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Academic Journal

Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).

Subjects: Brain/Brain/Brain/*metabolism ; Enzyme Inhibitors/Enzyme Inhibitors/Enzyme Inhibitors/*chemical synthesis ; Enzyme Inhibitors/Enzyme Inhibitors/Enzyme Inhibitors/*pharmacokinetics

  • Source: Journal of medicinal chemistry [J Med Chem] 2015 Oct 22; Vol. 58 (20), pp. 8182-99. Date of Electronic Publication: 2015 Oct 02.Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet

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Academic Journal

Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system.

  • Authors : Thomas AA; Array BioPharma , 3200 Walnut Street, Boulder, Colorado 80301, United States.; Hunt KW

Subjects: Amyloid Precursor Protein Secretases/Amyloid Precursor Protein Secretases/Amyloid Precursor Protein Secretases/*antagonists & inhibitors ; Amyloid beta-Peptides/Amyloid beta-Peptides/Amyloid beta-Peptides/*metabolism ; Aspartic Acid Endopeptidases/Aspartic Acid Endopeptidases/Aspartic Acid Endopeptidases/*antagonists & inhibitors

  • Source: Journal of medicinal chemistry [J Med Chem] 2014 Feb 13; Vol. 57 (3), pp. 878-902. Date of Electronic Publication: 2014 Jan 22.Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet

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Academic Journal

Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

  • Authors : Estrada AA; Departments of †Discovery Chemistry, ‡Neurosciences, §Biochemical and Cellular Pharmacology, ∥Drug Metabolism and Pharmacokinetics, ⊥Safety Assessment, and #Structural Biology, Genentech, Inc. , 1 DNA Way, South San Francisco, California 94080, United States.; Chan BK

Subjects: Brain/Brain/Brain/*metabolism ; Protein Serine-Threonine Kinases/Protein Serine-Threonine Kinases/Protein Serine-Threonine Kinases/*antagonists & inhibitors ; Pyrazoles/Pyrazoles/Pyrazoles/*chemistry

  • Source: Journal of medicinal chemistry [J Med Chem] 2014 Feb 13; Vol. 57 (3), pp. 921-36. Date of Electronic Publication: 2014 Jan 15.Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet

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Academic Journal

Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

  • Authors : Estrada AA; Department of Discovery Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, USA. ; Liu X

Subjects: Brain/Brain/Brain/*metabolism ; Morpholines/Morpholines/Morpholines/*pharmacology ; Parkinson Disease/Parkinson Disease/Parkinson Disease/*drug therapy

  • Source: Journal of medicinal chemistry [J Med Chem] 2012 Nov 26; Vol. 55 (22), pp. 9416-33. Date of Electronic Publication: 2012 Oct 15.Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet

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