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- W2783152909 abstract "Significance Subtype-selective modulation of ion channels is often important, but extremely difficult to achieve for drug development. Using Nav1.7 as an example, we show that this challenge could be attributed to poor design in ion channel assays, which fail to detect most potent and selective compounds and are biased toward nonselective mechanisms. By exploiting different drug binding sites and modes of channel gating, we successfully direct a membrane potential assay toward non–pore-blocking mechanisms and identify Nav1.7-selective compounds. Our mechanistic approach to assay design addresses a significant hurdle in Nav1.7 drug discovery and is applicable to many other ion channels." @default.
- W2783152909 created "2018-01-26" @default.
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- W2783152909 date "2018-01-08" @default.
- W2783152909 modified "2023-10-12" @default.
- W2783152909 title "Mechanism-specific assay design facilitates the discovery of Nav1.7-selective inhibitors" @default.
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- W2783152909 doi "https://doi.org/10.1073/pnas.1713701115" @default.
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