未登录Design and identification of brain-penetrant, potent, and selective 1,3-oxazole-based cholesterol 24-hydroxylase (CH24H) inhibitors
Ito, Yoshiteru; Kimura, Eiji; Nomura, Izumi; Watanabe, Etsurou; Yano, Jason; Skene, Robert; Miyamoto, Maki; Ishii, Tsuyoshi; Nishi, Toshiya; Koike, Tatsuki .png)
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收藏分享 收藏 In Silico Enabled Discovery of KAI-11101, a Preclinical DLK Inhibitor for the Treatment of Neurodegenerative Disease and Neuronal InjuryLagiakos, H. Rachel; Zou, Yefen; Igawa, Hideyuki; Therrien, Eric; Lawrenz, Morgan; Kato, Mitsunori; Svensson, Mats; Gray, Felicia; Jensen, Kristian; Dahlgren, Markus K.; Pelletier, Robert D.; Dingley, Karen; Bell, Jeffrey A.; Liu, Zhijian; Jiang, Yuansong; Zhou, Hua; Skene, Robert J.; Nie, Zhe 分享 收藏 Discovery of a Novel Class of D-Amino Acid Oxidase Inhibitors Usingthe Schro?dinger Computational PlatformTang, Haifeng; Jensen, Kristian; Houang, Evelyne; McRobb, Fiona M.; Bhat, Sathesh; Svensson, Mats; Bochevarov, Art; Day, Tyler; Dahlgren, Markus K.; Bell, Jeffery A.; Frye, Leah; Skene, Robert J.; Lewis, James H.; Osborne, James D.; Tierney, Jason P.; Gordon, James A.; Palomero, Maria A.; Gallati, Caroline; Chapman, Robert S. L.; Jones, Daniel R.; Hirst, Kim L.; Sephton, Mark; Chauhan, Alka; Sharpe, Andrew; Tardia, Piero; Dechaux, Elsa A.; Taylor, Andrea; Waddell, Ross D.; Valentine, Andrea; Janssens, Holden B.; Aziz, Omar; Bloomfield, Dawn E.; Ladha, Sandeep; Fraser, Ian J.; Ellard, John M. 分享 收藏 Identification of Novel Carbocyclic Pyrimidine Cyclic Dinucleotide STING Agonists for Antitumor Immunotherapy Using Systemic Intravenous RouteVyskocil, Stepan; Cardin, David; Ciavarri, Jeffrey; Conlon, Joe; Cullis, Courtney; England, Dylan; Gershman, Rachel; Gigstad, Kenneth; Gipson, Krista; Gould, Alexandra; Greenspan, Paul; Griffin, Robert; Gulavita, Nanda; Harrison, Sean; Hu, Zhigen; Hu, Yongbo; Hata, Akito; Huang, Jian; Huang, Shih-Chung; Janowick, Dave; Jones, Matthew; Kolev, Vihren; Langston, Steven P.; Lee, Hong Myung; Li, Gang; Lok, David; Ma, Liting; Mai, Doanh; Malley, Jenna; Matsuda, Atsushi; Mizutani, Hirotake; Mizutani, Miho; Molchanova, Nina; Nunes, Elise; Pusalkar, Sandeep; Renou, Christelle; Rowland, Scott; Sato, Yosuke; Shaw, Michael; Shen, Luhua; Shi, Zhan; Skene, Robert; Soucy, Francois; Stroud, Steve; Xu, He; Xu, Tianlin; Abu-Yousif, Adnan O.; Zhang, Ji 分享 收藏 Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor AgentKurasawa, Osamu; Miyazaki, Tohru; Homma, Misaki; Oguro, Yuya; Imada, Takashi; Uchiyama, Noriko; Iwai, Kenichi; Yamamoto, Yukiko; Ohori, Momoko; Hara, Hideto; Sugimoto, Hiroshi; Iwata, Kentaro; Skene, Robert; Hoffman, Isaac; Ohashi, Akihiro; Nomura, Toshiyuki; Cho, Nobuo 分享 收藏 Design and Synthesis of Conformationally Constrained RORγt Inverse AgonistsSato, Ayumu; Fukase, Yoshiyuki; Kono, Mitsunori; Ochida, Atsuko; Oda, Tsuneo; Sasaki, Yusuke; Ishii, Naoki; Tomata, Yoshihide; Fukumoto, Shoji; Imai, Yumi N.; Uga, Keiko; Shibata, Akira; Yamasaki, Masashi; Nakagawa, Hideyuki; Shirasaki, Mikio; Skene, Robert; Hoffman, Isaac; Sang, Bi-Ching; Snell, Gyorgy; Shirai, Junya; Yamamoto, Satoshi 分享 收藏 The dynamic conformational landscape of the protein methyltransferase SETD8Chen, Shi; Wiewiora, Rafal P.; Meng, Fanwang; Babault, Nicolas; Ma, Anqi; Yu, Wenyu; Qian, Kun; Hu, Hao; Zou, Hua; Wang, Junyi; Fan, Shijie; Blum, Gil; Pittella-Silva, Fabio; Beauchamp, Kyle A.; Tempel, Wolfram; Jiang, Hualiang; Chen, Kaixian; Skene, Robert J.; Zheng, Yujun George; Brown, Peter J.; Jin, Jian; Luo, Cheng; Chodera, John D.; Luo, Minkui 分享 收藏 Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt AgonistYukawa, Tomoya; Nara, Yoshi; Kono, Mitsunori; Sato, Ayumu; Oda, Tsuneo; Takagi, Terufumi; Sato, Takayuki; Banno, Yoshihiro; Taya, Naohiro; Imada, Takashi; Shiokawa, Zenyu; Negoro, Nobuyuki; Kawamoto, Tetsuji; Koyama, Ryokichi; Uchiyama, Noriko; Skene, Robert; Hoffman, Isaac; Chen, Chien-Hung; Sang, BiChing; Snell, Gyorgy; Katsuyama, Ryosuke; Yamamoto, Satoshi; Shirai, Junya 分享 收藏 Discovery of (&ITcis&IT-3-({(5&ITR&IT)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1&ITH&IT-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5&ITH&IT)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse AgonistKono, Mitsunori; Ochida, Atsuko; Oda, Tsuneo; Imada, Takashi; Banno, Yoshihiro; Taya, Naohiro; Masada, Shinichi; Kawamoto, Tetsuji; Yonemori, Kazuko; Nara, Yoshi; Fukase, Yoshiyuki; Yukawa, Tomoya; Tokuhara, Hidekazu; Skene, Robert; Sang, Bi-Ching; Hoffman, Isaac D.; Snell, Gyorgy P.; Uga, Keiko; Shibata, Akira; Igaki, Keiko; Nakamura, Yoshiki; Nakagawa, Hideyuki; Tsuchimori, Noboru; Yamasaki, Masashi; Shirai, Junya; Yamamoto, Satoshi 分享 收藏 Identification of novel quinazolinedione derivatives as RORγt inverse agonistFukase, Yoshiyuki; Sato, Ayumu; Tomata, Yoshihide; Ochida, Atsuko; Kono, Mitsunori; Yonemori, Kazuko; Koga, Keiko; Okui, Toshitake; Yamasaki, Masashi; Fujitani, Yasushi; Nakagawa, Hideyuki; Koyama, Ryoukichi; Nakayama, Masaharu; Skene, Robert; Sang, Bi-Ching; Hoffman, Isaac; Shirai, Junya; Yamamoto, Satoshi 分享 收藏 Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffoldsShirai, Junya; Tomata, Yoshihide; Kono, Mitsunori; Ochida, Atsuko; Fukase, Yoshiyuki; Sato, Ayumu; Masada, Shinichi; Kawamoto, Tetsuji; Yonemori, Kazuko; Koyama, Ryoukichi; Nakagawa, Hideyuki; Nakayama, Masaharu; Uga, Keiko; Shibata, Akira; Koga, Keiko; Okui, Toshitake; Shirasaki, Mikio; Skene, Robert; Sang, BiChing; Hoffman, Isaac; Lane, Wes; Fujitani, Yasushi; Yamasaki, Masashi; Yamamoto, Satoshi 分享 收藏 1,2,4-Triazolo-[1,5-a]pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors With a Novel Monodentate Binding InteractionAhmed, Saleh; Ayscough, Andrew; Barker, Greg R.; Canning, Hannah E.; Davenport, Richard; Downham, Robert; Harrison, David; Jenkins, Kerry; Kinsella, Natasha; Livermore, David G.; Wright, Susanne; Ivetac, Anthony D.; Skene, Robert; Wilkens, Steven J.; Webster, Natalie A.; Hendrick, Alan G. 分享 收藏 Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-onesKurasawa, Osamu; Oguro, Yuya; Miyazaki, Tohru; Homma, Misaki; Mori, Kouji; Iwai, Kenichi; Hara, Hideto; Skene, Robert; Hoffman, Isaac; Ohashi, Akihiro; Yoshida, Sei; Ishikawa, Tomoyasu; Cho, Nobuo 分享 收藏 Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 InhibitorsYogo, Takatoshi; Nagamiya, Hiroyuki; Seto, Masaki; Sasaki, Satoshi; Shih-Chung, Huang; Ohba, Yusuke; Tokunaga, Norihito; Lee, Gil Nam; Rhim, Chul Yun; Yoon, Cheol Hwan; Cho, Suk Young; Skene, Robert; Yamamoto, Syunsuke; Satou, Yousuke; Kuno, Masako; Miyazaki, Takahiro; Nakagawa, Hideyuki; Okabe, Atsutoshi; Marui, Shogo; Aso, Kazuyoshi; Yoshida, Masato 分享 收藏 Discovery and characterization of novel allosteric FAK inhibitorsIwatani, Misa; Iwata, Hidehisa; Okabe, Atsutoshi; Skene, Robert J.; Tomita, Naoki; Hayashi, Yoko; Aramaki, Yoshio; Hosfield, David J.; Hori, Akira; Baba, Atsuo; Miki, Hiroshi 分享 收藏 Structural Analysis of the Mechanism of Inhibition and Allosteric Activation of the Kinase Domain of HER2 ProteinAertgeerts, Kathleen; Skene, Robert; Yano, Jason; Sang, Bi-Ching; Zou, Hua; Snell, Gyorgy; Jennings, Andy; Iwamoto, Keiji; Habuka, Noriyuki; Hirokawa, Aki; Ishikawa, Tomoyasu; Tanaka, Toshimasa; Miki, Hiroshi; Ohta, Yoshikazu; Sogabe, Satoshi 分享 收藏 Design and Synthesis of Pyrimidinone and Pyrimidinedione Inhibitors of Dipeptidyl Peptidase IVZhang, Zhiyuan; Wallace, Michael B.; Feng, Jun; Stafford, Jeffrey A.; Skene, Robert J.; Shi, Lihong; Lee, Bumsup; Aertgeerts, Kathleen; Jennings, Andy; Xu, Rongda; Kassel, Daniel B.; Kaldor, Stephen W.; Navre, Marc; Webb, David R.; Gwaltney, Stephen L., II 分享 收藏 Discovery of alogliptin: A potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV (vol 50, pg 2297, 2007)Feng, Jun; Zhang, Zhiyuan; Wallace, Micahel B.; Stafford, Jeffrey A.; Stephen, W. Kaldor; Kassel, Danil B.; Navre, Marc; Shi, Lihong; Skene, Robert J.; Asakawa, Tomoko; Takeuchi, Koji; Xu, Rongda; Webb, David R.; Gwaltney, Stephen L., II 分享 收藏 Discovery of alogliptin: A potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IVFeng, Jun; Zhang, Zhiyuan; Wallace, Michael B.; Stafford, Jeffrey A.; Kaldor, Stephen W.; Kassel, Daniel B.; Navre, Marc; Shi, Lihong; Skene, Robert J.; Asakawa, Tomoko; Takeuchi, Koji; Xu, Rongda; Webb, David R.; Gwaltney, Stephen L., II 分享 收藏 
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