Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1 von Schoepfer, Joseph, Jahnke, Wolfgang, Berellini, Giuliano, Buonamici, Silvia, Cotesta, Simona, Cowan-Jacob, Sandra W, Dodd, Stephanie, Drueckes, Peter, Fabbro, Doriano, Gabriel, Tobias, Groell, Jean-Marc, Grotzfeld, Robert M, Hassan, A. Quamrul, Henry, Chrystèle, Iyer, Varsha, Jones, Darryl, Lombardo, Franco, Loo, Alice, Manley, Paul W, Pellé, Xavier, Rummel, Gabriele, Salem, Bahaa, Warmuth, Markus, Wylie, Andrew A, Zoller, Thomas, Marzinzik, Andreas L, Furet, Pascal

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The allosteric inhibitor ABL001 enables dual targeting of BCR–ABL1 von Wylie, Andrew A., Schoepfer, Joseph, Jahnke, Wolfgang, Cowan-Jacob, Sandra W., Loo, Alice, Furet, Pascal, Marzinzik, Andreas L., Pelle, Xavier, Donovan, Jerry, Zhu, Wenjing, Buonamici, Silvia, Hassan, A. Quamrul, Lombardo, Franco, Iyer, Varsha, Palmer, Michael, Berellini, Giuliano, Dodd, Stephanie, Thohan, Sanjeev, Bitter, Hans, Branford, Susan, Ross, David M., Hughes, Timothy P., Petruzzelli, Lilli, Vanasse, K. Gary, Warmuth, Markus, Hofmann, Francesco, Keen, Nicholas J., Sellers, William R.

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Structural States of Hdm2 and HdmX: X‐ray Elucidation of Adaptations and Binding Interactions for Different Chemical Compound Classes von Kallen, Joerg, Izaac, Aude, Chau, Suzanne, Wirth, Emmanuelle, Schoepfer, Joseph, Mah, Robert, Schlapbach, Achim, Stutz, Stefan, Vaupel, Andrea, Guagnano, Vito, Masuya, Keiichi, Stachyra, Therese‐Marie, Salem, Bahaa, Chene, Patrick, Gessier, Francois, Holzer, Philipp, Furet, Pascal

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Combining Hit Identification Strategies: Fragment-Based and in Silico Approaches to Orally Active 2-Aminothieno[2,3-d]pyrimidine Inhibitors of the Hsp90 Molecular Chaperone von Brough, Paul A, Barril, Xavier, Borgognoni, Jenifer, Chene, Patrick, Davies, Nicholas G. M, Davis, Ben, Drysdale, Martin J, Dymock, Brian, Eccles, Suzanne A, Garcia-Echeverria, Carlos, Fromont, Christophe, Hayes, Angela, Hubbard, Roderick E, Jordan, Allan M, Jensen, Michael Rugaard, Massey, Andrew, Merrett, Angela, Padfield, Antony, Parsons, Rachel, Radimerski, Thomas, Raynaud, Florence I, Robertson, Alan, Roughley, Stephen D, Schoepfer, Joseph, Simmonite, Heather, Sharp, Swee Y, Surgenor, Allan, Valenti, Melanie, Walls, Steven, Webb, Paul, Wood, Mike, Workman, Paul, Wright, Lisa

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Discovery of a Potent and Selective Protein Kinase CK2 Inhibitor by High-Throughput Docking von Vangrevelinghe, Eric, Zimmermann, Kaspar, Schoepfer, Joseph, Portmann, Robert, Fabbro, Doriano, Furet, Pascal

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Preclinical antitumor activity of the orally available heat shock protein 90 inhibitor NVP-BEP800 von Massey, Andrew J, Schoepfer, Joseph, Brough, Paul A, Brueggen, Josef, Chène, Patrick, Drysdale, Martin J, Pfaar, Ulrike, Radimerski, Thomas, Ruetz, Stephan, Schweitzer, Alain, Wood, Mike, Garcia-Echeverria, Carlos, Jensen, Michael Rugaard

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Biochemical and three-dimensional-structural study of the specific inhibition of protein kinase CK2 by [5-oxo-5,6-dihydroindolo-(1,2-a)quinazolin-7-yl]acetic acid (IQA) von Sarno, Stefania, de Moliner, Erika, Ruzzene, Maria, Pagano, Mario A, Battistutta, Roberto, Bain, Jenny, Fabbro, Doriano, Schoepfer, Joseph, Elliott, Matthew, Furet, Pascal, Meggio, Flavio, Zanotti, Giuseppe, Pinna, Lorenzo A

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Structure-Based Design and Synthesis of 2-Benzylidene-benzofuran-3-ones as Flavopiridol Mimics von Schoepfer, Joseph, Fretz, Heinz, Chaudhuri, Bhabatosh, Muller, Lionel, Seeber, Egge, Meijer, Laurent, Lozach, Olivier, Vangrevelinghe, Eric, Furet, Pascal

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Capmatinib (INC280) Is Active Against Models of Non-Small Cell Lung Cancer and Other Cancer Types with Defined Mechanisms of MET Activation von Baltschukat, Sabrina, Engstler, Barbara Schacher, Huang, Alan, Hao, Huai-Xiang, Tam, Angela, Wang, Hui Qin, Liang, Jinsheng, DiMare, Matthew T, Bhang, Hyo-Eun Carrie, Wang, Youzhen, Furet, Pascal, Sellers, William R, Hofmann, Francesco, Schoepfer, Joseph, Tiedt, Ralph

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A kinase inhibitor which specifically targets the ABL myristate pocket (STAMP), but unlike asciminib crosses the blood–brain barrier von Manley, Paul W., Huth, Felix, Moussaoui, Saliha, Schoepfer, Joseph

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Selective GRB2 SH2 inhibitors as anti‐Ras therapy von Gay, Brigitte, Suarez, Stéphanie, Caravatti, Giorgio, Furet, Pascal, Meyer, Thomas, Schoepfer, Joseph

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Preclinical Evaluation of [11C]YC-72-AB85 for In Vivo Visualization of Heat Shock Protein 90 in Brain and Cancer with Positron Emission Tomography von Vermeulen, Koen, Cools, Romy, Briard, Emmanuelle, Auberson, Yves, Schoepfer, Joseph, Koole, Michel, Cawthorne, Christopher, Bormans, Guy

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Discovery of WRN inhibitor HRO761 with synthetic lethality in MSI cancers von Ferretti, Stephane, Hamon, Jacques, de Kanter, Ruben, Scheufler, Clemens, Andraos-Rey, Rita, Barbe, Stephanie, Bechter, Elisabeth, Blank, Jutta, Bordas, Vincent, Dammassa, Ernesta, Decker, Andrea, Di Nanni, Noemi, Dourdoigne, Marion, Gavioli, Elena, Hattenberger, Marc, Heuser, Alisa, Hemmerlin, Christelle, Hinrichs, Jürgen, Kerr, Grainne, Laborde, Laurent, Jaco, Isabel, Núñez, Eloísa Jiménez, Martus, Hans-Joerg, Quadt, Cornelia, Reschke, Markus, Romanet, Vincent, Schaeffer, Fanny, Schoepfer, Joseph, Schrapp, Maxime, Strang, Ross, Voshol, Hans, Wartmann, Markus, Welly, Sarah, Zécri, Frédéric, Hofmann, Francesco, Möbitz, Henrik, Cortés-Cros, Marta

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Structure-Based Design and Synthesis of High Affinity Tripeptide Ligands of the Grb2-SH2 Domain von Furet, Pascal, Gay, Brigitte, Caravatti, Giorgio, García-Echeverría, Carlos, Rahuel, Joseph, Schoepfer, Joseph, Fretz, Heinz

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Preclinical Evaluation of [11C]YC-72-AB85 for In Vivo Visualization of Heat Shock Protein 90 in Brain and Cancer with Positron Emission Tomography von Vermeulen, Koen, Cools, Romy, Briard, Emmanuelle, Auberson, Yves, Schoepfer, Joseph, Koole, Michel, Cawthorne, Christopher, Bormans, Guy

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Discovery of a new class of catalytic topoisomerase II inhibitors targeting the ATP-binding site by structure based design. Part I von Furet, Pascal, Schoepfer, Joseph, Radimerski, Thomas, Chène, Patrick

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Structure-Based Design, Synthesis, and X-ray Crystallography of a High-Affinity Antagonist of the Grb2-SH2 Domain Containing an Asparagine Mimetic von Furet, Pascal, García-Echeverría, Carlos, Gay, Brigitte, Schoepfer, Joseph, Zeller, Martin, Rahuel, Joseph

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A Drug Resistance Screen Using a Selective MET Inhibitor Reveals a Spectrum of Mutations That Partially Overlap with Activating Mutations Found in Cancer Patients von TIEDT, Ralph, DEGENKOLBE, Elisa, BLANK, Jutta, HAASEN, Dorothea, DRUECKES, Peter, WARTMANN, Markus, MCCARTHY, Clive, SELLERS, William R, HOFMANN, Francesco, FURET, Pascal, APPLETON, Brent A, WAGNER, Sabrina, SCHOEPFER, Joseph, BUCK, Emily, RUDDY, David A, MONAHAN, John E, JONES, Michael D

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Effect of Potent and Selective Inhibitors of the Grb2 SH2 Domain on Cell Motility von Gay, Brigitte, Suarez, Stéphanie, Weber, Christine, Rahuel, Joseph, Fabbro, Doriano, Furet, Pascal, Caravatti, Giorgio, Schoepfer, Joseph

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Structural basis for the high affinity of amino-aromatic SH2 phosphopeptide ligands von Rahuel, Joseph, Garcı́a-Echeverrı́a, Carlos, Furet, Pascal, Strauss, André, Caravatti, Giorgio, Fretz, Heinz, Schoepfer, Joseph, Gay, Brigitte

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