Not logged inDiscovery of IPN60090, a Clinical Stage Selective Glutaminase-1 (GLS-1) Inhibitor with Excellent Pharmacokinetic and Physicochemical Properties
Soth, Michael J.; Le, Kang; Di Francesco, Maria Emilia; Hamilton, Matthew M.; Liu, Gang; Burke, Jason P.; Carroll, Chris L.; Kovacs, Jeffrey J.; Bardenhagen, Jennifer P.; Bristow, Christopher A.; Cardozo, Mario; Czako, Barbara; de Stanchina, Elisa; Feng, Ningping; Garvey, Jill R.; Gay, Jason P.; Do, Mary K. Geck; Greer, Jennifer; Han, Michelle; Harris, Angela; Herrera, Zachary; Huang, Sha; Giuliani, Virginia; Jiang, Yongying; Johnson, Sarah B.; Johnson, Troy A.; Kang, Zhijun; Leonard, Paul G.; Liu, Zhen; McAfoos, Timothy; Miller, Meredith; Morlacchi, Pietro; Mullinax, Robert A.; Palmer, Wylie S.; Pang, Jihai; Rogers, Norma; Rudin, Charles M.; Shepard, Hannah E.; Spencer, Nakia D.; Theroff, Jay; Wu, Qi; Xu, Alan; Yau, Ju Anne; Draetta, Giulio; Toniatti, Carlo; Heffernan, Timothy P.; Jones, Philip .png)
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SaveDiscovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an α-Hydroxy Phenylacetic Acid Pharmacophore or BioisostereRescourio, Gwenaella; Gonzalez, Ana Z.; Jabri, Salman; Belmontes, Brian; Moody, Gordon; Whittington, Doug; Huang, Xin; Caenepeel, Sean; Cardozo, Mario; Cheng, Alan C.; Chow, David; Dou, Hannah; Jones, Adrie; Kelly, Ron C.; Li, Yihong; Lizarzaburu, Mike; Lo, Mei-Chu; Mallari, Rommel; Meleza, Cesar; Rew, Yosup; Simonovich, Scott; Sun, Daqing; Turcotte, Simon; Yan, Xuelei; Wong, Simon G.; Yanez, Evelyn; Zancanella, Manuel; Houze, Jonathan; Medina, Julio C.; Hughes, Paul E.; Brown, Sean P. Share Save Genetic and pharmacologic evaluation of the ubiquitin ligase CBL-B as a small-molecule, tumor immunotherapy targetGosling, Jennifa; Rountree, Ryan; Taherbhoy, Asad; Wang, Chenbo; Cummins, Thomas; Cohen, Frederick; Tanaka, Hiroko; Weiss, Dahlia; Cardozo, Mario; Karim, Christopher; Tan, May; Juan, Joseph; Tenn-McClellan, Austin; von Soly, Szerenke Kiss; Sheung, Julie; Boyle, Kathleen; Dhamnaskar, Ketki; Kurylo, Katherine; Bruffey, Jilliane; McKinnell, Jennifer; Karr, Dane; Christianson, Andria; de Vries, Anne-Renee Van der Vuurst; Sivakumar, Pallavur; Gallop, Mark; Barsanti, Paul A.; Saha, Anjanabha; Bence, Neil F.; Zapf, Christoph W. Share Save Prospective discovery of small molecule enhancers of an E3 ligase-substrate interactionSimonetta, Kyle R.; Taygerly, Joshua; Boyle, Kathleen; Basham, Stephen E.; Padovani, Chris; Lou, Yan; Cummins, Thomas J.; Yung, Stephanie L.; von Soly, Szerenke Kiss; Kayser, Frank; Kuriyan, John; Rape, Michael; Cardozo, Mario; Gallop, Mark A.; Bence, Neil F.; Barsanti, Paul A.; Saha, Anjanabha Share Save AMG 176, a Selective MCL1 Inhibitor, Is Effective in Hematologic Cancer Models Alone and in Combination with Established TherapiesCaenepeel, Sean; Brown, Sean P.; Belmontes, Brian; Moody, Gordon; Keegan, Kathleen S.; Chui, Danny; Whittington, Douglas A.; Huang, Xin; Poppe, Leszek; Cheng, Alan C.; Cardozom, Mario; Houze, Jonathan; Li, Yunxiao; Lucas, Brian; Paras, Nick A.; Wang, Xianghong; Taygerly, Joshua P.; Vimolratana, Marc; Zancanella, Manuel; Zhu, Liusheng; Cajulis, Elaina; Osgood, Tao; Sun, Jan; Damon, Leah; Egan, Regina K.; Greninger, Patricia; McClanaghan, Joseph D.; Gong, Jianan; Moujalled, Donia; Pomilio, Giovanna; Beltran, Pedro; Benes, Cyril H.; Roberts, Andrew W.; Huang, David C.; Wei, Andrew; Canon, Jude; Coxon, Angela; Hughes, Paul E. Share Save Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridiny1)-4-quinolinecarboxamide (AM-1430)de Turiso, Felix Gonzalez-Lopez; Hao, Xiaolin; Shin, Youngsook; Bui, Minna; Campuzano, Iain D. G.; Cardozo, Mario; Dunn, Michelle C.; Duquette, Jason; Fisher, Benjamin; Foti, Robert S.; Henne, Kirk; He, Xiao; Hu, Yi-Ling; Kelly, Ron C.; Johnson, Michael G.; Lucas, Brian S.; McCarter, John; McGee, Lawrence R.; Medina, Julio C.; Metz, Daniela; Miguel, Tisha San; Mohn, Deanna; Thuy Tran; Vissinga, Christine; Wannberg, Sharon; Whittington, Douglas A.; Whoriskey, John; Yu, Gang; Zalameda, Leeanne; Zhang, Xuxia; Cushing, Timothy D. Share Save 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved PropertiesKohn, Todd J.; Du, Xiaohui; Lai, SuJen; Xiong, YuMei; Komorowski, Renee; Veniant, Murielle; Fu, Zice; Jiao, Xianyun; Pattaropong, Vatee; Chow, David; Cardozo, Mario; Jin, Lixia; Conn, Marion; DeWolf, Walter E., Jr.; Kraser, Christopher F.; Hinklin, Ronald J.; Boys, Mark L.; Medina, Julio C.; Houze, Jonathan; Dransfield, Paul; Coward, Peter Share Save Discovery, Optimization, and in Vivo Evaluation of Benzimidazole Derivatives AM-8508 and AM-9635 as Potent and Selective PI3Kδ InhibitorsShin, Youngsook; Suchomel, Julia; Cardozo, Mario; Duquette, Jason; He, Xiao; Henne, Kirk; Hu, Yi-Ling; Kelly, Ron C.; McCarter, John; McGee, Lawrence R.; Medina, Julio C.; Metz, Daniela; Miguel, Tisha San; Mohn, Deanna; Thuy Tran; Vissinga, Christine; Wong, Simon; Wannberg, Sharon; Whittington, Douglas A.; Whoriskey, John; Yu, Gang; Zalameda, Leeanne; Zhang, Xuxia; Cushing, Timothy D. Share Save Observed bromodomain flexibility reveals histone peptide- and small molecule ligand-compatible forms of ATAD2Poncet-Montange, Guillaume; Zhan, Yanai; Bardenhagen, Jennifer P.; Petrocchi, Alessia; Leo, Elisabetta; Shi, Xi; Lee, Gilbert R.; Leonard, Paul G.; Do, Mary K. Geck; Cardozo, Mario G.; Andersen, Jannik N.; Palmer, Wylie S.; Jones, Philip; Ladbury, John E. Share Save Discovery and in Vivo Evaluation of (S)-N-(1-(7-Fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and Related PI3Kδ Inhibitors for Inflammation and Autoimmune DiseaseCushing, Timothy D.; Hao, Xiaolin; Shin, Youngsook; Andrews, Kristin; Brown, Matthew; Cardozo, Mario; Chen, Yi; Duquette, Jason; Fisher, Ben; de Turiso, Felix Gonzalez-Lopez; He, Xiao; Henne, Kirk R.; Hu, Yi-Ling; Hungate, Randall; Johnson, Michael G.; Kelly, Ron C.; Lucas, Brian; McCarter, John D.; McGee, Lawrence R.; Medina, Julio C.; San Miguel, Tisha; Mohn, Deanna; Pattaropong, Vatee; Pettus, Liping H.; Reichelt, Andreas; Rzasa, Robert M.; Seganish, Jennifer; Tasker, Andrew S.; Wahl, Robert C.; Wannberg, Sharon; Whittington, Douglas A.; Whoriskey, John; Yu, Gang; Zalameda, Leeanne; Zhang, Dawei; Metz, Daniela P. Share Save Discovery and in Vivo Evaluation of Dual PI3Kβ/δ Inhibitorsde Turiso, Felix Gonzalez-Lopez; Shin, Youngsook; Brown, Matthew; Cardozo, Mario; Chen, Yi; Fong, David; Hao, Xiaolin; He, Xiao; Henne, Kirk; Hu, Yi-Ling; Johnson, Michael G.; Kohn, Todd; Lohman, Julia; McBride, Helen J.; McGee, Lawrence R.; Medina, Julio C.; Metz, Daniela; Miner, Kent; Mohn, Deanna; Pattaropong, Vatee; Seganish, Jennifer; Simard, Jillian L.; Wannberg, Sharon; Whittington, Douglas A.; Yu, Gang; Cushing, Timothy D. Share Save Structure-Guided Design, Synthesis, and Evaluation of Guanine-Derived Inhibitors of the eIF4E mRNA-Cap InteractionChen, Xiaoqi; Kopecky, David J.; Mihalic, Jeff; Jeffries, Shawn; Min, Xiaoshan; Heath, Julie; Deignan, Jeff; Lai, SuJen; Fu, Zice; Guimaraes, Cristiano; Shen, Shanling; Li, Shyun; Johnstone, Sheree; Thibault, Stephen; Xu, Haoda; Cardozo, Mario; Shen, Wang; Walker, Nigel; Kayser, Frank; Wang, Zhulun Share Save Share Save Share Save Identification and Functional Characterization of Allosteric Agonists for the G Protein-Coupled Receptor FFA2Lee, Taeweon; Schwandner, Ralf; Swaminath, Gayathri; Weiszmann, Jennifer; Cardozo, Mario; Greenberg, Joanne; Jaeckel, Peter; Ge, Hongfei; Wang, Yingcai; Jiao, Xianyun; Liu, Jiwen; Kayser, Frank; Tian, Hui; Li, Yang Share Save Share Save Share Save Evolution of the thienopyridine class of inhibitors of IκB kinase-β:: Part I:: Hit-to-lead strategiesMorwick, Tina; Berry, Angela; Brickwood, Janice; Cardozo, Mario; Catron, Katrina; DeTuri, Molly; Emeigh, Jonathan; Homon, Carol; Hrapchak, Matt; Jacober, Stephen; Jakes, Scott; Kaplita, Paul; Kelly, Terence A.; Ksiazek, John; Liuzzi, Michel; Magolda, Ronald; Mao, Can; Marshall, Daniel; McNeil, Daniel; Prokopowicz, Anthony, III; Sarko, Christopher; Scouten, Erika; Sledziona, Cynthia; Sun, Sanxing; Watrous, Jane; Wu, Jiang Ping; Cywin, Charles L. Share Save NOVEL NONNUCLEOSIDE INHIBITORS OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 REVERSE-TRANSCRIPTASE .5. 4-SUBSTITUTED AND 2,4-DISUBSTITUTED ANALOGS OF NEVIRAPINEKELLY, TA; PROUDFOOT, JR; MCNEIL, DW; PATEL, UR; DAVID, E; HARGRAVE, KD; GROB, PM; CARDOZO, M; AGARWAL, A; ADAMS, J Share Save NOVEL NONNUCLEOSIDE INHIBITORS OF HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1 (HIV-1) REVERSE-TRANSCRIPTASE .4. 2-SUBSTITUTED DIPYRIDODIAZEPINONES AS POTENT INHIBITORS OF BOTH WILD-TYPE AND CYSTEINE-181 HIV-1 REVERSE-TRANSCRIPTASE ENZYMESPROUDFOOT, JR; HARGRAVE, KD; KAPADIA, SR; PATEL, UR; GROZINGER, KG; MCNEIL, DW; CULLEN, E; CARDOZO, M; TONG, L; KELLY, TA; ROSE, J; DAVID, E; MAULDIN, SC; FUCHS, VU; VITOUS, J; HOERMANN, M; KLUNDER, JM; RAGHAVAN, P; SKILES, JW; MUI, P; RICHMAN, DD; SULLIVAN, JL; SHIH, CK; GROB, PM; ADAMS, J Share Save 
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