High-Throughput Purification Platform in Support of Drug Discovery
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- 作者：Min Liu ; Kuanchang Chen ; Denny Christian ; Tazeen Fatima ; Natalya Pissarnitski ; Eric Streckfuss ; Chaowei Zhang ; Lei Xia ; Scott Borges ; Zhicai Shi ; Petr Vachal ; James Tata ; John Athanasopoulos
- 刊名：ACS Combinatorial Science
- 出版年：2012
- 出版时间：January 9, 2012
- 年：2012
- 卷：14
- 期：1
- 页码：51-59
- 全文大小：653K
- 年卷期：v.14,no.1(January 9, 2012)
- ISSN：2156-8944
文摘
The application of parallel synthesis is an efficient approach to explore the chemical space and to rapidly develop meaningful structure activity relationship (SAR) data for drug discovery programs. However, the effectiveness of the parallel synthesis requires a high throughput purification workflow that can process a large number of crude samples within a meaningful time frame. This paper describes a high throughput purification platform that has been adopted at Merck鈥檚 Rahway research site. The platform includes the evaluation of crude samples, mass-directed HPLC purification, fraction analysis, compound registration, final compound purity assessment and assay distribution. Assisting with the sample tracking and the data management is the internally designed laboratory information management system, Light Automation Framework (LAF). Using this process and the tools described herein, the group has successfully achieved purities of 95% or greater for 90% of samples.r>