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鉴定命中靶点行动计划(APHID):以 KAT6A 为例。

Action plan for hit identification (APHID): KAT6A as a case study.

机构信息

School of Pharmaceutical Sciences, Nanjing Tech University, Number 30 South Puzhu Road, Nanjing, 211816, PR China.

Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.

出版信息

Future Med Chem. 2020 Mar;12(5):423-437. doi: 10.4155/fmc-2019-0212. Epub 2020 Feb 17.

Abstract

Here, we describe our action plan for hit identification (APHID) that guides the process of hit triage, with elimination of less tractable hits and retention of more tractable hits. We exemplify the process with reference to our high-throughput screening (HTS) campaign against the enzyme, KAT6A, that resulted in successful identification of a tractable hit. We hope that APHID could serve as a useful, concise and digestible guide for those involved in HTS and hit triage, especially those that are relatively new to this exciting and continually evolving technology.

摘要

在这里,我们描述了我们的命中鉴定行动计划(APHID),该计划指导命中分类过程,淘汰较难处理的命中,保留较易处理的命中。我们以我们针对酶 KAT6A 的高通量筛选 (HTS) 活动为例来说明这一过程,该活动成功鉴定了一个易处理的命中。我们希望 APHID 可以为参与 HTS 和命中分类的人员,特别是那些对这项令人兴奋且不断发展的技术相对较新的人员提供有用、简洁和易于理解的指南。

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