Massively Parallel, Single-Molecule Assessment of Synthetic Fidelity and Drug-Like Properties in a DNA-Encoded Library.

Grant Koch¹, Meghan F Lawler², Adam Murray¹, Neil Carlson², Alexander Engstrom¹, Panpan Zhang¹, Mariel Steiner¹, Sarah Beth Avila¹, Kaileigh Cloutier-Leblanc², Sumudu Leelananda², LaShadric C Grady², Jaru Taechalertpaisarn¹, Conor Corcoran¹, Nicolas Tilmans², R Scott Lokey¹

¹Address: Department of Chemistry and Biochemistry, University of California, Santa Cruz; 1156 High Street, Santa Cruz, California95064, United States.

²Address: Anagenex, 20 Maguire Rd Suite 302, Lexington, Massachusetts02421, United States.

PubMed DOI

Abstract

DNA-encoded libraries (DELs) are powerful drug discovery tools, enabling rapid hit generation against immobilized protein targets. However, translating these hits is often hampered by synthetic inefficiency and, for libraries of "beyond-Rule-of-5" compounds such as macrocyclic peptides, by enrichment of poorly cell-permeable members. Here we introduce LC-seq, a sequencing-based chromatographic str…

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