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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. Among authors: phillips t. 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. Among authors: phillips t. 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 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. Among authors: phillips t. 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
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. Among authors: phillips t. 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 potent CRTh2 (DP2) receptor antagonists.
Birkinshaw TN, Teague SJ, Beech C, Bonnert RV, Hill S, Patel A, Reakes S, Sanganee H, Dougall IG, Phillips TT, Salter S, Schmidt J, Arrowsmith EC, Carrillo JJ, Bell FM, Paine SW, Weaver R. Birkinshaw TN, et al. Among authors: phillips tt. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4287-90. doi: 10.1016/j.bmcl.2006.05.062. Epub 2006 Jun 5. Bioorg Med Chem Lett. 2006. PMID: 16753296
2,798 results