FIGURE 3.
Representative hit validation in 96-well plates. Dose-dependent inhibition of 50 nm purified His6-SOS1cat (black circle)-mediated GDP for GTP nucleotide exchange upon 2 μm His6-H-Ras (residues 1–166) (gray circle) in both the 96-well BODIPY-FL-GDP dissociation and BODIPY-TR-GTP loading assays by the five validated hit compounds that displayed activity in both complementary experiments. Chemical structures of the five hit compounds are displayed on the left side of their respective experimental data. Data are expressed as percent change of fluorescence units normalized to the initial time point. Data were performed in triplicate and represent the mean.