Chemical Libraries and High-Throughput Screening

Modern drug discovery relies heavily on high-throughput screening of vast chemical libraries to identify promising small molecule drug candidates. Chemical libraries contain millions of synthetic small molecules and natural product extracts that can be rapidly tested for biological activity. State-of-the-art automation allows thousands of compounds to be screened per day against targets of interest. This high-throughput approach casts a wide net to efficiently discover hits that may not have beenpredicted based on target biology alone. Companies spend billions to develop proprietary libraries optimized for qualities like diversity, developability, and intellectual property protection.

Target Identification and Validation

The targets selected for screening campaigns must be carefully validated to increase the odds of Small Molecule Drug Discovery clinically useful therapeutics. A clear link between the target and a disease process must be established along with an understanding of how modulating target activity could provide clinical benefit. Relevant biomarkers and assays are developed to measure target engagement by screened compounds to detect and quantify hits. Knowledge of a target's biology, interacting partners, expression patterns, and potential adverse effects guides selectivity optimization efforts during lead discovery and development.

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