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Discovery of ART5537: A Potent and Selective Small-Molecule Probe for EXO1 Mann, Sam E.; Davis, Owen A.; Bomke, Jorg; Cornaciu, Irina; Elinati, Elias; Follows, Bruce; Galbiati, Alessandro; Geo, Lerin; Grande, Diego; Jorand-Lebrun, Catherine; Lademann, Claudio A.; Lefranc, Julien; Leuthner, Birgitta; Mason, Bethany; Mcwhirter, Claire L.; Musil, Djordje; Pehl, Ulrich; Petersson, Carl; Pica, Andrea; Pinto, Maria Filipa; Rajendra, Eeson; Rakers, Christin; Rego, Ana Toste; Robinson, Helen M. R.; Schwarz, Daniel; Smith, Graeme C. M.; Sorrell, Fiona J.; Zenke, Frank T.; Heald, Robert A.; Burgdorf, Lars T. 分享 收藏
Phenotypic Hit Identification and Optimization of Novel Pan-TEAD and Subtype-Selective Inhibitors 表型筛选识别和优化新型泛TEAD及亚型选择性抑制剂 Heinrich, Timo; Gambardella, Alessia; Schwarz, Daniel; Petersson, Carl; Gunera, Jakub; Garg, Sakshi; Schneider, Richard; Keil, Marina; Grimmeisen, Lisa; Unzue Lopez, Andrea; Schilke, Heike; Weitzel, Thomas; Kolb, Christian; Diehl, Patrizia; Doerfel, Benjamin; Anlauf, Uwe; Reither, Vivian; Rettig, Corinna; Opelt, Beate; Delp, Andrea; Wildner, Nicole; Musil, Djordje; Friedrich, Erik; Burgdorf, Lars; Fuchss, Thomas; Albers, Lisa; Sousa, Pedro M. F.; Freire, Filipe; M. Bandeiras, Tiago; Wienke, Dirk 分享 收藏
MoA Studies of the TEAD P-Site Binding Ligand MSC-4106 and Its Optimization to TEAD1-Selective Amide M3686 Heinrich, Timo; Schwarz, Daniel; Petersson, Carl; Gunera, Jakub; Garg, Sakshi; Schneider, Richard; Keil, Marina; Grimmeisen, Lisa; Unzue Lopez, Andrea; Albers, Lisa; Schlesiger, Sarah; Gambardella, Alessia; Bomke, Joerg; Carswell, Emma; Schilke, Heike; Diehl, Patrizia; Doerfel, Benjamin; Musil, Djordje; Trivier, Elisabeth; Broome, Rebecca; Marshall, Sam; Balsiger, Alexander; Friedrich, Erik; Lemos, Ana R.; Santos, Sandra P.; Sousa, Pedro M. F.; Freire, Filipe; Bandeiras, Tiago M.; Bortoluzzi, Alessio; Wienke, Dirk 分享 收藏
Discovery of quinazoline HPK1 inhibitors with high cellular potency Toure, Momar; Johnson, Theresa; Li, Bin; Schmidt, Ralf; Ma, Hong; Neagu, Constantin; Lopez, Andrea Unzue; Wang, Yanping; Guler, Satenig; Xiao, YuFang; Henkes, Renate; Ho, Kevin; Zhang, Susan; Chu, Chia Lin; Gundra, Uma Mahesh; Porichis, Filippos; Li, Long; Maurer, Christine Katharina; Fang, Zhizhou; Musil, Djordje; DiPoto, Maria; Friis, Emily; Jones, Reinaldo; Jones, Christopher; Cummings, James; Chekler, Eugene; Tanzer, Eva Maria; Huck, Bayard; Sherer, Brian 分享 收藏
Discovery of Cycloalkyl[c]thiophenes as Novel Scaffolds for Hypoxia-Inducible Factor-2α Inhibitors Buchstaller, Hans-Peter; Sala-Hojman, Ada; Leiendecker, Matthias; Albers, Joachim; Anlauf, Uwe; Berges, Nina; Dong, Liming; Fuchss, Thomas; Germann, Martina; Knehans, Tim; Krier, Mireille; Lecomte, Marc; Mueller, Daniel; Mueller, Sandra R. R.; Leuthner, Birgitta; Lindemann, Ralph; Musil, Djordje; Nowak, Mateusz; Reither, Vivian; Rettig, Corinna; Schindler, Christina E. M.; Pakulska, Urszula; Spuck, Dieter; Wegener, Ansgar; Zarebski, Adrian 分享 收藏
Selective Wee1 Inhibitors Led to Antitumor Activity In Vitro and Correlated with Myelosuppression 选择性Wee1抑制剂导致体外抗肿瘤活性并与骨髓抑制相关 Guler, Satenig; DiPoto, Maria C.; Crespo, Alejandro; Caldwell, Richard; Doerfel, Benjamin; Grossmann, Nina; Ho, Kevin; Huck, Bayard; Jones, Christopher C., V; Lan, Ruoxi; Musil, Djordje; Potnick, Justin; Schilke, Heike; Sherer, Brian; Simon, Stephanie; Sirrenberg, Christian; Zhang, Zhuo; Liu-Bujalski, Lesley 分享 收藏
R399E, A Mutated Form of Growth and Differentiation Factor 5, for Disease Modification of Osteoarthritis Gigout, Anne; Werkmann, Daniela; Menges, Stephanie; Brenneis, Christian; Henson, Frances; Cowan, Kyra J.; Musil, Djordje; Thudium, Christian S.; Guehring, Hans; Michaelis, Martin; Kleinschmidt-Doerr, Kerstin 分享 收藏
Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106 Heinrich, Timo; Peterson, Carl; Schneider, Richard; Garg, Sakshi; Schwarz, Daniel; Gunera, Jakub; Seshire, Anita; Koetzner, Lisa; Schlesiger, Sarah; Musil, Djordje; Schilke, Heike; Doerfel, Benjamin; Diehl, Patrizia; Boepple, Pia; Lemos, Ana R.; Sousa, Pedro M. F.; Freire, Filipe; Bandeiras, Tiago M.; Carswell, Emma; Pearson, Nicholas; Sirohi, Sameer; Hooker, Mollie; Trivier, Elisabeth; Broome, Rebecca; Balsiger, Alexander; Crowden, Abigail; Dillon, Christian; Wienke, Dirk 分享 收藏
Optimization of a Screening Hit toward M2912, an Oral Tankyrase Inhibitor with Antitumor Activity in Colorectal Cancer Models Buchstaller, Hans-Peter; Anlauf, Uwe; Dorsch, Dieter; Kogler, Sarah; Kuhn, Daniel; Lehmann, Martin; Leuthner, Birgitta; Lodholz, Sara; Musil, Djordje; Radtki, Daniela; Rettig, Corinna; Ritzert, Claudio; Rohdich, Felix; Schneider, Richard; Wegener, Ansgar; Weigt, Stefan; Wilkinson, Kai; Esdar, Christina 分享 收藏
Structure-Based Optimization and Discovery of M3258, a Specific Inhibitor of the Immunoproteasome Subunit LMP7 (β5i) Klein, Markus; Busch, Michael; Friese-Hamim, Manja; Crosignani, Stefano; Fuchss, Thomas; Musil, Djordje; Rohdich, Felix; Sanderson, Michael P.; Seenisamy, Jeyaprakashnarayanan; Walter-Bausch, Gina; Zanelli, Ugo; Hewitt, Philip; Esdar, Christina; Schadt, Oliver 分享 收藏
M3258 Is a Selective Inhibitor of the Immunoproteasome Subunit LMP7 (β5i) Delivering Efficacy in Multiple Myeloma Models Sanderson, Michael P.; Friese-Hamim, Manja; Walter-Bausch, Gina; Busch, Michael; Gaus, Stefanie; Musil, Djordje; Rohdich, Felix; Zanelli, Ugo; Downey-Kopyscinski, Sondra L.; Mitsiades, Constantine S.; Schadt, Oliver; Klein, Markus; Esdar, Christina 分享 收藏
Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2 Berger, Benedict-Tilman; Amaral, Marta; Kokh, Daria B.; Nunes-Alves, Ariane; Musil, Djordje; Heinrich, Timo; Schroeder, Martin; Neil, Rebecca; Wang, Jing; Navratilova, Iva; Bomke, Joerg; Elkins, Jonathan M.; Mueller, Susanne; Frech, Matthias; Wade, Rebecca C.; Knapp, Stefan 分享 收藏
Discovery of M5049: A Novel Selective Toll-Like Receptor 7/8 Inhibitor for Treatment of Autoimmunitys Vlach, Jaromir; Bender, Andrew T.; Przetak, Melinda; Pereira, Albertina; Deshpande, Aditee; Johnson, Theresa L.; Reissig, Sonja; Tzvetkov, Evgeni; Musil, Djordje; Morse, Noune Tahmassian; Haselmayer, Philipp; Zimmerli, Simone C.; Okitsu, Shinji L.; Walsky, Robert L.; Sherer, Brian 分享 收藏
Large-Scale Assessment of Binding Free Energy Calculations in Active Drug Discovery Projects 活性药物发现项目中结合自由能计算的大规模评估 Schindler, Christina E. M.; Baumann, Hannah; Blum, Andreas; Boese, Dietrich; Buchstaller, Hans-Peter; Burgdorf, Lars; Cappel, Daniel; Chekler, Eugene; Czodrowski, Paul; Dorsch, Dieter; Eguida, Merveille K., I; Follows, Bruce; Fuchss, Thomas; Graedler, Ulrich; Gunera, Jakub; Johnson, Theresa; Lebrun, Catherine Jorand; Karra, Srinivasa; Klein, Markus; Knehans, Tim; Koetzner, Lisa; Krier, Mireille; Leiendecker, Matthias; Leuthner, Birgitta; Li, Liwei; Mochalkin, Igor; Musil, Djordje; Neagu, Constantin; Rippmann, Friedrich; Schiemann, Kai; Schulz, Robert; Steinbrecher, Thomas; Tanzer, Eva-Maria; Lopez, Andrea Unzue; Follis, Ariele Viacava; Wegener, Ansgar; Kuhn, Daniel 分享 收藏
Identification and characterization of M6903, an antagonistic anti-TIM-3 monoclonal antibody Zhang, Dong; Jiang, Feng; Zaynagetdinov, Rinat; Huang, Hui; Sood, Vanita D.; Wang, Hong; Zhao, Xinyan; Jenkins, Molly H.; Ji, Qingyong; Wang, Youbin; Nannemann, David P.; Musil, Djordje; Wesolowski, John; Paoletti, Andrea; Bartholomew, Tin; Derner, Melissa G.; An, Qi; Iffland, Christel; Halle, Joern-Peter 分享 收藏
Identification of Methionine Aminopeptidase-2 (MetAP-2) Inhibitor M8891: A Clinical Compound for the Treatment of Cancer Heinrich, Timo; Seenisamy, Jeyaprakashnarayanan; Becker, Frank; Blume, Beatrix; Bomke, Joerg; Dietz, Melanie; Eckert, Uwe; Friese-Hamim, Manja; Gunera, Jakub; Hansen, Kerrin; Leuthner, Birgitta; Musil, Djordje; Pfalzgraf, Jens; Rohdich, Felix; Siegl, Christian; Spuck, Dieter; Wegener, Ansgar; Zenker, Frank T. 分享 收藏
Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity Buchstaller, Hans-Peter; Anlauf, Uwe; Dorsch, Dieter; Kuhn, Daniel; Lehmann, Martin; Leuthner, Birgitta; Musil, Djordje; Radtki, Daniela; Ritzert, Claudio; Rohdich, Felix; Schneider, Richard; Esdar, Christina 分享 收藏
Discovery and profiling of M3258, a potent and selective LMP7 inhibitor demonstrating high efficacy in multiple myeloma models Klein, Markus; Busch, Michael; Esdar, Christina; Friese-Hamim, Manja; Krier, Mireille; Musil, Djordje; Rohdich, Felix; Sanderson, Michael; Walter, Gina; Schadt, Oliver; Zanelli, Ugo; Ma, Jianguo 分享 收藏
First-time disclosure of M3258: A selective inhibitor of the immunoproteasome subunit LMP7 with potential for improved therapeutic utility in multiple myeloma compared to pan-proteasome inhibitors Sanderson, Michael; Busch, Michael; Esdar, Christina; Friese-Hamim, Manja; Krier, Mireille; Ma, Jianguo; Musil, Djordje; Rohdich, Felix; Sloot, Willem; Walter, Gina; Zanelli, Ugo; Schadt, Oliver; Klein, Markus 分享 收藏
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