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Biological and Medicinal Chemistry

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structure-based design

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5 results in Keywords: structure-based design

Biological and Medicinal Chemistry

Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor

Ricardo Serafim, André Santiago, Caio dos Reis, Jessica Takarada, Priscila Mezzomo, Katlin Massirer, Martin P. Schwalm, Mark Kudolo, Stefan Gerstenecker, Apirat Chaikuad, Stefan Knapp, Stefan Laufer, Rafael Counago, Matthias Gehringer

Version 1 posted 20 May 2021

894

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Biological and Medicinal Chemistry

Exploring the NCS-382 Scaffold for CaMKIIα Modulation: Synthesis, Pharmacology, and Biophysical Characterization of Ph-HTBA as a Novel High-Affinity Brain-Penetrant Stabilizer of the CaMKIIα Hub Domain

Yongsong Tian, Mohamed Shehata, Stine Gauger, Carolina Veronesi, Louise Hamborg, Louise Thiesen, Jesper Bruus-Jensen, Johanne Schlieper Royssen, Ulrike Leurs, Anne Sofie Larsen, Jacob Krall, Sara Solbak, Petrine Wellendorph, Bente Frølund

Version 1 posted 30 May 2022

234

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Biological and Medicinal Chemistry

The Structure-Based Design of SARS-CoV-2 Nsp14 Methyltransferase Ligands Yields Nanomolar Inhibitors

Tomáš Otava, Michal Šála, Fengling Li, Jindřich Fanfrlík, Kanchan Devkota, Paknoosh Pakarian, Pavel Hobza, Masoud Vedadi, Evzen Boura, Radim Nencka

Version 1 posted 23 February 2021

585

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2

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Biological and Medicinal Chemistry

Development of Highly Potent and Selective Covalent FGFR4 Inhibitors Based on SNAr Electrophiles

Moritz Schwarz, Maksym Kurkunov, Florian Wittlinger, Ramona Rudalska, Guiqun Wang, Martin P. Schwalm, Alexander Rasch, Benedikt Wagner, Stefan A. Laufer, Stefan Knapp, Daniel Dauch, Matthias Gehringer

Version 2 posted 25 March 2024

821

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Biological and Medicinal Chemistry

The origin of potency and mutant-selective inhibition by bivalent ATP-allosteric EGFR inhibitors

Florian Wittlinger, Surbhi P Chitnis, Calvin D Pham, Tahereh Damghani, Ilse K Schaeffner, Matthew Q Deng, Blessing C Ogboo, Alexander Rasch, Tyler S Beyett, Brian Buckley, Frederic Feru, Tatiana Shaurova, Cornelius Knappe, Michael J Eck, Pamela A Hershberger, David A Scott, Stefan A Laufer, David E Heppner

Version 1 posted 26 September 2023

323

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1

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