Discussion

Multiple technologies for DNA-encoded library (DEL) synthesis and target screening have been explored with the aim to improve the lead discovery process. Our data from the application of DELs suggests that a comprehensive coverage of chemical space at the fragment level is pivotal for a successful screening outcome. Consequently, the number, diversity and density coverage of fragments and not merely the number of final compounds is essential for identification of hits with comprehensive SAR and the best optimization properties. Here, the principle of the DNA-encoding technology and its application for hit identification against epigenetic targets will be presented.