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Page 1
Discovery of a Series of Orally Bioavailable Androgen Receptor Degraders for the Treatment of Prostate Cancer.
Bagal SK, Astles PC, Diène C, Argyrou A, Crafter C, Cassar DJ, Fallan C, Hock A, Jones T, Moreau K, Lamont GM, Lamont S, Michaloglou C, Packer MJ, Pike A, Ramos-Montoya A, Scott JS, Shaw J, Shologu Z. Bagal SK, et al. Among authors: packer mj. J Med Chem. 2024 Jul 25;67(14):11732-11750. doi: 10.1021/acs.jmedchem.4c00269. Epub 2024 Jul 11. J Med Chem. 2024. PMID: 38991141
Discovery and characterisation of quinazolines and 8-Azaquinazolines as NLRP3 agonists with oral bioavailability in mice.
O' Donovan DH, Baker D, Ciotta G, Degorce SL, Demanze S, Dockerill M, Escudero-Ibarz L, Ireland L, Mao Y, Packer MJ, Robinson J, Scarfe G, Tang H, Valge-Archer V. O' Donovan DH, et al. Among authors: packer mj. Bioorg Med Chem Lett. 2023 Nov 15;96:129518. doi: 10.1016/j.bmcl.2023.129518. Epub 2023 Oct 12. Bioorg Med Chem Lett. 2023. PMID: 37838344
Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations.
Thomson C, Barton P, Braybrooke E, Colclough N, Dong Z, Evans L, Floc'h N, Guérot C, Hargreaves D, Khurana P, Li S, Li X, Lister A, McCoull W, McWilliams L, Orme JP, Packer MJ, Swaih AM, Ward RA, Winlow P, Ye Y. Thomson C, et al. Among authors: packer mj. J Med Chem. 2024 Jun 13;67(11):8988-9027. doi: 10.1021/acs.jmedchem.4c00227. Epub 2024 May 21. J Med Chem. 2024. PMID: 38770784
Optimization of Potent, Efficacious, Selective and Blood-Brain Barrier Penetrating Inhibitors Targeting EGFR Exon20 Insertion Mutations.
Thomson C, Braybrooke E, Colclough N, Davies NL, Floc'h N, Greenwood R, Guérot C, Hargreaves D, Johnstrom P, Khurana P, Kostomiris DH, Li S, Lister A, Lorthioir O, Martin S, McCoull W, McLean NJ, McWilliams L, Orme JP, Packer MJ, Pearson S, Swaih AM, Tentarelli S, Tucker MJ, Ward RA, Wilkinson S, Winlow P, Wood IL. Thomson C, et al. Among authors: packer mj. J Med Chem. 2024 Sep 28. doi: 10.1021/acs.jmedchem.4c01792. Online ahead of print. J Med Chem. 2024. PMID: 39340451
Fragment-Based Discovery of Novel MUS81 Inhibitors.
Collie GW, Börjesson U, Chen Y, Dong Z, Di Fruscia P, Gohlke A, Hoyle A, Hunt TA, Jesani MH, Luo H, Luptak J, Milbradt AG, Narasimhan P, Packer M, Patel S, Qiao J, Storer RI, Stubbs CJ, Tart J, Truman C, Wang AT, Wheeler MG, Winter-Holt J. Collie GW, et al. ACS Med Chem Lett. 2024 Jun 7;15(7):1151-1158. doi: 10.1021/acsmedchemlett.3c00453. eCollection 2024 Jul 11. ACS Med Chem Lett. 2024. PMID: 39015284 Free PMC article.
Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor.
Johannes JW, Balazs AYS, Barratt D, Bista M, Chuba MD, Cosulich S, Critchlow SE, Degorce SL, Di Fruscia P, Edmondson SD, Embrey KJ, Fawell S, Ghosh A, Gill SJ, Gunnarsson A, Hande SM, Heightman TD, Hemsley P, Illuzzi G, Lane J, Larner CJB, Leo E, Liu L, Madin A, McWilliams L, O'Connor MJ, Orme JP, Pachl F, Packer MJ, Pei X, Pike A, Schimpl M, She H, Staniszewska AD, Talbot V, Underwood E, Varnes JG, Xue L, Yao T, Zhang K, Zhang AX, Zheng X. Johannes JW, et al. Among authors: packer mj. J Med Chem. 2024 Dec 10. doi: 10.1021/acs.jmedchem.4c01725. Online ahead of print. J Med Chem. 2024. PMID: 39655996
62 results