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Drug Discov Today. 2004 Jul 15;9(14):595-602.

Reliable high-throughput functional screening with 3-FABS.

Author information

1
Chemistry Department, Nerviano Medical Science, Viale Pasteur 10, 20014 Nerviano (MI), Italy. claudio.dalvit@nervianoms.com

Abstract

An NMR method called 3-FABS has extended the capabilities of NMR, enabling rapid, efficient and reliable high-throughput functional screening for the identification of inhibitors and for measuring their 50% mean inhibition concentration (IC(50)) with accuracy. The substrate is tagged with a CF(3) moiety and (19)F NMR spectroscopy is used for the detection of the substrate and product components. We provide comprehensive insight into 3-FABS, a discussion of its strength and weakness when compared with other HTS techniques and a presentation of some of its applications to the screening of different enzymes and to multiple screening.

PMID:
15239978
DOI:
10.1016/S1359-6446(04)03161-7
[Indexed for MEDLINE]

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