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

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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 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

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An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells von 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

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From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors von Liang, Jun, Labadie, Sharada, Zhang, Birong, Ortwine, Daniel F., Patel, Snahel, Vinogradova, Maia, Kiefer, James R., Mauer, Till, Gehling, Victor S., Harmange, Jean-Christophe, Cummings, Richard, Lai, Tommy, Liao, Jiangpeng, Zheng, Xiaoping, Liu, Yichin, Gustafson, Amy, Van der Porten, Erica, Mao, Weifeng, Liederer, Bianca M., Deshmukh, Gauri, An, Le, Ran, Yingqing, Classon, Marie, Trojer, Patrick, Dragovich, Peter S., Murray, Lesley

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Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies von Liang, Jun, Zhang, Birong, Labadie, Sharada, Ortwine, Daniel F., Vinogradova, Maia, Kiefer, James R., Gehling, Victor S., Harmange, Jean-Christophe, Cummings, Richard, Lai, Tommy, Liao, Jiangpeng, Zheng, Xiaoping, Liu, Yichin, Gustafson, Amy, Van der Porten, Erica, Mao, Weifeng, Liederer, Bianca M., Deshmukh, Gauri, Classon, Marie, Trojer, Patrick, Dragovich, Peter S., Murray, Lesley

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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.

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Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors von Gehling, Victor S, Hewitt, Michael C, Vaswani, Rishi G, Leblanc, Yves, Côté, Alexandre, Nasveschuk, Christopher G, Taylor, Alexander M, Harmange, Jean-Christophe, Audia, James E, Pardo, Eneida, Joshi, Shivangi, Sandy, Peter, Mertz, Jennifer A, Sims, Robert J, Bergeron, Louise, Bryant, Barbara M, Bellon, Steve, Poy, Florence, Jayaram, Hariharan, Sankaranarayanan, Ravichandran, Yellapantula, Sreegouri, Bangalore Srinivasamurthy, Nandana, Birudukota, Swarnakumari, Albrecht, Brian K

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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.

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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.

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Design, Synthesis, and Pharmacological Evaluation of Second Generation EZH2 Inhibitors with Long Residence Time von Khanna, Avinash, Côté, Alexandre, Arora, Shilpi, Moine, Ludivine, Gehling, Victor S., Brenneman, Jehrod, Cantone, Nico, Stuckey, Jacob I., Apte, Shruti, Ramakrishnan, Ashwin, Bruderek, Kamil, Bradley, William D., Audia, James E., Cummings, Richard T., Sims, Robert J., Trojer, Patrick, Levell, Julian R.

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A Practical Synthesis of Indoles via a Pd-Catalyzed C–N Ring Formation von Vaswani, Rishi G, Albrecht, Brian K, Audia, James E, Côté, Alexandre, Dakin, Les A, Duplessis, Martin, Gehling, Victor S, Harmange, Jean-Christophe, Hewitt, Michael C, Leblanc, Yves, Nasveschuk, Christopher G, Taylor, Alexander M

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Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors von Gehling, Victor S, McGrath, John P, Duplessis, Martin, Khanna, Avinash, Brucelle, Francois, Vaswani, Rishi G, Côté, Alexandre, Stuckey, Jacob, Watson, Venita, Cummings, Richard T, Balasubramanian, Srividya, Iyer, Priyadarshini, Sawant, Priyanka, Good, Andrew C, Albrecht, Brian K, Harmange, Jean-Christophe, Audia, James E, Bellon, Steven F, Trojer, Patrick, Levell, Julian R

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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

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Development of methyl isoxazoleazepines as inhibitors of BET von Hewitt, Michael C, Leblanc, Yves, Gehling, Victor S, Vaswani, Rishi G, Côté, Alexandre, Nasveschuk, Christopher G, Taylor, Alexander M, Harmange, Jean-Christophe, Audia, James E, Pardo, Eneida, Cummings, Rich, Joshi, Shivangi, Sandy, Peter, Mertz, Jennifer A, Sims, 3rd, Robert J, Bergeron, Louise, Bryant, Barbara M, Bellon, Steve, Poy, Florence, Jayaram, Hariharan, Jayaran, Hariharan, Tang, Yong, Albrecht, Brian K

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EZH2 Inhibitor Efficacy in Non-Hodgkin’s Lymphoma Does Not Require Suppression of H3K27 Monomethylation von Bradley, William D., Arora, Shilpi, Busby, Jennifer, Balasubramanian, Srividya, Gehling, Victor S., Nasveschuk, Christopher G., Vaswani, Rishi G., Yuan, Chih-Chi, Hatton, Charlie, Zhao, Feng, Williamson, Kaylyn E., Iyer, Priyadarshini, Méndez, Jacqui, Campbell, Robert, Cantone, Nico, Garapaty-Rao, Shivani, Audia, James E., Cook, Andrew S., Dakin, Les A., Albrecht, Brian K., Harmange, Jean-Christophe, Daniels, Danette L., Cummings, Richard T., Bryant, Barbara M., Normant, Emmanuel, Trojer, Patrick

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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)-1 H -indole-3-carboxamide (CPI-1... 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.

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From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors von Liang, Jun, Labadie, Sharada, Zhang, Birong, Ortwine, Daniel F., Patel, Snahel, Vinogradova, Maia, Kiefer, James R., Mauer, Till, Gehling, Victor S., Harmange, Jean-Christophe, Cummings, Richard, Lai, Tommy, Liao, Jiangpeng, Zheng, Xiaoping, Liu, Yichin, Gustafson, Amy, Van der Porten, Erica, Mao, Weifeng, Liederer, Bianca M., Deshmukh, Gauri, An, Le, Ran, Yingqing, Classon, Marie, Trojer, Patrick, Dragovich, Peter S., Murray, Lesley

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Abstract 5526: Inhibition of the histone methyl transferase EZH2 causes viability defects in multiple myeloma von Arora, Shilpi, Balasubramanian, Vidya, Williamson, Kaylyn, Gehling, Victor, Nasveschuk, Chris, Vaswani, Rishi, Busby, Jennifer, Garapaty, Shivani, Iyer, Priya, Zhao, Feng, Campbell, Robert, Cummings, Richard, Audia, Jim, Harmange, JC, Albrecht, Brian, Cook, Andrew, Dakin, Les, Normant, Emmanuel, Trojer, Patrick

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CRYSTALLINE FORMS OF 7-CHLORO-2-(4-(3-METHOXYAZETIDIN-1-YL)CYCLOHEXYL)-2,4-DIMETHYL-N-((6-METHYL-4-(METHYLTHIO)-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL)BENZO[D][1,3]DIOXOLE-5-CARBOXAM... von BANDA, Alamelu, GEHLING, Victor

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CRYSTALLINE FORMS OF 7-CHLORO-2-(4-(3-METHOXYAZETIDIN-1-YL)CYCLOHEXYL)-2,4-DIMETHYL-N-((6-METHYL-4-(METHYLTHIO)-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL)BENZO[D][1,3]DIOXOLE-5-CARBOXAM... von BANDA, Alamelu, GEHLING, Victor

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