Advanced Cellular Dynamics


A collection exceeding sixty commercially available kinase inhibitors have been tested for their ability to inhibit each of 62 kinases, which collectively represent more than two-thirds of the tyrosine kinome. The measured half-maximal inhibitory potentials were subsequently compared and used to construct a dendrogram representing a virtual map of the ATP binding pocket. The resulting KinoScope® groups different kinases by virtue of these mapped spaces, rather than traditional parsing based on amino acid sequence homologies. This alternative method reveals similarities that might otherwise not be anticipated. For instance, our data reveal more similarities between the Janus, NTRK and FGFR subfamilies than would be anticipated based on protein homology alone. The adjacent KinoScope® reflects the activities measured using Sprycel (Dasatinib).