Fig. 6.

In vitro inhibition assay for selected E-3810 interactors. Eight kinase proteins were selected from among the candidate interactors identified in chemical proteomics experiments to assess whether E-3810 could inhibit their enzymatic activity; FGFR2 was included as a positive control. A, table showing inhibition constant (K_{i E-3810}) and half-maximal inhibitory concentration (IC_{50 E-3810}) values calculated from the in vitro assay, with the corresponding dissociation constant calculated from the chemical proteomics assay (K_{d imm E-3810}). The value of K_i > 50 μm for SRC suggests that this kinase was not specifically inhibited by E-3810 at the concentrations tested in the assay. B, comparative ranking of the E-3810 targets based on K_{i E-3810} and K_{d imm E-3810} values, referring to the drug's efficacy and affinity, respectively.