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 [...]
SJ995973: A Bifunctional Degrader
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
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