Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase
Angst, Daniela, Gessier, François, Janser, Philipp, Vulpetti, Anna, Wälchli, Rudolf, Beerli, Christian, Littlewood-Evans, Amanda, Dawson, Janet, Nuesslein-Hildesheim, Barbara, Wieczorek, Grazyna, Gutmann, Sascha, Scheufler, Clemens, Hinniger, Alexandra, Zimmerlin, Alfred, Funhoff, Enrico G, Pulz, Robert, Cenni, Bruno
Published in Journal of medicinal chemistry (28.05.2020)
Published in Journal of medicinal chemistry (28.05.2020)
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Journal Article
Discovery of Novel Dot1L Inhibitors through a Structure-Based Fragmentation Approach
Chen, Chao, Zhu, Hugh, Stauffer, Frédéric, Caravatti, Giorgio, Vollmer, Susanne, Machauer, Rainer, Holzer, Philipp, Möbitz, Henrik, Scheufler, Clemens, Klumpp, Martin, Tiedt, Ralph, Beyer, Kim S, Calkins, Keith, Guthy, Daniel, Kiffe, Michael, Zhang, Jeff, Gaul, Christoph
Published in ACS medicinal chemistry letters (11.08.2016)
Published in ACS medicinal chemistry letters (11.08.2016)
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Journal Article
Optimization of a Fragment-Based Screening Hit toward Potent DOT1L Inhibitors Interacting in an Induced Binding Pocket
Scheufler, Clemens, Möbitz, Henrik, Gaul, Christoph, Ragot, Christian, Be, Céline, Fernández, César, Beyer, Kim S, Tiedt, Ralph, Stauffer, Frédéric
Published in ACS medicinal chemistry letters (11.08.2016)
Published in ACS medicinal chemistry letters (11.08.2016)
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Journal Article
Discovery of Potent, Selective, and Structurally Novel Dot1L Inhibitors by a Fragment Linking Approach
Möbitz, Henrik, Machauer, Rainer, Holzer, Philipp, Vaupel, Andrea, Stauffer, Frédéric, Ragot, Christian, Caravatti, Giorgio, Scheufler, Clemens, Fernandez, Cesar, Hommel, Ulrich, Tiedt, Ralph, Beyer, Kim S, Chen, Chao, Zhu, Hugh, Gaul, Christoph
Published in ACS medicinal chemistry letters (09.03.2017)
Published in ACS medicinal chemistry letters (09.03.2017)
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Journal Article
Large Scale Meta-Analysis of Fragment-Based Screening Campaigns: Privileged Fragments and Complementary Technologies
Kutchukian, Peter S., Wassermann, Anne Mai, Lindvall, Mika K., Wright, S. Kirk, Ottl, Johannes, Jacob, Jaison, Scheufler, Clemens, Marzinzik, Andreas, Brooijmans, Natasja, Glick, Meir
Published in Journal of biomolecular screening (01.06.2015)
Published in Journal of biomolecular screening (01.06.2015)
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Journal Article
Identification of a Novel Allosteric Inhibitory Site on Tryptophan Hydroxylase 1 Enabling Unprecedented Selectivity Over all Related Hydroxylases
Petrassi, Mike, Barber, Rob, Be, Celine, Beach, Sarah, Cox, Brian, D'Souza, Anne-Marie, Duggan, Nick, Hussey, Martin, Fox, Roy, Hunt, Peter, Jarai, Gabor, Kosaka, Takatoshi, Oakley, Paul, Patel, Viral, Press, Neil, Rowlands, David, Scheufler, Clemens, Schmidt, Oliver, Srinivas, Honnappa, Turner, Mary, Turner, Rob, Westwick, John, Wolfreys, Alison, Pathan, Nuzhat, Watson, Simon, Thomas, Matthew
Published in Frontiers in pharmacology (05.05.2017)
Published in Frontiers in pharmacology (05.05.2017)
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Discovery of the Clinical Candidate MAK683: An EED-Directed, Allosteric, and Selective PRC2 Inhibitor for the Treatment of Advanced Malignancies
Huang, Ying, Sendzik, Martin, Zhang, Jeff, Gao, Zhenting, Sun, Yongfeng, Wang, Long, Gu, Justin, Zhao, Kehao, Yu, Zhengtian, Zhang, Lijun, Zhang, Qiong, Blanz, Joachim, Chen, Zijun, Dubost, Valérie, Fang, Douglas, Feng, Lijian, Fu, Xingnian, Kiffe, Michael, Li, Ling, Luo, Fangjun, Luo, Xiao, Mi, Yuan, Mistry, Prakash, Pearson, David, Piaia, Alessandro, Scheufler, Clemens, Terranova, Remi, Weiss, Andreas, Zeng, Jue, Zhang, Hailong, Zhang, Jiangwei, Zhao, Mengxi, Dillon, Michael P, Jeay, Sebastien, Qi, Wei, Moggs, Jonathan, Pissot-Soldermann, Carole, Li, En, Atadja, Peter, Lingel, Andreas, Oyang, Counde
Published in Journal of medicinal chemistry (14.04.2022)
Published in Journal of medicinal chemistry (14.04.2022)
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The First Class of Small Molecules Potently Disrupting the YAP‐TEAD Interaction by Direct Competition
Furet, Pascal, Bordas, Vincent, Le Douget, Mickaël, Salem, Bahaa, Mesrouze, Yannick, Imbach‐Weese, Patricia, Sellner, Holger, Voegtle, Markus, Soldermann, Nicolas, Chapeau, Emilie, Wartmann, Markus, Scheufler, Clemens, Fernandez, Cesar, Kallen, Joerg, Guagnano, Vito, Chène, Patrick, Schmelzle, Tobias
Published in ChemMedChem (06.10.2022)
Published in ChemMedChem (06.10.2022)
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Discovery and In Vivo Exploration of 1,3,4-Oxadiazole and α‑Fluoroacrylate Containing IL-17 Inhibitors
Velcicky, Juraj, Bauer, Matthias R., Schlapbach, Achim, Lapointe, Guillaume, Meyer, Arndt, Vögtle, Markus, Blum, Ernst, Ngo, Estelle, Rolando, Catherine, Nimsgern, Pierre, Teixeira-Fouchard, Sylvie, Lehmann, Hansjoerg, Furet, Pascal, Berst, Frédéric, Schümann, Jens, Stringer, Rowan, Larger, Patrice, Schmid, Cindy, Prendergast, Catriona T., Riek, Simone, Schmutz, Patrick, Lehmann, Sylvie, Berghausen, Jörg, Scheufler, Clemens, Rondeau, Jean-Michel, Burkhart, Christoph, Knoepfel, Thomas, Gommermann, Nina
Published in Journal of medicinal chemistry (26.09.2024)
Published in Journal of medicinal chemistry (26.09.2024)
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Front Cover: The First Class of Small Molecules Potently Disrupting the YAP‐TEAD Interaction by Direct Competition (ChemMedChem 19/2022)
Furet, Pascal, Bordas, Vincent, Le Douget, Mickaël, Salem, Bahaa, Mesrouze, Yannick, Imbach‐Weese, Patricia, Sellner, Holger, Voegtle, Markus, Soldermann, Nicolas, Chapeau, Emilie, Wartmann, Markus, Scheufler, Clemens, Fernandez, Cesar, Kallen, Joerg, Guagnano, Vito, Chène, Patrick, Schmelzle, Tobias
Published in ChemMedChem (06.10.2022)
Published in ChemMedChem (06.10.2022)
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Journal Article
New Potent DOT1L Inhibitors for in Vivo Evaluation in Mouse
Stauffer, Frédéric, Weiss, Andreas, Scheufler, Clemens, Möbitz, Henrik, Ragot, Christian, Beyer, Kim S, Calkins, Keith, Guthy, Daniel, Kiffe, Michael, Van Eerdenbrugh, Bernard, Tiedt, Ralph, Gaul, Christoph
Published in ACS medicinal chemistry letters (12.12.2019)
Published in ACS medicinal chemistry letters (12.12.2019)
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Journal Article
Optimization of a Class of Dihydrobenzofurane Analogs toward Orally Efficacious YAP‐TEAD Protein‐Protein Interaction Inhibitors
Sellner, Holger, Chapeau, Emilie, Furet, Pascal, Voegtle, Markus, Salem, Bahaa, Le Douget, Mickaël, Bordas, Vincent, Groell, Jean‐Marc, Le Goff, Anne‐Laure, Rouzet, Christine, Wietlisbach, Thomas, Zimmermann, Thomas, McKenna, Joseph, Brocklehurst, Cara E., Chène, Patrick, Wartmann, Markus, Scheufler, Clemens, Kallen, Joerg, Williams, Gareth, Harlfinger, Stephanie, Traebert, Martin, Dumotier, Bérengère M., Schmelzle, Tobias, Soldermann, Nicolas
Published in ChemMedChem (01.06.2023)
Published in ChemMedChem (01.06.2023)
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