Components of successful lead generation

被引:80
作者
Davis, AM
Keeling, DJ
Steele, J
Tomkinson, NP
Tinker, AC
机构
[1] AstraZeneca R&D Charnwood, Dept Med Chem, Loughborough LE11 5RH, Leics, England
[2] AstraZeneca R&D Charnwood, Dept Biol Mol, Loughborough LE11 5RH, Leics, England
[3] AstraZeneca R&D Charnwood, Dept Phys, Loughborough LE11 5RH, Leics, England
[4] AstraZeneca R&D Charnwood, Dept Metab Sci, Loughborough LE11 5RH, Leics, England
关键词
D O I
10.2174/1568026053828411
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
This review aims to give an overview of current good practice in the prosecution of Lead Generation. it will assess experiences across the field as judged from the contents of the limited number of peer-review disclosures to date. It will also rely heavily on the experiences of the authors from many campaigns within this organisation. Its focus will be on the assembly of an appropriate compound collection for application in High Throughput Screening (HTS), the prosecution of HTS, the profiling of HTS output and, lastly the Hit-to-Lead optimisation of selected HTS output. Excluded from the scope are detailed aspects of library design [1], parallel synthesis [2], virtual library applications [3], virtual screening [4] and fragment screening [5] approaches, all of which have been the subject of recent reviews.
引用
收藏
页码:421 / 439
页数:19
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