Fig. 2

Evaluation of compounds for their effect on internalization of Grb2. a Schematic of EGFR internalization cycle through Grb2-positive early endosomes (EE) and late endosomes (LE) [23]. b SCC61 cells treated with vehicle or EGF, visualized with antibody to Grb2. Right panels represent image overlayed with object mask generated by the Transfluor module. c Representative fields for untreated versus EGF-treated cells pre-incubated with controls (vehicle, erlotinib, cetuximab) or indicated compounds. d Quantitation of changes in pit count ratio; numbers over the bars indicate the docking boxes for each compound; + indicates that docking pose predicts EGF interaction. Class 1 and 2 compounds are reported comparing EGF-to-vehicle ratio in the absence of compounds versus EGF-to-vehicle ratio in the presence of compound, representative screening data. Compound classes are indicated. Representative screening data for Class 4 compounds are reported comparing pit count ratio for compound alone normalized to vehicle indicating activity in the absence of EGF