An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19 von Owen, Dafydd R., Allerton, Charlotte M. N., Anderson, Annaliesa S., Aschenbrenner, Lisa, Avery, Melissa, Berritt, Simon, Boras, Britton, Cardin, Rhonda D., Carlo, Anthony, Coffman, Karen J., Dantonio, Alyssa, Di, Li, Eng, Heather, Ferre, RoseAnn, Gajiwala, Ketan S., Gibson, Scott A., Greasley, Samantha E., Hurst, Brett L., Kadar, Eugene P., Kalgutkar, Amit S., Lee, Jack C., Lee, Jisun, Liu, Wei, Mason, Stephen W., Noell, Stephen, Novak, Jonathan J., Obach, R. Scott, Ogilvie, Kevin, Patel, Nandini C., Pettersson, Martin, Rai, Devendra K., Reese, Matthew R., Sammons, Matthew F., Sathish, Jean G., Singh, Ravi Shankar P., Steppan, Claire M., Stewart, Al E., Tuttle, Jamison B., Updyke, Lawrence, Verhoest, Patrick R., Wei, Liuqing, Yang, Qingyi, Zhu, Yuao

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The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies von Vangamudi, Bhavatarini, Paul, Thomas A, Shah, Parantu K, Kost-Alimova, Maria, Nottebaum, Lisa, Shi, Xi, Zhan, Yanai, Leo, Elisabetta, Mahadeshwar, Harshad S, Protopopov, Alexei, Futreal, Andrew, Tieu, Trang N, Peoples, Mike, Heffernan, Timothy P, Marszalek, Joseph R, Toniatti, Carlo, Petrocchi, Alessia, Verhelle, Dominique, Owen, Dafydd R, Draetta, Giulio, Jones, Philip, Palmer, Wylie S, Sharma, Shikhar, Andersen, Jannik N

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PFI-1, a Highly Selective Protein Interaction Inhibitor, Targeting BET Bromodomains von PICAUD, Sarah, DA COSTA, David, BRADNER, James E, TANIERE, Philippe, O'SULLIVAN, Brendan, MÜLLER, Susanne, SCHWALLER, Juerg, STANKOVIC, Tatjana, KNAPP, Stefan, THANASOPOULOU, Angeliki, FILIPPAKOPOULOS, Panagis, FISH, Paul V, PHILPOTT, Martin, FEDOROV, Oleg, BRENNAN, Paul, BUNNAGE, Mark E, OWEN, Dafydd R

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SETD7 Controls Intestinal Regeneration and Tumorigenesis by Regulating Wnt/β-Catenin and Hippo/YAP Signaling von Oudhoff, Menno J., Braam, Mitchell J.S., Freeman, Spencer A., Wong, Denise, Rattray, David G., Wang, Jia, Antignano, Frann, Snyder, Kimberly, Refaeli, Ido, Hughes, Michael R., McNagny, Kelly M., Gold, Michael R., Arrowsmith, Cheryl H., Sato, Toshiro, Rossi, Fabio M.V., Tatlock, John H., Owen, Dafydd R., Brown, Peter J., Zaph, Colby

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Rapid assessment of a novel series of selective CB2 agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis von Ryckmans, Thomas, Edwards, Martin P., Horne, Val A., Correia, Ana Monica, Owen, Dafydd R., Thompson, Lisa R., Tran, Isabelle, Tutt, Michelle F., Young, Tim

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Discovery of High-Affinity Small-Molecule Binders of the Epigenetic Reader YEATS4 von Londregan, Allyn T., Aitmakhanova, Karlygash, Bennett, James, Byrnes, Laura J., Canterbury, Daniel P., Cheng, Xiayun, Christott, Thomas, Clemens, Jennifer, Coffey, Steven B., Dias, João 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., Sáez, Laura Díaz, Stock, Ingrid A., Thuma, Benjamin A., Tsai, Andy, Varghese, Alison E.

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Identification of a Chemical Probe for Bromo and Extra C‑Terminal Bromodomain Inhibition through Optimization of a Fragment-Derived Hit von Fish, Paul V, Filippakopoulos, Panagis, Bish, Gerwyn, Brennan, Paul E, Bunnage, Mark E, Cook, Andrew S, Federov, Oleg, Gerstenberger, Brian S, Jones, Hannah, Knapp, Stefan, Marsden, Brian, Nocka, Karl, Owen, Dafydd R, Philpott, Martin, Picaud, Sarah, Primiano, Michael J, Ralph, Michael J, Sciammetta, Nunzio, Trzupek, John D

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Structure and Inhibitor Binding Characterization of Oncogenic MLLT1 Mutants von Ni, Xiaomin, Londregan, Allyn T, Owen, Dafydd R, Knapp, Stefan, Chaikuad, Apirat

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A data science roadmap for open science organizations engaged in early-stage drug discovery von Edfeldt, Kristina, Edwards, Aled M., Engkvist, Ola, Günther, Judith, Hartley, Matthew, Hulcoop, David G., Leach, Andrew R., Marsden, Brian D., Menge, Amelie, Misquitta, Leonie, Müller, Susanne, Owen, Dafydd R., Schütt, Kristof T., Skelton, Nicholas, Steffen, Andreas, Tropsha, Alexander, Vernet, Erik, Wang, Yanli, Wellnitz, James, Willson, Timothy M., Clevert, Djork-Arné, Haibe-Kains, Benjamin, Schiavone, Lovisa Holmberg, Schapira, Matthieu

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Lysine Methyltransferase SETD7 (SET7/9) Regulates ROS Signaling through mitochondria and NFE2L2/ARE pathway von He, Shuying, Owen, Dafydd R., Jelinsky, Scott A., Lin, Lih-Ling

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Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases von Gerstenberger, Brian S, Ambler, Catherine, Arnold, Eric P, Banker, Mary-Ellen, Brown, Matthew F, Clark, James D, Dermenci, Alpay, Dowty, Martin E, Fensome, Andrew, Fish, Susan, Hayward, Matthew M, Hegen, Martin, Hollingshead, Brett D, Knafels, John D, Lin, David W, Lin, Tsung H, Owen, Dafydd R, Saiah, Eddine, Sharma, Raman, Vajdos, Felix F, Xing, Li, Yang, Xiaojing, Yang, Xin, Wright, Stephen W

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The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification von Wells, Carrow I., Al-Ali, Hassan, Andrews, David M., Asquith, Christopher R. M., Axtman, Alison D., Dikic, Ivan, Ebner, Daniel, Ettmayer, Peter, Fischer, Christian, Frederiksen, Mathias, Futrell, Robert E., Gray, Nathanael S., Hatch, Stephanie B., Knapp, Stefan, Luecking, Ulrich, Michaelides, Michael, Mills, Caitlin E., Mueller, Susanne, Owen, Dafydd, Picado, Alfredo, Saikatendu, Kumar S., Schroeder, Martin, Stolz, Alexandra, Tellechea, Mariana, Turunen, Brandon J., Vilar, Santiago, Wang, Jinhua, Zuercher, William J., Willson, Timothy M., Drewry, David H.

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Recent Advances in the Medicinal Chemistry of the Metabotropic Glutamate Receptor 1 (mGlu1) von Owen, Dafydd R

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Design and Identification of a Novel, Functionally Subtype Selective GABA A Positive Allosteric Modulator (PF-06372865) von Owen, Robert M, Blakemore, David, Cao, Lishuang, Flanagan, Neil, Fish, Rebecca, Gibson, Karl R, Gurrell, Rachel, Huh, Chan Woo, Kammonen, Juha, Mortimer-Cassen, Elisabeth, Nickolls, Sarah A, Omoto, Kiyoyuki, Owen, Dafydd, Pike, Andy, Pryde, David C, Reynolds, David S, Roeloffs, Rosemarie, Rose, Colin, Stead, Clara, Takeuchi, Mifune, Warmus, Joseph S, Watson, Christine

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Enantioselective Catalytic Intramolecular Cyclopropanation using Modified Cinchona Alkaloid Organocatalysts von Johansson, Carin C. C., Bremeyer, Nadine, Ley, Steven V., Owen, Dafydd R., Smith, Stephen C., Gaunt, Matthew J.

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Discovery of PFI-6, a small-molecule chemical probe for the YEATS domain of MLLT1 and MLLT3 von Raux, Brigitt, Buchan, Karly A., Bennett, James, Christott, Thomas, Dowling, Matthew S., Farnie, Gillian, Fedorov, Oleg, Gamble, Vicki, Gileadi, Carina, Giroud, Charline, Huber, Kilian V.M., Korczynska, Magdalena, Limberakis, Chris, Narayanan, Arjun, Owen, Dafydd R., Sáez, Laura Díaz, Stock, Ingrid A., Londregan, Allyn T.

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A chemical probe to modulate human GID4 Pro/N-degron interactions von Owens, Dominic D. G., Maitland, Matthew E. R., Khalili Yazdi, Aliakbar, Song, Xiaosheng, Reber, Viviane, Schwalm, Martin P., Machado, Raquel A. C., Bauer, Nicolas, Wang, Xu, Szewczyk, Magdalena M., Dong, Cheng, Dong, Aiping, Loppnau, Peter, Calabrese, Matthew F., Dowling, Matthew S., Lee, Jisun, Montgomery, Justin I., O’Connell, Thomas N., Subramanyam, Chakrapani, Wang, Feng, Adamson, Ella C., Schapira, Matthieu, Gstaiger, Matthias, Knapp, Stefan, Vedadi, Masoud, Min, Jinrong, Lajoie, Gilles A., Barsyte-Lovejoy, Dalia, Owen, Dafydd R., Schild-Poulter, Caroline, Arrowsmith, Cheryl H.

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Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies von Igoe, Niall, Bayle, Elliott D, Fedorov, Oleg, Tallant, Cynthia, Savitsky, Pavel, Rogers, Catherine, Owen, Dafydd R, Deb, Gauri, Somervaille, Tim C. P, Andrews, David M, Jones, Neil, Cheasty, Anne, Ryder, Hamish, Brennan, Paul E, Müller, Susanne, Knapp, Stefan, Fish, Paul V

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Choosing your druggability battle von Owen, Dafydd

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Selective, Small-Molecule Co-Factor Binding Site Inhibition of a Su(var)3–9, Enhancer of Zeste, Trithorax Domain Containing Lysine Methyltransferase von Taylor, Alexandria P, Swewczyk, Magdalena, Kennedy, Steven, Trush, Viacheslav V, Wu, Hong, Zeng, Hong, Dong, Aiping, Ferreira de Freitas, Renato, Tatlock, John, Kumpf, Robert A, Wythes, Martin, Casimiro-Garcia, Agustin, Denny, Rajiah Aldrin, Parikh, Mihir D, Li, Fengling, Barsyte-Lovejoy, Dalia, Schapira, Matthieu, Vedadi, Masoud, Brown, Peter J, Arrowsmith, Cheryl H, Owen, Dafydd R

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