Solution-Based Indirect Affinity Selection Mass Spectrometry鈥擜 General Tool For High-Throughput Screening Of Pharmaceutical Compound Libraries

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• 作者：Thomas N. O鈥機onnell ; Jason Ramsay ; Steven F. Rieth ; Michael J. Shapiro ; Justin G. Stroh
• 刊名：Analytical Chemistry
• 出版年：2014
• 出版时间：August 5, 2014
• 年：2014
• 卷：86
• 期：15
• 页码：7413-7420
• 全文大小：554K
• ISSN：1520-6882

文摘

We show here that an automated solution-based affinity selection mass spectrometry (ASMS) system can be built exclusively from commercially available parts. The value of this technology lies in the throughput (1 脳 10⁵ compounds/day) coupled with a low hit rate. The system, being a binding assay, requires little development time yielding a fast timeline between target availability and hit identification. In addition, the use of exact mass simplifies the hit identification. We demonstrate this system using carbonic anhydrase as the target and a library of 144,000 proprietary compounds.