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Page 1
Protease-activated receptor-2 ligands reveal orthosteric and allosteric mechanisms of receptor inhibition.
Kennedy AJ, Sundström L, Geschwindner S, Poon EKY, Jiang Y, Chen R, Cooke R, Johnstone S, Madin A, Lim J, Liu Q, Lohman RJ, Nordqvist A, Fridén-Saxin M, Yang W, Brown DG, Fairlie DP, Dekker N. Kennedy AJ, et al. Among authors: madin a. Commun Biol. 2020 Dec 17;3(1):782. doi: 10.1038/s42003-020-01504-0. Commun Biol. 2020. PMID: 33335291 Free PMC article.
A small molecule inhibitor of HER3: a proof-of-concept study.
Colomba A, Fitzek M, George R, Weitsman G, Roberts S, Zanetti-Domingues L, Hirsch M, Rolfe DJ, Mehmood S, Madin A, Claus J, Kjaer S, Snijders AP, Ng T, Martin-Fernandez M, Smith DM, Parker PJ. Colomba A, et al. Among authors: madin a. Biochem J. 2020 Sep 18;477(17):3329-3347. doi: 10.1042/BCJ20200496. Biochem J. 2020. PMID: 32815546 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
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.
Cyclic sulfamide gamma-secretase inhibitors.
Sparey T, Beher D, Best J, Biba M, Castro JL, Clarke E, Hannam J, Harrison T, Lewis H, Madin A, Shearman M, Sohal B, Tsou N, Welch C, Wrigley J. Sparey T, et al. Among authors: madin a. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4212-6. doi: 10.1016/j.bmcl.2005.06.084. Bioorg Med Chem Lett. 2005. PMID: 16054361
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.
28 results