High-throughput Screening (HTS)

The process of looking for a new drug against a specific target for a certain disease commonly involves high-throughput screening (HTS), wherein large libraries of chemicals are tested for their ability to modulate the biological activity of the target. For instance, if the target is a novel GPCR, compounds will be screened for their ability to inhibit or stimulate the receptor; if the target is a protein kinase, the chemicals will be tested for their ability to inhibit the kinase. Creative Biostructure provides custom high-throughput screening services, and our biochemical/cell-based HTS technologies allow us to efficiently screen hits from a variety of compound libraries.

HTS is a technology system that combines a variety of technical approaches, usually involving robotics, liquid handling devices, detectors, and specialized software for instrument control and data processing. It is based on molecular and/or cell-based experimental methods and is performed in the form of microplates as experimental tools. An automatic operating system is needed to execute the experimental procedure. During the experiment, the data is collected by fast and sensitive detectors and then processed and analyzed by specialized software.

The high-throughput equipment of Creative Biostructure supports the screening of corresponding compound libraries by various detection methods, such as optical, fluorescence, radioactive detection technology, crystallography, and the multi-functional microplate detection system.

Our HTS compound libraries including but not limited to:

• Natural product libraries
• Full-scale hit screening libraries
• Known bioactive and FDA approved drug libraries
• Target-specific libraries (e.g. GPCR, kinase, ion channel, protease)
• Research area-specific libraries (e.g. epigenetics, autophagy)
• Disease-specific libraries (e.g. cancer, virus infection)

Our libraries support high-throughput screening in typical formats including 96-, 384-, 1536- and even 3456-well plates. During the HTS process, we strictly abide by industry standards to monitor all key steps. At the beginning of an HTS program, we first revise the HTS approach, and then carry out the screening of the reference compound, subsequently perform the preliminary screening of the compound, hit analysis, hit confirmation, IC50 value confirmation and early structure-activity relationship (SAR) analysis.

Figure 1. Our general procedure for high-throughput screening.

Advantages of our High-throughput Screening services:

• We can perform a wide range of HTS approaches and multiple compound library screening.
• We have strict quality control (QC) criteria to control the effectiveness of the HTS process.
• Our team has extensive experience in running automation platforms and large-scale assays.
• We can develop, optimize, and validate HTS approaches according to specific targets or other research requirements.
• Our achievements in the development and automation of high-throughput crystallography methods allow us to efficiently screen many small molecules for their ability to bind to targets, thereby accelerating the process of finding innovative drug candidates.

Creative Biostructure is a reliable partner in drug discovery. For each HTS program, we recommend suitable screening strategy and protocol according to the specific research needs of customers and then conduct screening experiments and data collection required for the project.