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• W2016121750 startingPage "8603" @default.
• W2016121750 abstract "The 5-HT₃ receptor, a pentameric ligand-gated ion channel (pLGIC), is an important therapeutic target. During a recent fragment screen, 6-chloro-N-methyl-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine (1) was identified as a 5-HT₃ hit fragment. Here we describe the synthesis and structure-activity relationships (SAR) of a series of (iso)quinoline and quinazoline compounds that were synthesized and screened for 5-HT₃ R affinity using a [³H]granisetron displacement assay. These studies resulted in the discovery of several high affinity ligands of which compound 22 showed the highest affinity (pK(i) > 10) for the 5-HT₃ receptor. The observed SAR is in agreement with established pharmacophore models for 5-HT₃ ligands and is used for ligand-receptor binding mode prediction using homology modeling and in silico docking approaches." @default.
• W2016121750 created "2016-06-24" @default.
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• W2016121750 date "2012-10-12" @default.
• W2016121750 modified "2023-09-29" @default.
• W2016121750 title "Design, Synthesis, and Structure–Activity Relationships of Highly Potent 5-HT₃ Receptor Ligands" @default.
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• W2016121750 doi "https://doi.org/10.1021/jm300801u" @default.
• W2016121750 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3504484" @default.
• W2016121750 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/23006041" @default.
• W2016121750 hasPublicationYear "2012" @default.
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