High Throughput Screening of Small Molecule Inhibitory Action on Proteins Using LC-MS

摘要

We demonstrate a feasible method to screen large inhibitory libraries. Strong binders are present in the control experiment and absent in the binding experiment. Thus far, the method has identified zero false positive hits: All library compounds that were observed in the control experiment were also observed in the binding experiment except the known inhibitors. The screen minimizes protein consumption. About 50 nmol of protein is required to screen a 10K compound library for inhibitors with a Ki of 50 pM.