Test molecule cytotoxicity may affect the assay outcome (because cell tox will lead to lower luciferase signal and hence lower assay performance) – we will test your sample as is
  • Test molecule absorbtion at 450 nm will affect the assay outcome (less luciferase signal gets transfered for BRET) – we will test your sample as is
  • Test molecule emission at 610 nm (after 450 nm excitation) will affect the assay outcome (artificially higher signal on the tracer channel) – we will test your sample as is

If you have a special request about a target that is not yet covered, please feel free to contact us!

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