Harnessing the Biophysical Fragment Screening Sweet Spot to Discover New Chemotypes for BRPF1 Inhibition

The efficient sampling of the chemical universe is at the heart of the fragment screening hit identification paradigm. The smaller the fragments, the more efficient the sampling. How small we can go is determined by our ability to detect very weak binding events between small molecules and target proteins. At Concept Life Sciences and Creoptix, we joined forces to develop a unique fragment screening platform combining a purpose-built collection efficiently sampling the biophysically accessible chemical universe with the cutting-edge Grating-Coupled Interferometry (GCI) technology.

By operating in this biophysical “sweet spot”, we aim to identify the most efficient fragment hits in a matter of days; thus providing highly desirable start points for fragment hit optimization campaigns and a quicker path to candidate nomination. We report below our initial studies using our platform to identify new fragments efficiently binding the BRPF1 bromodomain.

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