The phosphoinositide-3-kinase (PI3K) pathway has been linked to a variety of diseases, such as cancer, diabetes, cardiovascular disease and even Alzheimer’s. As a result, these enzymes are a compelling class of targets for the identification of small molecule inhibitors. Utilizing our DNA-encoded discovery platform (DEX™), we were able to identify potent pan-active and nanomolar isoform selective (δ and γ) inhibitors for this intriguing class of enzymes. The two pan-active series were discovered from two separate heterocyclic core based DNA encoded libraries, while a δ-selective and γ-selective series was identified from the same linear based DNA encoded library.

Discovery of pan-active and isoform selective inhibitors of class I phosphoinositide-3-kinases (PI3Ks) utilizing a DNA-encoded discovery platform

254th National Meeting (2017)

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