HTS is a drug-discovery process widely used in the pharmaceutical companies and biomedical research institutes. Using robotics, data processing and control software, liquid handling devices and sensitive detectors, HTS conduct extremely scalable assay to test the biological or biochemical activity of a large number of small molecules for discovering active agents for receptors, enzymes, ion-channels or other pharmacological targets in the molecular and cellular level of biomolecular pathway. Typically, HTS assays are performed in microtiter plates with a 96 or 384 well format. HTS is one of main facilities in our lab to provide comprehensive services including the use of HTS technology, compounds in various libraries, a database of results from screens and lead optimization. On a collaborative basis, HTS has the capability to support cellular and biochemical assays using absorbance, fluorescent kinetics, fluorescence resonance energy transfer, AlphaScreen, bioluminescence and cellular fluorescence imaging. In addition, HTS has expertise in adapting those biological and biochemical bench-top assays into high-throughput screening settings. Our HTS libraries are designed for diversity around not only well-established pharmacophore, but also very strict molecular property profiles that were balanced between diversity, physicochemical favorability, intrinsic complexity, and synthetic tractability. Encouraged by the fact that a significant number of marketed drugs are derived from natural products, we are also interested in expanding natural chemical products in compound libraries and developing effective strategy to diversify the core backbone structure of natural products. We will design and explore biomimetric synthetic pathways to build up the molecule efficiently. Easily modified structure and high selective strategy will be preferred. The organocascade type assembling of complex structure will eventually result in the discovery of novel bio-valuable molecules to diversify the library.