Solution-Based Indirect Affinity Selection Mass Spectrometry-A General Tool For High-Throughput Screening Of Pharmaceutical Compound Libraries
Solution-Based Indirect Affinity Selection Mass Spectrometry-A General Tool For High-Throughput Screening Of Pharmaceutical Compound Libraries
复制标题
DOI：
10.1021/ac500938y
复制
发表时间：
2014-08-05
影响因子：
7.4
通讯作者：
Stroh, Justin G.
中科院分区：
文献类型：
--
作者：
O'Connell, Thomas N.;Ramsay, Jason;Stroh, Justin G.
我们在这里展示了一个自动化的基于溶液的亲和选择质谱（ASMS）系统可以完全由市售部件构建。该技术的价值在于吞吐量（类似于1 x 10(5)个化合物/天）以及低命中率。该系统是一种结合分析，需要很少的开发时间，在目标可用性和命中识别之间产生快速的时间线。此外，精确质量的使用简化了命中识别。我们以碳酸酐酶为靶标和144,000个专有化合物的文库来演示该系统。
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 (similar to 1 x 10(5) 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.