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Design, Synthesis and Characterization of Covalent KDM5 Inhibitors

Saleta Vazquez-Rodriguez, Miranda Wright, Catherine Rogers, Adam Cribbs, Srikannathasan Velupillai, Martin Philpott, Henry Lee, James E. Dunford, Kilian Huber, Matthew B. Robers, Jim Vasta, Marie-Laetitia Thezenas, Sarah Bonham, Benedikt M. Kessler, James Bennett, Oleg Fedorov, Florence Raynaud, Adam Donovan, Julian Blagg, Vassilios Bavetsias, Udo Oppermann, Akane Kawamura, Paul Brennan

Version 1 posted 11 September 2018

899

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1

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Biological and Medicinal Chemistry

Working Paper

Isotopically Labeled Desthiobiotin Azide (isoDTB) Tags Enable Global Profiling of the Bacterial Cysteinome

Patrick R. A. Zanon, Lisa Lewald, Stephan M. Hacker

Version 1 posted 20 September 2019

1,207

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Biological and Medicinal Chemistry

Working Paper

Light-Activatable, 2,5-Disubstituted Tetrazoles for the Proteome-Wide Profiling of Aspartates and Glutamates in Living Bacteria

Kathrin Bach, Bert L. H. Beerkens, Patrick R. A. Zanon, Stephan M. Hacker

Version 1 posted 18 December 2019

899

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Biological and Medicinal Chemistry

Working Paper

Rationally Designed Potent BMX Inhibitors Reveals Mode of Covalent Binding at the Atomic Level

João D. Seixas, Bárbara B. Sousa, Marta C. Marques, Ana Guerreiro, Rui Traquete, Tiago Rodrigues, Inês S. Albuquerque, Marcos Sousa, Ana R. Lemos, Pedro M. F. Sousa, Tiago M. Bandeiras, Di Wu, Shelby K. Doyle, Carol V. Robinson, Angela Koehler, Francisco Corzana, Pedro Matias, Gonçalo Bernardes

Version 1 posted 09 January 2020

1,150

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Biological and Medicinal Chemistry

Working Paper

Covalent Protein Inhibitors via Tyrosine Conjugation with Cyclic Imine Mannich Electrophiles

Sijie Wang, Marco Hadisurya, W. Andy Tao, Emily Dykhuizen, Casey Krusemark

Version 1 posted 18 October 2022

2,499

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1

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Biological and Medicinal Chemistry

Working Paper

The Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19

Robert Hoffman, Robert S. Kania, Mary A. Brothers, Jay F. Davies, Rose A. Ferre, Ketan S. Gajiwala, Mingying He, Robert Jeff Hogan, Kirk Kozminski, Lilian Y. Li, Jonathan W. Lockner, Jihong Lou, Michelle T. Marra, Lennert J. Mitchell J. Mitchell Jr, Brion W. Murray, James A. Nieman, Stephen Noell, Simon P. Planken, Thomas Rowe, Kevin Ryan, George J. Smith III, James E. Solowiej, Claire M. Steppan, Barbara Taggart

Version 1 posted 22 July 2020

2,288

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1

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Organic Chemistry

Working Paper

Aryl Fluorosulfate-Based Inhibitors that Covalently Target the SIRT5 Lysine Deacylase

Julie E. Bolding, Pablo Martín-Gago, Nima Rajabi, Luke F. Gamon, Tobias N. Hansen, Michael Jonathan Davies, Christian Adam Olsen

Version 1 posted 23 February 2022

521

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1

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Biological and Medicinal Chemistry

Review

Systematic exploration of privileged warheads for covalent kinase drug discovery

Zheng Zhao, Philip E. Bourne

Version 1 posted 16 August 2022

1,753

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1

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Organic Chemistry

Review

Advances in sulfur fluoride exchange for chemical biology

Tobias N. Hansen, Marcos San Segundo, Annika M. Mergel, Christian Adam Olsen

Version 2 posted 08 January 2025

566

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Biological and Medicinal Chemistry

Working Paper

Reactive Docking: a computational method for high-throughput virtual screenings of reactive species

Giulia Bianco, Matthew Holcomb, Diogo Santos-Martins, Andreas Tillack, Althea Hansel-Harris, Stefano Forli

Version 1 posted 19 May 2023

464

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18 results in Covalent inhibitors in Keywords: Covalent inhibitors

Design, Synthesis and Characterization of Covalent KDM5 Inhibitors

Isotopically Labeled Desthiobiotin Azide (isoDTB) Tags Enable Global Profiling of the Bacterial Cysteinome

Light-Activatable, 2,5-Disubstituted Tetrazoles for the Proteome-Wide Profiling of Aspartates and Glutamates in Living Bacteria

Rationally Designed Potent BMX Inhibitors Reveals Mode of Covalent Binding at the Atomic Level

Covalent Protein Inhibitors via Tyrosine Conjugation with Cyclic Imine Mannich Electrophiles

The Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19

Aryl Fluorosulfate-Based Inhibitors that Covalently Target the SIRT5 Lysine Deacylase

Systematic exploration of privileged warheads for covalent kinase drug discovery

Advances in sulfur fluoride exchange for chemical biology

Reactive Docking: a computational method for high-throughput virtual screenings of reactive species

18 results in Keywords: Covalent inhibitors