4.6. KINOMEscan

The KINOMEscan screening platform (DiscoverX, CA, USA) was employed to measure the interactions of M1 (10 μM in 0.1% DMSO) with 468 kinases covering more than 80% of the human kinome and disease-relevant mutant variants. The KINOMEscan kinase assay is an ATP-independent active site-directed competition binding assay and thus reports true thermodynamic interaction affinities [47]. The kinase dendrogram was generated using TREEspot software (http://treespot.discoverx.com/). The readout from the KINOMEscan assay is “percent of control,” where the control is 0.1% DMSO and 100% indicates no inhibition of the kinase by M1 at 10 μM.