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Page 1
Identification of type-II inhibitors using kinase structures.
Lovering F, McDonald J, Whitlock GA, Glossop PA, Phillips C, Bent A, Sabnis Y, Ryan M, Fitz L, Lee J, Chang JS, Han S, Kurumbail R, Thorarensen A. Lovering F, et al. Among authors: thorarensen a. Chem Biol Drug Des. 2012 Nov;80(5):657-64. doi: 10.1111/j.1747-0285.2012.01443.x. Epub 2012 Sep 3. Chem Biol Drug Des. 2012. PMID: 22759374
The 2010 patent landscape for spleen tyrosine kinase inhibitors.
Moretto AF, Dehnhardt C, Kaila N, Papaioannou N, Thorarensen A. Moretto AF, et al. Among authors: thorarensen a. Recent Pat Inflamm Allergy Drug Discov. 2012 May;6(2):97-120. doi: 10.2174/187221312800166895. Recent Pat Inflamm Allergy Drug Discov. 2012. PMID: 22292554 Review.
Structure based design of novel irreversible FAAH inhibitors.
Wang JL, Bowen SJ, Schweitzer BA, Madsen HM, McDonald J, Pelc MJ, Tenbrink RE, Beidler D, Thorarensen A. Wang JL, et al. Among authors: thorarensen a. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5970-4. doi: 10.1016/j.bmcl.2009.07.101. Epub 2009 Jul 25. Bioorg Med Chem Lett. 2009. PMID: 19765986
Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 1: identification of 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4.5]decane as lead scaffolds.
Meyers MJ, Long SA, Pelc MJ, Wang JL, Bowen SJ, Walker MC, Schweitzer BA, Madsen HM, Tenbrink RE, McDonald J, Smith SE, Foltin S, Beidler D, Thorarensen A. Meyers MJ, et al. Among authors: thorarensen a. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6538-44. doi: 10.1016/j.bmcl.2011.08.055. Epub 2011 Aug 22. Bioorg Med Chem Lett. 2011. PMID: 21924614
Microfluidic-Enabled Intracellular Delivery of Membrane Impermeable Inhibitors to Study Target Engagement in Human Primary Cells.
Li J, Wang B, Juba BM, Vazquez M, Kortum SW, Pierce BS, Pacheco M, Roberts L, Strohbach JW, Jones LH, Hett E, Thorarensen A, Telliez JB, Sharei A, Bunnage M, Gilbert JB. Li J, et al. Among authors: thorarensen a. ACS Chem Biol. 2017 Dec 15;12(12):2970-2974. doi: 10.1021/acschembio.7b00683. Epub 2017 Nov 13. ACS Chem Biol. 2017. PMID: 29088528
Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.
Casimiro-Garcia A, Trujillo JI, Vajdos F, Juba B, Banker ME, Aulabaugh A, Balbo P, Bauman J, Chrencik J, Coe JW, Czerwinski R, Dowty M, Knafels JD, Kwon S, Leung L, Liang S, Robinson RP, Telliez JB, Unwalla R, Yang X, Thorarensen A. Casimiro-Garcia A, et al. Among authors: thorarensen a. J Med Chem. 2018 Dec 13;61(23):10665-10699. doi: 10.1021/acs.jmedchem.8b01308. Epub 2018 Nov 30. J Med Chem. 2018. PMID: 30423248
The advantages of describing covalent inhibitor in vitro potencies by IC50 at a fixed time point. IC50 determination of covalent inhibitors provides meaningful data to medicinal chemistry for SAR optimization.
Thorarensen A, Balbo P, Banker ME, Czerwinski RM, Kuhn M, Maurer TS, Telliez JB, Vincent F, Wittwer AJ. Thorarensen A, et al. Bioorg Med Chem. 2021 Jan 1;29:115865. doi: 10.1016/j.bmc.2020.115865. Epub 2020 Nov 18. Bioorg Med Chem. 2021. PMID: 33285410
43 results