Certain points of consideration in High Throughput Screening (HTS)

High Throughput Screening

Drug discovery needs a particular attention as it is facing many productivity challenges. “Post-genome era” has introduced so many new targets of therapeutic interest but financial pressures and the safety profiles are among the two most important factors affecting the production of new molecular entities (NMEs) annually that work against 3-4 new targets.

High Throughput Screening (HTS) is consisted of many processes and involved in drug discovery and is considered to be an important relevant process in the field of biology and chemistry. The concept of HTS is not so much old. First paper in PubMed citing “HTS” in its title was published in 1991. Remember, drug discovery from initial time, i.e. target identification, to approval is currently taking on average, 13.5 years costing about U.S. $1.5billion per drug. HTS optimization to reduce this drug discovery process and cost is one of the most important research targets.

According to the researchers, many factors are contributing to the seemingly failure of HTS.

These factors include poorly validated targets, early non-drug-like compound collections, small screening libraries, a limited follow-up capacity, highly artificial and non-physiological assay systems, a limited informatics capacity, a severe lack of appropriate animal models, unpredictable toxicities and a bias against attributing the origins of compounds to HTS.

These factors can be studied in detail to make HTS optimal with time.

How to achieve an optimal composition and size of the screening library, i.e. chemical compounds library, is an important question in the pharmaceutical research while considering HTS. Getting composition in compound libraries is often considered as an important process in screening. However, designing and maintaining a high-quality screening library is expensive. Another important aspect in screening libraries is that the libraries often include dye and fine chemical activities without giving much attention to the development of libraries suitable for drug discovery. However, “the concept of chemical diversity is evolving from ‘more is better’ to ‘more chemotypes are better’” and in this concept more and more companies and researchers are now considering the question “what is the optimal composition of a screening collection?”

However, in drug research, HTS in combination with other novel biological, biotechnological and bioinformatical techniques can help in further enhancement of the drug research.


Ricardo Macarron, Martyn N. Banks, Dejan Bojanic, David J. Burns, Dragan A. Cirovic, Tina Garyantes, Darren V. S. Green, Robert P. Hertzberg, William P. Janzen, Jeff W. Paslay, Ulrich Schopfer and G. Sitta Sittampalam, (2011). Impact of high-throughput screening in biomedical research. Nature Reviews; Drug Discovery, doi:10.1038/nrd3368


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