This presentation will cover a recent application of AbbVie’s revamped fragment library to the bromodomains. Following the redesign of the fragment library, this talk highlights an example where a fragment was rapidly elaborated to a lead series with high BEI, LE, and LipE as well as good oral bioavailability. The unique properties associated with fragments with high sp3 character and some lessons learned on the efficiency of chemistry to evolve fragment hits will also be discussed.

Fragment to lead: Discovery and optimization of a novel bromodomain inhibitor

ACS Fall 2021

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.