Discovery of 5-HT₆ receptor ligands based on virtual HTS

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• 作者：Stefan Tasler ; Jü ; rgen Kraus ; Andreas Wuzik ; Oliver Mü ; ller ; Andrea Aschenbrenner ; Elena Cubero ; Rosalia Pascual ; Jordi-Ramon Quintana-Ruiz ; Alberto Dordal ; Ramon Mercè ; ; Xavier Codony
• 关键词：Serotonin receptor ; 5-HT₆ ; GPCR ; Molecular modeling ; vHTS
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2007
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 November 2007
• 卷：17
• 期：22
• 页码：6224-6229
• 文件大小：167 K

摘要

Based on a pharmacophore alignment on a 5-HT₆ ligand applying 4SCan^® technology, a new lead series was identified and further structurally investigated. K_is down to 8 nM were achieved.