未登录 The discovery of potent KAT6 inhibitors that demonstrate anti-tumor activity in preclinical models of ER plus breast cancer Palanisamy, Gopinath S.; Venkateshappa, Chandregowda; Goyal, Megha; Barrett, Susanna A.; Heam, Brian R.; Daginakatte, Girish; Aravind, A. B.; Samiulla, D. S.; Bera, Kalisankar; Sangeetha, S.; Khare, Leena; Parisian, Alison D.; Heerding, Dirk A.; Ng, Raymond A.; Harmon, Cyrus L.; Samajdar, Susanta; Ramachandra, Murali; Myles, David C. 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
Cell-Based Drug Discovery: Identification and Optimization of Small Molecules that Reduce c-MYC Protein Levels in Cells Medina, Jesus R.; Tian, Xinrong; Li, William H.; Suarez, Dominic; Mack, James F.; LaFrance, Louis; Martyr, Cuthbert; Brackley, James; Di Marco, Christina; Rivero, Ralph; Heerding, Dirk A.; McHugh, Charles; Minthorn, Elisabeth; Bhaskar, Aishwarya; Rubin, Jacob; Butticello, Michael; Carpenter, Christopher; Nartey, Eldridge N.; Berrodin, Thomas J.; Kallal, Lorena A.; Mangatt, Biju 分享 收藏
Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia Pappalardi, Melissa B.; Keenan, Kathryn; Cockerill, Mark; Kellner, Wendy A.; Stowell, Alexandra; Sherk, Christian; Wong, Kristen; Pathuri, Sarath; Briand, Jacques; Steidel, Michael; Chapman, Philip; Groy, Arthur; Wiseman, Ashley K.; McHugh, Charles F.; Campobasso, Nino; Graves, Alan P.; Fairweather, Emma; Werner, Thilo; Raoof, Ali; Butlin, Roger J.; Rueda, Lourdes; Horton, John R.; Fosbenner, David T.; Zhang, Cunyu; Handler, Jessica L.; Muliaditan, Morris; Mebrahtu, Makda; Jaworski, Jon-Paul; McNulty, Dean E.; Burt, Charlotte; Eberl, H. Christian; Taylor, Amy N.; Ho, Thau; Merrihew, Susan; Foley, Shawn W.; Rutkowska, Anna; Li, Mei; Romeril, Stuart P.; Goldberg, Kristin; Zhang, Xing; Kershaw, Christopher S.; Bantscheff, Marcus; Jurewicz, Anthony J.; Minthorn, Elisabeth; Grandi, Paola; Patel, Mehul; Benowitz, Andrew B.; Mohammad, Helai P.; Gilmartin, Aidan G.; Prinjha, Rab K.; Ogilvie, Donald; Carpenter, Christopher; Heerding, Dirk; Baylin, Stephen B.; Jones, Peter A.; Cheng, Xiaodong; King, Bryan W.; Luengo, Juan, I; Jordan, Allan M.; Waddell, Ian; Kruger, Ryan G.; McCabe, Michael T. 分享 收藏
Discovery of Isoxazole Amides as Potent and Selective SMYD3 Inhibitors Su, Dai-Shi; Qu, Junya; Schulz, Mark; Blackledge, Chuck W.; Yu, Hongyi; Zeng, Jenny; Burgess, Joelle; Reif, Alexander; Stern, Melissa; Nagarajan, Raman; Pappalardi, Melissa Baker; Wong, Kristen; Graves, Alan P.; Bonnette, William; Wang, Liping; Elkins, Patricia; Knapp-Reed, Beth; Carson, Jeffrey D.; McHugh, Charles; Mohammad, Helai; Kruger, Ryan; Luengo, Juan; Heerding, Dirk A.; Creasy, Caretha L. 分享 收藏
Discovery of small-molecule compounds targeting c-MYC using a novel cell-based screen Mangatt, Biju; Pietra, Anthony D.; Waszkiewicz, Anna; Jaworski, Jon-Paul; Ghidelli-Disse, Sonja; Berrodin, Thomas J.; Sherk, Christian S.; Meinhold, Derrick W.; Rutkowska-Klute, Anna; Sundaram, Shanker K.; Ganji, Gopinath; Halsey, Wendy S.; Livi, George P.; Li, William; Mack, James; Romeril, Stuart P.; Minthorn, Elisabeth A.; Kumar, Rakesh; Drewes, Gerard C.; Heerding, Dirk A.; Kallal, Lorena A.; Buser, Carolyn A.; Medina, Jesus R. 分享 收藏
Discovery of selective, noncovalent small molecule inhibitors of DNMT1 as an alternative to traditional DNA hypomethylating agents Pappalardi, Melissa B.; Cockerill, Mark; Handler, Jessica L.; Stowell, Alexandra; Keenan, Kathryn; Sherk, Christian S.; Minthorn, Elisabeth A.; McHugh, Charles F.; Burt, Charlotte; Wong, Kristen; Fosbenner, David T.; Patel, Mehul; Briand, Jacques; Mohammad, Helai; Rueda, Lourdes; Benowitz, Andrew; Prinjha, Rab; Heerding, Dirk; Kruger, Ryan G.; Raoof, Ali; Jordan, Allan; King, Bryan W.; McCabe, Michael T. 分享 收藏
Long-Range Inhibitor-Induced Conformational Regulation of Human IRE1α Endoribonuclease Activity Concha, Nestor O.; Smallwood, Angela; Bonnette, William; Totoritis, Rachel; Zhang, Guofeng; Federowicz, Kelly; Yang, Jingsong; Qi, Hongwei; Chen, Stephanie; Campobasso, Nino; Choudhry, Anthony E.; Shuster, Leanna E.; Evans, Karen A.; Ralph, Jeff; Sweitzer, Sharon; Heerding, Dirk A.; Buser, Carolyn A.; Su, Dai-Shi; DeYoung, M. Phillip 分享 收藏
Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction Gilmartin, Aidan G.; Faitg, Thomas H.; Richter, Mark; Groy, Arthur; Seefeld, Mark A.; Darcy, Michael G.; Peng, Xin; Federowicz, Kelly; Yang, Jingsong; Zhang, Shu-Yun; Minthorn, Elisabeth; Jaworski, Jon-Paul; Schaber, Michael; Martens, Stan; McNulty, Dean E.; Sinnamon, Robert H.; Zhang, Hong; Kirkpatrick, Robert B.; Nevins, Neysa; Cui, Guanglei; Pietrak, Beth; Diaz, Elsie; Jones, Amber; Brandt, Martin; Schwartz, Benjamin; Heerding, Dirk A.; Kumar, Rakesh 分享 收藏
Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development GSK2656157的发现: 一种用于临床前开发的优化PERK抑制剂 Axten, Jeffrey M.; Romeril, Stuart P.; Shu, Arthur; Ralph, Jeffrey; Medina, Jesus R.; Feng, Yanhong; Li, William Hoi Hong; Grant, Seth W.; Heerding, Dirk A.; Minthorn, Elisabeth; Mencken, Thomas; Gaul, Nathan; Goetz, Aaron; Stanley, Thomas; Hassell, Annie M.; Gampe, Robert T.; Atkins, Charity; Kumar, Rakesh 分享 收藏
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
Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors Medina, Jesus R.; Becker, Christopher J.; Blackledge, Charles W.; Duquenne, Celine; Feng, Yanhong; Grant, Seth W.; Heerding, Dirk; Li, William H.; Miller, William H.; Romeril, Stuart P.; Scherzer, Daryl; Shu, Arthur; Bobko, Mark A.; Chadderton, Antony R.; Dumble, Melissa; Gardiner, Christine M.; Gilbert, Seth; Liu, Qi; Rabindran, Sridhar K.; Sudakin, Valery; Xiang, Hong; Brady, Pat G.; Campobasso, Nino; Ward, Paris; Axten, Jeffrey M. 分享 收藏
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Identification of 4-(2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-{[(3S)-3-piperidinylmethyl]oxy}-1H-imidazo[4,5-c]pyridin-4-yl)-2-methyl-3-butyn-2-ol (GSK690693), a novel inhibitor of AKT kinase Heerding, Dirk A.; Rhodes, Nelson; Leber, Jack D.; Clark, Tammy J.; Keenan, Richard M.; Lafrance, Louis V.; Li, Mei; Safonov, Igor G.; Takata, Dennis T.; Venslavsky, Joseph W.; Yamashita, Dennis S.; Choudhry, Anthony E.; Copeland, Robert A.; Lai, Zhihong; Schaber, Michael D.; Tummino, Peter J.; Strum, Susan L.; Wood, Edgar R.; Duckett, Derek R.; Eberwein, Derek; Knick, Victoria B.; Lansing, Timothy J.; McConnell, Randy T.; Zhang, ShuYun; Minthorn, Elisabeth A.; Concha, Nestor O.; Warren, Gregory L.; Kumar, Rakesh 分享 收藏
Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity Rhodes, Nelson; Heerding, Dirk A.; Duckett, Derek R.; Eberwein, Derek J.; Knick, Victoria B.; Lansing, Timothy J.; McConnell, Randy T.; Gilmer, Tona M.; Zhang, Shu-Yun; Robell, Kimberly; Kahana, Jason A.; Geske, Robert S.; Kleymenova, Elena V.; Choudhry, Anthony E.; Lai, Zhihong; Leber, Jack D.; Minthornn, Elisabeth A.; Strum, Susan L.; Wood, Edgar R.; Huang, Pearl S.; Copeland, Robert A.; Kumar, Rakesh 分享 收藏
Discovery of a novel and potent class of fabI-directed antibacterial agents Payne, DJ; Miller, WH; Berry, V; Brosky, J; Burgess, WJ; Chen, E; DeWolf, WE; Fosberry, AP; Greenwood, R; Head, MS; Heerding, DA; Janson, CA; Jaworski, DD; Keller, PM; Manley, PJ; Moore, TD; Newlander, KA; Pearson, S; Polizzi, BJ; Qiu, XY; Rittenhouse, SF; Slater-Radosti, C; Salyers, KL; Seefeld, MA; Smyth, MG; Takata, DT; Uzinskas, IN; Vaidya, K; Wallis, NG; Winram, SB; Yuan, CCK; Huffman, WF 分享 收藏
Discovery of aminopyridine-based inhibitors of bacterial enoyl-ACP reductase (FabI) Miller, WH; Seefeld, MA; Newlander, KA; Uzinskas, IN; Burgess, WJ; Heerding, DA; Yuan, CCK; Head, MS; Payne, DJ; Rittenhouse, SF; Moore, TD; Pearson, SC; Berry, V; DeWolf, WE; Keller, PM; Polizzi, BJ; Qiu, XY; Janson, CA; Huffman, WF 分享 收藏
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Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic Miller, WH; Alberts, DP; Bhatnagar, PK; Bondinell, WE; Callahan, JF; Calvo, RR; Cousins, RD; Erhard, KF; Heerding, DA; Keenan, RM; Kwon, C; Manley, PJ; Newlander, KA; Ross, ST; Samanen, JM; Uzinskas, IN; Venslavsky, JW; Yuan, CCK; Haltiwanger, RC; Gowen, M; Hwang, SM; James, IE; Lark, MW; Rieman, DJ; Stroup, GB; Azzarano, LM; Salyers, KL; Smith, BR; Ward, KW; Johanson, KO; Huffman, WF 分享 收藏
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