Encoded Library Technologies as Integrated Lead Finding Platforms for Drug Discovery.

Area of Science:

• Pharmaceutical research and development
• Medicinal chemistry
• Drug discovery

Background:

• Pharmaceutical research increasingly targets novel, uncharted biological entities.
• Existing compound collections struggle to provide suitable chemical matter for these new targets.
• Encoded library technologies offer a solution for rapid, large-scale chemical space exploration.

Purpose of the Study:

• To review the application of two complementary encoded library platforms at Novartis.
• To highlight the benefits of in-house implementation of DNA-encoded and peptide libraries.
• To demonstrate the utility of encoded libraries in identifying ligands for challenging targets.

Main Methods:

• Application of DNA-encoded libraries for identifying low-molecular weight ligands.
• Utilization of encoded peptide libraries for identifying cyclic peptides.
• In-house operation of both encoded library platforms to accelerate drug discovery programs.

Main Results:

• Encoded libraries enable rapid exploration of vast chemical space.
• Identified ligands serve as crucial tools for target validation and assay development.
• These ligands also act as starting points for medicinal chemistry optimization.

Conclusions:

• Internalizing DNA-encoded and peptide library platforms enhances drug discovery initiation.
• Running both pipelines in-house provides a comprehensive approach to ligand identification.
• Encoded library technologies are vital for addressing the challenges of modern pharmaceutical research.