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Bioorg Med Chem Lett. 2006 Jun 1;16(11):3005-8. Epub 2006 Mar 10.

High-throughput screening for Hsp90 ATPase inhibitors.

Author information

1
Department of Medicinal Chemistry, The University of Kansas, 1251 Wescoe Hall Drive, Malott 4070, Lawrence, KS 66045-7563, USA.

Abstract

Recently, we reported a useful assay for the determination of yeast Hsp90 ATPase activity. Using this assay, high-throughput screening of approximately 10,000 compounds was performed to determine the feasibility of this assay on large scale. Results from high-throughput screening indicated that the assay was reproducible (av Z-factor = 0.80) and identified 0.57% of the compounds as Hsp90 inhibitors that exhibited IC50s less than 20 microM. The structures of several of these inhibitory scaffolds are reported along with their IC50 values.

PMID:
16530412
DOI:
10.1016/j.bmcl.2006.02.063
[Indexed for MEDLINE]

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