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Material Type: Artigo
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Discovery and Optimization of Selective Brain-Penetrant EBP Inhibitors that Enhance Oligodendrocyte FormationDorel, Ruth ; Sun, Dawei ; Carruthers, Nicholas ; Castanedo, Georgette M. ; Ung, Peter M.-U. ; Factor, Daniel C. ; Li, Tianbo ; Baumann, Hannah ; Janota, Danielle ; Pang, Jodie ; Salphati, Laurent ; Meklemburg, Robert ; Korman, Allison J. ; Harper, Halie E. ; Stubblefield, Samantha ; Payandeh, Jian ; McHugh, Daniel ; Lang, Bradley T. ; Tesar, Paul J. ; Dere, Edward ; Masureel, Matthieu ; Adams, Drew J. ; Volgraf, Matthew ; Braun, Marie-GabrielleJournal of medicinal chemistry, 2024-03, Vol.67 (6), p.4819-4832 [Periódico revisado por pares]United States: American Chemical SocietyTexto completo disponível |
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Material Type: Artigo
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Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3KαHanan, Emily J. ; Braun, Marie-Gabrielle ; Heald, Robert A. ; MacLeod, Calum ; Chan, Connie ; Clausen, Saundra ; Edgar, Kyle A. ; Eigenbrot, Charles ; Elliott, Richard ; Endres, Nicholas ; Friedman, Lori S. ; Gogol, Emily ; Gu, Xiao-Hui ; Thibodeau, Rebecca Hong ; Jackson, Philip S. ; Kiefer, James R. ; Knight, Jamie D. ; Nannini, Michelle ; Narukulla, Raman ; Pace, Amanda ; Pang, Jodie ; Purkey, Hans E. ; Salphati, Laurent ; Sampath, Deepak ; Schmidt, Stephen ; Sideris, Steve ; Song, Kyung ; Sujatha-Bhaskar, Swathi ; Ultsch, Mark ; Wallweber, Heidi ; Xin, Jianfeng ; Yeap, SiewKuen ; Young, Amy ; Zhong, Yu ; Staben, Steven T.Journal of medicinal chemistry, 2022-12, Vol.65 (24), p.16589-16621 [Periódico revisado por pares]United States: American Chemical SocietyTexto completo disponível |
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Material Type: Artigo
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Discovery, Characterization, and Structure-Based Optimization of Small-Molecule In Vitro and In Vivo Probes for Human DNA Polymerase ThetaStockley, Martin L. ; Ferdinand, Amanda ; Benedetti, Giovanni ; Blencowe, Peter ; Boyd, Susan M. ; Calder, Mat ; Charles, Mark D. ; Edwardes, Lucy V. ; Ekwuru, Tennyson ; Finch, Harry ; Galbiati, Alessandro ; Geo, Lerin ; Grande, Diego ; Grinkevich, Vera ; Holliday, Nicholas D. ; Krajewski, Wojciech W. ; MacDonald, Ellen ; Majithiya, Jayesh B. ; McCarron, Hollie ; McWhirter, Claire L. ; Patel, Viral ; Pedder, Chris ; Rajendra, Eeson ; Ranzani, Marco ; Rigoreau, Laurent J. M. ; Robinson, Helen M. R. ; Schaedler, Theresia ; Sirina, Julija ; Smith, Graeme C. M. ; Swarbrick, Martin E. ; Turnbull, Andrew P. ; Willis, Simon ; Heald, Robert A.Journal of medicinal chemistry, 2022-10, Vol.65 (20), p.13879-13891 [Periódico revisado por pares]United States: American Chemical SocietyTexto completo disponível |
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Material Type: Artigo
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Parallel Optimization of Potency and Pharmacokinetics Leading to the Discovery of a Pyrrole Carboxamide ERK5 Kinase Domain InhibitorMiller, Duncan C. ; Reuillon, Tristan ; Molyneux, Lauren ; Blackburn, Timothy ; Cook, Simon J. ; Edwards, Noel ; Endicott, Jane A. ; Golding, Bernard T. ; Griffin, Roger J. ; Hardcastle, Ian ; Harnor, Suzannah J. ; Heptinstall, Amy ; Lochhead, Pamela ; Martin, Mathew P. ; Martin, Nick C. ; Myers, Stephanie ; Newell, David R. ; Noble, Richard A. ; Phillips, Nicole ; Rigoreau, Laurent ; Thomas, Huw ; Tucker, Julie A. ; Wang, Lan-Zhen ; Waring, Michael J. ; Wong, Ai-Ching ; Wedge, Stephen R. ; Noble, Martin E. M. ; Cano, CelineJournal of medicinal chemistry, 2022-05, Vol.65 (9), p.6513-6540 [Periódico revisado por pares]United States: American Chemical SocietyTexto completo disponível |
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Material Type: Artigo
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Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1)Williamson, Douglas S ; Smith, Garrick P ; Acheson-Dossang, Pamela ; Bedford, Simon T ; Chell, Victoria ; Chen, I-Jen ; Daechsel, Justus C. A ; Daniels, Zoe ; David, Laurent ; Dokurno, Pawel ; Hentzer, Morten ; Herzig, Martin C ; Hubbard, Roderick E ; Moore, Jonathan D ; Murray, James B ; Newland, Samantha ; Ray, Stuart C ; Shaw, Terry ; Surgenor, Allan E ; Terry, Lindsey ; Thirstrup, Kenneth ; Wang, Yikang ; Christensen, Kenneth VJournal of medicinal chemistry, 2017-11, Vol.60 (21), p.8945-8962 [Periódico revisado por pares]United States: American Chemical SocietyTexto completo disponível |
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Material Type: Artigo
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Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing PropertiesDyck, Brian ; Branstetter, Bryan ; Gharbaoui, Tawfik ; Hudson, Andrew R ; Breitenbucher, J. Guy ; Gomez, Laurent ; Botrous, Iriny ; Marrone, Tami ; Barido, Richard ; Allerston, Charles K ; Cedervall, E. Peder ; Xu, Rui ; Sridhar, Vandana ; Barker, Ryan ; Aertgeerts, Kathleen ; Schmelzer, Kara ; Neul, David ; Lee, Dong ; Massari, Mark Eben ; Andersen, Carsten B ; Sebring, Kristen ; Zhou, Xianbo ; Petroski, Robert ; Limberis, James ; Augustin, Martin ; Chun, Lawrence E ; Edwards, Thomas E ; Peters, Marco ; Tabatabaei, AliJournal of medicinal chemistry, 2017-04, Vol.60 (8), p.3472-3483 [Periódico revisado por pares]United States: American Chemical SocietyTexto completo disponível |
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Material Type: Artigo
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New 6‑Aminoquinoxaline Derivatives with Neuroprotective Effect on Dopaminergic Neurons in Cellular and Animal Parkinson Disease ModelsLe Douaron, Gael ; Ferrié, Laurent ; Sepulveda-Diaz, Julia E ; Amar, Majid ; Harfouche, Abha ; Séon-Méniel, Blandine ; Raisman-Vozari, Rita ; Michel, Patrick P ; Figadère, BrunoJournal of medicinal chemistry, 2016-07, Vol.59 (13), p.6169-6186 [Periódico revisado por pares]United States: American Chemical SocietyTexto completo disponível |
8 |
Material Type: Artigo
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Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1Llona-Minguez, Sabin ; Höglund, Andreas ; Jacques, Sylvain A ; Johansson, Lars ; Calderón-Montaño, José Manuel ; Claesson, Magnus ; Loseva, Olga ; Valerie, Nicholas C. K ; Lundbäck, Thomas ; Piedrafita, Javier ; Maga, Giovanni ; Crespan, Emmanuele ; Meijer, Laurent ; Burgos Morón, Estefanía ; Baranczewski, Pawel ; Hagbjörk, Ann-Louise ; Svensson, Richard ; Wiita, Elisee ; Almlöf, Ingrid ; Visnes, Torkild ; Jeppsson, Fredrik ; Sigmundsson, Kristmundur ; Jensen, Annika Jenmalm ; Artursson, Per ; Jemth, Ann-Sofie ; Stenmark, Pål ; Warpman Berglund, Ulrika ; Scobie, Martin ; Helleday, ThomasJournal of medicinal chemistry, 2016-02, Vol.59 (3), p.1140-1148 [Periódico revisado por pares]United States: American Chemical SocietyTexto completo disponível |
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Material Type: Artigo
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Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3Boyd, Scott ; Brookfield, Joanna L ; Critchlow, Susan E ; Cumming, Iain A ; Curtis, Nicola J ; Debreczeni, Judit ; Degorce, Sébastien L ; Donald, Craig ; Evans, Nicola J ; Groombridge, Sam ; Hopcroft, Philip ; Jones, Neil P ; Kettle, Jason G ; Lamont, Scott ; Lewis, Hilary J ; MacFaull, Philip ; McLoughlin, Sheila B ; Rigoreau, Laurent J. M ; Smith, James M ; St-Gallay, Steve ; Stock, Julie K ; Turnbull, Andrew P ; Wheatley, Edward R ; Winter, Jon ; Wingfield, JonathanJournal of medicinal chemistry, 2015-04, Vol.58 (8), p.3611-3625 [Periódico revisado por pares]United States: American Chemical SocietyTexto completo disponível |
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Material Type: Artigo
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Structure–Activity Relationships and Design of Viral Mutagens and Application to Lethal MutagenesisBonnac, Laurent F ; Mansky, Louis M ; Patterson, Steven EJournal of medicinal chemistry, 2013-12, Vol.56 (23), p.9403-9414 [Periódico revisado por pares]United States: American Chemical SocietyTexto completo disponível |