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Mechanistic insights into a heterobifunctional degrader-induced PTPN2/N1 complex Hao, Qi; Rathinaswamy, Manoj K.; Klinge, Kelly L.; Bratkowski, Matthew; Mafi, Amirhossein; Baumgartner, Christina K.; Hamel, Keith M.; Veits, Gesine K.; Jain, Rinku; Catalano, Claudio; Fitzgerald, Mark; Hird, Alexander W.; Park, Eunice; Vora, Harit U.; Henderson, James A.; Longenecker, Kenton; Hutchins, Charles W.; Qiu, Wei; Scapin, Giovanna; Sun, Qi; Stoll, Vincent S.; Sun, Chaohong; Li, Ping; Eaton, Dan; Stokoe, David; Fisher, Stewart L.; Nasveschuk, Christopher G.; Paddock, Marcia; Kort, Michael E. 分享 收藏
Discovery of Small Molecule Interleukin 17A Inhibitors with Novel Binding Mode and Stoichiometry: Optimization of DNA-Encoded Chemical Library Hits to In Vivo Active Compounds Ramos, Ashley L.; Goedken, Eric R.; Frank, Kristine E.; Argiriadi, Maria A.; Bazzaz, Sana; Bian, Zhiguo; Brown, Jesse T. C.; Centrella, Paolo A.; Chen, Hui-Ju; Disch, Jeremy S.; Donner, Pamela L.; Duignan, David B.; Gikunju, Diana; Greszler, Stephen N.; Guie, Marie-Aude; Habeshian, Sevan; Hartl, Hajnalka E.; Hein, Christopher D.; Hutchins, Charles W.; Jetson, Rachael; Keefe, Anthony D.; Khan, Hasan; Li, Huan-Qiu; Olszewski, Allison; Ortiz Cardona, Benjamin J.; Osuma, Augustine; Panchal, Sanjay C.; Phelan, Ryan; Qiu, Wei; Shotwell, J. Brad; Shrestha, Anurupa; Srikumaran, Myron; Su, Zhi; Sun, Chaohong; Upadhyay, Anup K.; Wood, Michael D.; Wu, Haihong; Zhang, Ruijie; Zhang, Ying; Zhao, Gang; Zhu, Haizhong; Webster, Matthew P. 分享 收藏
Discovery of a Potent Chloroacetamide GPX4 Inhibitor with Bioavailability to Enable Target Engagement in Mice, a Potential Tool Compound for Inducing Ferroptosis In Vivo Randolph, John T.; O'Connor, Matthew J.; Han, Fei; Hutchins, Charles W.; Siu, Y. Amy; Cho, Min; Zheng, Yunan; Hickson, Jonathan A.; Markley, Jana L.; Manaves, Vlasios; Algire, Mikkel; Baker, Kenton A.; Chapman, Alex M.; Gopalakrishnan, Sujatha M.; Panchal, Sanjay C.; Foster-Duke, Kelly; Stolarik, DeAnne F.; Kempf-Grote, Anita; Dammeier, Darby; Fossey, Stacey; Sun, Qi; Sun, Chaohong; Shen, Yu; Dart, Michael J.; Kati, Warren M.; Lai, Albert; Firestone, Ari J.; Kort, Michael E. 分享 收藏
Identification and structure-based drug design of cell-active inhibitors of interleukin 17A at a novel C-terminal site Goedken, Eric R.; Argiriadi, Maria A.; Dietrich, Justin D.; Petros, Andrew M.; Krishnan, Navasona; Panchal, Sanjay C.; Qiu, Wei; Wu, Haihong; Zhu, Haizhong; Adams, Ashley M.; Bodelle, Pierre M.; Goguen, Lucas; Richardson, Paul L.; Slivka, Peter F.; Srikumaran, Myron; Upadhyay, Anup K.; Wu, Bainan; Judge, Russell A.; Vasudevan, Anil; Gopalakrishnan, Sujatha M.; Cox, Philip B.; Stoll, Vincent S.; Sun, Chaohong 分享 收藏
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The HPK1 Inhibitor A-745 Verifies the Potential of Modulating T Cell Kinase Signaling for Immunotherapy Malchow, Sven; Korepanova, Alla; Panchal, Sanjay C.; McClure, Ryan A.; Longenecker, Kenton L.; Qiu, Wei; Zhao, Hongyu; Cheng, Min; Guo, Jun; Klinge, Kelly L.; Trusk, Patricia; Pratt, Steven D.; Li, Tao; Kurnick, Matthew D.; Duan, Lishu; Shoemaker, Alex R.; Gopalakrishnan, Sujatha M.; Warder, Scott E.; Shotwell, J. Brad; Lai, Albert; Sun, Chaohong; Osuma, Augustine T.; Pappano, William N. 分享 收藏
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Structure-Based Design of A-1293102, a Potent and Selective BCL-XL Inhibitor Tao, Zhi-Fu; Wang, Xilu; Chen, Jun; Ingram, Justin P.; Jin, Sha; Judge, Russell A.; Kovar, Peter J.; Park, Chang; Sun, Chaohong; Wakefield, Brian D.; Zhou, Li; Zhang, Haichao; Elmore, Steven W.; Phillips, Darren C.; Judd, Andrew S.; Leverson, Joel D.; Souers, Andrew J. 分享 收藏
Discovery of a Potent and Selective Covalent p300/CBP Inhibitor Mastracchio, Anthony; Lai, Chunqiu; Digiammarino, Enrico; Ready, Damien B.; Lasko, Loren M.; Bromberg, Kenneth D.; McClellan, William J.; Montgomery, Debra; Manaves, Vlasios; Shaw, Bailin; Algire, Mikkel; Patterson, Melanie J.; Sun, Chaohong C.; Rosenberg, Saul; Lai, Albert; Michaelides, Michael R. 分享 收藏
Development of Orally Efficacious Allosteric Inhibitors of TNFα via Fragment-Based Drug Design Dietrich, Justin D.; Longenecker, Kenton L.; Wilson, Noel S.; Goess, Christian; Panchal, Sanjay C.; Swann, Steven L.; Petros, Andrew M.; Hobson, Adrian D.; Ihle, David; Song, Danying; Richardson, Paul; Comess, Kenneth M.; Cox, Philip B.; Dombrowski, Amanda; Sarris, Kathy; Donnelly-Roberts, Diana L.; Duignan, David B.; Gomtsyan, Arthur; Jung, Paul; Krueger, A. Chris; Mathieu, Suzanne; McClure, Andrea; Stoll, Vincent S.; Wetter, Jill; Mankovich, John A.; Hajduk, Philip J.; Vasudevan, Anil; Stoffel, Robert H.; Sun, Chaohong 分享 收藏
Small Molecule IL-36γ Antagonist as a Novel Therapeutic Approach for Plaque Psoriasis Todorovic, Viktor; Su, Zhi; Putman, C. Brent; Kakavas, Stevan J.; Salte, Katherine M.; McDonald, Heath A.; Wetter, Joseph B.; Paulsboe, Stephanie E.; Sun, Qi; Gerstein, Clare E.; Medina, Limary; Sielaff, Bernhard; Sadhukhan, Ramkrishna; Stockmann, Henning; Richardson, Paul L.; Qiu, Wei; Argiriadi, Maria A.; Henry, Rodger F.; Herold, J. Martin; Shotwell, J. Brad; McGaraughty, Steve P.; Honore, Prisca; Gopalakrishnan, Sujatha M.; Sun, Chaohong C.; Scott, Victoria E. 分享 收藏
Fragment-Based Discovery of an Apolipoprotein E4 (apoE4) Stabilizer Petros, Andrew M.; Korepanova, Alla; Jakob, Clarissa G.; Qiu, Wei; Panchal, Sanjay C.; Wang, Jie; Dietrich, Justin D.; Brewer, Jason T.; Pohlki, Frauke; Kling, Andreas; Wilcox, Kyle; Lakics, Viktor; Bahnassawy, Lamiaa; Reinhardt, Peter; Partha, Sarathy Karunan; Bodelle, Pierre M.; Lake, Marc; Charych, Erik I.; Stoll, Vincent S.; Sun, Chaohong; Mohler, Eric G. 分享 收藏
Novel Modes of Inhibition of Wild-Type Isocitrate Dehydrogenase 1 (IDH1): Direct Covalent Modification of His315 Jakob, Clarissa G.; Upadhyay, Anup K.; Donner, Pamela L.; Nicholl, Emily; Addo, Sadiya N.; Qiu, Wei; Ling, Christopher; Gopalakrishnan, Sujatha M.; Torrent, Maricel; Cepa, Steven P.; Shanley, Jason; Shoemaker, Alexander R.; Sun, Chaohong C.; Vasudevan, Anil; Woller, Kevin R.; Shotwell, J. Brad; Shaw, Bailin; Bian, Zhiguo; Hutti, Jessica E. 分享 收藏
Identification of small molecule IL-36 antagonists using a novel high-throughput TR-FRET binding assay and validation with cell based and biophysical assays Todorovic, V.; Putman, B.; Kakavas, S.; Limary, M.; Wang, L.; Sielaff, B.; Gerstein, C.; Shotwell, B.; Ramkrishna, S.; Sun, C.; Gopalakrishnan, S.; Scott, V. 分享 收藏
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Quantitative ligand and receptor binding studies reveal the mechanism of interleukin-36 (IL-36) pathway activation Zhou, Li; Todorovic, Viktor; Kakavas, Steve; Sielaff, Bernhard; Medina, Limary; Wang, Leyu; Sadhukhan, Ramkrishna; Stockmann, Henning; Richardson, Paul L.; DiGiammarino, Enrico; Sun, Chaohong; Scott, Victoria 分享 收藏
Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor McDaniel, Keith F.; Wang, Le; Soltwedel, Todd; Fidanze, Steven D.; Hasvold, Lisa A.; Liu, Dachun; Mantei, Robert A.; Pratt, John K.; Sheppard, George S.; Bui, Mai H.; Faivre, Emily J.; Huang, Xiaoli; Li, Leiming; Lin, Xiaoyu; Wang, Rongqi; Warder, Scott E.; Wilcox, Denise; Albert, Daniel H.; Magoc, Terrance J.; Rajaraman, Ganesh; Park, Chang H.; Hutchins, Charles W.; Shen, Jianwei J.; Edalji, Rohinton P.; Sun, Chaohong C.; Martin, Ruth; Gao, Wenqing; Wong, Shekman; Fang, Guowei; Elmore, Steven W.; Shen, Yu; Kati, Warren M. 分享 收藏
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The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex (vol 13, pg 389, 2017) He, Yupeng; Selvaraju, Sujatha; Curtin, Michael L.; Jakob, Clarissa G.; Zhu, Haizhong; Comess, Kenneth M.; Shaw, Bailin; The, Juliana; Lima-Fernandes, Evelyne; Szewczyk, Magdalena M.; Cheng, Dong; Klinge, Kelly L.; Li, Huan-Qiu; Pliushchev, Marina; Algire, Mikkel A.; Maag, David; Guo, Jun; Dietrich, Justin; Panchal, Sanjay C.; Petros, Andrew M.; Sweis, Ramzi F.; Torrent, Maricel; Bigelow, Lance J.; Senisterra, Guillermo; Li, Fengling; Kennedy, Steven; Wu, Qin; Osterling, Donald J.; Lindley, David J.; Gao, Wenqing; Galasinski, Scott; Barsyte-Lovejoy, Dalia; Vedadi, Masoud; Buchanan, Fritz G.; Arrowsmith, Cheryl H.; Chiang, Gary G.; Sun, Chaohong; Pappano, William N. 分享 收藏
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