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Page 1
Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.
Wu YJ, Davis CD, Dworetzky S, Fitzpatrick WC, Harden D, He H, Knox RJ, Newton AE, Philip T, Polson C, Sivarao DV, Sun LQ, Tertyshnikova S, Weaver D, Yeola S, Zoeckler M, Sinz MW. Wu YJ, et al. Among authors: davis cd. J Med Chem. 2003 Aug 28;46(18):3778-81. doi: 10.1021/jm034111v. J Med Chem. 2003. PMID: 12930139
Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain.
Wu YJ, Conway CM, Sun LQ, Machet F, Chen J, Chen P, He H, Bourin C, Calandra V, Polino JL, Davis CD, Heman K, Gribkoff VK, Boissard CG, Knox RJ, Thompson MW, Fitzpatrick W, Weaver D, Harden DG, Natale J, Dworetzky SI, Starrett JE Jr. Wu YJ, et al. Among authors: davis cd. Bioorg Med Chem Lett. 2013 Nov 15;23(22):6188-91. doi: 10.1016/j.bmcl.2013.08.092. Epub 2013 Sep 8. Bioorg Med Chem Lett. 2013. PMID: 24070783
Cytochrome P450 reaction-phenotyping: an industrial perspective.
Zhang H, Davis CD, Sinz MW, Rodrigues AD. Zhang H, et al. Among authors: davis cd. Expert Opin Drug Metab Toxicol. 2007 Oct;3(5):667-87. doi: 10.1517/17425255.3.5.667. Expert Opin Drug Metab Toxicol. 2007. PMID: 17916054 Review.
Discovery of Indazoles as Potent, Orally Active Dual Neurokinin 1 Receptor Antagonists and Serotonin Transporter Inhibitors for the Treatment of Depression.
Degnan AP, Tora GO, Huang H, Conlon DA, Davis CD, Hanumegowda UM, Hou X, Hsiao Y, Hu J, Krause R, Li YW, Newton AE, Pieschl RL, Raybon J, Rosner T, Sun JH, Taber MT, Taylor SJ, Wong MK, Zhang H, Lodge NJ, Bronson JJ, Macor JE, Gillman KW. Degnan AP, et al. Among authors: davis cd. ACS Chem Neurosci. 2016 Dec 21;7(12):1635-1640. doi: 10.1021/acschemneuro.6b00337. Epub 2016 Oct 18. ACS Chem Neurosci. 2016. PMID: 27744678
Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficient intranasal exposure.
Degnan AP, Chaturvedula PV, Conway CM, Cook DA, Davis CD, Denton R, Han X, Macci R, Mathias NR, Moench P, Pin SS, Ren SX, Schartman R, Signor LJ, Thalody G, Widmann KA, Xu C, Macor JE, Dubowchik GM. Degnan AP, et al. Among authors: davis cd. J Med Chem. 2008 Aug 28;51(16):4858-61. doi: 10.1021/jm800546t. Epub 2008 Jul 30. J Med Chem. 2008. PMID: 18665579
NK1 receptor antagonism lowers occupancy requirement for antidepressant-like effects of SSRIs in the gerbil forced swim test.
Lelas S, Li YW, Wallace-Boone TL, Taber MT, Newton AE, Pieschl RL, Davis CD, Molski TF, Newberry KS, Parker MF, Gillman KW, Bronson JJ, Macor JE, Lodge NJ. Lelas S, et al. Among authors: davis cd. Neuropharmacology. 2013 Oct;73:232-40. doi: 10.1016/j.neuropharm.2013.05.038. Epub 2013 Jun 12. Neuropharmacology. 2013. PMID: 23770339
The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 1.
Han X, Civiello RL, Conway CM, Cook DA, Davis CD, Macci R, Pin SS, Ren SX, Schartman R, Signor LJ, Thalody G, Widmann KA, Xu C, Chaturvedula PV, Macor JE, Dubowchik GM. Han X, et al. Among authors: davis cd. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4723-7. doi: 10.1016/j.bmcl.2012.05.074. Epub 2012 Jun 1. Bioorg Med Chem Lett. 2012. PMID: 22727645
340 results