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. Author manuscript; available in PMC: 2018 May 24.
Published in final edited form as: Angew Chem Int Ed Engl. 2017 Apr 18;56(21):5738–5743. doi: 10.1002/anie.201611281

Figure 1.

Figure 1

Design and characterization of thienopyridinone BRD9-targeted degraders. A) Structures of select BRD9 bromodomain probes. B) Schematic representation of degrader design. C) Vehicle-normalized BRD9(bd) displacement (AlphaScreen quadruplicate means +/− SEM). D) Compound-induced ternary complex formation of recombinant BRD9(bd) and CRBN-DDB1 (AlphaScreen quadruplicate means +/− SEM). E) Cocrystal structure of 3 with BRD9(bd) (PDB 5TWX). F) Docking of (E) into the published CRBN-DDB1 (4CI3).