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Integrity profiling of high throughput screening hits using LC-MS and related techniques
Authors:Kerns Edward H  Di Li  Bourassa Jim  Gross Jonathan  Huang Nelson  Liu Hanlan  Kleintop Teresa  Nogle Lisa  Mallis Larry  Petucci Chris  Petusky Susan  Tischler Mark  Sabus Chantel  Sarkahian Ani  Young Mairead  Zhang Mei-Yi  Huryn Donna  McConnell Oliver  Carter Guy
Affiliation:Chemical and Screening Sciences, Wyeth Research Princeton, NJ 08543-8000, USA. kernse@wyeth.com
Abstract:Integrity profiling of HTS hits is valuable for verification of the hit identity and purity. This provides early discovery researchers with more confident SAR theories. Methodology for integrity profiling of HTS hits must be high throughput, consume little material, and selectively provide structure-based data. Analytical techniques that can be utilized for integrity profiling methods are reviewed for their appropriateness in sample preparation, component separation, detection, purity quantitation, identity confirmation, and follow-up.
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