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High-throughput screening for Hsp90 ATPase inhibitors.

Basic Information

ID: ALA1148663

Journal: Bioorg Med Chem Lett

Title: High-throughput screening for Hsp90 ATPase inhibitors.

Authors: Avila C, Hadden MK, Ma Z, Kornilayev BA, Ye QZ, Blagg BS.

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.

CiteXplore: 16530412

DOI: 10.1016/j.bmcl.2006.02.063

Patent ID: