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Machine Learning ADME Models in Practice: Four Guidelines from a Successful Lead Optimization Case Study Rich, Alexander S.; Chan, Yvonne H.; Birnbaum, Benjamin; Haider, Kamran; Haimson, Joshua; Hale, Michael; Han, Yongxin; Hickman, William; Hoeflich, Klaus P.; Ortwine, Daniel; Ozen, Aysegul; Belanger, David 分享 收藏
Discovery of MK-1084: An Orally Bioavailable and Low-Dose KRASG12C Inhibitor MK-1084的发现: 一种口服生物利用度和低剂量的KRASG12C抑制剂 Ma, Xiaoshen; Sloman, David L.; Duggal, Ruchia; Anderson, Kenneth D.; Ballard, Jeanine E.; Bharathan, Indu; Brynczka, Christopher; Gathiaka, Symon; Henderson, Timothy J.; Lyons, Thomas W.; Miller, Richard; Munsell, Erik V.; Orth, Peter; Otte, Ryan D.; Palani, Anandan; Rankic, Danica A.; Robinson, Michelle R.; Sather, Aaron C.; Solban, Nicolas; Song, Xuelei Sherry; Wen, Xin; Xu, Zangwei; Yang, Yi; Yang, Ruojing; Day, Phil J.; Stoeck, Alexander; Bennett, David Jonathan; Han, Yongxin 分享 收藏
The Pan-RAF-MEK Nondegrading Molecular Glue NST-628 Is a Potent and Brain-Penetrant Inhibitor of the RAS-MAPK Pathway with Activity across Diverse RAS- and RAF-Driven Cancers Ryan, Meagan B.; Quade, Bradley; Schenk, Natasha; Fang, Zhong; Zingg, Marshall; Cohen, Steven E.; Swalm, Brooke M.; Li, Chun; Ozen, Aysegul; Ye, Chaoyang; Ritorto, Maria Stella; Huang, Xin; Dar, Arvin C.; Han, Yongxin; Hoeflich, Klaus P.; Hale, Michael; Hagel, Margit 分享 收藏
NST-628 is a novel, potent, fully brain-penetrant MAPK pathway molecular glue that inhibits RAS- and RAF-driven cancers Ryan, Meagan B.; Quade, Bradley; Schenk, Natasha; Fang, Zhong; Zingg, Marshall; Cohen, Steven E.; Li, Chun; Swalm, Brooke M.; Ozen, Aysegul; Ye, Chaoyang; Ritorto, Maria Stella; Huang, Xin; Dar, Arvin C.; Han, Yongxin; Hale, Michael; Hagel, Margit; Hoeflich, Klaus P. 分享 收藏
NST-628 is a potent, best-in-class MAPK pathway molecular glue that inhibits RAS- and RAF-driven cancers Ryan, Meagan B.; Schenk, Natasha; Zingg, Marshall; Koehler, Matthew; Sealm, Brooke; Quade, Bradley; Ye, Chaoyang; Dar, Arvin C.; Han, Yongxin; Hoeflich, Klaus P.; Hale, Michael R.; Hagel, Margit 分享 收藏
Discovery of MK-1084, a low dose selective clinical stage KRAS G12C inhibitor Maddess, Matthew L.; Sloman, David L.; Ma, Xiaoshen; Palani, Anandan; Stoeck, Alexander; Sather, Aaron C.; Solban, Nicolas; Duggal, Ruchia; Ballard, Jeanine; Munsell, Erik V.; Chen, Lin-Chi; Han, Yongxin; Miller, Richard; Gathiaka, Symon; Brynczka, Christopher; Li, Hongming; Yang, Ruojing; Brynczka, Christopher; Day, Phil 分享 收藏
NST-628 is a novel molecular glue that inhibits signaling and pathway reactivation in oncogenic RAS-MAPK cancers Quade, Bradley; Ryan, Meagan; Swalm, Brooke; Cohen, Steven; Fang, Zhong; Ozen, Aysegul; Huang, Xin; Dar, Arvin C.; Han, Yongxin; Hoeflich, Klaus P.; Hagel, Margit; Hale, Michael 分享 收藏
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Discovery of MK-8768, a Potent and Selective mGluR2 Negative Allosteric Modulator Rudd, Michael T.; Manley, Peter J.; Hanney, Barbara; Meng, Zhaoyang; Shu, Youheng; de Leon, Pablo; Frie, Jessica L.; Han, Yongxin; Wai, Jenny Miu-Chun; Yang, Zhi-Qiang; Perkins, James J.; Hurzy, Danielle M.; Manikowski, Jesse J.; Zhu, Hong; Bungard, Christopher J.; Converso, Antonella; Meissner, Robert S.; Cosden, Mali L.; Hayashi, Ikuo; Ma, Lei; O'Brien, Julie; Uebele, Victor N.; Schachter, Joel B.; Bhandari, Neetesh; Ward, Gwendolyn J.; Fillgrove, Kerry L.; Lu, Bing; Liang, Yuexia; Dubost, David C.; Puri, Vanita; Eddins, Donnie M.; Vardigan, Joshua D.; Drolet, Robert E.; Kern, Jonathan T.; Uslaner, Jason M. 分享 收藏
Oxetane Promise Delivered: Discovery of Long-Acting IDO1Inhibitors Suitable for Q3W Oral or Parenteral Dosing Li, Derun; Sloman, David L.; Achab, Abdelghani; Zhou, Hua; McGowan, Meredeth A.; White, Catherine; Gibeau, Craig; Zhang, Hongjun; Pu, Qinglin; Bharathan, Indu; Hopkins, Brett; Liu, Kun; Ferguson, Heidi; Fradera, Xavier; Lesburg, Charles A.; Martinot, Theodore A.; Qi, Ji; Song, Zhiguo J.; Yin, Jingjun; Zhang, Huangguang; Song, Licheng; Wan, Baoqiang; DAddio, Suzanne; Solban, Nicolas; Miller, J. Richard; Zamlynny, Beata; Bass, Alan; Freeland, Elizabeth; Ykoruk, Bridget; Hilliard, Catherine; Ferraro, Jude; Zhai, Jin; Knemeyer, Ian; Otte, Karin M.; Vincent, Stella; Sciammetta, Nunzio; Pasternak, Alexander; Bennett, David Jonathan; Han, Yongxin 分享 收藏
Utilization of Metabolite Identification and Structural Data to Guide Design of Low-Dose IDO1 Inhibitors Hopkins, Brett; Zhang, Hongjun; Bharathan, Indu; Li, Derun; Pu, Qinglin; Zhou, Hua; Martinot, Theodore A.; Fradera, Xavier; Lammens, Alfred; Lesburg, Charles A.; Cohen, Ryan D.; Ballard, Jeanine; Knemeyer, Ian; Otte, Karin; Vincent, Stella; Miller, J. Richard; Solban, Nicolas; Cheng, Mangeng; Geda, Prasanthi; Smotrov, Nadya; Song, Xuelei; Bennett, David Jonathan; Han, Yongxin 分享 收藏
Combination of EP4 antagonist MF-766 and anti-PD-1 promotes anti-tumor efficacy by modulating both lymphocytes and myeloid cells Wang, Yun; Cui, Long; Georgiev, Peter; Singh, Latika; Zheng, Yanyan; Yu, Ying; Grein, Jeff; Zhang, Chunsheng; Muise, Eric S.; Sloman, David L.; Ferguson, Heidi; Yu, Hongshi; Pierre, Cristina St.; Dakle, Pranal J.; Pucci, Vincenzo; Baker, James; Loboda, Andrey; Linn, Doug; Brynczka, Christopher; Wilson, Doug; Haines, Brian B.; Long, Brian; Wnek, Richard; Sadekova, Svetlana; Rosenzweig, Michael; Haidle, Andrew; Han, Yongxin; Ranganath, Sheila H. 分享 收藏
Carbamate and N-Pyrimidine Mitigate Amide Hydrolysis: Structure-Based Drug Design of Tetrahydroquinoline IDO1 Inhibitors Li, Derun; Deng, Yongqi; Achab, Abdelghani; Bharathan, Indu; Hopkins, Brett Andrew; Yu, Wensheng; Zhang, Hongjun; Sanyal, Sulagna; Pu, Qinglin; Zhou, Hua; Liu, Kun; Lim, Jongwon; Fradera, Xavier; Lesburg, Charles A.; Lammens, Alfred; Martinot, Theodore A.; Cohen, Ryan D.; Doty, Amy C.; Ferguson, Heidi; Nickbarg, Elliott B.; Cheng, Mangeng; Spacciapoli, Peter; Geda, Prasanthi; Song, Xuelei; Smotrov, Nadya; Abeywickrema, Pravien; Andrews, Christine; Chamberlin, Chad; Mabrouk, Omar; Curran, Patrick; Richards, Matthew; Saradjian, Peter; Miller, J. Richard; Knemeyer, Ian; Otte, Karin M.; Vincent, Stella; Sciammetta, Nunzio; Pasternak, Alexander; Bennett, David Jonathan; Han, Yongxin 分享 收藏
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Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors 发现有效且可口服的双环 [1.1.1] 戊烷衍生的Indoleamine-2，3-双加氧酶1 (IDO1) 抑制剂 Pu, Qinglin; Zhang, Hongjun; Guo, Liangqin; Cheng, Mangeng; Doty, Amy C.; Ferguson, Heidi; Fradera, Xavier; Lesburg, Charles A.; McGowan, Meredeth A.; Miller, J. Richard; Geda, Prasanthi; Song, Xuelei; Otte, Karin; Sciammetta, Nunzio; Solban, Nicolas; Yu, Wensheng; Sloman, David L.; Zhou, Hua; Lammens, Alfred; Neumann, Lars; Bennett, David Jonathan; Pasternak, Alexander; Han, Yongxin 分享 收藏
Strategic Incorporation of Polarity in Heme-Displacing Inhibitors of Indoleamine-2,3-dioxygenase-1 (IDO1) 在Indoleamine-2，3-双加氧酶-1 (IDO1) 的血红素置换抑制剂中战略性地掺入极性 White, Catherine; McGowan, Meredeth A.; Zhou, Hua; Sciammetta, Nunzio; Fradera, Xavier; Lim, Jongwon; Joshi, Elizabeth M.; Andrews, Christine; Nickbarg, Elliott B.; Cowley, Phillip; Trewick, Sarah; Augustin, Martin; von Koeenig, Konstanze; Lesburg, Charles A.; Otte, Karin; Knemeyer, Ian; Woo, Hyun; Yu, Wensheng; Cheng, Mangeng; Spacciapoli, Peter; Geda, Prasanthi; Song, Xuelei; Smotrov, Nadya; Curran, Patrick; Heo, Mee Ra; Abeywickrema, Pravien; Miller, J. Richard; Bennett, David Jonathan; Han, Yongxin 分享 收藏
Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy 发现用于癌症免疫疗法的氨基-环丁基芳烃衍生的Indoleamine-2，3-双加氧酶1 (IDO1) 抑制剂 Zhang, Hongjun; Liu, Kun; Pu, Qinglin; Achab, Abdelghani; Ardolino, Michael J.; Cheng, Mangeng; Deng, Yongqi; Doty, Amy C.; Ferguson, Heidi; Fradera, Xavier; Knemeyer, Ian; Kurukulasuriya, Ravi; Lam, Yu-hong; Lesburg, Charles A.; Martinot, Theodore A.; McGowan, Meredeth A.; Miller, J. Richard; Otte, Karin; Biju, Purakattle J.; Sciammetta, Nunzio; Solban, Nicolas; Yu, Wensheng; Zhou, Hua; Wang, Xiao; Bennett, David Jonathan; Han, Yongxin 分享 收藏
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