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Identification of the Clinical Candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): A Selective Glucocorticoid Receptor (GR) Antagonist.
Hunt HJ, Belanoff JK, Walters I, Gourdet B, Thomas J, Barton N, Unitt J, Phillips T, Swift D, Eaton E. Hunt HJ, et al. J Med Chem. 2017 Apr 27;60(8):3405-3421. doi: 10.1021/acs.jmedchem.7b00162. Epub 2017 Apr 17. J Med Chem. 2017. PMID: 28368581
FKBP5 mRNA Expression Is a Biomarker for GR Antagonism.
Bali U, Phillips T, Hunt H, Unitt J. Bali U, et al. J Clin Endocrinol Metab. 2016 Nov;101(11):4305-4312. doi: 10.1210/jc.2016-1624. Epub 2016 Jul 26. J Clin Endocrinol Metab. 2016. PMID: 27459525 Clinical Trial.
Discovery of AZD-2098 and AZD-1678, Two Potent and Bioavailable CCR4 Receptor Antagonists.
Kindon N, Andrews G, Baxter A, Cheshire D, Hemsley P, Johnson T, Liu YZ, McGinnity D, McHale M, Mete A, Reuberson J, Roberts B, Steele J, Teobald B, Unitt J, Vaughan D, Walters I, Stocks MJ. Kindon N, et al. ACS Med Chem Lett. 2017 Sep 1;8(9):981-986. doi: 10.1021/acsmedchemlett.7b00315. eCollection 2017 Sep 14. ACS Med Chem Lett. 2017. PMID: 28947948 Free PMC article.
Discovery of small molecule human C5a receptor antagonists.
Sanganee HJ, Baxter A, Barber S, Brown AJ, Grice D, Hunt F, King S, Laughton D, Pairaudeau G, Thong B, Weaver R, Unitt J. Sanganee HJ, et al. Bioorg Med Chem Lett. 2009 Feb 15;19(4):1143-7. doi: 10.1016/j.bmcl.2008.12.104. Epub 2008 Dec 31. Bioorg Med Chem Lett. 2009. PMID: 19171482
Discovery of pyrazoles as novel FPR1 antagonists.
Morley AD, Cook A, King S, Roberts B, Lever S, Weaver R, Macdonald C, Unitt J, Fagura M, Phillips T, Lewis R, Wenlock M. Morley AD, et al. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6456-60. doi: 10.1016/j.bmcl.2011.08.085. Epub 2011 Sep 6. Bioorg Med Chem Lett. 2011. PMID: 21955939
Discovery of small molecule human FPR1 receptor antagonists.
Unitt J, Fagura M, Phillips T, King S, Perry M, Morley A, MacDonald C, Weaver R, Christie J, Barber S, Mohammed R, Paul M, Cook A, Baxter A. Unitt J, et al. Bioorg Med Chem Lett. 2011 May 15;21(10):2991-7. doi: 10.1016/j.bmcl.2011.03.049. Epub 2011 Mar 21. Bioorg Med Chem Lett. 2011. PMID: 21486695
33 results