High Throughput Screening (HTS)

High Throughput Screening (HTS) designates automated methodologies rapidly testing large compound libraries against biological targets, enabling efficient identification of active molecules in drug discovery through miniaturised assays, robotic liquid handling, sensitive detection systems, and sophisticated data management. These platforms screen thousands to millions of compounds within days or weeks.

The pharmaceutical industry relies on HTS as foundational drug discovery tool identifying starting points for development programmes. Assay development optimises conditions for robust, reproducible performance in miniaturised formats, validating through Z-factor and signal-to-noise metrics. Screening strategies employ single-concentration primary screens followed by dose-response confirmation of active compounds. Follow-up includes counter-screening against related targets assessing selectivity, cytotoxicity evaluation, and structural cluster analysis. Alternative approaches include high-content screening incorporating imaging, fragment-based screening, and virtual screening computationally filtering libraries. As compound libraries grow and artificial intelligence enhances hit identification, HTS evolves through miniaturisation and integration with computational approaches.