未登录 Discovery of [1,2,4]Triazolo[1,5-a]pyridine Derivatives as Potent and Orally Bioavailable RORγt Inverse Agonists [1,2,4] 三唑并 [1,5-a] 吡啶衍生物作为有效和口服生物可利用的ror γ t反向激动剂的发现 Nakajima, Ryota; Oono, Hiroyuki; Sugiyama, Sakae; Matsueda, Yohei; Ida, Tomohide; Kakuda, Shinji; Hirata, Jun; Baba, Atsushi; Makino, Akito; Matsuyama, Ryo; White, Ryan D.; Wurz, Ryan P.; Shin, Youngsook; Min, Xiaoshan; Guzman-Perez, Angel; Wang, Zhulun; Symons, Antony; Singh, Sanjay K.; Mothe, Srinivasa Reddy; Belyakov, Sergei; Chakrabarti, Anjan; Shuto, Satoshi 分享 收藏
Analyzing Learned Molecular Representations for Property Prediction (vol 59, pg 3370, 2019) Yang, Kevin; Swanson, Kyle; Jin, Wengong; Coley, Connor; Eiden, Philipp; Gao, Hua; Guzman-Perez, Angel; Hopper, Timothy; Kelley, Brian; Mathea, Miriam; Palmer, Andrew; Settels, Volker; Jaakkola, Tommi; Jensen, Klavs; Barzilay, Regina 分享 收藏
Analyzing Learned Molecular Representations for Property Prediction 分析学习的分子表示以进行属性预测 Yang, Kevin; Swanson, Kyle; Jin, Wengong; Coley, Connor; Eiden, Philipp; Gao, Hua; Guzman-Perez, Angel; Hopper, Timothy; Kelley, Brian; Mathea, Miriam; Palmer, Andrew; Settels, Volker; Jaakkola, Tommi; Jensen, Klavs; Barzilay, Regina 分享 收藏
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Applications of parallel synthetic lead hopping and pharmacophore-based virtual screening in the discovery of efficient glycine receptor potentiators Chakka, Nagasree; Andrews, Kristin L.; Berry, Loren M.; Bregman, Howard; Gunaydin, Hakan; Huang, Liyue; Guzman-Perez, Angel; Plant, Matthew H.; Simard, Jeffrey R.; Gingras, Jacinthe; DiMauro, Erin F. 分享 收藏
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities Weiss, Matthew M.; Dineen, Thomas A.; Marx, Isaac E.; Altmann, Steven; Boezio, Alessandro; Bregman, Howard; Chu-Moyer, Margaret; DiMauro, Erin F.; Bojic, Elma Feric; Foti, Robert S.; Gao, Hua; Graceffa, Russell; Gunaydin, Hakan; Guzman-Perez, Angel; Huang, Hongbing; Huang, Liyue; Jarosh, Michael; Kornecook, Thomas; Kreiman, Charles R.; Ligutti, Joseph; La, Daniel S.; Lin, Min-Hwa Jasmine; Liu, Dong; Moyer, Bryan D.; Nguyen, Hanh N.; Peterson, Emily A.; Rose, Paul E.; Taborn, Kristin; Youngblood, Beth D.; Yu, Violeta; Fremeau, Robert T., Jr. 分享 收藏
Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity Graceffa, Russell F.; Boezio, Alessandro A.; Able, Jessica; Altmann, Steven; Berry, Loren M.; Boezio, Christiane; Butler, John R.; Chu-Moyer, Margaret; Cooke, Melanie; DiMauro, Erin F.; Dineen, Thomas A.; Bojic, Elma Feric; Foti, Robert S.; Fremeau, Robert T., Jr.; Guzman-Perez, Angel; Gao, Hua; Gunaydin, Hakan; Huang, Hongbing; Huang, Liyue; Ilch, Christopher; Jarosh, Michael; Kornecook, Thomas; Kreiman, Charles R.; La, Daniel S.; Ligutti, Joseph; Milgram, Benjamin C.; Lin, Min-Hwa Jasmine; Marx, Isaac E.; Nguyen, Hanh N.; Peterson, Emily A.; Rescourio, Gwen; Roberts, John; Schenkel, Laurie; Shimanovich, Roman; Sparling, Brian A.; Stellwagen, John; Taborn, Kristin; Vaida, Karina R.; Wang, Jean; Yeoman, John; Yu, Violeta; Zhu, Dawn; Moyer, Bryan D.; Weiss, Matthew M. 分享 收藏
The Discovery and Hit-to-Lead Optimization of Tricyclic Sulfonamides as Potent and Efficacious Potentiators of Glycine Receptors Bregman, Howard; Simard, Jeffrey R.; Andrews, Kristin L.; Ayube, Shawn; Chen, Hao; Gunaydin, Hakan; Guzman-Perez, Angel; Hu, Jiali; Huang, Liyue; Huang, Xin; Krolikowski, Paul H.; Lehto, Sonya G.; Lewis, Richard T.; Michelsen, Klaus; Pegman, Pamela; Plant, Matthew H.; Shaffer, Paul L.; Teffera, Yohannes; Yi, Shuyan; Zhang, Maosheng; Gingras, Jacinthe; DiMauro, Erin F. 分享 收藏
Application of a Parallel Synthetic Strategy in the Discovery of Biaryl Acyl Sulfonamides as Efficient and Selective NaV1.7 Inhibitors DiMauro, Erin F.; Altmann, Stephen; Berry, Loren M.; Bregman, Howard; Chakka, Nagasree; Chu-Moyer, Margaret; Bojic, Elma Feric; Foti, Robert S.; Fremeau, Robert; Gao, Hua; Gunaydin, Hakan; Guzman-Perez, Angel; Hall, Brian E.; Huang, Hongbing; Jarosh, Michael; Korneook, Thomas; Lee, Josie; Ligutti, Joseph; Liu, Dong; Moyer, Bryan D.; Ortuno, Daniel; Rose, Paul E.; Schenkel, Laurie B.; Taborn, Kristin; Wang, Jean; Wang, Yan; Yu, Violeta; Weiss, Matthew M. 分享 收藏
Optimization of a Novel Quinazolinone-Based Series of Transient Receptor Potential A1 (TRPA1) Antagonists Demonstrating Potent in Vivo Activity Schenkel, Laurie B.; Olivieri, Philip R.; Boezio, Alessandro A.; Deak, Holly L.; Emkey, Renee; Graceffa, Russell F.; Gunaydin, Hakan; Guzman-Perez, Angel; Lee, Josie H.; Teffera, Yohannes; Wang, Weiya; Youngblood, Beth D.; Yu, Violeta L.; Zhang, Maosheng; Gavva, Narender R.; Lehto, Sonya G.; Geuns-Meyer, Stephanie 分享 收藏
Development of Novel Dual Binders as Potent, Selective, and Orally Bioavailable Tankyrase Inhibitors Hua, Zihao; Bregman, Howard; Buchanan, John L.; Chakka, Nagasree; Guzman-Perez, Angel; Gunaydin, Hakan; Huang, Xin; Gu, Yan; Berry, Virginia; Liu, Jingzhou; Teffera, Yohannes; Huang, Liyue; Egge, Bryan; Emkey, Renee; Mullady, Erin L.; Schneider, Steve; Andrews, Paul S.; Acquaviva, Lisa; Dovey, Jennifer; Mishra, Ankita; Newcomb, John; Saffran, Douglas; Serafino, Randy; Strathdee, Craig A.; Turci, Susan M.; Stanton, Mary; Wilson, Cindy; DiMauro, Erin F. 分享 收藏
Defining the key pharmacophore elements of PF-04620110: Discovery of a potent, orally-active, neutral DGAT-1 inhibitor (vol 21, pg 5081, 2013) Dow, Robert L.; Andrews, Melissa P.; Li, Jian-Cheng; Gibbs, E. Michael; Guzman-Perez, Angel; LaPerle, Jennifer L.; Li, Qifang; Mather, Dawn; Munchhof, Michael J.; Niosi, Mark; Patel, Leena; Perreault, Christian; Tapley, Susan; Zavadoski, William J. 分享 收藏
Structure-Based Design of 2-Aminopyridine Oxazolidinones as Potent and Selective Tankyrase Inhibitors Huang, Hongbing; Guzman-Perez, Angel; Acquaviva, Lisa; Berry, Virginia; Bregman, Howard; Dovey, Jennifer; Gunaydin, Hakan; Huang, Xin; Huang, Liyue; Saffran, Doug; Serafino, Randy; Schneider, Steve; Wilson, Cindy; DiMauro, Erin F. 分享 收藏
Defining the key pharmacophore elements of PF-04620110: Discovery of a potent, orally-active, neutral DGAT-1 inhibitor Dow, Robert L.; Andrews, Melissa P.; Li, Jian-Cheng; Gibbs, E. Michael; Guzman-Perez, Angel; LaPerle, Jennifer L.; Li, Qifang; Mather, Dawn; Munchhof, Michael J.; Niosi, Mark; Patel, Leena; Perreault, Christian; Tapley, Susan; Zavadoski, William J. 分享 收藏
Discovery of Novel, Induced-Pocket Binding Oxazolidinones as Potent, Selective, and Orally Bioavailable Tankyrase Inhibitors Bregman, Howard; Chakka, Nagasree; Guzman-Perez, Angel; Gunaydin, Hakan; Gu, Yan; Huang, Xin; Berry, Virginia; Liu, Jingzhou; Teffera, Yohannes; Huang, Liyue; Egge, Bryan; Mullady, Erin L.; Schneider, Steve; Andrews, Paul S.; Mishra, Ankita; Newcomb, John; Serafino, Randy; Strathdee, Craig A.; Turci, Susan M.; Wilson, Cindy; DiMauro, Erin F. 分享 收藏
Exploring Aromatic Chemical Space with NEAT: Novel and Electronically Equivalent Aromatic Template Tu, Meihua; Rai, Brajesh K.; Mathiowetz, Alan M.; Didiuk, Mary; Pfefferkorn, Jeffrey A.; Guzman-Perez, Angel; Benbow, John; Guimaraes, Cristiano R. W.; Mente, Scot; Hayward, Matthew M.; Liras, Spiros 分享 收藏
Discovery of (S)-6-(3-Cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic Acid as a Hepatoselective Glucokinase Activator Clinical Candidate for Treating Type 2 Diabetes Mellitus Pfefferkorn, Jeffrey A.; Guzman-Perez, Angel; Litchfield, John; Aiello, Robert; Treadway, Judith L.; Pettersen, John; Minich, Martha L.; Filipski, Kevin J.; Jones, Christopher S.; Tu, Meihua; Aspnes, Gary; Risley, Hud; Bian, Jianwei; Stevens, Benjamin D.; Bourassa, Patricia; D'Aquila, Theresa; Baker, Levenia; Barucci, Nicole; Robertson, Alan S.; Bourbonais, Francis; Derksen, David R.; MacDougall, Margit; Cabrera, Over; Chen, Jing; Lapworth, Amanda Lee; Landro, James A.; Zavadoski, William J.; Atkinson, Karen; Haddish-Berhane, Nahor; Tan, Beijing; Yao, Lili; Kosa, Rachel E.; Varma, Manthena V.; Feng, Bo; Duignan, David B.; El-Kattan, Ayman; Murdande, Sharad; Liu, Shenping; Ammirati, Mark; Knafels, John; DaSilva-Jardine, Paul; Sweet, Laurel; Liras, Spiros; Rolph, Timothy P. 分享 收藏
Maximizing Lipophilic Efficiency: The Use of Free-Wilson Analysis in the Design of Inhibitors of Acetyl-CoA Carboxylase Freeman-Cook, Kevin D.; Amor, Paul; Bader, Scott; Buzon, Leanne M.; Coffey, Steven B.; Corbett, Jeffrey W.; Dirico, Kenneth J.; Doran, Shawn D.; Elliott, Richard L.; Esler, William; Guzman-Perez, Angel; Henegar, Kevin E.; Houser, Janet A.; Jones, Christopher S.; Limberakis, Chris; Loomis, Katherine; McPherson, Kirk; Murdande, Sharad; Nelson, Kendra L.; Phillion, Dennis; Pierce, Betsy S.; Song, Wei; Sugarman, Eliot; Tapley, Susan; Tu, Meihua; Zhao, Zhengrong 分享 收藏
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Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1 Dow, Robert L.; Li, Jian-Cheng; Pence, Michael P.; Gibbs, E. Michael; LaPerle, Jennifer L.; Litchfield, John; Piotrowski, David W.; Munchhof, Michael J.; Manion, Tara B.; Zavadoski, William J.; Walker, Gregory S.; McPherson, R. Kirk; Tapley, Susan; Sugarman, Eliot; Guzman-Perez, Angel; DaSilva-Jardine, Paul 分享 收藏