Nonleadlikeness and leadlikeness in biochemical screening

被引：308

作者：

Rishton, GM ^{[1
]}

机构：

[1] Amgen Inc, Thousand Oaks, CA 91320 USA

来源：

DRUG DISCOVERY TODAY | 2003年 / 8卷 / 02期

关键词：

D O I：

10.1016/S1359644602025722

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Biochemical assays have largely supplanted functional biological assays as drug screening tools in the early stages of drug discovery. The de-selection of compounds that are 'nonleadlike' binders (and bonders) and the proactive selection of those compounds that are 'leadlike' in their binding to the target are vital components of the screening effort. The physiochemical properties of leadlikeness and the surprising differences between those properties and the now classical definitions of druglikeness are becoming apparent.

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页码：86 / 96

页数：11

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