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Conception
With the improvement of combinatorial chemistry, millions of compounds can be synthesized in a short time. But face so many molecules, what we need is a new technique to detect them. So, HTS was developed. Using automatic systems, micro-plate carriers, Sensitive detectors, and data processing and control software, High Throughput Screening allows a researcher to conduct millions of biochemical, genetic or pharmacological tests at the same time and to rapidly select out what he want.
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The device used in HTS
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Component

Automatic system Sample library Sensitive detectors Data processing devices Other assisted equipments
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Automation is an important element in HTS. Typically, an integrated robot system consisting of one or more robots transports assay-microplates from station to station for sample or reagent addition, mixing, dilution, incubation, and finally detection. Sample library usually include the compound library in which most of these compounds are small molecule synthesized in the lab, natural products that are importa nt to design of new drug, and combinatorial peptide libraries.
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Fluorescence analysis
Homogeneous time resolved fluorescence analysis (HTRF) Fluorescence polarization analysis (FP) Others

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HTRF is a technology based on fluorescence emission, using pulse laser as light source. and the fluorescence that test substance radiates has a special half-lives, then the researcher can choose a suitable time to detect fluorescence’s change of test substance , without any other interference.
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With more and more advantages of HTS being found, the HTS field continues to be dynamic and very competitive. In the future, HTS will be essential to chemistry, biology, pharmacy and so on.
FP is also widely applied in immunoassay.
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fluorescence polarization immunoassay (FPIA).
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Emergence of HTS has deeply improved the efficiency of screening and also make drug screening enter into a new stage. At present, the methods of HTS are applied to the screening of drug-discovery, genomics, protein, and peptide libraries. But, The goal of HTS is to accelerate drug discovery by screening large libraries often composed of hundreds of thousands of compounds (drug candidates) at a rate that may exceed 20,000 compounds per weeNow in most pharmaceutical and biotechnology companies HTS is a central function in the drug discovery process. This process can be described as the phase from Target to Lead. Target choice Assay development Screening collection HTS implementation Data capture, storage and analysis Lead compound
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HTRF DEVICE
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FP is usually used for analysis of molecular interaction in chemistry and biology. The most important element to FP is fluorescently labeled small molecule, which is also competitor to test substance. The researcher can detect these small molecule s’ polarization coefficients in free state and combination state to screen the substance.
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Screening model
Model based on level of molecule: receptor screening model ion channel screening model enzyme screening model. Model based on level of cell: reporter gene assay. The former could provide us with straightforward informations about compounds’ activity, while the latter can not reflect definite pathway or target cells that compounds have effects on.
High Throughput Screening
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OUTLINE 1. Conception of HTS 2. Component 3. Screening model 4. Methods of detection 5. Application of HTS
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Method of detection
To quickly and efficiently screen a large number of compounds, new methods, such as fluorescence analysis and radioisotope technique, have been builded.