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Nat Rev Drug Discov. 2003 Apr;2(4):259-66.

Designing screens: how to make your hits a hit.

Author information

1
Vertex Pharmaceuticals, 130 Waverley Street, Cambridge, Massachusetts 02139, USA.

Abstract

The basic goal of small-molecule screening is the identification of chemically 'interesting' starting points for elaboration towards a drug. A number of innovative approaches for pursuing this goal have evolved, and the right approach is dictated by the target class being pursued and the capabilities of the organization involved. A recent trend in high-throughput screening has been to place less emphasis on the number of data points that can be produced, and to focus instead on the quality of the data obtained. Several computational and technological advances have aided in the selection of compounds for screening and widened the variety of assay formats available for screening. The effect on the efficiency of the screening process is discussed.

PMID:
12669025
DOI:
10.1038/nrd1063
[Indexed for MEDLINE]

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