Pharmaceutical profiling in drug discovery

被引:217
作者
Kerns, EH [1 ]
Di, L [1 ]
机构
[1] Wyeth Ayerst Res, Chem Sci, Discovery Analyt Chem, Princeton, NJ 08543 USA
关键词
D O I
10.1016/S1359-6446(03)02649-7
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Drug discovery research organizations are building capability for measuring an ensemble of crucial 'drug-like' properties. These structure-property relationship (SPR) data complement current SAR information. This pharmaceutical profiling strategy enables research teams to better plan and interpret discovery experiments, be alerted to potential 'show stoppers', improve property liabilities, and select the best candidates for advancement. High throughput property assays for physicochemical properties - solubility, permeability, lipophilicity, stability, and pK(a) - in vitro ADME - metabolism, transporters, protein binding and CYP inhibition - and in vivo PK/exposure provide a wealth of data for teams to make informed decisions.
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页码:316 / 323
页数:8
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