High-throughput Screening

High-throughput screening (HTS) plays a critical role in the lead discovery of drug exploration. With the advancement of the pharmaceutical industry, the application of HTS in basic and applied research has also received more and more attention. At present, HTS has become a mature technology that is also the basis of the starting for drug discovery. Creative Biolabs is a recognized expert who is good at applying advanced HTS technology to the drug discovery process. With many years of rich experience, our scientists can provide efficient HTS services to precisely meet the needs of global customers.

Current drug discovery is based on a large number of screenings of specific chemical libraries to find new chemical forms that are needed. In fact, a successful drug relies on a large number of screened compounds. Therefore, drug discovery is a time-consuming and highly complex process. As an effective strategy, HTS can be used to collect a large amount of experimental data in a relatively short time.

Introduction of HTS

HTS is mainly a process of screening and analyzing a large number of biological compounds for specific targets. In modern drug discovery, HTS is usually defined as testing 10,000 to 100,000 compounds per day. HTS is suitable for combinatorial chemistry, genomics, protein and peptide library screening. The main goal of this technology is to speed up the drug discovery process by screening large compound libraries in a short period. HTS includes several steps, including target identification, compound management, reagent preparation, analytical development, and high-throughput library screening.

Steps involved in drug discovery. Fig.1 Steps involved in drug discovery. (Aldewachi, 2021)

Advantages of HTS

HTS has the characteristics of fast, low cost, simple, and high efficiency. What is more, HTS is closely related to automated operating platforms, high-sensitivity detection systems, specific screening models, abundant component libraries, and data collection and processing systems. A variety of technologies including nuclear magnetic resonance (NMR), DNA microarray, fluorescence, and other new technologies have the potential to screen more than 100,000 samples per day. A key feature of NMR technology is that it can provide direct information on the binding position of compounds and proteins. DNA microarrays can be used in HTS to further explore the expression of biological targets related to human diseases, thereby opening up new directions for drug discovery.

Applications and Development

HTS is widely used in new drug discovery, replacing traditional methods to determine therapeutic targets. When little is known about the target, HTS usually becomes the appropriate method, which excludes structure-based drug design, but it can also be used in parallel with other strategies including computational techniques and fragment-based drug design. In addition, the combination of HTS and porous cell-related platforms can identify some small molecule modulators. More importantly, HTS not only facilitates drug discovery but also helps to explore existing drug components to optimize their activity. Currently, fluorescence-based technologies are likely to be one of the most important detection methods for HTS because they possess high sensitivity and allow for miniaturization.

Creative Biolabs can provide a variety of HTS services to support your research through our advanced technology platform and the most professional team of scientists. Please feel free to contact us for more details.


  1. Aldewachi, H.; et al. High-throughput screening platforms in the discovery of novel drugs for neurodegenerative diseases. Bioengineering. 2021, 8(2): 30.
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