This presentation will describe the application of chemical biology probes towards the understanding of target engagement, selectivity/off-target identification and binding site ID across multiple drug discovery projects. A series of vignettes will be presented which include the use of clickable photoaffinity probes to identify off-targets of BACE inhibitors, evaluation of a series of cleavable linkers to aid in the binding site identification of gamma secretase inhibitors and profiling covalent adduct stability of irreversible MAGL inhibitors. Additional emphasis will be focused on the use of chemical biology monomer sets to support the rapid assembly of new probe compounds, as well as the development of new tools and technologies to further enable chemical biology in drug discovery.

Chemical biology impacting drug discovery

2019 Spring National Meeting

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