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Dual Inhibitors

Mat Todd edited this page May 11, 2022 · 3 revisions

Six potential dual MurD/MurE inhibitors were identified as part of the MurD round 1 biochemical assays:

Plans for following up these compounds include:

  1. Dose-response assays for all six compounds.
  2. Crystal soaking compounds of interest to MurD (and possibly MurE)
  3. Design of round 2 inhibitors. @KatoLeonard's SAR analysis may be found here and a list of current synthetic targets may be found here.

The dose response curves carried out with the dual inhibitor compounds can be seen below (originally here) with the Hill Slope and IC50 of each compound being shown in the figure legend. Becca Steventon was able to achieve this for all dual inhibitors apart from OSA_788 which started to precipitate whenever it was attempted to use it within an assay. Screenshot 2022-05-09 at 10 37 17

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