Fig 5. Rescue of ptc>dRetM955T flies by 2 and its analogs.
(A) ptc>dRetM955T viability assay. 2 showed increased efficacy when co-administrated with 200 μM sorafenib. (-), vehicle control. Error bars represent standard error in triplicate experiments. *P < 0.05 in one-sided Student’s t-test as compared with no-drug control. (B) Chemical structure of 2 and its analogs. (C) Docking pose of 2 and its analogs in a RET DFG-out model. These compounds are proposed to be putative type-II kinase inhibitors that bind in the DFG-pocket through their 1H-indole moiety and interact with the conserved αC-helix glutamate side chain and DFG-Aspartate backbone (broken yellow lines).