10.1021/acs.jmedchem.8b01550.s001 Guanglin Luo Guanglin Luo Ling Chen Ling Chen Amy Easton Amy Easton Amy Newton Amy Newton Clotilde Bourin Clotilde Bourin Eric Shields Eric Shields Kathy Mosure Kathy Mosure Matthew G. Soars Matthew G. Soars Ronald J. Knox Ronald J. Knox Michele Matchett Michele Matchett Rick L. Pieschl Rick L. Pieschl Debra J. Post-Munson Debra J. Post-Munson Shuya Wang Shuya Wang James Herrington James Herrington John Graef John Graef Kimberly Newberry Kimberly Newberry Digavalli V. Sivarao Digavalli V. Sivarao Arun Senapati Arun Senapati Linda J. Bristow Linda J. Bristow Nicholas A. Meanwell Nicholas A. Meanwell Lorin A. Thompson Lorin A. Thompson Carolyn Dzierba Carolyn Dzierba Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective Na<sub>V</sub>1.7 Inhibitors for the Treatment of Pain American Chemical Society 2018 Pain 3- Aryl-indole CCI mouse formalin assay Na v 1.7 inhibitors IP Na V 1.7 potency Compound 29 Selective Na V 1.7 Inhibitors constriction injury CFA mouse dorsal root ganglion exposure 3- aryl-indazole derivatives neuropathic pain 2018-12-21 00:00:00 Dataset https://acs.figshare.com/articles/dataset/Discovery_of_Indole-_and_Indazole-acylsulfonamides_as_Potent_and_Selective_Na_sub_V_sub_1_7_Inhibitors_for_the_Treatment_of_Pain/7562126 3-Aryl-indole and 3-aryl-indazole derivatives were identified as potent and selective Na<sub>v</sub>1.7 inhibitors. Compound <b>29</b> was shown to be efficacious in the mouse formalin assay and also reduced complete Freund’s adjuvant (CFA)-induced thermal hyperalgesia and chronic constriction injury (CCI) induced cold allodynia and models of inflammatory and neuropathic pain, respectively, following intraperitoneal (IP) doses of 30 mg/kg. The observed efficacy could be correlated with the mouse dorsal root ganglion exposure and Na<sub>V</sub>1.7 potency associated with <b>29</b>.