High‐Throughput Screening: Evolution of Technology and Methods

Abstract

High‐throughput screening (HTS) can be defined as a process by which hundreds of thousands to millions of compounds are tested for activity against disease targets of interest with the goal of identifying truly active, progressible “hits”. Over the last 20 years high‐throughput screening (HTS) has become a successful, reliable component of the drug discovery process. This article focuses on the variety of screening plate formats and the implications of their usage on the supporting technologies and assay designs.

Best Practices in Compound Management for Preserving Compound Integrity and Accurately Providing Samples for Assays

“…1 This large and diverse set of compound entities that comprise the primary screening set can be stored for a number of years and subjected to a variety of compound-handling processes. Therefore, construction and preservation of compound sets using validated processes are of paramount importance in generating compounds that could potentially make their way into the development pipeline.…”

GPCR Assay Automation for Leveraging Lead Optimization

“…3,4 Given the many drug targets and the quantity of compounds synthesized on a regular basis by pharmaceutical chemistry teams, lead optimization has become more and more dependent on employing high-throughput screening (HTS) technology to efficiently and rapidly enable the characterization of novel chemotypes. [5][6][7] To increase efficiency of the lead evaluation process, screening methods must be faster, cost-effective, and highly reproducible to enable quicker result turnaround time to monitor SAR efforts. To achieve this objective, assay miniaturization with precise, automated execution and rapid data delivery has become the industry goal.…”