Identification of (R)‑N‑((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)‑1H‑indole-3-carboxamide (CPI-1205),... von Vaswani, Rishi G, Gehling, Victor S, Dakin, Les A, Cook, Andrew S, Nasveschuk, Christopher G, Duplessis, Martin, Iyer, Priyadarshini, Balasubramanian, Srividya, Zhao, Feng, Good, Andrew C, Campbell, Robert, Lee, Christina, Cantone, Nico, Cummings, Richard T, Normant, Emmanuel, Bellon, Steven F, Albrecht, Brian K, Harmange, Jean-Christophe, Trojer, Patrick, Audia, James E, Zhang, Ying, Justin, Neil, Chen, Shuyang, Wilson, Jon R, Gamblin, Steven J

Volltext

Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials von Albrecht, Brian K, Gehling, Victor S, Hewitt, Michael C, Vaswani, Rishi G, Côté, Alexandre, Leblanc, Yves, Nasveschuk, Christopher G, Bellon, Steve, Bergeron, Louise, Campbell, Robert, Cantone, Nico, Cooper, Michael R, Cummings, Richard T, Jayaram, Hariharan, Joshi, Shivangi, Mertz, Jennifer A, Neiss, Adrianne, Normant, Emmanuel, O’Meara, Michael, Pardo, Eneida, Poy, Florence, Sandy, Peter, Supko, Jeffrey, Sims, Robert J, Harmange, Jean-Christophe, Taylor, Alexander M, Audia, James E

Volltext

Histone Modifications and Cancer von Audia, James E, Campbell, Robert M

Volltext

Collaboration and knowledge integration for successful brain therapeutics - lessons learned from the pandemic von Loza, Maria Isabel, Hmeljak, Julija, Bountra, Chas, Audia, James E, Chowdhury, Sohini, Weiman, Shannon, Merchant, Kalpana, Blanco, Maria-Jesus

Volltext

Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2 von Nasveschuk, Christopher G, Gagnon, Alexandre, Garapaty-Rao, Shivani, Balasubramanian, Srividya, Campbell, Robert, Lee, Christina, Zhao, Feng, Bergeron, Louise, Cummings, Richard, Trojer, Patrick, Audia, James E, Albrecht, Brian K, Harmange, Jean-Christophe P

Volltext

The promise and peril of chemical probes von Arrowsmith, Cheryl H, Audia, James E, Austin, Christopher, Baell, Jonathan, Bennett, Jonathan, Blagg, Julian, Bountra, Chas, Brennan, Paul E, Brown, Peter J, Bunnage, Mark E, Buser-Doepner, Carolyn, Campbell, Robert M, Carter, Adrian J, Cohen, Philip, Copeland, Robert A, Cravatt, Ben, Dahlin, Jayme L, Dhanak, Dashyant, Edwards, Aled M, Frederiksen, Mathias, Frye, Stephen V, Gray, Nathanael, Grimshaw, Charles E, Hepworth, David, Howe, Trevor, Huber, Kilian V M, Jin, Jian, Knapp, Stefan, Kotz, Joanne D, Kruger, Ryan G, Lowe, Derek, Mader, Mary M, Marsden, Brian, Mueller-Fahrnow, Anke, Müller, Susanne, O'Hagan, Ronan C, Overington, John P, Owen, Dafydd R, Rosenberg, Saul H, Ross, Ruth, Roth, Bryan, Schapira, Matthieu, Schreiber, Stuart L, Shoichet, Brian, Sundström, Michael, Superti-Furga, Giulio, Taunton, Jack, Toledo-Sherman, Leticia, Walpole, Chris, Walters, Michael A, Willson, Timothy M, Workman, Paul, Young, Robert N, Zuercher, William J

Volltext

Preparation and biological evaluation of conformationally constrained BACE1 inhibitors von Winneroski, Leonard L., Schiffler, Matthew A., Erickson, Jon A., May, Patrick C., Monk, Scott A., Timm, David E., Audia, James E., Beck, James P., Boggs, Leonard N., Borders, Anthony R., Boyer, Robert D., Brier, Richard A., Hudziak, Kevin J., Klimkowski, Valentine J., Garcia Losada, Pablo, Mathes, Brian M., Stout, Stephanie L., Watson, Brian M., Mergott, Dustin J.

Volltext

Discovery of Benzotriazolo[4,3‑d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains von Taylor, Alexander M, Vaswani, Rishi G, Gehling, Victor S, Hewitt, Michael C, Leblanc, Yves, Audia, James E, Bellon, Steve, Cummings, Richard T, Côté, Alexandre, Harmange, Jean-Christophe, Jayaram, Hari, Joshi, Shivangi, Lora, Jose M, Mertz, Jennifer A, Neiss, Adrianne, Pardo, Eneida, Nasveschuk, Christopher G, Poy, Florence, Sandy, Peter, Setser, Jeremy W, Sims, Robert J, Tang, Yong, Albrecht, Brian K

Volltext

Ilaprazole and Other Novel Prazole-Based Compounds That Bind Tsg101 Inhibit Viral Budding of Herpes Simplex Virus 1 and 2 and Human Immunodeficiency Virus from Cells von Leis, Jonathan, Luan, Chi-Hao, Audia, James E, Dunne, Sara F, Heath, Carissa M

Volltext

The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans von May, Patrick C, Willis, Brian A, Lowe, Stephen L, Dean, Robert A, Monk, Scott A, Cocke, Patrick J, Audia, James E, Boggs, Leonard N, Borders, Anthony R, Brier, Richard A, Calligaro, David O, Day, Theresa A, Ereshefsky, Larry, Erickson, Jon A, Gevorkyan, Hykop, Gonzales, Celedon R, James, Douglas E, Jhee, Stanford S, Komjathy, Steven F, Li, Linglin, Lindstrom, Terry D, Mathes, Brian M, Martényi, Ferenc, Sheehan, Scott M, Stout, Stephanie L, Timm, David E, Vaught, Grant M, Watson, Brian M, Winneroski, Leonard L, Yang, Zhixiang, Mergott, Dustin J

Volltext

Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains von Crawford, Terry D, Tsui, Vickie, Flynn, E. Megan, Wang, Shumei, Taylor, Alexander M, Côté, Alexandre, Audia, James E, Beresini, Maureen H, Burdick, Daniel J, Cummings, Richard, Dakin, Les A, Duplessis, Martin, Good, Andrew C, Hewitt, Michael C, Huang, Hon-Ren, Jayaram, Hariharan, Kiefer, James R, Jiang, Ying, Murray, Jeremy, Nasveschuk, Christopher G, Pardo, Eneida, Poy, Florence, Romero, F. Anthony, Tang, Yong, Wang, Jian, Xu, Zhaowu, Zawadzke, Laura E, Zhu, Xiaoyu, Albrecht, Brian K, Magnuson, Steven R, Bellon, Steve, Cochran, Andrea G

Volltext

Robust central reduction of amyloid-β in humans with an orally available, non-peptidic β-secretase inhibitor von May, Patrick C, Dean, Robert A, Lowe, Stephen L, Martenyi, Ferenc, Sheehan, Scott M, Boggs, Leonard N, Monk, Scott A, Mathes, Brian M, Mergott, Dustin J, Watson, Brian M, Stout, Stephanie L, Timm, David E, Smith Labell, Elizabeth, Gonzales, Celedon R, Nakano, Masako, Jhee, Stanford S, Yen, Mark, Ereshefsky, Larry, Lindstrom, Terry D, Calligaro, David O, Cocke, Patrick J, Greg Hall, D, Friedrich, Stuart, Citron, Martin, Audia, James E

Volltext

Mentoring Matters in Drug Discovery von Blanco, Maria-Jesus, Audia, James E

Volltext

GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1 von Taylor, Alexander M., Bailey, Chris, Belmont, Lisa D., Campbell, Robert, Cantone, Nico, Côté, Alexandre, Crawford, Terry D., Cummings, Richard, DeMent, Kevin, Duplessis, Martin, Flynn, Megan, Good, Andrew C., Huang, Hon-Ren, Joshi, Shivangi, Leblanc, Yves, Murray, Jeremy, Nasveschuk, Christopher G., Neiss, Adrianne, Poy, Florence, Romero, F. Anthony, Sandy, Peter, Tang, Yong, Tsui, Vickie, Zawadzke, Laura, Sims, Robert J., Audia, James E., Bellon, Steven F., Magnuson, Steven R., Albrecht, Brian K., Cochran, Andrea G.

Volltext

Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition von Ghosh, Srimoyee, Taylor, Alexander, Chin, Melissa, Huang, Hon-Ren, Conery, Andrew R., Mertz, Jennifer A., Salmeron, Andres, Dakle, Pranal J., Mele, Deanna, Cote, Alexandre, Jayaram, Hari, Setser, Jeremy W., Poy, Florence, Hatzivassiliou, Georgia, DeAlmeida-Nagata, Denise, Sandy, Peter, Hatton, Charlie, Romero, F. Anthony, Chiang, Eugene, Reimer, Thornik, Crawford, Terry, Pardo, Eneida, Watson, Venita G., Tsui, Vickie, Cochran, Andrea G., Zawadzke, Laura, Harmange, Jean-Christophe, Audia, James E., Bryant, Barbara M., Cummings, Richard T., Magnuson, Steven R., Grogan, Jane L., Bellon, Steve F., Albrecht, Brian K., Sims, Robert J., Lora, Jose M.

Volltext

Comparison of the effects of serotonin selective, norepinephrine selective, and dual serotonin and norepinephrine reuptake inhibitors on lower urinary tract function in cats von Katofiasc, Mary A, Nissen, Jeffrey, Audia, James E, Thor, Karl B

Volltext

Identification and characterization of second-generation EZH2 inhibitors with extended residence times and improved biological activity von Stuckey, Jacob I., Cantone, Nico R., Côté, Alexandre, Arora, Shilpi, Vivat, Valerie, Ramakrishnan, Ashwin, Mertz, Jennifer A., Khanna, Avinash, Brenneman, Jehrod, Gehling, Victor S., Moine, Ludivine, Sims, Robert J., Audia, James E., Trojer, Patrick, Levell, Julian R., Cummings, Richard T.

Volltext

Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637) von Taylor, Alexander M, Côté, Alexandre, Hewitt, Michael C, Pastor, Richard, Leblanc, Yves, Nasveschuk, Christopher G, Romero, F. Anthony, Crawford, Terry D, Cantone, Nico, Jayaram, Hariharan, Setser, Jeremy, Murray, Jeremy, Beresini, Maureen H, de Leon Boenig, Gladys, Chen, Zhongguo, Conery, Andrew R, Cummings, Richard T, Dakin, Leslie A, Flynn, E. Megan, Huang, Oscar W, Kaufman, Susan, Keller, Patricia J, Kiefer, James R, Lai, Tommy, Li, Yingjie, Liao, Jiangpeng, Liu, Wenfeng, Lu, Henry, Pardo, Eneida, Tsui, Vickie, Wang, Jian, Wang, Yongyun, Xu, Zhaowu, Yan, Fen, Yu, Dong, Zawadzke, Laura, Zhu, Xiaoqin, Zhu, Xiaoyu, Sims, Robert J, Cochran, Andrea G, Bellon, Steve, Audia, James E, Magnuson, Steven, Albrecht, Brian K

Volltext

Identification of potent, selective KDM5 inhibitors von Gehling, Victor S., Bellon, Steven F., Harmange, Jean-Christophe, LeBlanc, Yves, Poy, Florence, Odate, Shobu, Buker, Shane, Lan, Fei, Arora, Shilpi, Williamson, Kaylyn E., Sandy, Peter, Cummings, Richard T., Bailey, Christopher M., Bergeron, Louise, Mao, Weifeng, Gustafson, Amy, Liu, Yichin, VanderPorten, Erica, Audia, James E., Trojer, Patrick, Albrecht, Brian K.

Volltext

Discovery, design, and synthesis of indole-based EZH2 inhibitors von Gehling, Victor S., Vaswani, Rishi G., Nasveschuk, Christopher G., Duplessis, Martin, Iyer, Priyadarshini, Balasubramanian, Srividya, Zhao, Feng, Good, Andrew C., Campbell, Robert, Lee, Christina, Dakin, Les A., Cook, Andrew S., Gagnon, Alexandre, Harmange, Jean-Christophe, Audia, James E., Cummings, Richard T., Normant, Emmanuel, Trojer, Patrick, Albrecht, Brian K.

Volltext