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Lead-Seeking Approaches (Paperback, 2010 ed.)
Loot Price: R4,210
Discovery Miles 42 100
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Lead-Seeking Approaches (Paperback, 2010 ed.)
Series: Topics in Medicinal Chemistry, 5
Expected to ship within 10 - 15 working days
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High 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].
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