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17 results

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Page 1
Discovery, optimization, and biological evaluation of 5-(2-(trifluoromethyl)phenyl)indazoles as a novel class of transient receptor potential A1 (TRPA1) antagonists.
Rooney L, Vidal A, D'Souza AM, Devereux N, Masick B, Boissel V, West R, Head V, Stringer R, Lao J, Petrus MJ, Patapoutian A, Nash M, Stoakley N, Panesar M, Verkuyl JM, Schumacher AM, Petrassi HM, Tully DC. Rooney L, et al. Among authors: head v. J Med Chem. 2014 Jun 26;57(12):5129-40. doi: 10.1021/jm401986p. Epub 2014 Jun 13. J Med Chem. 2014. PMID: 24884675
Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C.
Weiss A, Lorthiois E, Barys L, Beyer KS, Bomio-Confaglia C, Burks H, Chen X, Cui X, de Kanter R, Dharmarajan L, Fedele C, Gerspacher M, Guthy DA, Head V, Jaeger A, Núñez EJ, Kearns JD, Leblanc C, Maira SM, Murphy J, Oakman H, Ostermann N, Ottl J, Rigollier P, Roman D, Schnell C, Sedrani R, Shimizu T, Stringer R, Vaupel A, Voshol H, Wessels P, Widmer T, Wilcken R, Xu K, Zecri F, Farago AF, Cotesta S, Brachmann SM. Weiss A, et al. Among authors: head v. Cancer Discov. 2022 Jun 2;12(6):1500-1517. doi: 10.1158/2159-8290.CD-22-0158. Cancer Discov. 2022. PMID: 35404998 Free PMC article.
Development of autotaxin inhibitors: A series of tetrazole cinnamides.
Thomson CG, Le Grand D, Dowling M, Beattie D, Elphick L, Faller M, Freeman M, Hardaker E, Head V, Hemmig R, Hill J, Lister A, Pascoe D, Rieffel S, Shrestha B, Steward O, Zink F. Thomson CG, et al. Among authors: head v. Bioorg Med Chem Lett. 2021 Jan 1;31:127663. doi: 10.1016/j.bmcl.2020.127663. Epub 2020 Nov 4. Bioorg Med Chem Lett. 2021. PMID: 33160025
Development of autotaxin inhibitors: A series of zinc binding triazoles.
Thomson CG, Le Grand D, Dowling M, Brocklehurst CE, Chinn C, Elphick L, Faller M, Freeman M, Furminger V, Gasser C, Hamadi A, Hardaker E, Head V, Hill JC, Janus DI, Pearce D, Poulaud AS, Stanley E, Sviridenko L. Thomson CG, et al. Among authors: head v. Bioorg Med Chem Lett. 2018 Jul 15;28(13):2279-2284. doi: 10.1016/j.bmcl.2018.05.030. Epub 2018 May 21. Bioorg Med Chem Lett. 2018. PMID: 29798825
Discovery of a novel 2-aminopyrazine-3-carboxamide as a potent and selective inhibitor of Activin Receptor-Like Kinase-2 (ALK2) for the treatment of fibrodysplasia ossificans progressiva.
Ullrich T, Arista L, Weiler S, Teixeira-Fouchard S, Broennimann V, Stiefl N, Head V, Kramer I, Guth S. Ullrich T, et al. Among authors: head v. Bioorg Med Chem Lett. 2022 May 15;64:128667. doi: 10.1016/j.bmcl.2022.128667. Epub 2022 Mar 8. Bioorg Med Chem Lett. 2022. PMID: 35276359
17 results