High-throughput screening for Hsp90 ATPase inhibitors

Bioorganic & Medicinal Chemistry Letters
Christopher AvilaBrian S J Blagg

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.

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Citations

Jun 3, 2006·Journal of Molecular Medicine : Official Organ of the Gesellschaft Deutscher Naturforscher Und Ärzte·Masahiro WazaGen Sobue
Jul 16, 2011·Journal of Chemical Information and Modeling·Xiao Yan HuangXiao Yun Zhang
Apr 14, 2012·Journal of Pharmaceutical and Biomedical Analysis·Manuela BartoliniVincenza Andrisano
Dec 31, 2010·Journal of Enzyme Inhibition and Medicinal Chemistry·Ghassan Abu SheikhaMutasem O Taha
Aug 30, 2016·Journal of Enzyme Inhibition and Medicinal Chemistry·Mahmoud A Al-Sha'erAlaa Abudayyh
Sep 24, 2016·Journal of Experimental & Clinical Cancer Research : CR·Zhirui ZhangHao Liu
Oct 19, 2007·Journal of Biomolecular Screening·Yuhong DuGabriela Chiosis
Nov 28, 2020·Pharmacology & Therapeutics·Monimoy BanerjeeBrian S J Blagg
Sep 14, 2010·Journal of Chemical Information and Modeling·Mahmoud A Al-Sha'er, Mutasem O Taha
Nov 30, 2006·Journal of the American Chemical Society·Joseph A BurlisonBrian S J Blagg

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