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Design of an automated enhanced-throughput platform for functional characterization of positive allosteric modulator-induced leftward shifts in apparent agonist potency in vitro.
Hendricson A, Matchett M, Ferrante M, Ferrante C, Hunnicutt E, Westphal R, Kostich W, Huang Y, Masias N, Hong D, Bertekap R, Burford N, Watson J, Alt A, Myslik J, Zhang L, Knox R. Hendricson A, et al. Among authors: knox r. J Lab Autom. 2012 Apr;17(2):104-15. doi: 10.1177/2211068211435301. Epub 2012 Feb 1. J Lab Autom. 2012. PMID: 22357567
Discovery of D1 Dopamine Receptor Positive Allosteric Modulators: Characterization of Pharmacology and Identification of Residues that Regulate Species Selectivity.
Lewis MA, Hunihan L, Watson J, Gentles RG, Hu S, Huang Y, Bronson J, Macor JE, Beno BR, Ferrante M, Hendricson A, Knox RJ, Molski TF, Kong Y, Cvijic ME, Rockwell KL, Weed MR, Cacace AM, Westphal RS, Alt A, Brown JM. Lewis MA, et al. Among authors: knox rj. J Pharmacol Exp Ther. 2015 Sep;354(3):340-9. doi: 10.1124/jpet.115.224071. Epub 2015 Jun 24. J Pharmacol Exp Ther. 2015. PMID: 26109678
Development of a high-throughput calcium flux assay for identification of all ligand types including positive, negative, and silent allosteric modulators for G protein-coupled receptors.
Noblin DJ, Bertekap RL Jr, Burford NT, Hendricson A, Zhang L, Knox R, Banks M, O'Connell J, Alt A. Noblin DJ, et al. Among authors: knox r. Assay Drug Dev Technol. 2012 Oct;10(5):457-67. doi: 10.1089/adt.2011.443. Epub 2012 Jun 29. Assay Drug Dev Technol. 2012. PMID: 22746835
Discovery of a novel series of quinolone α7 nicotinic acetylcholine receptor agonists.
McDonald IM, Mate RA, Zusi FC, Huang H, Post-Munson DJ, Ferrante MA, Gallagher L, Bertekap RL Jr, Knox RJ, Robertson BJ, Harden DG, Morgan DG, Lodge NJ, Dworetzky SI, Olson RE, Macor JE. McDonald IM, et al. Bioorg Med Chem Lett. 2013 Mar 15;23(6):1684-8. doi: 10.1016/j.bmcl.2013.01.070. Epub 2013 Jan 29. Bioorg Med Chem Lett. 2013. PMID: 23414838
Design and Synthesis of a New Series of 4-Heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes as α7 Nicotinic Receptor Agonists. 1. Development of Pharmacophore and Early Structure-Activity Relationship.
Cook J, Zusi FC, McDonald IM, King D, Hill MD, Iwuagwu C, Mate RA, Fang H, Zhao R, Wang B, Cutrone J, Ma B, Gao Q, Knox RJ, Matchett M, Gallagher L, Ferrante M, Post-Munson D, Molski T, Easton A, Miller R, Jones K, Digavalli S, Healy F, Lentz K, Benitex Y, Clarke W, Natale J, Siuciak JA, Lodge N, Zaczek R, Denton R, Morgan D, Bristow LJ, Macor JE, Olson RE. Cook J, et al. Among authors: knox rj. J Med Chem. 2016 Dec 22;59(24):11171-11181. doi: 10.1021/acs.jmedchem.6b01506. Epub 2016 Dec 13. J Med Chem. 2016. PMID: 27958732
Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain.
Luo G, Chen L, Easton A, Newton A, Bourin C, Shields E, Mosure K, Soars MG, Knox RJ, Matchett M, Pieschl RL, Post-Munson DJ, Wang S, Herrington J, Graef J, Newberry K, Sivarao DV, Senapati A, Bristow LJ, Meanwell NA, Thompson LA, Dzierba C. Luo G, et al. J Med Chem. 2019 Jan 24;62(2):831-856. doi: 10.1021/acs.jmedchem.8b01550. Epub 2019 Jan 8. J Med Chem. 2019. PMID: 30576602
Discovery of morpholine-based aryl sulfonamides as Nav1.7 inhibitors.
Wu YJ, Guernon J, McClure A, Venables B, Rajamani R, Robbins KJ, Knox RJ, Matchett M, Pieschl RL, Herrington J, Bristow LJ, Meanwell NA, Olson R, Thompson LA, Dzierba C. Wu YJ, et al. Among authors: knox rj. Bioorg Med Chem Lett. 2018 Mar 1;28(5):958-962. doi: 10.1016/j.bmcl.2018.01.035. Epub 2018 Feb 1. Bioorg Med Chem Lett. 2018. PMID: 29439904
Discovery of new indole-based acylsulfonamide Nav1.7 inhibitors.
Wu YJ, Venables B, Guernon J, Chen J, Sit SY, Rajamani R, Knox RJ, Matchett M, Pieschl RL, Herrington J, Bristow LJ, Meanwell NA, Thompson LA, Dzierba C. Wu YJ, et al. Among authors: knox rj. Bioorg Med Chem Lett. 2019 Feb 15;29(4):659-663. doi: 10.1016/j.bmcl.2018.12.013. Epub 2018 Dec 6. Bioorg Med Chem Lett. 2019. PMID: 30638874
663 results