High-Throughput Screening
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High-Throughput Screening

High-throughput screening (HTS) allows researchers to perform millions of biological, chemical, genetic, or pharmacological tests in a short time. It is mainly used in the drug discovery process to identify biologically relevant compounds. HTS is a useful tool for evaluating, for example, pharmacological targets, pharmacological profiling, and receptor antagonists (such as GPCRs) and enzymes.

Introduction of High-Throughput Screening

High-throughput screening is based on experimental approaches at the molecular and cellular levels. It takes the microplate as the experimental tool carrier, then performs the test process with an automated operating system. Experimental data is automatically collected with sensitive and fast detection instruments. HTS can test tens of millions of samples at the same time and get the corresponding database to support the operation of the technical system. HTS technology provides more rapid, sensitive, and accurate tools compared with conventional method.

Classification of High-Throughput Screening

1. According to different experimental models

  • Molecular level screening (Experimental method includes Enzyme-linked immunosorbent assay (ELISA), Fluorescence resonance energy transfer (FRET), Fluorescence polarization immunoassay (FPIA), surface plasmon resonance (SPR), Alphascreen, ADP-Glo, etc.)
  • Cell level screening (Experimental method includes CCK-8, Celltiter-Glo, etc.)

2. According to different screening strategies

  • Target-based screening
  • Phenotype-based screening

High throughput screening process

  • Design screening scheme
  • Preliminary experiment and optimization
  • Small scale test
  • Prepare screening resources
  • Purchasing agent
  • High-throughput drug screening
  • Data analysis


  • HTS makes full use of pharmaceutical resources to achieve the scale of drug screening, improve the probability of drug discovery, and improve the quality of new drugs.
  • The micro-screening system saves the sample resources, lays the material foundation of "one drug, multiple screening", and reduces the cost of single drug screening.
  • The highly automated operation reduces the occurrence of operation errors and improves the screening efficiency and the accuracy of results.
  • In the process of high-throughput screening, pharmacological techniques and theories are applied, and closely combined with medicinal chemistry, molecular biology, cell biology, mathematics, microbiology, computer science, and other disciplines. The combination of multiple disciplines has produced a large number of new topics in drug screening, and promotes the development of drug screening theory and technology.


  1. Hertzberg RP; et al. High-throughput screening: new technology for the 21st century. Curr Opin Chem Biol. 2000 Aug; 4(4): 445-51.
  2. Mayr L M; et al. The future of high-throughput screening. SLAS Discovery. 2008, 13(6): 443-448.
  3. Wildey M.J.; et al. High-throughput screening. Annual Reports in Medicinal Chemistry. 2017, 50, pp.149-195.