Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b00141
Abstract: Using structure- and ligand-based design principles, a novel series of piperidyl chromane arylsulfonamide Nav1.7 inhibitors was discovered. Early optimization focused on improvement of potency through refinement of the low energy ligand conformation and mitigation of… read more here.
Keywords: ligand based; nav1 inhibitors; arylsulfonamide nav1; structure ligand ... See more keywords
Discovery of Arylsulfonamide Nav1.7 Inhibitors: IVIVC, MPO Methods, and Optimization of Selectivity Profile.
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DOI: 10.1021/acsmedchemlett.1c00218
Abstract: The voltage-gated sodium channel Nav1.7 continues to be a high-profile target for the treatment of various pain afflictions due to its strong human genetic validation. While isoform selective molecules have been discovered and advanced into… read more here.
Keywords: selectivity profile; nav1 inhibitors; arylsulfonamide nav1; optimization ... See more keywords
Correlation of Optical and Automated Patch Clamp Electrophysiology for Identification of NaV1.7 Inhibitors
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DOI: 10.1177/2472555220914532
Abstract: The voltage-gated sodium channel Nav1.7 is a genetically validated target for pain; pharmacological blockers are promising as a new class of nonaddictive therapeutics. The search for Nav1.7 subtype selective inhibitors requires a reliable, scalable, and… read more here.
Keywords: spiking hek; hek assay; nav1 inhibitors; optopatch spiking ... See more keywords