Lead-Seeking Approaches
Matthew M. Hayward
mar. 2010 · Topics in Medicinal Chemistry Bog 5 · Springer Science & Business Media
E-bog
217
Sider
reportBedømmelser og anmeldelser verificeres ikke Få flere oplysninger
Om denne e-bog
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].
Bedøm denne e-bog
Fortæl os, hvad du mener.
Oplysninger om læsning
Smartphones og tablets
Installer appen Google Play Bøger til Android og iPad/iPhone. Den synkroniserer automatisk med din konto og giver dig mulighed for at læse online eller offline, uanset hvor du er.
Bærbare og stationære computere
Du kan høre lydbøger, du har købt i Google Play via browseren på din computer.
e-læsere og andre enheder
Hvis du vil læse på e-ink-enheder som f.eks. Kobo-e-læsere, skal du downloade en fil og overføre den til din enhed. Følg den detaljerede vejledning i Hjælp for at overføre filerne til understøttede e-læsere.
