DDC-03-024-01

The allosteric EGFR probe may be useful for elucidating biology and offers an alternative mechanism of inhibition to EFGR orthosteric inhibitors. The cell data suggest a significant disconnect between biochemical and cellular potencies and this may be a facet of physicochemical properties, which would be important to bear in mind. Further, whilst the kinase profiling is helpful, these assays are perhaps more helpful to assess selectivity vs orthosteric/ATP binding inhibitors and selectivity data vs key benzodiazepine off-targets may be equally important before interpreting potential future in vivo studies. One of the central tenets of valuable probe compounds is their accessibility to the community and it's therefore a shame the full details of this probe sit behind a paywall, rather than being Open Access...

There are not target engagement assays.

Very selective allosteric kinase inhibitor. The antiproliferative effect is shown in cells. An additional target engagement assay would be nice. Synthetic modifications of the structure of the compound could be interesting for further investigations.