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Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs.
Johannes JW, Balazs A, Barratt D, Bista M, Chuba MD, Cosulich S, Critchlow SE, Degorce SL, Di Fruscia P, Edmondson SD, Embrey K, Fawell S, Ghosh A, Gill SJ, Gunnarsson A, Hande SM, Heightman TD, Hemsley P, Illuzzi G, Lane J, Larner C, Leo E, Liu L, Madin A, Martin S, 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: madin a. J Med Chem. 2021 Oct 14;64(19):14498-14512. doi: 10.1021/acs.jmedchem.1c01012. Epub 2021 Sep 27. J Med Chem. 2021. PMID: 34570508
Discovery of a selective c-MET inhibitor with a novel binding mode.
Collie GW, Barlind L, Bazzaz S, Börjesson U, Dale IL, Disch JS, Habeshian S, Jetson R, Khurana P, Madin A, Michaelides IN, Peng L, Snijder A, Stubbs CJ. Collie GW, et al. Among authors: madin a. Bioorg Med Chem Lett. 2022 Nov 1;75:128948. doi: 10.1016/j.bmcl.2022.128948. Epub 2022 Aug 17. Bioorg Med Chem Lett. 2022. PMID: 35987508 Free article.
AiZynth impact on medicinal chemistry practice at AstraZeneca.
Shields JD, Howells R, Lamont G, Leilei Y, Madin A, Reimann CE, Rezaei H, Reuillon T, Smith B, Thomson C, Zheng Y, Ziegler RE. Shields JD, et al. Among authors: madin a. RSC Med Chem. 2024 Feb 16;15(4):1085-1095. doi: 10.1039/d3md00651d. eCollection 2024 Apr 24. RSC Med Chem. 2024. PMID: 38665822
7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.
Carling RW, Madin A, Guiblin A, Russell MG, Moore KW, Mitchinson A, Sohal B, Pike A, Cook SM, Ragan IC, McKernan RM, Quirk K, Ferris P, Marshall G, Thompson SA, Wafford KA, Dawson GR, Atack JR, Harrison T, Castro JL, Street LJ. Carling RW, et al. Among authors: madin a. J Med Chem. 2005 Nov 17;48(23):7089-92. doi: 10.1021/jm058034a. J Med Chem. 2005. PMID: 16279764
Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1).
Chan BK, Seward E, Lainchbury M, Brewer TF, An L, Blench T, Cartwright MW, Chan GKY, Choo EF, Drummond J, Elliott RL, Gancia E, Gazzard L, Hu B, Jones GE, Luo X, Madin A, Malhotra S, Moffat JG, Pang J, Salphati L, Sneeringer CJ, Stivala CE, Wei B, Wang W, Wu P, Heffron TP. Chan BK, et al. Among authors: madin a. ACS Med Chem Lett. 2021 Dec 8;13(1):84-91. doi: 10.1021/acsmedchemlett.1c00473. eCollection 2022 Jan 13. ACS Med Chem Lett. 2021. PMID: 35059127 Free PMC article.
Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition.
Ellard JM, Madin A, Philps O, Hopkin M, Henderson S, Birch L, O'Connor D, Arai T, Takase K, Morgan L, Reynolds D, Talma S, Howley E, Powney B, Payne AH, Hall A, Gartlon JE, Dawson LA, Castro L, Atkinson PJ. Ellard JM, et al. Among authors: madin a. Bioorg Med Chem Lett. 2015 Dec 15;25(24):5792-6. doi: 10.1016/j.bmcl.2015.10.050. Epub 2015 Oct 17. Bioorg Med Chem Lett. 2015. PMID: 26531152
Tool inhibitors and assays to interrogate the biology of the TRAF2 and NCK interacting kinase.
Read J, Collie IT, Nguyen-McCarty M, Lucaj C, Robinson J, Conway L, Mukherjee J, McCall E, Donohoe G, Flavell E, Peciak K, Warwicker J, Dix C, Van den Hoven BG, Madin A, Brown DG, Moss S, Haggarty SJ, Brandon NJ, Bürli RW. Read J, et al. Among authors: madin a. Bioorg Med Chem Lett. 2019 Aug 1;29(15):1962-1967. doi: 10.1016/j.bmcl.2019.05.032. Epub 2019 May 18. Bioorg Med Chem Lett. 2019. PMID: 31153805
27 results