未登录 Applications of contemporary tools to measure plasma protein binding of targeted protein degraders 当代工具在靶向蛋白降解剂血浆蛋白结合测量中的应用 Niosi, Mark; Zhang, Sam; Burchett, Woodrow; Heck, Carley J. S.; Goetz, Gilles H.; Federico, James J.; Gernhardt, Steven; Jordan, Samantha; Gilbert, Adam M.; Calabrese, Matthew F.; Obach, R. Scott; Steyn, Stefanus J. 分享 收藏
An allosteric cyclin E-CDK2 site mapped by paralog hopping with covalent probes Zhang, Yuanjin; Liu, Zhonglin; Hirschi, Marscha; Brodsky, Oleg; Johnson, Eric; Won, Sang Joon; Nagata, Asako; Bezwada, Divya; Petroski, Matthew D.; Majmudar, Jaimeen D.; Niessen, Sherry; Vanarsdale, Todd; Gilbert, Adam M.; Hayward, Matthew M.; Stewart, Al E.; Nager, Andrew R.; Melillo, Bruno; Cravatt, Benjamin F. 分享 收藏
Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor Butler, Christopher R.; Popiolek, Michael; McAllister, Laura A.; LaChapelle, Erik A.; Kramer, Melissa; Beck, Elizabeth M.; Mente, Scot; Brodney, Michael A.; Brown, Matthew; Gilbert, Adam; Helal, Chris; Ogilvie, Kevin; Starr, Jeremy; Uccello, Daniel; Grimwood, Sarah; Edgerton, Jeremy; Garst-Orozko, Jonathan; Kozak, Rouba; Lotarski, Susan; Rossi, Amie; Smith, Deborah; O'Connor, Rebecca; Lazzaro, John; Steppan, Claire; Steyn, Stefanus J. 分享 收藏
Discovery and characterization of selective heterobifunctional degraders of EP300 in hematopoietic malignancies Derheimer, Frederick A.; Givarkes, Ninvita; Miller, Natalie; Grantner, Rita; Quinlan, Casey; Brun, Sonja; Paul, Thomas; Ruefli-Brasse, Astrid; Steyn, Stefan; Bartlett, Derek; Hayward, Matthew; Brown, Matthew; Uccello, Daniel; Burke, Benjamin J.; Borzilleri, Kris; Gilbert, Adam; Hemkens, Michelle 分享 收藏
REL-1017 (Esmethadone) as Adjunctive Treatment in Patients With Major Depressive Disorder: A Phase 2a Randomized Double-Blind Trial Fava, Maurizio; Stahl, Stephen; Pani, Luca; De Martin, Sara; Pappagallo, Marco; Guidetti, Clotilde; Alimonti, Andrea; Bettini, Ezio; Mangano, Richard M.; Wessel, Thomas; de Somer, Marc; Caron, Judy; Vitolo, Ottavio V.; DiGuglielmo, Gina R.; Gilbert, Adam; Mehta, Hiren; Kearney, Morgan; Mattarei, Andrea; Gentilucci, Marco; Folli, Franco; Traversa, Sergio; Inturrisi, Charles E.; Manfredi, Paolo L. 分享 收藏
Intramolecular Ring-Opening Decomposition of Aryl Azetidines Bai, Guoyun; O'Connell, Thomas N.; Brodney, Michael A.; Butler, Christopher R.; Czabaniuk, Lara C.; Gilbert, Adam M.; LaChapelle, Erik A.; Li, Chao; McAllister, Laura A.; Ogilvie, Kevin; Philippe, Laurence; Salomon-Ferrer, Romelia; Shapiro, Michael J.; Starr, Jeremy T.; Uccello, Daniel P.; Withka, Jane M.; Yan, Jiangli; Brown, Matthew F. 分享 收藏
Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes Schiemer, James; Horst, Reto; Meng, Yilin; Montgomery, Justin I.; Xu, Yingrong; Feng, Xidong; Borzilleri, Kris; Uccello, Daniel P.; Leverett, Carolyn; Brown, Stephen; Che, Ye; Brown, Matthew F.; Hayward, Matthew M.; Gilbert, Adam M.; Noe, Mark C.; Calabrese, Matthew F. 分享 收藏
Delineating the role of cooperativity in the design of potent PROTACs for BTK Zorba, Adelajda; Chuong Nguyen; Xu, Yingrong; Starr, Jeremy; Borzilleri, Kris; Smith, James; Zhu, Hongyao; Farley, Kathleen A.; Ding, WeiDong; Schiemer, James; Feng, Xidong; Chang, Jeanne S.; Uccello, Daniel P.; Young, Jennifer A.; Garcia-Irrizary, Carmen N.; Czabaniuk, Lara; Schuff, Brandon; Oliver, Robert; Montgomery, Justin; Hayward, Matthew M.; Coe, Jotham; Chen, Jinshan; Niosi, Mark; Luthra, Suman; Shah, Jaymin C.; El-Kattan, Ayman; Qiu, Xiayang; West, Graham M.; Noe, Mark C.; Shanmugasundaram, Veerabahu; Gilbert, Adam M.; Brown, Matthew F.; Calabrese, Matthew F. 分享 收藏
Discovery of Trifluoromethyl Glycol Carbamates as Potent and Selective Covalent Monoacylglycerol Lipase (MAGL) Inhibitors for Treatment of Neuroinflammation McAllister, Laura A.; Butler, Christopher R.; Mente, Scot; O'neil, Steven, V; Fonseca, Kari R.; Piro, Justin R.; Cianfrogna, Julie A.; Foley, Timothy L.; Gilbert, Adam M.; Harris, Anthony R.; Helal, Christopher J.; Johnson, Douglas S.; Montgomery, Justin, I; Nason, Deane M.; Noell, Stephen; Pandit, Jayvardhan; Rogers, Bruce N.; Samad, Tarek A.; Shaffer, Christopher L.; da Silva, Rafael G.; Uccello, Daniel P.; Webb, Damien; Brodney, Michael A. 分享 收藏
Structure-Based Approach To Identify 5-[4-Hydroxyphenyl]pyrrole-2-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators Unwalla, Ray; Mousseau, James J.; Fadeyi, Olugbeminiyi O.; Choi, Chulho; Parris, Kevin; Hu, Baihua; Kenney, Thomas; Chippari, Susan; McNally, Christopher; Vishwanathan, Karthick; Kilbourne, Edward; Thompson, Catherine; Nagpal, Sunil; Wrobel, Jay; Yudt, Matthew; Morris, Carl A.; Powell, Dennis; Gilbert, Adam M.; Chekler, Eugene L. Piatnitski 分享 收藏
Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-(2s,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-y1)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans Thorarensen, Atli; Dowty, Martin E.; Banker, Mary Ellen; Juba, Brian; Jussif, Jason; Lin, Tsung; Vincent, Fabien; Czerwinski, Robert M.; Casimiro-Garcia, Agustin; Unwalla, Ray; Trujillo, John I.; Liang, Sidney; Balbo, Paul; Che, Ye; Gilbert, Adam M.; Brown, Matthew F.; Hayward, Matthew; Montgomery, Justin; Leung, Louis; Yang, Xin; Soucy, Sarah; Hegen, Martin; Coe, Jotham; Langille, Jonathan; Vajdos, Felix; Chrencik, Jill; Telliez, Jean-Baptiste 分享 收藏
Chiral Sulfoxide-Induced Single Turn Peptide α-Helicity Zhang, Qingzhou; Jiang, Fan; Zhao, Bingchuan; Lin, Huacan; Tian, Yuan; Xie, Mingsheng; Bai, Guoyun; Gilbert, Adam M.; Goetz, Gilles H.; Liras, Spiros; Mathiowetz, Alan A.; Price, David A.; Song, Kun; Tu, Meihua; Wu, Yujie; Wang, Tao; Flanagan, Mark E.; Wu, Yun-Dong; Li, Zigang 分享 收藏
Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition JAK3-Selective抑制剂的发现: JAK3-Selective抑制对pan-jak或JAK1-Selective抑制的功能分化 Telliez, Jean-Baptiste; Dowty, Martin E.; Wang, Lu; Jussif, Jason; Lin, Tsung; Li, Li; Moy, Erick; Balbo, Paul; Li, Wei; Zhao, Yajuan; Crouse, Kimberly; Dickinson, Caitlyn; Symanowicz, Peter; Hegen, Martin; Banker, Mary Ellen; Vincent, Fabien; Unwalla, Ray; Liang, Sidney; Gilbert, Adam M.; Brown, Matthew F.; Hayward, Matthew; Montgomery, Justin; Yang, Xin; Bauman, Jonathan; Trujillo, John I.; Casimiro-Garcia, Agustin; Vajdos, Felix F.; Leung, Louis; Geoghegan, Kieran F.; Quazi, Amira; Xuan, Dejun; Jones, Lyn; Hett, Erik; Wright, Katherine; Clark, James D.; Thorarensen, Atli 分享 收藏
Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism Ahn, Kay; Boehm, Markus; Brown, Matthew F.; Calloway, Jessica; Che, Ye; Chen, Jinshan; Fennell, Kimberly F.; Geoghegan, Kieran F.; Gilbert, Adam M.; Gutierrez, Jemy A.; Kalgutkar, Amit S.; Lanba, Adhiraj; Limberalds, Chris; Magee, Thomas V.; O'Doherty, Inish; Oliver, Robert; Pabst, Brandon; Pandit, Jayvardhan; Parris, Kevin; Pfefferkorn, Jeffrey A.; Rolph, Timothy P.; Patel, Rushi; Schuff, Brandon; Shanmugasundaram, Veerabahu; Starr, Jeremy T.; Varghese, Alison H.; Vera, Nicholas B.; Vernochet, Cecile; Yan, Jiangli 分享 收藏
Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family Huard, Kim; Gosset, James R.; Montgomery, Justin I.; Gilbert, Adam; Hayward, Matthew M.; Magee, Thomas V.; Cabral, Shawn; Uccello, Daniel P.; Bahnck, Kevin; Brown, Janice; Purkal, Julie; Gorgoglione, Matthew; Lanba, Adhiraj; Futatsugi, Kentaro; Herr, Michael; Genung, Nathan E.; Aspnes, Gary; Polivkova, Jana; Garcia-Irizarry, Carmen N.; Li, Qifang; Canterbury, Daniel; Niosi, Mark; Vera, Nicholas B.; Li, Zhenhong; Khunte, Bhagyashree; Siderewicz, Jaclyn; Rolph, Timothy; Erion, Derek M. 分享 收藏
Developing predictive assays: The phenotypic screening rule of 3 Vincent, Fabien; Loria, Paula; Pregel, Marko; Stanton, Robert; Kitching, Linda; Nocka, Karl; Doyonnas, Regis; Steppan, Claire; Gilbert, Adam; Schroeter, Thomas; Peakman, Marie-Claire 分享 收藏
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Chemical and Computational Methods for the Characterization of Covalent Reactive Groups for the Prospective Design of Irreversible Inhibitors 用于表征不可逆抑制剂前瞻性设计的共价反应基团的化学和计算方法 Flanagan, Mark E.; Abramite, Joseph A.; Anderson, Dennis P.; Aulabaugh, Ann; Dahal, Upendra P.; Gilbert, Adam M.; Li, Chao; Montgomery, Justin; Oppenheimer, Stacey R.; Ryder, Tim; Schuff, Brandon P.; Uccello, Daniel P.; Walker, Gregory S.; Wu, Yan; Brown, Matthew F.; Chen, Jinshan M.; Hayward, Matthew M.; Noe, Mark C.; Obach, R. Scott; Philippe, Laurence; Shanmugasundaram, Veerabahu; Shapiro, Michael J.; Starr, Jeremy; Stroh, Justin; Che, Ye 分享 收藏
A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors Lannine, Bryan R.; Whitby, Landon R.; Dix, Melissa M.; Douhan, John; Gilbert, Adam M.; Hett, Erik C.; Johnson, Theodore; Joslynl, Chris; Kath, John C.; Niessen, Sherry; Roberts, Lee R.; Schnute, Mark E.; Wang, Chu; Hulce, Jonathan J.; Wei, Baoxian; Whiteley, Laurence O.; Hayward, Matthew M.; Cravatt, Benjamin F. 分享 收藏
1-(2-Hydroxy-2-methyl-3-phenoxypropanoyl)indoline-4-carbonitrile Derivatives as Potent and Tissue Selective Androgen Receptor Modulators Chekler, Eugene L. Piatnitski; Unwalla, Rayomond; Khan, Taukeer A.; Tangirala, Raghuram S.; Johnson, Mark; St Andre, Michael; Anderson, James T.; Kenney, Thomas; Chiparri, Sue; McNally, Chris; Kilbourne, Edward; Thompson, Catherine; Nagpal, Sunil; Weber, Gregory; Schelling, Scott; Owens, Jane; Morris, Carl A.; Powell, Dennis; Verhoest, Patrick R.; Gilbert, Adam M. 分享 收藏
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