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Apparent Activity in High-throughput Screening: Origins of Compound-dependent Assay Interference by Natasha Thorne; Douglas S Auld; James Inglese is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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Expansive compound collections made up of structurally heterogeneous chemicals, the activities of which are largely undefined, present challenging problems for high-throughput screening (HTS). Foremost is differentiating whether the activity for a given compound in an assay is directed against the targeted biology, or is the result of surreptitious compound activity involving the assay detection system. Such compound interference can be especially difficult to identify if it is reproducible and concentration-dependentcharacteristics generally attributed to compounds with genuine activity. While reactive chemical groups on compounds were once thought to be the primary source of compound interference in assays used in HTS, recent work suggests that other factors, such as compound aggregation, may play a more significant role in many assay formats. Considerable progress has been made to profile representative compound libraries in an effort to identify chemical classes susceptible to producing compound interference, such as compounds commonly found to inhibit the reporter enzyme firefly luciferase. Such work has also led to the development of practices that have the potential to signi

Who reads Apparent Activity in High-throughput Screening: Origins of Compound-dependent Assay Interference?

Author

Natasha Thorne; Douglas S Auld; James Inglese

Publisher

Elsevier Science; Elsevier ; Elsevier BV (ISSN 1367-5931)

Published

2010

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)