Observations on screening-based research and some concerning trends in the literature

被引：95

作者：

Baell, Jonathan B. ^{[1
,2
]}

机构：

[1] Univ Melbourne, Walter & Eliza Hall Inst Med Res, Dept Med Biol, Bundoora, Vic 3086, Australia

[2] Canc Therapeut CRC Pty Ltd, Bundoora, Vic 3086, Australia

来源：

FUTURE MEDICINAL CHEMISTRY | 2010年 / 2卷 / 10期

关键词：

SMALL-MOLECULE INHIBITORS; FALSE POSITIVES; IDENTIFICATION; RECEPTOR; BINDING; ASSAY; COMPLEXES; COVALENT;

D O I：

10.4155/FMC.10.237

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Academic drug discovery is being accompanied by a plethora of publications that report screening hits as good starting points for drug discovery or as useful tool compounds, whereas in many cases this is not so. These compounds may be protein-reactive but can also interfere in bioassays via a number of other means, and it can be very hard to prove early on that they represent false starts. This, for instance, makes it difficult for journals in their assessment of manuscripts submitted for publication. Wider awareness and recognition of these problematic compounds will help the academic drug-discovery community focus on and publish genuinely optimizable screening hits. This will be of general benefit.

引用

页码：1529 / 1546

页数：18

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