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Synthesis and pharmacological characterization of C4-disubstituted analogs of 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylate: identification of a potent, selective metabotropic glutamate receptor agonist and determination of agonist-bound human mGlu2 and mGlu3 amino terminal domain structures.
Monn JA, Prieto L, Taboada L, Pedregal C, Hao J, Reinhard MR, Henry SS, Goldsmith PJ, Beadle CD, Walton L, Man T, Rudyk H, Clark B, Tupper D, Baker SR, Lamas C, Montero C, Marcos A, Blanco J, Bures M, Clawson DK, Atwell S, Lu F, Wang J, Russell M, Heinz BA, Wang X, Carter JH, Xiang C, Catlow JT, Swanson S, Sanger H, Broad LM, Johnson MP, Knopp KL, Simmons RM, Johnson BG, Shaw DB, McKinzie DL. Monn JA, et al. Among authors: beadle cd. J Med Chem. 2015 Feb 26;58(4):1776-94. doi: 10.1021/jm501612y. Epub 2015 Feb 5. J Med Chem. 2015. PMID: 25602126
Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective mGlu2 Receptor Agonist.
Monn JA, Prieto L, Taboada L, Hao J, Reinhard MR, Henry SS, Beadle CD, Walton L, Man T, Rudyk H, Clark B, Tupper D, Baker SR, Lamas C, Montero C, Marcos A, Blanco J, Bures M, Clawson DK, Atwell S, Lu F, Wang J, Russell M, Heinz BA, Wang X, Carter JH, Getman BG, Catlow JT, Swanson S, Johnson BG, Shaw DB, McKinzie DL. Monn JA, et al. Among authors: beadle cd. J Med Chem. 2015 Sep 24;58(18):7526-48. doi: 10.1021/acs.jmedchem.5b01124. J Med Chem. 2015. PMID: 26313429
Synthesis and Pharmacological Characterization of 2-(2,6-Dichlorophenyl)-1-((1S,3R)-5-(3-hydroxy-3-methylbutyl)-3-(hydroxymethyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl)ethan-1-one (LY3154207), a Potent, Subtype Selective, and Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor.
Hao J, Beck JP, Schaus JM, Krushinski JH, Chen Q, Beadle CD, Vidal P, Reinhard MR, Dressman BA, Massey SM, Boulet SL, Cohen MP, Watson BM, Tupper D, Gardinier KM, Myers J, Johansson AM, Richardson J, Richards DS, Hembre EJ, Remick DM, Coates DA, Bhardwaj RM, Diseroad BA, Bender D, Stephenson G, Wolfangel CD, Diaz N, Getman BG, Wang XS, Heinz BA, Cramer JW, Zhou X, Maren DL, Falcone JF, Wright RA, Mitchell SN, Carter G, Yang CR, Bruns RF, Svensson KA. Hao J, et al. Among authors: beadle cd. J Med Chem. 2019 Oct 10;62(19):8711-8732. doi: 10.1021/acs.jmedchem.9b01234. Epub 2019 Sep 30. J Med Chem. 2019. PMID: 31532644
Acetylcholinesterase Inhibition of Diversely Functionalized Quinolinones for Alzheimer's Disease Therapy.
Bautista-Aguilera ÓM, Ismaili L, Chioua M, Andrys R, Schmidt M, Bzonek P, Martínez-Grau MÁ, Beadle CD, Vetman T, López-Muñoz F, Iriepa I, Refouvelet B, Musilek K, Marco-Contelles J. Bautista-Aguilera ÓM, et al. Among authors: beadle cd. Int J Mol Sci. 2020 May 30;21(11):3913. doi: 10.3390/ijms21113913. Int J Mol Sci. 2020. PMID: 32486316 Free PMC article.
The Chemotype of Chromanones as a Privileged Scaffold for Multineurotarget Anti-Alzheimer Agents.
Keuler T, Lemke C, Elsinghorst PW, Iriepa I, Chioua M, Martínez-Grau MA, Beadle CD, Vetman T, López-Muñoz F, Wille T, Bartz U, Deuther-Conrad W, Marco-Contelles J, Gütschow M. Keuler T, et al. Among authors: beadle cd. ACS Pharmacol Transl Sci. 2022 Oct 12;5(11):1097-1108. doi: 10.1021/acsptsci.2c00097. eCollection 2022 Nov 11. ACS Pharmacol Transl Sci. 2022. PMID: 36407962 Free PMC article.
Chromenones as Multineurotargeting Inhibitors of Human Enzymes.
Lemke C, Christmann J, Yin J, Alonso JM, Serrano E, Chioua M, Ismaili L, Martínez-Grau MA, Beadle CD, Vetman T, Dato FM, Bartz U, Elsinghorst PW, Pietsch M, Müller CE, Iriepa I, Wille T, Marco-Contelles J, Gütschow M. Lemke C, et al. Among authors: beadle cd. ACS Omega. 2019 Dec 11;4(26):22161-22168. doi: 10.1021/acsomega.9b03409. eCollection 2019 Dec 24. ACS Omega. 2019. PMID: 31891098 Free PMC article.