Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRASG12C Inhibitor von Bröker, Joachim, Waterson, Alex G., Smethurst, Chris, Kessler, Dirk, Böttcher, Jark, Mayer, Moriz, Gmaschitz, Gerhard, Phan, Jason, Little, Andrew, Abbott, Jason R., Sun, Qi, Gmachl, Michael, Rudolph, Dorothea, Arnhof, Heribert, Rumpel, Klaus, Savarese, Fabio, Gerstberger, Thomas, Mischerikow, Nikolai, Treu, Matthias, Herdeis, Lorenz, Wunberg, Tobias, Gollner, Andreas, Weinstabl, Harald, Mantoulidis, Andreas, Krämer, Oliver, McConnell, Darryl B., W. Fesik, Stephen

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Tumor cell‐specific inhibition of MYC function using small molecule inhibitors of the HUWE1 ubiquitin ligase von Peter, Stefanie, Bultinck, Jennyfer, Myant, Kevin, Jaenicke, Laura A, Walz, Susanne, Müller, Judith, Gmachl, Michael, Treu, Matthias, Boehmelt, Guido, Ade, Carsten P, Schmitz, Werner, Wiegering, Armin, Otto, Christoph, Popov, Nikita, Sansom, Owen, Kraut, Norbert, Eilers, Martin

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Low-Pressure Hydrogenation of Arenecarboxylic Acids to Aryl Aldehydes von Gooßen, Lukas J., Khan, Bilal Ahmad, Fett, Thomas, Treu, Matthias

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Palladium-Catalyzed α-Arylation of Cycloalkanones with Sterically Hindered Bromoazines under Neat Conditions von Fett, Niels Thomas, Muratore, Michael E., Gmaschitz, Gerhard, Treu, Matthias

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Synthesis of (±)-6H-benzofuro[3a,3,2,ef][3]benzazepine: an unnatural analog of (−)-galanthamine von Poschalko, Alexander, Welzig, Stefan, Treu, Matthias, Nerdinger, Sven, Mereiter, Kurt, Jordis, Ulrich

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Chasing Red Herrings: Palladium Metal Salt Impurities Feigning KRAS Activity in Biochemical Assays von Gerstberger, Thomas, Berger, Helmut, Büttner, Frank H., Gmachl, Michael, Kessler, Dirk, Koegl, Manfred, Lucas, Simon, Martin, Laetitia J., Mayer, Moriz, McConnell, Darryl B., Mitzner, Sophie, Scholz, Guido, Treu, Matthias, Wolkerstorfer, Bernhard, Zahn, Stephan, Zak, Krzysztof M., Jaeger, Philipp A., Ettmayer, Peter

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Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor BI-4924 Disrupts Serine Biosynthesis von Weinstabl, Harald, Treu, Matthias, Rinnenthal, Joerg, Zahn, Stephan K, Ettmayer, Peter, Bader, Gerd, Dahmann, Georg, Kessler, Dirk, Rumpel, Klaus, Mischerikow, Nikolai, Savarese, Fabio, Gerstberger, Thomas, Mayer, Moriz, Zoephel, Andreas, Schnitzer, Renate, Sommergruber, Wolfgang, Martinelli, Paola, Arnhof, Heribert, Peric-Simov, Biljana, Hofbauer, Karin S, Garavel, Géraldine, Scherbantin, Yvonne, Mitzner, Sophie, Fett, Thomas N, Scholz, Guido, Bruchhaus, Jens, Burkard, Michelle, Kousek, Roland, Ciftci, Tuncay, Sharps, Bernadette, Schrenk, Andreas, Harrer, Christoph, Haering, Daniela, Wolkerstorfer, Bernhard, Zhang, Xuechun, Lv, Xiaobing, Du, Alicia, Li, Dongyang, Li, Yali, Quant, Jens, Pearson, Mark, McConnell, Darryl B

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Abstract 1472: Novel EGFR WT sparing, HER2 selective inhibitors for the treatment of HER2 exon 20 insertion driven tumors address a clear unmet medical need von Neumüller, Ralph A., Wilding, Birgit, Scharn, Dirk, Böse, Dietrich, Santoro, Valeria, Gerlach, Daniel, Ettmayer, Peter, Gerstberger, Thomas, Fuchs, Julian, Treu, Matthias, Zahn, Stephan, Baum, Anke, Chetta, Paolo, Pearson, Mark, McConnell, Darryl B., Kraut, Norbert, Solca, Flavio

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Fragment Optimization of Reversible Binding to the Switch II Pocket on KRAS Leads to a Potent, In Vivo Active KRAS G12C Inhibitor von Bröker, Joachim, Waterson, Alex G., Smethurst, Chris, Kessler, Dirk, Böttcher, Jark, Mayer, Moriz, Gmaschitz, Gerhard, Phan, Jason, Little, Andrew, Abbott, Jason R., Sun, Qi, Gmachl, Michael, Rudolph, Dorothea, Arnhof, Heribert, Rumpel, Klaus, Savarese, Fabio, Gerstberger, Thomas, Mischerikow, Nikolai, Treu, Matthias, Herdeis, Lorenz, Wunberg, Tobias, Gollner, Andreas, Weinstabl, Harald, Mantoulidis, Andreas, Krämer, Oliver, McConnell, Darryl B., W. Fesik, Stephen

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4a,5,9,10,11,12-Hexahydro-6H-benzo[a]cyclohepta[hi]benzofuran - Synthesis of Unnatural Galanthamine Analogs von Treu, Matthias, Jordis, Ulrich

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Abstract 1271: In vitro and in vivo characterization of BI 1823911 - a novel KRASG12C selective small molecule inhibitor von Savarese, Fabio, Gollner, Andreas, Rudolph, Dorothea, Lipp, Jesse, Popow, Johannes, Hofmann, Marco H., Arnhof, Heribert, Rinnenthal, Jörg, Trapani, Francesca, Gmachl, Michael, Gerlach, Daniel, Broeker, Joachim, Ettmayer, Peter, Mantoulidis, Andreas, Phan, Jason, Smethurst, Christian A., Treu, Matthias, Waterson, Alex G., Lu, Hengyu, Machado, Annette, Daniele, Joseph, Fesik, Stephan W., Vellano, Christopher P., Heffernan, Timothy P., Marszalek, Joseph R., McConnell, Darryl B., Petronczki, Mark, Kraut, Norbert, Waizenegger, Irene C.

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Pharmacological Profile of BI 847325, an Orally Bioavailable, ATP-Competitive Inhibitor of MEK and Aurora Kinases von Sini, Patrizia, Gürtler, Ulrich, Zahn, Stephan K, Baumann, Christoph, Rudolph, Dorothea, Baumgartinger, Rosa, Strauss, Eva, Haslinger, Christian, Tontsch-Grunt, Ulrike, Waizenegger, Irene C, Solca, Flavio, Bader, Gerd, Zoephel, Andreas, Treu, Matthias, Reiser, Ulrich, Garin-Chesa, Pilar, Boehmelt, Guido, Kraut, Norbert, Quant, Jens, Adolf, Günther R

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BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis von Sanderson, Michael P, Apgar, Joshua, Garin-Chesa, Pilar, Hofmann, Marco H, Kessler, Dirk, Quant, Jens, Savchenko, Alexander, Schaaf, Otmar, Treu, Matthias, Tye, Heather, Zahn, Stephan K, Zoephel, Andreas, Haaksma, Eric, Adolf, Günther R, Kraut, Norbert

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Synthesis of Precursors for the Oxidative Tandem Cyclization of Diphenols to Galanthamine Analogs von Treu, Matthias, Jordis, Ulrich

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Preparation of Shortened Norbelladine Analogs von Treu, Matthias, Fröhlich, Johannes, Jordis, Ulrich

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Discovery of potent and selective HER2 inhibitors with efficacy against HER2 exon 20 insertion-driven tumors, which preserve wild-type EGFR signaling von Wilding, Birgit, Scharn, Dirk, Böse, Dietrich, Baum, Anke, Santoro, Valeria, Chetta, Paolo, Schnitzer, Renate, Botesteanu, Dana A., Reiser, Christoph, Kornigg, Stefan, Knesl, Petr, Hörmann, Alexandra, Köferle, Anna, Corcokovic, Maja, Lieb, Simone, Scholz, Guido, Bruchhaus, Jens, Spina, Markus, Balla, Josef, Peric-Simov, Biljana, Zimmer, Jasmin, Mitzner, Sophie, Fett, Thomas N., Beran, Alexandra, Lamarre, Lyne, Gerstberger, Thomas, Gerlach, Daniel, Bauer, Markus, Bergner, Andreas, Schlattl, Andreas, Bader, Gerd, Treu, Matthias, Engelhardt, Harald, Zahn, Stephan, Fuchs, Julian E., Zuber, Johannes, Ettmayer, Peter, Pearson, Mark, Petronczki, Mark, Kraut, Norbert, McConnell, Darryl B., Solca, Flavio, Neumüller, Ralph A.

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Abstract A085: BI KRASmulti, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in preclinical models and validat... von Tedeschi, Antonio, Herdeis, Lorenz, Santoro, Valeria, Savarese, Fabio, Wilding, Birgit, Treu, Matthias, Fuchs, Julian, Bröker, Joachim, Wunberg, Tobias, Gmachl, Michael, Klaus, Rumpel, Schischlik, Fiorella, Lipp, Jesse, Peng, David H., Williams, Mariah, Deckard, Charles, Ramamoorthy, Vandhana, Daniele, Joseph R., Ajani, Jaffer A., Meric-Bernstam, Funda, Vellano, Christopher P., Marszalek, Joseph R., Heffernan, Timothy P., McConnell, Darryl, Pearson, Mark, Kraut, Norbert, Rudolph, Dorothea

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Abstract A092: Determinants of sensitivity to BI KRASmulti inhibitor using high-throughput in-vitro drug screens von Schischlik, Fiorella, Tedeschi, Antonio, Rudolph, Dorothea, Gerlach, Daniel, Wilding, Birgit, Treu, Matthias, Fuchs, Julian, Herdeis, Lorenz, Broeker, Joachim, Wunberg, Tobias, Boghossian, Andrew S., Rees, Matthew G., Ronan, Melissa M., Roth, Jennifer A., McConnell, Darryl, Pearson, Mark, Kraut, Norbert, Haslinger, Christian, Lipp, Jesse

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Abstract C140: BI 1810631 is a novel EGFR wild-type sparing, HER2-selective small molecule inhibitor that efficiently blocks HER2 mutant-driven lung cancer von Neumüller, Ralph A., Wilding, Birgit, Scharn, Dirk, Baum, Anke, Augsten, Martin, Waizenegger, Irene, Kohsaka, Shinji, Santoro, Valeria, Chetta, Paolo, Woelflingseder, Lydia, Popow, Johannes, Gerlach, Daniel, Ettmayer, Peter, Gerstberger, Thomas, Fuchs, Julian, Treu, Matthias, Zahn, Stephan, Pearson, Mark, Petronczki, Mark, McConnell, Darryl B., Kraut, Norbert, Solca, Flavio

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Abstract A087: BI KRASmulti, a first-in-class, orally bioavailable and direct inhibitor of diverse oncogenic KRAS variants drives tumor regression in KRAS G12V-driven preclinical m... von Peng, David H, Tedeschi, Antonio, Herdeis, Lorenz, Savarese, Fabio, Rocchetti, Francesca, Johannes, Popow, Huber, Heinrich J, Melillo, Nicola, Dickinson, Jake, Mistry, Hitesh B, Wilding, Birgit, Treu, Matthias, Fuchs, Julian, Broker, Joachim, Wunberg, Tobias, Schischlik, Fiorella, Lipp, Jesse, Ramamoorthy, Vandhana, Daniele, Joseph R, Kopetz, Scott, Kim, Michael, Gibbons, Don L, Vellano, Christopher P, Marszalek, Joseph R, Heffernan, Timothy P, McConnell, Darryl, Pearson, Mark, Kraut, Norbert, Rudolph, Dorothea

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