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   Compound screening services

Lack of compound screening capability was one of the weakest components in China’s drug innovation system and a “bottleneck” in the transformation, from imitation to innovation, of its pharmaceutical industry. Adopting modern drug screening technologies, the National Center for Drug Screening will fundamentally change the methodology currently employed in China’s drug discovery practices and thus expedite the drug innovation process.

High-throughput screening (HTS) is an innovative approach within the drug discovery paradigm that combines the application of multi-disciplinary knowledge with the integration of advanced technologies to expedite the identification and development of active molecules or "hits" into potential drug ‘leads’ with desired therapeutic activity. The Center utilizes internationally validated HTS technologies, which have advantages such as the rapid detection of trace quantities with high sensitivity and accuracy. HTS decreases the amount of testing compound required such that only microgram quantities are needed, which permits certain natural products that are difficult to isolate and purify and for compounds that are difficult to synthesize to be assayed. Also compounds can be tested multiple times in different screening models, thereby increasing the probability of discovering new leads and drug candidates.

The Center is among the first in China to establish a high content screening (HCS) platform with appropriate technical personnel support. HCS is based on automated high-resolution fluorescent microscopy imaging technology. It is a multi-parameter functional analysis system that can provide a large amount of biological information including cell growth, differentiation, migration, apoptosis, metabolic and signal transduction pathways. Insights from these information-rich analyses could help scientists to understand pharmacological and toxic properties of a lead compound at the early stage of discovery, thereby significantly improving the efficiency of candidate confirmation and resultant success rate of drug development.

Presently, the Center is applying more than 200 in vitro and in vivo bioassays, including over 100 HTS or HCS models, with the screening capacity reaching approximately 100,000 samples per day. The Center routinely performs HTS/HCS studies both as internal research programs and as services provided to several hundred drug research and development entities across China. Through years of accumulation and in-depth investigations, it has discovered a number of new leads or drug candidates with great promise, some of them have already entered pre-clinical or clinical studies, and relevant patent applications have been filed.