Laura Guasch; Michael Reutlinger; Daniel Stoffler; Moreno Wichert
Chimia, 2021, 75(1), 105-107
https://doi.org/10.2533/chimia.2021.105

Abstract

DNA-encoded library (DEL) technology has emerged as one of the fastest and most cost-effective screening platforms available in industry both for hit discovery as well as more recently for druggability and tractability assessments and successive prioritization of therapeutic targets in the early phase of drug discovery programs. The key principle of DELs is based on the combinatorial assembly (synthesis) of library members from chemical building blocks (BBs) and the corresponding tagging of each BB with unique DNA sequences (barcodes) in an alternating fashion of chemical reactions and DNA ligations. In analogy to phage display technology, this physical linkage of small organic molecules with distinctive DNA barcodes enables to deconvolute the chemical identity (structure) of each and every molecule by next-generation sequencing (NGS) at any time.