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Hit optimization strategies

Glaser V. Optimizing strategies for hit-to-lead process. Gen. Engin. Biotech. News. 2005 25 31-37. [Pg.1975]

A detailed description of screening methods used in FBLG is beyond the scope of this chapter many FBLG reviews are available [34-39]. We will just briefly outline some of the assays used for fi agment hit identification before exploring strategies and tactics employed in hit optimization. [Pg.135]

Each screening center has medicinal and synthetic chemistry expertise in order to optimize hits identified from HTS campaigns and develop them into chemical probes. Specific capabilities vary, however typical strategies employed include parallel synthesis, computational and informatics analysis, and analytical capabilities such as LC/MS techniques. The structures of novel compounds that are prepared, their synthetic protocols, analytical data and biological data are all available, and samples of final probes developed are deposited into the MLSMR. A Working Group comprised of chemists from each center meets regularly to share information, best practices, and insure optimal use of resources. [Pg.408]

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