A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain
Cox OB., Krojer T., Collins P., Monteiro O., Talon R., Bradley A., Fedorov O., Amin J., Marsden BD., Spencer J., von Delft F., Brennan PE.
High concentration crystal soaking of poised fragments and one-step elaboration identified compound 17 as an inhibitor of the PHIP(2) bromodomain.