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Covalent Inhibitors of S100A4 Block the Formation of a Pro-Metastasis Non-Muscle Myosin 2A Complex Giroud, Charline; Szommer, Tamas; Coxon, Carmen; Monteiro, Octovia; Grimes, Thomas; Zarganes-Tzitzikas, Tryfon; Christott, Thomas; Bennett, James; Buchan, Karly; Brennan, Paul E.; Fedorov, Oleg 分享 收藏
Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist Balikci, Esra; Marques, Anne-Sophie M. C.; Bauer, Ludwig G.; Seupel, Raina; Bennett, James; Raux, Brigitt; Buchan, Karly; Simelis, Klemensas; Singh, Usha; Rogers, Catherine; Ward, Jennifer; Cheng, Carol; Szommer, Tamas; Schutzenhofer, Kira; Elkins, Jonathan M.; Sloman, David L.; Ahel, Ivan; Fedorov, Oleg; Brennan, Paul E.; Huber, Kilian V. M. 分享 收藏
Imidazo[1,2-b]pyridazines as inhibitors of DYRK kinases Henderson, Scott H.; Sorrell, Fiona J.; Bennett, James M.; Fedorov, Oleg; Hanley, Marcus T.; Godoi, Paulo H.; de Sousa, Roberta Ruela; Robinson, Sean; Navratilova, Iva Hopkins; Elkins, Jonathan M.; Ward, Simon E. 分享 收藏
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Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4 Londregan, Allyn T.; Aitmakhanova, Karlygash; Bennett, James; Byrnes, Laura J.; Canterbury, Daniel P.; Cheng, Xiayun; Christott, Thomas; Clemens, Jennifer; Coffey, Steven B.; Dias, Joao M.; Dowling, Matthew S.; Farnie, Gillian; Fedorov, Oleg; Fennell, Kimberly F.; Gamble, Vicki; Gileadi, Carina; Giroud, Charline; Harris, Michael R.; Hollingshead, Brett D.; Huber, Kilian; Korczynska, Magdalena; Lapham, Kimberly; Loria, Paula M.; Narayanan, Arjun; Owen, Dafydd R. .; Raux, Brigitt; Sahasrabudhe, Parag, V; Ruggeri, Roger B.; Saez, Laura Diaz; Stock, Ingrid A. .; Thuma, Benjamin A. .; Tsai, Andy; Varghese, Alison E. 分享 收藏
Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold Serafim, Ricardo A. M.; Sorrell, Fiona J.; Berger, Benedict-Tilman; Collins, Ross J.; Vasconcelos, Stanley N. S.; Massirer, Katlin B.; Knapp, Stefan; Bennett, James; Fedorov, Oleg; Patel, Hitesh; Zuercher, William J.; Elkins, Jonathan M. 分享 收藏
Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors Henderson, Scott H.; Sorrell, Fiona; Bennett, James; Fedorov, Oleg; Hanley, Marcus T.; Godoi, Paulo H.; de Sousa, Roberta Ruela; Robinson, Sean; Ashall-Kelly, Alexander; Navratilova, Iva Hopkins; Walter, Daryl S.; Elkins, Jonathan M.; Ward, Simon E. 分享 收藏
Controlling Intramolecular Interactions in the Design of Selective, High-Affinity Ligands for the CREBBP Bromodomain Brand, Michael; Clayton, James; Moroglu, Mustafa; Schiedel, Matthias; Picaud, Sarah; Bluck, Joseph P.; Skwarska, Anna; Bolland, Hannah; Chan, Anthony K. N.; Laurin, Corentine M. C.; Scorah, Amy R.; See, Larissa; Rooney, Timothy P. C.; Andrews, Katrina H.; Fedorov, Oleg; Perell, Gabriella; Kalra, Prakriti; Vinh, Kayla B.; Cortopassi, Wilian A.; Heitel, Pascal; Christensen, Kirsten E.; Cooper, Richard, I; Paton, Robert S.; Pomerantz, William C. K.; Biggin, Philip C.; Hammond, Ester M.; Filippakopoulos, Panagis; Conway, Stuart J. 分享 收藏
Fragment binding to the Nsp3 macrodomain of SARS-CoV-2 identified through crystallographic screening and computational docking Schuller, Marion; Correy, Galen J.; Gahbauer, Stefan; Fearon, Daren; Wu, Taiasean; Diaz, Roberto Efrain; Young, Iris D.; Martins, Luan Carvalho; Smith, Dominique H.; Schulze-Gahmen, Ursula; Owens, Tristan W.; Deshpande, Ishan; Merz, Gregory E.; Thwin, Aye C.; Biel, Justin T.; Peters, Jessica K.; Moritz, Michelle; Herrera, Nadia; Kratochvil, Huong T.; Aimon, Anthony; Bennett, James M.; Neto, Jose Brandao; Cohen, Aina E.; Dias, Alexandre; Douangamath, Alice; Dunnett, Louise; Fedorov, Oleg; Ferla, Matteo P.; Fuchs, Martin R.; Gorrie-Stone, Tyler J.; Holton, James M.; Johnson, Michael G.; Krojer, Tobias; Meig, George; Powell, Ailsa J.; Rack, Johannes Gregor Matthias; Rangel, Victor L.; Russi, Silvia; Skyner, Rachael E.; Smith, Clyde A.; Soares, Alexei S.; Wierman, Jennifer L.; Zhu, Kang; O'Brien, Peter; Jura, Natalia; Ashworth, Alan; Irwin, John J.; Thompson, Michael C.; Gestwicki, Jason E.; von Delft, Frank; Shoichet, Brian K.; Fraser, James S.; Ahel, Ivan 分享 收藏
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Interaction of two strongly divergent archaellins stabilizes the structure of the Halorubrum archaellum Pyatibratov, Mikhail G.; Syutkin, Alexey S.; Quax, Tessa E. F.; Melnik, Tatjana N.; Papke, R. Thane; Gogarten, Johann Peter; Kireev, Igor I.; Surin, Alexey K.; Beznosov, Sergei N.; Galeva, Anna V.; Fedorov, Oleg V. 分享 收藏
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A Chemical Probe for Tudor Domain Protein Spindlin1 to Investigate Chromatin Function Fagan, Vincent; Johansson, Catrine; Gileadi, Carina; Monteiro, Octovia; Dunford, James E.; Nibhani, Reshma; Philpott, Martin; Malzahn, Jessica; Wells, Graham; Faram, Ruth; Cribbs, Adam P.; Halidi, Nadia; Li, Fengling; Chau, Irene; Greschik, Holger; Velupillai, Srikannathasan; Allali-Hassani, Abdellah; Bennett, James; Christott, Thomas; Giroud, Charline; Lewis, Andrew M.; Huber, Kilian V. M.; Athanasou, Nick; Bountrat, Chas; Jung, Manfred; Schuele, Roland; Vedadi, Masoud; Arrowsmith, Cheryl; Xion, Yan; Jin, Jian; Fedorov, Oleg; Farnie, Gillian; Brennan, Paul E.; Oppermann, Udo 分享 收藏
C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays Le Bihan, Yann-Vai; Lanigan, Rachel M.; Atrash, Butrus; McLaughlin, Mark G.; Velupillai, Srikannathasan; Malcolm, Andrew G.; England, Katherine S.; Ruda, Gian Filippo; Mok, N. Yi; Tumber, Anthony; Tomlin, Kathy; Saville, Harry; Shehu, Erald; McAndrew, Craig; Carmichael, LeAnne; Bennett, James M.; Jeganathan, Fiona; Eve, Paul; Donovan, Adam; Hayes, Angela; Wood, Francesca; Raynaud, Florence I.; Fedorov, Oleg; Brennan, Paul E.; Burke, Rosemary; van Montfort, Rob L. M.; Rossanese, Olivia W.; Blagg, Julian; Bavetsias, Vassilios 分享 收藏
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Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3 Boettcher, Jark; Dilworth, David; Reiser, Ulrich; Neumueller, Ralph A.; Schleicher, Michael; Petronczki, Mark; Zeeb, Markus; Mischerikow, Nikolai; Allali-Hassani, Abdellah; Szewczyk, Magdalena M.; Li, Fengling; Kennedy, Steven; Vedadi, Masoud; Barsyte-Lovejoy, Dalia; Brown, Peter J.; Huber, Kilian V. M.; Rogers, Catherine M.; Wells, Carrow, I; Fedorov, Oleg; Rumpel, Klaus; Zoephel, Andreas; Mayer, Moriz; Wunberg, Tobias; Boese, Dietrich; Zahn, Stephan; Arnhof, Heribert; Berger, Helmut; Reiser, Christoph; Hoermann, Alexandra; Krammer, Teresa; Corcokovic, Maja; Sharps, Bernadette; Winkler, Sandra; Haering, Daniela; Cockcroft, Xiao-Ling; Fuchs, Julian E.; Muellauer, Barbara; Weiss-Puxbaum, Alexander; Gerstberger, Thomas; Boehmelt, Guido; Vakoc, Christopher R.; Arrowsmith, Cheryl H.; Pearson, Mark; McConnell, Darryl B. 分享 收藏
Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1 (SPIN1) Xiong, Yan; Greschik, Holger; Johansson, Catrine; Seifert, Ludwig; Bacher, Johannes; Park, Kwang-su; Babault, Nicolas; Martini, Michael; Fagan, Vincent; Li, Fengling; Chau, Irene; Christott, Thomas; Dilworth, David; Barsyte-Lovejoy, Dalia; Vedadi, Masoud; Arrowsmith, Cheryl H.; Brennan, Paul; Fedorov, Oleg; Jung, Manfred; Farnie, Gillian; Liu, Jing; Oppermann, Udo; Schuele, Roland; Jin, Jian 分享 收藏
Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening Resnick, Efrat; Bradley, Anthony; Gan, Jinrui; Douangamath, Alice; Krojer, Tobias; Sethi, Ritika; Geurink, Paul P.; Aimon, Anthony; Amitai, Gabriel; Bellini, Dom; Bennett, James; Fairhead, Michael; Fedorov, Oleg; Gabizon, Ronen; Gan, Jin; Gu, Jingxu; Plotnikov, Alexander; Reznik, Nava; Ruda, Gian Filippo; Diaz-Saez, Laura; Straub, Verena M.; Szommer, Tamas; Velupillai, Srikannathasan; Zaidman, Daniel; Zhang, Yanling; Coker, Alun R.; Dowson, Christopher G.; Barr, Haim M.; Wang, Chu; Huber, Kilian V. M.; Brennan, Paul E.; Ovaa, Huib; von Delft, Frank; London, Nir 分享 收藏