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OverviewHigh quality leads provide the foundation for the discovery of successful clinical development candidates, and therefore the identi?cation of leads is an essential part of drug discovery. The process for the identi?cation of leads generally starts with the screening of a compound collection, either an HTS of a relatively large compound collection (hundreds of thousands to one million plus compounds) or a more focused screen of a smaller set of compounds that have been preselected for the target of interest. Virtual screening methods such as structure-based or pharmacophore-based searches can complement or replace one of the above approaches. Once hits are identi?ed from one or more of these screening methods, they need to be thoroughly characterized in order to con?rm activity and identify areas in need of optimization. Finally, once fully characterized hits are identi?ed, preliminary optimization through synthetic modi?cation is carried out to generate leads. Parallel optimization of all properties, including biological, physicochemical, and ADME is the most ef?cient approach to the identi?cation of leads. Hit characterization is described in the previous chapter. The focus of this chapter is on hit optimization and the identi?- tion of leads. After a general overview of these processes, examples taken from the literature since 2001 will be used to illustrate speci?c points. There are also a number of excellent reviews covering the lead identi?cation process [1–6]. Full Product DetailsAuthor: Matthew M. HaywardPublisher: Springer-Verlag Berlin and Heidelberg GmbH & Co. KG Imprint: Springer-Verlag Berlin and Heidelberg GmbH & Co. K Edition: 2010 ed. Volume: 5 Dimensions: Width: 15.50cm , Height: 1.20cm , Length: 23.50cm Weight: 0.361kg ISBN: 9783642261060ISBN 10: 364226106 Pages: 217 Publication Date: 14 March 2012 Audience: Professional and scholarly , Professional & Vocational Format: Paperback Publisher's Status: Active Availability: Manufactured on demand  We will order this item for you from a manufactured on demand supplier. Table of ContentsHit Triage: Medicinal Chemistry Strategies to Improve the Odds of Success in Discovery.- Lead Identification.- Lead Discovery Using Virtual Screening.- Overview of Hit to Lead: The Medicinal Chemist's Role from HTS Retest to Lead Optimization Hand Off.- NMR Spectroscopy in Fragment Based Drug Design.- High Throughput Screening in the Twenty-First Century.ReviewsAuthor InformationTab Content 6Author Website:Countries AvailableAll regions |
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