未登录 Discovery and SAR Study of Boronic Acid-Based Selective PDE3B Inhibitors from a Novel DNA-Encoded Library Rowley, Ann M.; Yao, Gang; Andrews, Logan; Bedermann, Aaron; Biddulph, Ross; Bingham, Ryan; Brady, Jennifer J.; Buxton, Rachel; Cecconie, Ted; Cooper, Rona; Csakai, Adam; Gao, Enoch N.; Grenier-Davies, Melissa C.; Lawler, Meghan; Lian, Yiqian; Macina, Justyna; Macphee, Colin; Marcaurelle, Lisa; Martin, John; McCormick, Patricia; Pindoria, Rekha; Rauch, Martin; Rocque, Warren; Shen, Yingnian; Shewchuk, Lisa M.; Squire, Michael; Stebbeds, Will; Tear, Westley; Wang, Xin; Ward, Paris; Xiao, Shouhua 分享 收藏
Discovery of Proline-Based p300/CBP Inhibitors Using DNA-Encoded Library Technology in Combination with High-Throughput Screening Tian, Xinrong; Suarez, Dominic; Thomson, Douglas; Li, William; King, Elizabeth A.; LaFrance, Louis; Boehm, Jeffrey; Barton, Linda; Di Marco, Christina; Martyr, Cuthbert; Thalji, Reema; Medina, Jesus; Knight, Steven; Heerding, Dirk; Gao, Enoch; Nartey, Eldridge; Cecconie, Ted; Nixon, Christopher; Zhang, Guofeng; Berrodin, Thomas J.; Phelps, Christopher; Patel, Amish; Bai, Xiaopeng; Lind, Ken; Prabhu, Ninad; Messer, Jeffrey; Zhu, Zhengrong; Shewchuk, Lisa; Reid, Rob; Graves, Alan P.; McHugh, Charles; Mangatt, Biju 分享 收藏
Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf Patterson, Jaclyn R.; Graves, Alan P.; Stoy, Patrick; Cheung, Mui; Desai, Tina A.; Fries, Harvey; Gatto, Gregory J., Jr.; Holt, Dennis A.; Shewchuk, Lisa; Totoritis, Rachel; Wang, Liping; Kallander, Lara S. 分享 收藏
In Vivo Half-Life Extension of BMP1/TLL Metalloproteinase Inhibitors Using Small-Molecule Human Serum Albumin Binders Vantourout, Julien C.; Mason, Andrew M.; Yuen, Josephine; Simpson, Graham L.; Evindar, Ghotas; Kuai, Letian; Hobbs, Michael; Edgar, Emma; Needle, Saul; Bai, Xiaopeng; Wilson, Steve; Scott-Stevens, Paul; Traylen, William; Lambert, Kim; Young, Neil; Bunally, Shenaz; Summerfield, Scott G.; Snell, Richard; Lad, Rakesh; Shi, Eric; Skinner, Steven; Shewchuk, Lisa; Watson, Allan J. B.; Chung, Chun-Wa; Pal, Sandeep; Holt, Dennis A.; Kallander, Lara S.; Prendergast, Joanne; Rivera, Katrina; Washburn, David G.; Harpel, Mark R.; Arico-Muendel, Christopher; Isidro-Llobet, Albert 分享 收藏
The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure Cadilla, Rodolfo; Deaton, David N.; Do, Young; Elkins, Patricia A.; Ennulat, Daniela; Guss, Jeffrey H.; Holt, Jason; Jeune, Michael R.; King, Andrew G.; Klapwijk, Jan C.; Kramer, H. Fritz; Kramer, Nicholas J.; Laffan, Susan B.; Masuria, Paresh, I; McDougal, Alan, V; Mortenson, Paul N.; Musetti, Caterina; Peckham, Gregory E.; Pietrak, Beth L.; Poole, Chuck; Price, Daniel J.; Rendina, Alan R.; Sati, Girish; Saxty, Gordon; Shearer, Barry G.; Shewchuk, Lisa M.; Sneddon, Helen F.; Stewart, Eugene L.; Stuart, J. Darren; Thomas, Dean N.; Thomson, Stephen A.; Ward, Paris; Wilson, Joseph W.; Xu, Tiahshun; Youngman, Mark A. 分享 收藏
Discovery of Pyrazolocarboxamides as Potent and Selective Receptor Interacting Protein 2 (RIP2) Kinase Inhibitors Haffner, Curt D.; Charnley, Adam K.; Aquino, Christopher J.; Casillas, Linda; Convery, Maire A.; Cox, Julie A.; Elban, Mark A.; Goodwin, Nicole C.; Gough, Peter J.; Haile, Pamela A.; Hughes, Terry V.; Knapp-Reed, Beth; Kreatsoulas, Constantine; Lakdawala, Ami S.; Li, Huijie; Lian, Yiqian; Lipshutz, David; Mehlmann, John F.; Ouellette, Michael; Romano, Joseph; Shewchuk, Lisa; Shu, Arthur; Votta, Bartholomew J.; Zhou, Huiqiang; Bertin, John; Marquis, Robert W. 分享 收藏
The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors Deaton, David N.; Do, Young; Holt, Jason; Jeune, Michael R.; Kramer, H. Fritz; Larkin, Andrew L.; Orband-Miller, Lisa A.; Peckham, Gregory E.; Poole, Chuck; Price, Daniel J.; Schaller, Lee T.; Shen, Ying; Shewchuk, Lisa M.; Stewart, Eugene L.; Stuart, J. Darren; Thomson, Stephen A.; Ward, Paris; Wilson, Joseph W.; Xu, Tianshun; Guss, Jeffrey H.; Musetti, Caterina; Rendina, Alan R.; Affleck, Karen; Anders, David; Hancock, Ashley P.; Hobbs, Heather; Hodgson, Simon T.; Hutchinson, Jonathan; Leveridge, Melanie V.; Nicholls, Harry; Smith, Ian E. D.; Somers, Don O.; Sneddon, Helen F.; Uddin, Sorif; Cleasby, Anne; Mortenson, Paul N.; Richardson, Caroline; Saxty, Gordon 分享 收藏
4,6-Diaminopyrimidines as Highly Preferred Troponin I-Interacting Kinase (TNNI3K) Inhibitors Philp, Joanne; Lawhorn, Brian G.; Graves, Alan P.; Shewchuk, Lisa; Rivera, Katrina L.; Jolivette, Larry J.; Holt, Dennis A.; Gatto, Gregory J., Jr.; Kallander, Lara S. 分享 收藏
Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines Thomson, Douglas W.; Wagner, Anne J.; Bantscheff, Marcus; Benson, R. Edward; Dittus, Lars; Duempelfeld, Birgit; Drewes, Gerard; Krause, Jana; Moore, John T.; Mueller, Katrin; Poeckel, Daniel; Rau, Christina; Salzer, Elsa; Shewchuk, Lisa; Hopf, Carsten; Emery, John G.; Muelbaier, Marcel 分享 收藏
Identification of Purines and 7-Deazapurines as Potent and Selective Type I Inhibitors of Troponin I-Interacting Kinase (TNNI3K) Lawhorn, Brian G.; Philp, Joanne; Zhao, Yongdong; Louer, Christopher; Hammond, Marlys; Cheung, Mui; Fries, Harvey; Graves, Alan P.; Shewchuk, Lisa; Wang, Liping; Cottom, Joshua E.; Qi, Hongwei; Zhao, Huizhen; Totoritis, Rachel; Zhang, Guofeng; Schwartz, Benjamin; Li, Hu; Sweitzer, Sharon; Holt, Dennis A.; Gatto, Gregory J., Jr.; Kallander, Lara S. 分享 收藏
Discovery of 4-Amino-8-quinoline Carboxamides as Novel, Submicromolar Inhibitors of NAD-Hydrolyzing Enzyme CD38 Becherer, J. David; Boros, Eric E.; Carpenter, Tiffany Y.; Cowan, David J.; Deaton, David N.; Haffner, Curt D.; Jeune, Michael R.; Kaldor, Istvan W.; Poole, J. Chuck; Preugschat, Frank; Rheault, Tara R.; Schulte, Christie A.; Shearer, Barry G.; Shearer, Todd W.; Shewchuk, Lisa M.; Smalley, Terrence L., Jr.; Stewart, Eugene L.; Stuart, J. Darren; Ulrich, John C. 分享 收藏
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Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1H-indol-5-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK) Axten, Jeffrey M.; Medina, Jesus R.; Feng, Yanhong; Shu, Arthur; Romeril, Stuart P.; Grant, Seth W.; Li, William Hoi Hong; Heerding, Dirk A.; Minthorn, Elisabeth; Mencken, Thomas; Atkins, Charity; Liu, Qi; Rabindran, Sridhar; Kumar, Rakesh; Hong, Xuan; Goetz, Aaron; Stanley, Thomas; Taylor, J. David; Sigethy, Scott D.; Tomberlin, Ginger H.; Hassell, Annie M.; Kahler, Kirsten M.; Shewchuk, Lisa M.; Gampe, Robert T. 分享 收藏
Discovery of an inhibitor of insulin-like growth factor 1 receptor activation: Implications for cellular potency and selectivity over insulin receptor 胰岛素样生长因子1受体激活抑制剂的发现: 对胰岛素受体的细胞效力和选择性的影响 Wood, Edgar R.; Shewchuk, Lisa; Hassel, Anne; Nichols, Jim; Truesdale, Anne T.; Smith, Danielle; Carter, H. Luke; Weaver, Kurt; Barrett, George; Leesnitzer, Tony; Alvarez, Emilio; Bardera, Ana Isabel; Alamillo, Amelia; Cantizani, Juan; Martin, Julio; Smith, Gary K.; Jensen, David E.; Xie, Hongbo; Mook, Robert; Kumar, Rakesh; Kuntz, Kevin 分享 收藏
6-Ethynylthieno[3,2-d]- and 6-ethynylthieno[2,3-d]pyrimidin-4-anilines as tunable covalent modifiers of ErbB kinases Wood, Edgar R.; Shewchuk, Lisa M.; Ellis, Byron; Brignola, Perry; Brashear, Ronald L.; Caferro, Thomas R.; Dickerson, Scott H.; Dickson, Hamilton D.; Donaldson, Kelly H.; Gaul, Michael; Griffin, Robert J.; Hassell, Anne M.; Keith, Barry; Mullin, Robert; Petrov, Kimberly G.; Reno, Michael J.; Rusnak, David W.; Tadepalli, Sarva M.; Ulrich, John C.; Wagner, Craig D.; Vanderwall, Dana E.; Waterson, Alex G.; Williams, Jon D.; White, Wendy L.; Uehling, David E. 分享 收藏
Impact of common epidermal growth factor receptor and HER2 variants on receptor activity and inhibition by lapatinib Gilmer, Tona M.; Cable, Louann; Alligood, Krystal; Rusnak, David; Spehar, Glenn; Gallagher, Kathleen T.; Woldu, Ermias; Carter, H. Luke; Truesdale, Anne T.; Shewchuk, Lisa; Wood, Edgar R. 分享 收藏
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A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): Relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells Wood, ER; Truesdale, AT; McDonald, OB; Yuan, D; Hassell, A; Dickerson, SH; Ellis, B; Pennisi, C; Horne, E; Lackey, K; Alligood, KJ; Rusnak, DW; Gilmer, TM; Shewchuk, L 分享 收藏
Design of potent, selective, and orally bioavailable inhibitors of cysteine protease cathepsin K Tavares, FX; Boncek, V; Deaton, DN; Hassell, AM; Long, ST; Miller, AB; Payne, AA; Miller, LR; Shewchuk, LM; Wells-Knecht, K; Willard, DH; Wright, LL; Zhou, HQ 分享 收藏
Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): Design, synthesis, enzymatic activities, and X-ray crystallographic analysis Bramson, HN; Corona, J; Davis, ST; Dickerson, SH; Edelstein, M; Frye, SV; Gampe, RT; Harris, PA; Hassell, A; Holmes, WD; Hunter, RN; Lackey, KE; Lovejoy, B; Luzzio, MJ; Montana, V; Rocque, WJ; Rusnak, D; Shewchuk, L; Veal, JM; Walker, DH; Kuyper, LF 分享 收藏
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