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A Chemical Probe for Dark Kinase STK17B Derives its Potency and High Selectivity Through a Unique P-loop Conformation

Alfredo Picado, Apirat Chaikuad, Carrow Wells, Safal Shrestha, William Zuercher, Julie E. Pickett, Frank Kwarcinski, Parvathi Sinha, Chandi de Silva, Reena Zutshi, Shubin Liu, Natarajan Kannan, Stefan Knapp, David Drewry, Tim Willson

Version 1 posted 07 July 2020

799

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Biological and Medicinal Chemistry

Working Paper

Discovery of an MLLT1/3 YEATS Domain Chemical Probe

Moses Moustakim, Thomas Christott, Octovia P. Monteiro, James Bennett, Charline Giroud, Jennifer Ward, Catherine Rogers, Paul Smith, Ioanna Panagakou, Laura Diaz Saez, Suet Ling Felce, Vicki Gamble, Carina Gileadi, Nadia Halidi, David Heidenreich, Apirat Chaikuad, Stefan Knapp, Kilian Huber, Gillian Farnie, Jag Heer, Nenad Manevski, Gennady Poda, Rima Al-awar, Darren J. Dixon, Paul E. Brennan, Oleg Fedorov

Version 1 posted 18 September 2018

573

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Biological and Medicinal Chemistry

Working Paper

An Activity-based Probe Targeting Non-catalytic, Highly Conserved Amino Acid Residues Within Bromodomains

Melissa D’Ascenzio, Kathryn Pugh, Rebecca Konietzny, Georgina Berridge, Cynthia Tallant, Shaima Hashem, Octovia P. Monteiro, Jason R. Thomas, Markus Schirle, Stefan Knapp, Brian D. Marsden, Oleg Fedorov, Chas Bountra, Benedikt M. Kessler, Paul E. Brennan

Version 1 posted 17 October 2018

466

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Biological and Medicinal Chemistry

Working Paper

Structure-guided design of a highly potent RXR agonist with superior physicochemical properties

Max Lewandowski, Melania Carmina, Loris Knümann, Minh Sai, Sabine Willems, Till Kasch, Julius Pollinger, Stefan Knapp, Julian A. Marschner, Apirat Chaikuad, Daniel Merk

Version 1 posted 12 December 2023

113

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Biological and Medicinal Chemistry

Working Paper

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

321

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1

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Catalysis

Working Paper

Photosensitization Enables Pauson-Khand-type Reactions with Nitrenes

Fang Li, W. Felix Zhu, Claire Empel, Oleksandr Datsenko, Adarsh Kumar, Yameng Xu, Johanna H. M. Ehrler, Iuliana Atodiresei, Stefan Knapp, Pavel K. Mykhailiuk, Ewgenij Proschak, Rene M. Koenigs

Version 1 posted 31 October 2023

1,033

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Biological and Medicinal Chemistry

Working Paper

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

Working Paper

Discovery of fully synthetic FKBP12-mTOR molecular glues

Robin C.E. Deutscher, Christian Meyners, Sabine C. Schäfer, Maximilian L. Repity, Wisely Oki Sugiarto, Jürgen Kolos, Tim Heymann, Thomas M. Geiger, Stefan Knapp, Felix Hausch

Version 1 posted 26 July 2023

1,961

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3

Citations

Biological and Medicinal Chemistry

Working Paper

Discovery of Potent Plasmodium falciparum Protein Kinase 6 (PfPK6) Inhibitors with a Type II Inhibitor Pharmacophore

Han Wee Ong, Anna Truong, Frank Kwarcinski, Chandi de Silva, Krisha Avalani, Tammy Havener, Michael Chirgwin, Kareem Galal, Caleb Willis, Andreas Krämer, Shubin Liu, Stefan Knapp, Emily Derbyshire, Reena Zutshi, David Drewry

Version 1 posted 16 June 2022

380

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Biological and Medicinal Chemistry

Working Paper

Identification of histone peptide binding specificity and small molecule ligands for the bromodomains of TRIM33α and TRIM33β

Angelina Sekirnik, Jessica Reynolds, Larissa See, Joseph Bluck, Amy Scorah, Cynthia Tallant, Bernadette Lee, Katarzyna Leszczynska, Rachel Grimley, Ian Storer, Marta Malattia, Sara Crespillo, Sofia Caria, Stephanie Duclos, Ester Hammond, Stefan Knapp, Garrett Morris, Fernanda Duarte, Philip Biggin, Stuart Conway

Version 1 posted 29 March 2022

448

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14 results in Stefan Knapp in Authors: Stefan Knapp

A Chemical Probe for Dark Kinase STK17B Derives its Potency and High Selectivity Through a Unique P-loop Conformation

Discovery of an MLLT1/3 YEATS Domain Chemical Probe

An Activity-based Probe Targeting Non-catalytic, Highly Conserved Amino Acid Residues Within Bromodomains

Structure-guided design of a highly potent RXR agonist with superior physicochemical properties

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

Photosensitization Enables Pauson-Khand-type Reactions with Nitrenes

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

Discovery of fully synthetic FKBP12-mTOR molecular glues

Discovery of Potent Plasmodium falciparum Protein Kinase 6 (PfPK6) Inhibitors with a Type II Inhibitor Pharmacophore

Identification of histone peptide binding specificity and small molecule ligands for the bromodomains of TRIM33α and TRIM33β

14 results in Authors: Stefan Knapp