未登录 Discovery of (R)-8-(6-Methyl-4-oxo-1,4,5,6-tetrahydropyrrolo[3,4-b]pyrrol-2-yl)-3-(1-methylcyclopropyl)-2-((1-methylcyclopropyl)amino)quinazolin-4(3H)-one, a Potent and Selective Pim-1/2 Kinase Inhibitor for Hematological Malignancies Wang, Hui-Ling; Andrews, Kristin L.; Booker, Shon K.; Canon, Jude; Cee, Victor J.; Chavez, Frank, Jr.; Chen, Yuping; Eastwood, Heather; Guerrero, Nadia; Herberich, Brad; Hickman, Dean; Lanman, Brian A.; Laszlo, Jimmy, III; Lee, Matthew R.; Lipford, J. Russell; Mattson, Bethany; Mohr, Christopher; Yen Nguyen; Norman, Mark H.; Pettus, Liping H.; Powers, David; Reed, Anthony B.; Rex, Karen; Sastri, Christine; Tamayo, Nuria; Wang, Paul; Winston, Jeffrey T.; Wu, Bin; Wu, Qiong; Wu, Tian; Wurz, Ryan P.; Xu, Yang; Zhou, Yihong; Tasker, Andrew S. 分享 收藏
Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling (vol 24, pg 2215, 2016) Liu, Longbin; Lee, Matthew R.; Kim, Joseph L.; Whittington, Douglas A.; Bregman, Howard; Hua, Zihao; Lewis, Richard T.; Martin, Matthew W.; Nishimura, Nobuko; Potashman, Michele; Yang, Kevin; Yi, Shuyan; Vaida, Karina R.; Epstein, Linda F.; Babij, Carol; Fernando, Manory; Carnahan, Josette; Norman, Mark H. 分享 收藏
Discovery and Optimization of Quinazolinone-pyrrolopyrrolones as Potent and Orally Bioavailable Pan-Pim Kinase Inhibitors Pettus, Liping H.; Andrews, Kristin L.; Booker, Shon K.; Chen, Jie; Cee, Victor J.; Chavez, Frank, Jr.; Chen, Yuping; Eastwood, Heather; Guerrero, Nadia; Herberich, Bradley; Hickman, Dean; Lanman, Brian A.; Laszlo, Jimmy, III; Lee, Matthew R.; Lipford, J. Russell; Mattson, Bethany; Mohr, Christopher; Yen Nguyen; Norman, Mark H.; Powers, David; Reed, Anthony B.; Rex, Karen; Sastri, Christine; Tamayo, Nuria; Wang, Paul; Winston, Jeffrey T.; Wu, Bin; Wu, Tian; Wurz, Ryan P.; Xu, Yang; Zhou, Yihong; Tasker, Andrew S.; Wang, Hui-Ling 分享 收藏
Purinylpyridinylamino-based DFG-in/αC-helix-out B-Raf inhibitors: Applying mutant versus wild-type B-Raf selectivity indices for compound profiling 嘌呤基吡啶基氨基dfg-in/α c-螺旋out b-raf抑制剂: 将突变体与野生型b-raf选择性指数应用于化合物分析 Liu, Longbin; Lee, Matthew R.; Kim, Joseph L.; Whittington, Douglas A.; Bregman, Howard; Hua, Zihao; Lewis, Richard T.; Martin, Matthew W.; Nishimura, Nobuko; Potashman, Michele; Yang, Kevin; Yi, Shuyan; Vaida, Karina R.; Epstein, Linda F.; Babij, Carol; Fernando, Manory; Carnahan, Josette; Norman, Mark H. 分享 收藏
Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint Pennington, Lewis D.; Bartberger, Michael D.; Croghan, Michael D.; Andrews, Kristin L.; Ashton, Kate S.; Bourbeau, Matthew P.; Chen, Jie; Chmait, Samer; Cupples, Rod; Fotsch, Christopher; Helmering, Joan; Hong, Fang-Tsao; Hungate, Randall W.; Jordan, Steven R.; Kong, Ke; Liu, Longbin; Michelsen, Klaus; Moyer, Carolyn; Nishimura, Nobuko; Norman, Mark H.; Reichelt, Andreas; Siegmund, Aaron C.; Sivits, Glenn; Tadesse, Seifu; Tegley, Christopher M.; Van, Gwyneth; Yang, Kevin C.; Yao, Guomin; Zhang, Jiandong; Lloyd, David J.; Hale, Clarence; St Jean, David J., Jr. 分享 收藏
Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis Tamayo, Nuria A.; Norman, Mark H.; Bartberger, Michael D.; Hong, Fang-Tsao; Bo, Yunxin; Liu, Longbin; Nishimura, Nobuko; Yang, Kevin C.; Tadesse, Seifu; Fotsch, Christopher; Chen, Jie; Chmait, Samer; Cupples, Rod; Hale, Clarence; Jordan, Steven R.; Lloyd, David J.; Sivits, Glenn; Van, Gwyneth; Jean, David J. St., Jr. 分享 收藏
Discovery of 1H-Pyrazol-3(2H)-ones as Potent and Selective Inhibitors of Protein Kinase R-like Endoplasmic Reticulum Kinase (PERK) Smith, Adrian L.; Andrews, Kristin L.; Beckmann, Holger; Bellon, Steven F.; Beltran, Pedro J.; Booker, Shon; Chen, Hao; Chung, Young-Ah; D'Angelo, Noel D.; Dao, Jennifer; Dellamaggiore, Kenneth R.; Jaeckel, Peter; Kendall, Richard; Labitzke, Katja; Long, Alexander M.; Materna-Reichelt, Silvia; Mitchell, Petia; Norman, Mark H.; Powers, David; Rose, Mark; Shaffer, Paul L.; Wu, Michelle M.; Lipford, J. Russell 分享 收藏
P450-Mediated O-Demethylated Metabolite Is Responsible for Rat Hepatobiliary Toxicity of Pyridyltriazine-Containing PI3K Inhibitors Subramanian, Raju; Aidasani, Divesh; Bailey, Keith; Branstetter, Dan; Everds, Nancy; Jiang, Jian; Norman, Mark H.; Primack, Ronya; Skiles, Gary L.; Soto, Irene; Stec, Markian M.; Wagner, Mylo; Wu, Tian; Zhu, Xiaochun; Lebrec, Herve 分享 收藏
Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 4. Exploration of a Novel Binding Pocket Hong, Fang-Tsao; Norman, Mark H.; Ashton, Kate S.; Bartberger, Michael D.; Chen, Jie; Chmait, Samer; Cupples, Rod; Fotsch, Christopher; Jordan, Steven R.; Lloyd, David J.; Sivits, Glenn; Tadesse, Seifu; Hale, Clarence; St Jean, David J., Jr. 分享 收藏
Small Molecule Disruptors of the Glucokinase Glucokinase Regulatory Protein Interaction: 3. Structure Activity Relationships within the Aryl Carbinol Region of the N-Arylsulfonamido-N'-arylpiperazine Series Nishimura, Nobuko; Norman, Mark H.; Liu, Longbin; Yang, Kevin C.; Ashton, Kate S.; Bartberger, Michael D.; Chmait, Samer; Chen, Jie; Cupples, Rod; Fotsch, Christopher; Helmering, Joan; Jordan, Steven R.; Kunz, Roxanne K.; Pennington, Lewis D.; Poon, Steve F.; Siegmund, Aaron; Sivits, Glenn; Lloyd, David J.; Hale, Clarence; St Jean, David J., Jr. 分享 收藏
Optimization of Potency and Pharmacokinetic Properties of Tetrahydroisoquinoline Transient Receptor Potential Melastatin 8 (TRPM8) Antagonists Horne, Daniel B.; Tamayo, Nuria A.; Bartberger, Michael D.; Bo, Yunxin; Clarine, Jeffrey; Davis, Carl D.; Gore, Vijay K.; Kaller, Matthew R.; Lehto, Sonya G.; Ma, Vu V.; Nishimura, Nobuko; Nguyen, Thomas T.; Tang, Phi; Wang, Weiya; Youngblood, Beth D.; Zhang, Maosheng; Gavva, Narender R.; Monenschein, Holger; Norman, Mark H. 分享 收藏
Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 2. Leveraging Structure-Based Drug Design to Identify Analogues with Improved Pharmacokinetic Profiles St Jean, David J., Jr.; Ashton, Kate S.; Bartberger, Michael D.; Chen, Jie; Chmait, Samer; Cupples, Rod; Galbreath, Elizabeth; Helmering, Joan; Hong, Fang-Tsao; Jordan, Steven R.; Liu, Longbin; Kunz, Roxanne K.; Michelsen, Klaus; Nishimura, Nobuko; Pennington, Lewis D.; Poon, Steve F.; Reid, Darren; Sivits, Glenn; Stec, Markian M.; Tadesse, Seifu; Tamayo, Nuria; Van, Gwyneth; Yang, Kevin C.; Zhang, Jiandong; Norman, Mark H.; Fotsch, Christopher; Lloyd, David J.; Hale, Clarence 分享 收藏
Selective Class I Phosphoinositide 3-Kinase Inhibitors: Optimization of a Series of Pyridyltriazines Leading to the Identification of a Clinical Candidate, AMG 511 (vol 55, pg 7796, 2012) Norman, Mark H.; Andrews, Kristin L.; Bo, Yunxin Y.; Booker, Shon K.; Caenepeel, Sean; Cee, Victor J.; D'Angelo, Noel D.; Freeman, Daniel J.; Herberich, Bradley J.; Hong, Fang-Tsao; Jackson, Claire L. M.; Jiang, Jian; Lanman, Brian A.; Liu, Longbin; McCarter, John D.; Mullady, Erin L.; Nishimura, Nobuko; Pettus, Liping H.; Reed, Anthony B.; Miguel, Tisha San; Smith, Adrian L.; Stec, Markian M.; Tadesse, Seifu; Tasker, Andrew; Aidasani, Divesh; Zhu, Xiaochun; Subramanian, Raju; Tamayo, Nuria A.; Wang, Ling; Whittington, Douglas A.; Wu, Bin; Wu, Tian; Wurz, Ryan P.; Yang, Kevin; Zalameda, Leeanne; Zhang, Nancy; Hughes, Paul E. 分享 收藏
Selective Class I Phosphoinositide 3-Kinase Inhibitors: Optimization of a Series of Pyridyltriazines Leading to the Identification of a Clinical Candidate, AMG 511 Norman, Mark H.; Andrews, Kristin L.; Bo, Yunxin Y.; Booker, Shon K.; Caenepeel, Sean; Cee, Victor J.; D'Angelo, Noel D.; Freeman, Daniel J.; Herberich, Bradley J.; Hong, Fang-Tsao; Jackson, Claire L. M.; Jiang, Jian; Lanman, Brian A.; Liu, Longbin; McCarter, John D.; Mullady, Erin L.; Nishimura, Nobuko; Pettus, Liping H.; Reed, Anthony B.; Miguel, Tisha San; Smith, Adrian L.; Stec, Markian M.; Tadesse, Seifu; Tasker, Andrew; Aidasani, Divesh; Zhu, Xiaochun; Subramanian, Raju; Tamayo, Nuria A.; Wang, Ling; Whittington, Douglas A.; Wu, Bin; Wu, Tian; Wurz, Ryan P.; Yang, Kevin; Zalameda, Leeanne; Zhang, Nancy; Hughes, Paul E. 分享 收藏
Structure-Based Design of a Novel Series of Potent, Selective Inhibitors of the Class I Phosphatidylinositol 3-Kinases Smith, Adrian L.; D'Angelo, Noel D.; Bo, Yurain Y.; Booker, Shon K.; Cee, Victor J.; Herberich, Brad; Hong, Fang-Tsao; Jackson, Claire L. M.; Lanman, Brian A.; Liu, Longbin; Nishimura, Nobuko; Pettus, Liping H.; Reed, Anthony B.; Tadesse, Seifu; Tamayo, Nuria A.; Wurz, Ryan P.; Yang, Kevin; Andrews, Kristin L.; Whittington, Douglas A.; McCarter, John D.; Miguel, Tisha San; Zalameda, Leeanne; Jiang, Jian; Subramanian, Raju; Mullady, Erin L.; Caenepeel, Sean; Freeman, Daniel J.; Wang, Ling; Zhang, Nancy; Wu, Tian; Hughes, Paul E.; Norman, Mark H. 分享 收藏
AMG 511, a potent and selective class I PI3K inhibitor, demonstrates anti-tumor activity in multiple xenograft models Zhang, Nancy; Caenepeel, Sean; Wang, Ling; Norman, Mark; Kendall, Richard; Burgess, Terri; Radinsky, Robert; Hughes, Paul; Freeman, Daniel J. 分享 收藏
In vitro characterization of AMG 511, a potent and selective class I PI3K inhibitor for the treatment of cancer Caenepeel, Sean; Zhang, Nancy; Wang, Ling; Norman, Mark H.; Burgess, Terri; Radinsky, Robert; Kendall, Rick; Freeman, Daniel; Hughes, Paul E. 分享 收藏
Structure-Based Design of Novel Class II c-Met Inhibitors: 2. SAR and Kinase Selectivity Profiles of the Pyrazolone Series Liu, Longbin; Norman, Mark H.; Lee, Matthew; Xi, Ning; Siegmund, Aaron; Boezio, Alessandro A.; Booker, Shon; Choquette, Debbie; D'Angelo, Noel D.; Germain, Julie; Yang, Kevin; Yang, Yajing; Zhang, Yihong; Bellon, Steven F.; Whittington, Douglas A.; Harmange, Jean-Christophe; Dominguez, Celia; Kim, Tae-Seong; Dussault, Isabelle 分享 收藏
Structure-Based Design of Novel Class II c-Met Inhibitors: 1. Identification of Pyrazolone-Based Derivatives Norman, Mark H.; Liu, Longbin; Lee, Matthew; Xi, Ning; Fellows, Ingrid; D'Angelo, Noel D.; Dominguez, Celia; Rex, Karen; Bellon, Steven F.; Kim, Tae-Seong; Dussault, Isabelle 分享 收藏
Fused Piperidines as a Novel Class of Potent and Orally Available Transient Receptor Potential Melastatin Type 8 (TRPM8) Antagonists Tamayo, Nuria A.; Bo, Yunxin; Gore, Vijay; Ma, Vu; Nishimura, Nobuko; Tang, Phi; Deng, Hong; Klionsky, Lana; Lehto, Sonya G.; Wang, Weiya; Youngblood, Brad; Chen, Jiyun; Correll, Tiffany L.; Bartberger, Michael D.; Gavva, Narender R.; Norman, Mark H. 分享 收藏
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