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Discovery of 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one (TAK-063), a highly potent, selective, and orally active phosphodiesterase 10A (PDE10A) inhibitor.
Kunitomo J, Yoshikawa M, Fushimi M, Kawada A, Quinn JF, Oki H, Kokubo H, Kondo M, Nakashima K, Kamiguchi N, Suzuki K, Kimura H, Taniguchi T. Kunitomo J, et al. Among authors: fushimi m. J Med Chem. 2014 Nov 26;57(22):9627-43. doi: 10.1021/jm5013648. Epub 2014 Nov 10. J Med Chem. 2014. PMID: 25384088
Discovery of Potent, Selective, and Brain-Penetrant 1 H-Pyrazol-5-yl-1 H-pyrrolo[2,3- b]pyridines as Anaplastic Lymphoma Kinase (ALK) Inhibitors.
Fushimi M, Fujimori I, Wakabayashi T, Hasui T, Kawakita Y, Imamura K, Kato T, Murakami M, Ishii T, Kikko Y, Kasahara M, Nakatani A, Hiura Y, Miyamoto M, Saikatendu K, Zou H, Lane SW, Lawson JD, Imoto H. Fushimi M, et al. J Med Chem. 2019 May 23;62(10):4915-4935. doi: 10.1021/acs.jmedchem.8b01630. Epub 2019 May 3. J Med Chem. 2019. PMID: 31009559
T-495, a novel low cooperative M1 receptor positive allosteric modulator, improves memory deficits associated with cholinergic dysfunction and is characterized by low gastrointestinal side effect risk.
Mandai T, Sako Y, Kurimoto E, Shimizu Y, Nakamura M, Fushimi M, Maeda R, Miyamoto M, Kimura H. Mandai T, et al. Among authors: fushimi m. Pharmacol Res Perspect. 2020 Feb;8(1):e00560. doi: 10.1002/prp2.560. Pharmacol Res Perspect. 2020. PMID: 31990455 Free PMC article.
Discovery of TDI-10229: A Potent and Orally Bioavailable Inhibitor of Soluble Adenylyl Cyclase (sAC, ADCY10).
Fushimi M, Buck H, Balbach M, Gorovyy A, Ferreira J, Rossetti T, Kaur N, Levin LR, Buck J, Quast J, van den Heuvel J, Steegborn C, Finkin-Groner E, Kargman S, Michino M, Foley MA, Miller M, Liverton NJ, Huggins DJ, Meinke PT. Fushimi M, et al. ACS Med Chem Lett. 2021 Jul 14;12(8):1283-1287. doi: 10.1021/acsmedchemlett.1c00273. eCollection 2021 Aug 12. ACS Med Chem Lett. 2021. PMID: 34413957 Free PMC article.
Prediction of Compound Bioactivities Using Heat-Diffusion Equation.
Hidaka T, Imamura K, Hioki T, Takagi T, Giga Y, Giga MH, Nishimura Y, Kawahara Y, Hayashi S, Niki T, Fushimi M, Inoue H. Hidaka T, et al. Among authors: fushimi m. Patterns (N Y). 2020 Nov 11;1(9):100140. doi: 10.1016/j.patter.2020.100140. eCollection 2020 Dec 11. Patterns (N Y). 2020. PMID: 33336198 Free PMC article.
105 results