BRD4 is an atypical kinase that phosphorylates Serine2 of the RNA Polymerase II carboxy-terminal domain
Devaiah, Ballachanda N, Lewis, Brian A, Cherman, Natasha, Hewitt, Michael C, Albrecht, Brian K, Robey, Pamela G, Ozato, Keiko, Sims, Robert J. III, Singer, Dinah S
Published in Proceedings of the National Academy of Sciences - PNAS (01.05.2012)
Published in Proceedings of the National Academy of Sciences - PNAS (01.05.2012)
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Discovery of (R)‑6-(1-(8-Fluoro-6-(1-methyl‑1H‑pyrazol-4-yl)-[1,2,4]triazolo[4,3‑a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)‑one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity
Boezio, Alessandro A, Copeland, Katrina W, Rex, Karen, K. Albrecht, Brian, Bauer, David, Bellon, Steven F, Boezio, Christiane, Broome, Martin A, Choquette, Deborah, Coxon, Angela, Dussault, Isabelle, Hirai, Satoko, Lewis, Richard, Lin, Min-Hwa Jasmine, Lohman, Julia, Liu, Jingzhou, Peterson, Emily A, Potashman, Michele, Shimanovich, Roman, Teffera, Yohannes, Whittington, Douglas A, Vaida, Karina R, Harmange, Jean-Christophe
Published in Journal of medicinal chemistry (24.03.2016)
Published in Journal of medicinal chemistry (24.03.2016)
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Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance
Crawford, Terry D., Vartanian, Steffan, Côté, Alexandre, Bellon, Steve, Duplessis, Martin, Flynn, E. Megan, Hewitt, Michael, Huang, Hon-Ren, Kiefer, James R., Murray, Jeremy, Nasveschuk, Christopher G., Pardo, Eneida, Romero, F. Anthony, Sandy, Peter, Tang, Yong, Taylor, Alexander M., Tsui, Vickie, Wang, Jian, Wang, Shumei, Zawadzke, Laura, Albrecht, Brian K., Magnuson, Steven R., Cochran, Andrea G., Stokoe, David
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
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Discovery of Potent and Selective 8‑Fluorotriazolopyridine c‑Met Inhibitors
Peterson, Emily A, Teffera, Yohannes, Albrecht, Brian K, Bauer, David, Bellon, Steven F, Boezio, Alessandro, Boezio, Christiane, Broome, Martin A, Choquette, Deborah, Copeland, Katrina W, Dussault, Isabelle, Lewis, Richard, Lin, Min-Hwa Jasmine, Lohman, Julia, Liu, Jingzhou, Potashman, Michele, Rex, Karen, Shimanovich, Roman, Whittington, Douglas A, Vaida, Karina R, Harmange, Jean-Christophe
Published in Journal of medicinal chemistry (12.03.2015)
Published in Journal of medicinal chemistry (12.03.2015)
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Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2
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
Published in ACS medicinal chemistry letters (10.04.2014)
Published in ACS medicinal chemistry letters (10.04.2014)
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Pharmacological effects of nonselective and subtype-selective nicotinic acetylcholine receptor agonists in animal models of persistent pain
Gao, BaoXi, Hierl, Markus, Clarkin, Kristie, Juan, Todd, Nguyen, Hung, Valk, Marissa van der, Deng, Hong, Guo, Wenhong, Lehto, Sonya G., Matson, David, McDermott, Jeff S., Knop, Johannes, Gaida, Kevin, Cao, Lei, Waldon, Dan, Albrecht, Brian K., Boezio, Alessandro A., Copeland, Katrina W., Harmange, Jean-Christophe, Springer, Stephanie K., Malmberg, Annika B., McDonough, Stefan I.
Published in Pain (Amsterdam) (01.04.2010)
Published in Pain (Amsterdam) (01.04.2010)
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A Concise, Total Synthesis of the TMC-95A/B Proteasome Inhibitors
Albrecht, Brian K., Williams, Robert M., Nicolaou, Kyriacos C.
Published in Proceedings of the National Academy of Sciences - PNAS (17.08.2004)
Published in Proceedings of the National Academy of Sciences - PNAS (17.08.2004)
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Discovery and Optimization of a Novel Series of N-Arylamide Oxadiazoles as Potent, Highly Selective and Orally Bioavailable Cannabinoid Receptor 2 (CB2) Agonists
Cheng, Yuan, Albrecht, Brian K, Brown, James, Buchanan, John L, Buckner, William H, DiMauro, Erin F, Emkey, Renee, Fremeau, Robert T, Harmange, Jean-Christophe, Hoffman, Beth J, Huang, Liyue, Huang, Ming, Lee, Josie Han, Lin, Fen-Fen, Martin, Matthew W, Nguyen, Hung Q, Patel, Vinod F, Tomlinson, Susan A, White, Ryan D, Xia, Xiaoyang, Hitchcock, Stephen A
Published in Journal of medicinal chemistry (28.08.2008)
Published in Journal of medicinal chemistry (28.08.2008)
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An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells
Vinogradova, Maia, Gehling, Victor S, Gustafson, Amy, Arora, Shilpi, Tindell, Charles A, Wilson, Catherine, Williamson, Kaylyn E, Guler, Gulfem D, Gangurde, Pranoti, Manieri, Wanda, Busby, Jennifer, Flynn, E Megan, Lan, Fei, Kim, Hyo-jin, Odate, Shobu, Cochran, Andrea G, Liu, Yichin, Wongchenko, Matthew, Yang, Yibin, Cheung, Tommy K, Maile, Tobias M, Lau, Ted, Costa, Michael, Hegde, Ganapati V, Jackson, Erica, Pitti, Robert, Arnott, David, Bailey, Christopher, Bellon, Steve, Cummings, Richard T, Albrecht, Brian K, Harmange, Jean-Christophe, Kiefer, James R, Trojer, Patrick, Classon, Marie
Published in Nature chemical biology (01.07.2016)
Published in Nature chemical biology (01.07.2016)
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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), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B‑Cell Lymphomas
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
Published in Journal of medicinal chemistry (10.11.2016)
Published in Journal of medicinal chemistry (10.11.2016)
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Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials
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
Published in Journal of medicinal chemistry (25.02.2016)
Published in Journal of medicinal chemistry (25.02.2016)
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GNE-781, A Highly Advanced Potent and Selective Bromodomain Inhibitor of Cyclic Adenosine Monophosphate Response Element Binding Protein, Binding Protein (CBP)
Romero, F. Anthony, Murray, Jeremy, Lai, Kwong Wah, Tsui, Vickie, Albrecht, Brian K, An, Le, Beresini, Maureen H, de Leon Boenig, Gladys, Bronner, Sarah M, Chan, Emily W, Chen, Kevin X, Chen, Zhongguo, Choo, Edna F, Clagg, Kyle, Clark, Kevin, Crawford, Terry D, Cyr, Patrick, de Almeida Nagata, Denise, Gascoigne, Karen E, Grogan, Jane L, Hatzivassiliou, Georgia, Huang, Wei, Hunsaker, Thomas L, Kaufman, Susan, Koenig, Stefan G, Li, Ruina, Li, Yingjie, Liang, Xiaorong, Liao, Jiangpeng, Liu, Wenfeng, Ly, Justin, Maher, Jonathan, Masui, Colin, Merchant, Mark, Ran, Yingqing, Taylor, Alexander M, Wai, John, Wang, Fei, Wei, Xiaocang, Yu, Dong, Zhu, Bing-Yan, Zhu, Xiaoyu, Magnuson, Steven
Published in Journal of medicinal chemistry (22.11.2017)
Published in Journal of medicinal chemistry (22.11.2017)
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Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains
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
Published in Journal of medicinal chemistry (09.06.2016)
Published in Journal of medicinal chemistry (09.06.2016)
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Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300
Crawford, Terry D, Romero, F. Anthony, Lai, Kwong Wah, Tsui, Vickie, Taylor, Alexander M, de Leon Boenig, Gladys, Noland, Cameron L, Murray, Jeremy, Ly, Justin, Choo, Edna F, Hunsaker, Thomas L, Chan, Emily W, Merchant, Mark, Kharbanda, Samir, Gascoigne, Karen E, Kaufman, Susan, Beresini, Maureen H, Liao, Jiangpeng, Liu, Wenfeng, Chen, Kevin X, Chen, Zhongguo, Conery, Andrew R, Côté, Alexandre, Jayaram, Hariharan, Jiang, Ying, Kiefer, James R, Kleinheinz, Tracy, Li, Yingjie, Maher, Jonathan, Pardo, Eneida, Poy, Florence, Spillane, Kerry L, Wang, Fei, Wang, Jian, Wei, Xiaocang, Xu, Zhaowu, Xu, Zhongya, Yen, Ivana, Zawadzke, Laura, Zhu, Xiaoyu, Bellon, Steven, Cummings, Richard, Cochran, Andrea G, Albrecht, Brian K, Magnuson, Steven
Published in Journal of medicinal chemistry (08.12.2016)
Published in Journal of medicinal chemistry (08.12.2016)
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GNE-064: A Potent, Selective, and Orally Bioavailable Chemical Probe for the Bromodomains of SMARCA2 and SMARCA4 and the Fifth Bromodomain of PBRM1
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.
Published in Journal of medicinal chemistry (25.08.2022)
Published in Journal of medicinal chemistry (25.08.2022)
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Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors
Hodous, Brian L., Geuns-Meyer, Stephanie D., Hughes, Paul E., Albrecht, Brian K., Bellon, Steve, Caenepeel, Sean, Cee, Victor J., Chaffee, Stuart C., Emery, Maurice, Fretland, Jenne, Gallant, Paul, Gu, Yan, Johnson, Rebecca E., Kim, Joseph L., Long, Alexander M., Morrison, Michael, Olivieri, Philip R., Patel, Vinod F., Polverino, Anthony, Rose, Paul, Wang, Ling, Zhao, Huilin
Published in Bioorganic & medicinal chemistry letters (15.05.2007)
Published in Bioorganic & medicinal chemistry letters (15.05.2007)
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Journal Article
Identification of EZH2 and EZH1 Small Molecule Inhibitors with Selective Impact on Diffuse Large B Cell Lymphoma Cell Growth
Garapaty-Rao, Shivani, Nasveschuk, Christopher, Gagnon, Alexandre, Chan, Eric Y., Sandy, Peter, Busby, Jennifer, Balasubramanian, Srividya, Campbell, Robert, Zhao, Feng, Bergeron, Louise, Audia, James E., Albrecht, Brian K., Harmange, Jean-Christophe, Cummings, Richard, Trojer, Patrick
Published in Chemistry & biology (21.11.2013)
Published in Chemistry & biology (21.11.2013)
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Journal Article
Regulatory T Cell Modulation by CBP/EP300 Bromodomain Inhibition
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.
Published in The Journal of biological chemistry (17.06.2016)
Published in The Journal of biological chemistry (17.06.2016)
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Identification of potent, selective KDM5 inhibitors
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.
Published in Bioorganic & medicinal chemistry letters (01.09.2016)
Published in Bioorganic & medicinal chemistry letters (01.09.2016)
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Journal Article
Discovery, design, and synthesis of indole-based EZH2 inhibitors
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.
Published in Bioorganic & medicinal chemistry letters (01.09.2015)
Published in Bioorganic & medicinal chemistry letters (01.09.2015)
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