High-throughput screening by mass spectrometry: comparison with the scintillation proximity assay with a focused-file screen of AKT1/PKB alpha |
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Authors: | Quercia Andrea K LaMarr William A Myung Jayhyuk Ozbal Can C Landro James A Lumb Kevin J |
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Institution: | Department of Research Technologies, Bayer Pharmaceuticals Corporation, West Haven, Connecticut 06516, USA. |
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Abstract: | Mass spectrometry is an emerging format for label-free high-throughput screening. The main limitation of mass spectrometry is throughput, due to the requirement to purify samples prior to ionization. Here the authors compare an automated high-throughput mass spectrometry (HTMS) system (RapidFire) with the scintillation proximity assay (SPA). The cancer therapy target AKT1/PKBalpha was screened against a focused library of kinase inhibitors and IC50 values determined for all compounds that exhibit > 50% inhibition. A selection of additional compounds that exhibited
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