Title of article
High-throughput screening for Hsp90 ATPase inhibitors
Author/Authors
Christopher Avila، نويسنده , , M. Kyle Hadden، نويسنده , , Zeqiang Ma، نويسنده , , Boris A. Kornilayev، نويسنده , , Qizhuang Ye، نويسنده , , Brian S.J. Blagg، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
4
From page
3005
To page
3008
Abstract
Recently, we reported a useful assay for the determination of yeast Hsp90 ATPase activity. Using this assay, high-throughput screening of 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 μM. The structures of several of these inhibitory scaffolds are reported along with their IC50 values.
Keywords
High-throughput screening , HSP90 , inhibitors
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796916
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