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Crystallographic and electrophilic fragment screening of the SARS-CoV-2 main protease.
Douangamath A, Fearon D, Gehrtz P, Krojer T, Lukacik P, Owen CD, Resnick E, Strain-Damerell C, Aimon A, Ábrányi-Balogh P, Brandão-Neto J, Carbery A, Davison G, Dias A, Downes TD, Dunnett L, Fairhead M, Firth JD, Jones SP, Keeley A, Keserü GM, Klein HF, Martin MP, Noble MEM, O'Brien P, Powell A, Reddi RN, Skyner R, Snee M, Waring MJ, Wild C, London N, von Delft F, Walsh MA. Douangamath A, et al. Among authors: noble mem. Nat Commun. 2020 Oct 7;11(1):5047. doi: 10.1038/s41467-020-18709-w. Nat Commun. 2020. PMID: 33028810 Free PMC article.
Identification and Characterization of an Irreversible Inhibitor of CDK2.
Anscombe E, Meschini E, Mora-Vidal R, Martin MP, Staunton D, Geitmann M, Danielson UH, Stanley WA, Wang LZ, Reuillon T, Golding BT, Cano C, Newell DR, Noble ME, Wedge SR, Endicott JA, Griffin RJ. Anscombe E, et al. Chem Biol. 2015 Sep 17;22(9):1159-64. doi: 10.1016/j.chembiol.2015.07.018. Epub 2015 Aug 27. Chem Biol. 2015. PMID: 26320860 Free PMC article.
Identification of a novel ligand for the ATAD2 bromodomain with selectivity over BRD4 through a fragment growing approach.
Miller DC, Martin MP, Adhikari S, Brennan A, Endicott JA, Golding BT, Hardcastle IR, Heptinstall A, Hobson S, Jennings C, Molyneux L, Ng Y, Wedge SR, Noble MEM, Cano C. Miller DC, et al. Among authors: noble mem. Org Biomol Chem. 2018 Mar 14;16(11):1843-1850. doi: 10.1039/c8ob00099a. Org Biomol Chem. 2018. PMID: 29469144 Free PMC article.
FragLites-Minimal, Halogenated Fragments Displaying Pharmacophore Doublets. An Efficient Approach to Druggability Assessment and Hit Generation.
Wood DJ, Lopez-Fernandez JD, Knight LE, Al-Khawaldeh I, Gai C, Lin S, Martin MP, Miller DC, Cano C, Endicott JA, Hardcastle IR, Noble MEM, Waring MJ. Wood DJ, et al. Among authors: noble mem. J Med Chem. 2019 Apr 11;62(7):3741-3752. doi: 10.1021/acs.jmedchem.9b00304. Epub 2019 Mar 26. J Med Chem. 2019. PMID: 30860382
An Alkynylpyrimidine-Based Covalent Inhibitor That Targets a Unique Cysteine in NF-κB-Inducing Kinase.
Al-Khawaldeh I, Al Yasiri MJ, Aldred GG, Basmadjian C, Bordoni C, Harnor SJ, Heptinstall AB, Hobson SJ, Jennings CE, Khalifa S, Lebraud H, Martin MP, Miller DC, Shrives HJ, de Souza JV, Stewart HL, Temple M, Thomas HD, Totobenazara J, Tucker JA, Tudhope SJ, Wang LZ, Bronowska AK, Cano C, Endicott JA, Golding BT, Hardcastle IR, Hickson I, Wedge SR, Willmore E, Noble MEM, Waring MJ. Al-Khawaldeh I, et al. Among authors: noble mem. J Med Chem. 2021 Jul 22;64(14):10001-10018. doi: 10.1021/acs.jmedchem.0c01249. Epub 2021 Jul 2. J Med Chem. 2021. PMID: 34212719
Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain Inhibitor.
Miller DC, Reuillon T, Molyneux L, Blackburn T, Cook SJ, Edwards N, Endicott JA, Golding BT, Griffin RJ, Hardcastle I, Harnor SJ, Heptinstall A, Lochhead P, Martin MP, Martin NC, Myers S, Newell DR, Noble RA, Phillips N, Rigoreau L, Thomas H, Tucker JA, Wang LZ, Waring MJ, Wong AC, Wedge SR, Noble MEM, Cano C. Miller DC, et al. Among authors: noble ra, noble mem. J Med Chem. 2022 May 12;65(9):6513-6540. doi: 10.1021/acs.jmedchem.1c01756. Epub 2022 Apr 25. J Med Chem. 2022. PMID: 35468293 Free PMC article.
152 results