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Chembiochem. 2017 May 4;18(9):837-842. doi: 10.1002/cbic.201700014. Epub 2017 Mar 24.

Discovering Drugs with DNA-Encoded Library Technology: From Concept to Clinic with an Inhibitor of Soluble Epoxide Hydrolase.

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GlaxoSmithKline R&D, 830 Winter Street, Waltham, MA, 02451, USA.
GlaxoSmithKline R&D, 709 Swedeland Road, King of Prussia, PA, 19406, USA.


DNA-encoded chemical library technology was developed with the vision of its becoming a transformational platform for drug discovery. The hope was that a new paradigm for the discovery of low-molecular-weight drugs would be enabled by combining the vast molecular diversity achievable with combinatorial chemistry, the information-encoding attributes of DNA, the power of molecular biology, and a streamlined selection-based discovery process. Here, we describe the discovery and early clinical development of GSK2256294, an inhibitor of soluble epoxide hydrolase (sEH, EPHX2), by using encoded-library technology (ELT). GSK2256294 is an orally bioavailable, potent and selective inhibitor of sEH that has a long half life and produced no serious adverse events in a first-time-in-human clinical study. To our knowledge, GSK2256294 is the first molecule discovered from this technology to enter human clinical testing and represents a realization of the vision that DNA-encoded chemical library technology can efficiently yield molecules with favorable properties that can be readily progressed into high-quality drugs.


DNA-encoded chemical library; clinical trials; drug development; drug discovery; hydrolases

[Indexed for MEDLINE]

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