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Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
Sams AG, Hentzer M, Mikkelsen GK, Larsen K, Bundgaard C, Plath N, Christoffersen CT, Bang-Andersen B. Sams AG, et al. Among authors: mikkelsen gk. J Med Chem. 2010 Sep 9;53(17):6386-97. doi: 10.1021/jm100697g. J Med Chem. 2010. PMID: 20684563
Synthesis and SAR studies of analogues of 4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-N-thiazol-2-yl-benzamide (Lu AA41063) as adenosine A2A receptor ligands with improved aqueous solubility.
Mikkelsen GK, Langgård M, Schrøder TJ, Kreilgaard M, Jørgensen EB, Brandt G, Griffon Y, Boffey R, Bang-Andersen B. Mikkelsen GK, et al. Bioorg Med Chem Lett. 2015 Mar 15;25(6):1212-6. doi: 10.1016/j.bmcl.2015.01.062. Epub 2015 Feb 7. Bioorg Med Chem Lett. 2015. PMID: 25701253
The design and SAR of a novel series of 2-aminopyridine based LRRK2 inhibitors.
Smith GP, Badolo L, Chell V, Chen IJ, Christensen KV, David L, Daechsel JA, Hentzer M, Herzig MC, Mikkelsen GK, Watson SP, Williamson DS. Smith GP, et al. Bioorg Med Chem Lett. 2017 Sep 15;27(18):4500-4505. doi: 10.1016/j.bmcl.2017.07.072. Epub 2017 Aug 1. Bioorg Med Chem Lett. 2017. PMID: 28802631
Design and Synthesis of Pyrrolo[2,3-d]pyrimidine-Derived Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Checkpoint Kinase 1 (CHK1)-Derived Crystallographic Surrogate.
Williamson DS, Smith GP, Mikkelsen GK, Jensen T, Acheson-Dossang P, Badolo L, Bedford ST, Chell V, Chen IJ, Dokurno P, Hentzer M, Newland S, Ray SC, Shaw T, Surgenor AE, Terry L, Wang Y, Christensen KV. Williamson DS, et al. Among authors: mikkelsen gk. J Med Chem. 2021 Jul 22;64(14):10312-10332. doi: 10.1021/acs.jmedchem.1c00720. Epub 2021 Jun 29. J Med Chem. 2021. PMID: 34184879 Free article.
Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist.
Sams AG, Mikkelsen GK, Larsen M, Langgård M, Howells ME, Schrøder TJ, Brennum LT, Torup L, Jørgensen EB, Bundgaard C, Kreilgård M, Bang-Andersen B. Sams AG, et al. Among authors: mikkelsen gk. J Med Chem. 2011 Feb 10;54(3):751-64. doi: 10.1021/jm1008659. Epub 2011 Jan 6. J Med Chem. 2011. PMID: 21210664
57 results