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Fluorescence Polarization Screening Assays for Small Molecule Allosteric Modulators of ABL Kinase Function

Fig 9

Concentration-dependent activation of the ABL kinase core protein by compound 142.

The wild type ABL kinase core was assayed in the presence of compound 142 and DPH at the indicated concentrations using a kinetic kinase assay (see Materials and Methods). Reaction velocities are plotted as a function of compound concentrations. The resulting data were curve-fit to determine the EC50, Kact and Vmax for each activator as described under Materials and Methods. Each of these parameters was determined in triplicate, and the mean values ± SE are presented in the table below the graph. The table also provides the ratio Vmax/Kact as a measure of overall enhancement of catalytic efficiency in the presence of each of these two ABL agonists.

Fig 9