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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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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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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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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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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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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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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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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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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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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Corrigendum to “Development of methyl isoxazoleazepines as inhibitors of BET” [Bioorg. Med. Chem. Lett. 25/9 (2015) 1842–1848] 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, Robert J., Bergeron, Louise, Bryant, Barbara M., Bellon, Steve, Poy, Florence, Jayaram, Hariharan, Tang, Yong, Albrecht, Brian K.

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7-클로로-2--2,4-디메틸-N-벤조[D][1,3]디옥솔-5-카르복사미드의 결정질 형태 von GEHLING VICTOR S, BANDA ALAMELU

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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, S

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