molecules of the month

compound 4c

degrader with simpler CRBN warhead

BRD4 DC50 = 0.87 nM, Dmax = 99%

from structure-based design

Angewandte Chemie Int. Ed.

Saint Jude Children’s Hospital, Memphis, TN

Chemical structure of molecule SJ995973 compound 4c
1 min read

 The bifunctional degrader, SJ995973, was nominated by Joachim Rudolph. “Instead of the thalidomide-based cereblon binder present in the established BET degrader tool dBET1, SJ995973 uses a novel cereblon binder containing a simple phenyl ring instead of the hydrolytically labile phthalimide group. Not only is SJ995973 an extremely potent BET degrader (BRD4 DC50 = 0.87 nM (Dmax = 99%)), but the alternative cereblon binder offers key advantages over thalidomide (and classical IMiDs used in PROTAC design in general), including chemical stability, smaller size and TPSA, and synthetic feasibility.” This novel cereblon binding motif is likely to be reused in many new applications.

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