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Leveraging High-Throughput Screening services to accelerate Drug Discovery and Development

Leveraging High-Throughput Screening services to accelerate Drug Discovery and Development

High-throughput screening (HTS) solutions enable rapid testing of chemical and biological compounds for various applications. Both enzyme/protein and cell-based assays are employed in combination with fluorescence, absorbance, luminescence, and scintillation detection methods. The complexity and need for significant upfront expenditures often drive drug developers to outsource HTS activities.

Expanding beyond Target Identification

HTS was initially used for lead identification and candidate optimization, and these two applications continue to remain prominent. It dramatically accelerates these activities, reducing the cost and time required for drug discovery and early-phase development. In addition, cost-effective, rapid screening of vast compound libraries, which can consist of many different types of small to large molecules, can find compounds that function via previously unknown mechanisms of action.

Today, high-throughput mass spectrometry solutions, DNA-encoded library technology (DELT), and advanced off-the-shelf, scalable software and automation tools are enabling the application of HTS to activities beyond target identification to include HT-ADME screening, tox studies, and the identification of optimum excipients and formulations.1 Use of artificial intelligence and machine learning, meanwhile, are facilitating in silico screening and the development of novel models.

There is also growing interest in more targeted HTS using representative subsets of massive compound libraries to reduce the likelihood of false hits and further lower the time and cost of these projects.1 Medium-throughput compound profiling assays are, for instance, used to gather pharmacokinetic properties and target selectivity data.2

As a result, while HTS is still applied to G-protein coupled receptors, ion channels, and kinases, R&D programs are increasingly exploring novel enzymes and immuno-oncology targets using technology.3 For instance, RNA interference3 and targeted protein degradation1 screens are helping to identify proteins involved in disease mechanisms previously thought to be undruggable.

Increased reliance on third-party HTS services

HTS benefits cannot be attained without significant upfront investment in specialized equipment and expertise required to perform these experiments and analyze the data they generate. Reliance on contract research organizations (CROs) has, not surprisingly, increased as a result.

Many CROs have responded by adding HTS capabilities to their portfolios. They typically perform screens, assay development, miniaturization, automation, and validation and provide data storage and analysis, among other services.

It is estimated that the value of the global HTS market will reach nearly $37 billion by 2030, expanding at a compound annual growth rate of 7.82%.4 The services segment is expected to grow fastest, as is the drug discovery segment (based on application) and the CRO segment (based on end-user).

Selecting the ‘right’ HTS outsourcing partner

With more CROs establishing flexible HTS capabilities, even small, emerging biopharma companies now have access to this effective means for accelerating drug discovery. When outsourcing HTS projects, drug developers must select CROs with trained and experienced staff, state-of-the-art equipment and software, numerous and varied compound libraries, and insight into when medium to ultra-high-throughput solutions are appropriate.

However, technical capabilities should not be the only consideration. To achieve maximal outcomes in HTS projects, the HTS service provider should act as a true partner, serving as an extension of their clients. A commitment to open communication and transparency and the provision of results on time, in full, and at the highest level of quality are equally important attributes.

By choosing the right CRO to support drug discovery and development efforts leveraging HTS techniques, drug developers can increase their chances of identifying truly novel candidates, accelerate projects, lower development costs, and reduce time-to-market.


  1. 20/15 Visioneers, “Trends in High Throughput Screening,” Bog, November 8, 2021, https://www.20visioneers15.com/post/throughput-screening
  2. D Cronk, “Chapter 8 – High-throughput screening” in Drug Discovery and Development (Second Edition), 2013 Pages 95-117. Ed. RG Hill and HP Rang
  3. Rachel Brazil, “Navigating Drug Discovery With High-Throughput Screening,” Technology Networks Drug Discovery, February 21, 2018. https://www.technologynetworks.com/drug-discovery/articles/navigating-drug-discovery-with-high-throughput-screening-297350
  4. Zion Market Research, “Global High-Throughput Screening Market Size is Projected to Grow to Be Worth USD 36.84 Billion by 2030, Expanding at a CAGR of 7.82%,” Press Release, January 23, 2023. https://www.globenewswire.com/en/news-release/2023/01/23/2593099/0/en/Global-High-Throughput-Screening-Market-Size-is-Projected-to-Grow-to-Be-Worth-USD-36-84-Billion-by-2030-Expanding-at-a-CAGR-of-7-82.html


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