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Updated: Jun 8, 2026

High-Throughput Screening to Obtain Crystal Hits for Protein Crystallography
Published on: March 10, 2023
Design and implementation of high throughput screening assays
Ricardo Macarrón1, Robert P Hertzberg
1Molecular Discovery Research, GlaxoSmithKline, 1250 S Collegeville Road, Collegeville, PA 19426, USA. Ricardo.macarron@gsk.com
Abstract:
High throughput screening (HTS) is at the core of the drug discovery process, and so it is critical to design and implement HTS assays in a comprehensive fashion involving scientists from the disciplines of biology, chemistry, engineering, and informatics. This requires careful analysis of many variables, starting with the choice of assay target and ending with the discovery of lead compounds. At every step in this process, there are decisions to be made that can greatly impact the outcome of the HTS effort, to the point of making it a success or a failure. Although specific guidelines should be established to insure that the screening assay reaches an acceptable level of quality, many choices require pragmatism and the ability to compromise opposing forces.

