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Development of Pyridine-Based Inhibitors for the Human Vaccinia-Related Kinases 1 and 2

Ricardo Serafim, Fernando de Souza Gama, Caio dos Reis, Stanley Vasconcelos, André Santiago, Jessica Takarada, Luiz Dutra, Fulvia Di Pillo, Hatylas Azevedo, Alessandra Mascarello, Jonathan Elkins, Katlin Massirer, Opher Gileadi, Cristiano Guimarães, Rafael Counago

Version 1 posted 04 March 2019

589

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Biological and Medicinal Chemistry

Working Paper

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

914

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Biological and Medicinal Chemistry

Working Paper

Novel dihydropteridinone derivatives as potent and selective inhibitors of the understudied human vaccinia-related kinase 1 (VRK1)

Fernando H. de Souza Gama, Luiz Dutra, Michael Hawgood, Caio Vinícius dos Reis, Ricardo Serafim, Marcos Ferreira Jr., Bruno V. M. Teodoro, Jéssica Takarada, André Santiago, Vitor M. Almeida, Carina Gileadi, Priscila Zonzini Ramos, Anita Salmazo, Stanley Vasconcelos, Micael Cunha, Dimitrios-Ilias Ballourdas, Susanne Mueller, Stefan Knapp, Katlin Massirer, Jonathan Elkins, Opher Gileadi, Alessandra Macarello, Bennie Lemmens, Cristiano R. W. Guimarães, Hatylas Azevedo, Rafael Couñago

Version 1 posted 04 December 2023

880

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Biological and Medicinal Chemistry

Working Paper

Hinge Binder Scaffold Hopping Identifies Potent Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CAMKK2) Inhibitor Chemotypes

benjamin eduful, Sean O'Byrne, Louisa Temme, Christopher R. M. Asquith, Yi Liang, Alfredo Picado, Joseph Pilotte, Carrow Wells, William Zuercher, Carolina Catta-Preta, Priscila Zonzini Ramos, André Santiago, rafael Counago, Christopher G Langendorf, Kevin Nay, Jonathan S Oakhill, Thomas L Pulliam, Chenchu Lin, Dominik Awad, Timothy M. Willson, Daniel E Frigo, John W. Scott, David Drewry

Version 1 posted 28 December 2020

448

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Biological and Medicinal Chemistry

Working Paper

Identification of P218 as a Potent Inhibitor of Mycobacteria Ulcerans DHFR

Gustavo Pelicioli Riboldi, Rachael Zigweid, Peter J. Myler, Stephen J. Mayclin, Rafael Counago, Bart L. Staker

Version 1 posted 01 September 2020

256

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Biological and Medicinal Chemistry

Working Paper

A Chemical Probe Targeting AAK1 and BMP2K

Carrow Wells, Rafael Counago, Juanita C. Limas, Tuanny L. Almeida, Jeanette G. Cook, David Drewry, Jonathan Elkins, Opher Gileadi, Nirav Kapadia, Álvaro Lorente-Macías, Julie E. Pickett, Alexander J. Riemen, Roberta R. Ruela-de-Sousa, Timothy M. Willson, Cunyu Zhang, William J. Zuercher, Reena Zutshi, Alison D. Axtman

Version 1 posted 04 September 2019

627

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Biological and Medicinal Chemistry

Working Paper

More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication

Han Wee Ong, Xuan Yang, Jeffery Smith, Rebekah Dickmander, Jason Brown, Tammy Havener, Sharon Taft-Benz, Stefanie Howell, Marcia Sanders, Jacob Capener, Rafael Couñago, Edcon Chang, Andreas Krämer, Nathaniel Moorman, Mark Heise, Alison Axtman, David Drewry, Timothy Willson

Version 1 posted 24 April 2024

145

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Biological and Medicinal Chemistry

Working Paper

Rational exploration of 2,4-diaminopyrimidines as DHFR inhibitors active against Mycobacterium abscessus and Mycobacterium avium, two emerging human pathogens

Matheus Meirelles, Vitor Almeida, Jaryd Sullivan, Ian de Toledo, Caio dos Reis, Micael Cunha, Rachael Zigweid, Abraham Shim, Banumathi Sankaran, Elijah Woodward, Steve Seibold, Lijun Liu, Mohammad Mian, Kevin Battaile, Jennifer Riley, Christina Duncan, Frederick Simeons, Liam Ferguson, Kevin Read, Scott Lovell, Bart Staker, Marcel Behr, Ronaldo Pilli, Rafael Couñago

Version 1 posted 15 July 2024

53

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Biological and Medicinal Chemistry

Working Paper

Strategic Fluorination to Achieve a Potent, Selective, Metabolically-Stable, and Orally-Bioavailable Inhibitor of CSNK2.

Han Wee Ong, Xuan Yang, Jeffery Smith, Sharon Taft-Benz, Stefanie Howell, Rebekah Dickmander, Tammy Havener, Marcia Sanders, Jason Brown, Rafael Couñago, Edcon Chang, Andreas Krämer, Nathaniel Moorman, Mark Heise, Alison Axtman, David Drewry, Timothy Willson

Version 1 posted 22 July 2024

0

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9 results in Rafael Couñago in Authors: Rafael Couñago

Development of Pyridine-Based Inhibitors for the Human Vaccinia-Related Kinases 1 and 2

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

Novel dihydropteridinone derivatives as potent and selective inhibitors of the understudied human vaccinia-related kinase 1 (VRK1)

Hinge Binder Scaffold Hopping Identifies Potent Calcium/Calmodulin-Dependent Protein Kinase Kinase 2 (CAMKK2) Inhibitor Chemotypes

Identification of P218 as a Potent Inhibitor of Mycobacteria Ulcerans DHFR

A Chemical Probe Targeting AAK1 and BMP2K

More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication

Rational exploration of 2,4-diaminopyrimidines as DHFR inhibitors active against Mycobacterium abscessus and Mycobacterium avium, two emerging human pathogens

Strategic Fluorination to Achieve a Potent, Selective, Metabolically-Stable, and Orally-Bioavailable Inhibitor of CSNK2.

9 results in Authors: Rafael Couñago