Rapid acquisition of 1H and 19F NMR experiments for direct and competition ligand-based screening

✍ Scribed by Claudio Dalvit; Alvar D. Gossert; Jérôme Coutant; Martial Piotto

• Publisher: John Wiley and Sons
• Year: 2011
• Tongue: English
• Weight: 158 KB
• Volume: 49
• Category: Article
• ISSN: 0749-1581
• DOI: 10.1002/mrc.2733

✦ Synopsis

Abstract

Direct and competition ligand‐based NMR experiments are often used in the screening of chemical fragment libraries against a protein target due to the high relative sensitivity of NMR for protein‐binding events. A plethora of NMR methods has been proposed for this purpose. Two of these techniques are the ^19^F T~2~ filter and the ^1^H selective T~2~ filter experiments. Modifications of the pulse sequences of these experiments have resulted in a ∼2‐fold reduction in the experiment time thus allowing an increase in the screening throughput and making NMR an attractive technique for screening large compound collections. Copyright © 2011 John Wiley & Sons, Ltd.