Predictive Model for Site-Selective Aryl and Heteroaryl C–H Functionalization via Organic Photoredox Catalysis von Margrey, Kaila A, McManus, Joshua B, Bonazzi, Simone, Zecri, Frederic, Nicewicz, David A

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JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors von Lorthiois, Edwige, Gerspacher, Marc, Beyer, Kim S., Vaupel, Andrea, Leblanc, Catherine, Stringer, Rowan, Weiss, Andreas, Wilcken, Rainer, Guthy, Daniel A., Lingel, Andreas, Bomio-Confaglia, Claudio, Machauer, Rainer, Rigollier, Pascal, Ottl, Johannes, Arz, Dorothee, Bernet, Pascal, Desjonqueres, Gaëlle, Dussauge, Solene, Kazic-Legueux, Malika, Lozac’h, Marie-Anne, Mura, Christophe, Sorge, Mickaël, Todorov, Milen, Warin, Nicolas, Zink, Florence, Voshol, Hans, Zecri, Frederic J., Sedrani, Richard C., Ostermann, Nils, Brachmann, Saskia M., Cotesta, Simona

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JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRAS G12C for the Treatment of Solid Tumors von Lorthiois, Edwige, Gerspacher, Marc, Beyer, Kim S, Vaupel, Andrea, Leblanc, Catherine, Stringer, Rowan, Weiss, Andreas, Wilcken, Rainer, Guthy, Daniel A, Lingel, Andreas, Bomio-Confaglia, Claudio, Machauer, Rainer, Rigollier, Pascal, Ottl, Johannes, Arz, Dorothee, Bernet, Pascal, Desjonqueres, Gaëlle, Dussauge, Solene, Kazic-Legueux, Malika, Lozac'h, Marie-Anne, Mura, Christophe, Sorge, Mickaël, Todorov, Milen, Warin, Nicolas, Zink, Florence, Voshol, Hans, Zecri, Frederic J, Sedrani, Richard C, Ostermann, Nils, Brachmann, Saskia M, Cotesta, Simona

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Persistent signaling induced by FTY720-phosphate is mediated by internalized S1P1 receptors von Mullershausen, Florian, Zecri, Frédéric, Cetin, Cihan, Billich, Andreas, Guerini, Danilo, Seuwen, Klaus

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The design and implementation of a generic lipopeptide scanning platform to enable the identification of ‘locally acting’ agonists for the apelin receptor von McKeown, Stephen C., Zecri, Frederic J., Fortier, Eric, Taggart, Andrew, Sviridenko, Lilya, Adams, Christopher M., McAllister, Kathryn H., Pin, Sokhom S.

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Medicinal Chemistry Profiling of Monocyclic 1,2‐Azaborines von Zhao, Peng, Nettleton, David O., Karki, Rajeshri G., Zécri, Frédéric J., Liu, Shih‐Yuan

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Absorption and Disposition of the Sphingosine 1-Phosphate Receptor Modulator Fingolimod (FTY720) in Healthy Volunteers: A Case of Xenobiotic Biotransformation Following Endogenous... von Zollinger, Markus, Gschwind, Hans-Peter, Jin, Yi, Sayer, Claudia, Zécri, Frédéric, Hartmann, Stefan

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Water-Compatible Cycloadditions of Oligonucleotide-Conjugated Strained Allenes for DNA-Encoded Library Synthesis von Westphal, Matthias V, Hudson, Liam, Mason, Jeremy W, Pradeilles, Johan A, Zécri, Frédéric J, Briner, Karin, Schreiber, Stuart L

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Rational Screening for Cooperativity in Small-Molecule Inducers of Protein–Protein Associations von Liu, Shuang, Tong, Bingqi, Mason, Jeremy W., Ostrem, Jonathan M., Tutter, Antonin, Hua, Bruce K., Tang, Sunny A., Bonazzi, Simone, Briner, Karin, Berst, Frédéric, Zécri, Frédéric J., Schreiber, Stuart L.

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Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C von Weiss, Andreas, Lorthiois, Edwige, Barys, Louise, Beyer, Kim S, Bomio-Confaglia, Claudio, Burks, Heather, Chen, Xueying, Cui, Xiaoming, de Kanter, Ruben, Dharmarajan, Lekshmi, Fedele, Carmine, Gerspacher, Marc, Guthy, Daniel Alexander, Head, Victoria, Jaeger, Ashley, Núñez, Eloísa Jiménez, Kearns, Jeffrey D, Leblanc, Catherine, Maira, Sauveur-Michel, Murphy, Jason, Oakman, Helen, Ostermann, Nils, Ottl, Johannes, Rigollier, Pascal, Roman, Danielle, Schnell, Christian, Sedrani, Richard, Shimizu, Toshio, Stringer, Rowan, Vaupel, Andrea, Voshol, Hans, Wessels, Peter, Widmer, Toni, Wilcken, Rainer, Xu, Kun, Zecri, Frederic, Farago, Anna F, Cotesta, Simona, Brachmann, Saskia M

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Modular Synthesis of Cyclopropane‐Fused N‐Heterocycles Enabled by Underexplored Diazo Reagents von Richter, Matthieu J. R., Zécri, Frédéric J., Briner, Karin, Schreiber, Stuart L.

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From Natural Product to the First Oral Treatment for Multiple Sclerosis: The Discovery of FTY720 (Gilenya™)? von Zécri, Frédéric J

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DNA-encoded library-enabled discovery of proximity-inducing small molecules von Mason, Jeremy W., Chow, Yuen Ting, Hudson, Liam, Tutter, Antonin, Michaud, Gregory, Westphal, Matthias V., Shu, Wei, Ma, Xiaolei, Tan, Zher Yin, Coley, Connor W., Clemons, Paul A., Bonazzi, Simone, Berst, Frédéric, Briner, Karin, Liu, Shuang, Zécri, Frédéric J., Schreiber, Stuart L.

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Covalent Chemical 5′-Functionalization of RNA with Diazo Reagents von Gampe, Christian M., Hollis-Symynkywicz, Micah, Zécri, Frédéric

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A Phenotypic Screen Identifies Calcium Overload as a Key Mechanism of β-Cell Glucolipotoxicity von Vogel, Jennifer, Yin, Jianning, Su, Liansheng, Wang, Sharon X, Zessis, Richard, Fowler, Sena, Chiu, Chun-Hao, Wilson, Aaron C, Chen, Amy, Zecri, Frederic, Turner, Gordon, Smith, Thomas M, DeChristopher, Brian, Xing, Heming, Rothman, Deborah M, Cai, Xinming, Berdichevsky, Alina

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Horner−Emmons Synthesis with Minimal Purification Using ROMPGEL:  A Novel High-Loading Matrix for Supported Reagents von Barrett, Anthony G. M, Cramp, Susan M, Roberts, Richard S, Zecri, Frederic J

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Discovery and characterization of a selective IKZF2 glue degrader for cancer immunotherapy von Bonazzi, Simone, d’Hennezel, Eva, Beckwith, Rohan E.J., Xu, Lei, Fazal, Aleem, Magracheva, Anna, Ramesh, Radha, Cernijenko, Artiom, Antonakos, Brandon, Bhang, Hyo-eun C., Caro, Roxana García, Cobb, Jennifer S., Ornelas, Elizabeth, Ma, Xiaolei, Wartchow, Charles A., Clifton, Matthew C., Forseth, Ry R., Fortnam, Bethany Hughes, Lu, Hongbo, Csibi, Alfredo, Tullai, Jennifer, Carbonneau, Seth, Thomsen, Noel M., Larrow, Jay, Chie-Leon, Barbara, Hainzl, Dominik, Gu, Yi, Lu, Darlene, Meyer, Matthew J., Alexander, Dylan, Kinyamu-Akunda, Jacqueline, Sabatos-Peyton, Catherine A., Dales, Natalie A., Zécri, Frédéric J., Jain, Rishi K., Shulok, Janine, Wang, Y. Karen, Briner, Karin, Porter, Jeffery A., Tallarico, John A., Engelman, Jeffrey A., Dranoff, Glenn, Bradner, James E., Visser, Michael, Solomon, Jonathan M.

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A ROMPGEL-Supported N-Hydroxysuccinimide:  A Host of Acylations with Minimal Purification von Barrett, Anthony G. M, Cramp, Susan M, Roberts, Richard S, Zecri, Frederic J

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Abstract P124: JDQ443, a covalent irreversible inhibitor of KRAS G12C, exhibits a novel binding mode and demonstrates potent anti-tumor activity and favorable pharmacokinetic prope... von Brachmann, Saskia M., Weiss, Andreas, Guthy, Daniel A., Beyer, Kim, Voshol, Johannes, Maira, Michel, Prahallad, Anirudh, Porta, Diana Graus, Schnell, Christian, Ostermann, Nils, Vaupel, Andrea, Gerspacher, Marc, Leblanc, Catherine, Erdmann, Dirk, Sterker, Dario, Kerr, Grainne, Jerome, Giovannoni, Head, Victoria, Stringer, Rowan, De Kanter, Ruben, Jeff, Kearns, Roman, Danielle, Widmer, Toni, Wessels, Peter, Nunez, Eloisa Jimenez, Sedrani, Richard, Zecri, Frederic, Hofmann, Francesco, Engleman, Jeff, Lorthiois, Edwige, Cotesta, Simona

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Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors von Hoegenauer, Klemens, Soldermann, Nicolas, Zécri, Frédéric, Strang, Ross S, Graveleau, Nadege, Wolf, Romain M, Cooke, Nigel G, Smith, Alexander B, Hollingworth, Gregory J, Blanz, Joachim, Gutmann, Sascha, Rummel, Gabriele, Littlewood-Evans, Amanda, Burkhart, Christoph

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