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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Discovery of 1H‑Pyrazol-3(2H)‑ones as Potent and Selective Inhibitors of Protein Kinase R‑like Endoplasmic Reticulum Kinase (PERK)
Smith, Adrian L, Andrews, Kristin L, Beckmann, Holger, Bellon, Steven F, Beltran, Pedro J, Booker, Shon, Chen, Hao, Chung, Young-Ah, D’Angelo, Noel D, Dao, Jennifer, Dellamaggiore, Kenneth R, Jaeckel, Peter, Kendall, Richard, Labitzke, Katja, Long, Alexander M, Materna-Reichelt, Silvia, Mitchell, Petia, Norman, Mark H, Powers, David, Rose, Mark, Shaffer, Paul L, Wu, Michelle M, Lipford, J. Russell
Published in Journal of medicinal chemistry (12.02.2015)
Published in Journal of medicinal chemistry (12.02.2015)
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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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Structure-Based Design of Novel Class II c-Met Inhibitors: 1. Identification of Pyrazolone-Based Derivatives
Norman, Mark H, Liu, Longbin, Lee, Matthew, Xi, Ning, Fellows, Ingrid, D’Angelo, Noel D, Dominguez, Celia, Rex, Karen, Bellon, Steven F, Kim, Tae-Seong, Dussault, Isabelle
Published in Journal of medicinal chemistry (08.03.2012)
Published in Journal of medicinal chemistry (08.03.2012)
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Structure-Based Design of Novel Class II c-Met Inhibitors: 2. SAR and Kinase Selectivity Profiles of the Pyrazolone Series
Liu, Longbin, Norman, Mark H, Lee, Matthew, Xi, Ning, Siegmund, Aaron, Boezio, Alessandro A, Booker, Shon, Choquette, Debbie, D’Angelo, Noel D, Germain, Julie, Yang, Kevin, Yang, Yajing, Zhang, Yihong, Bellon, Steven F, Whittington, Douglas A, Harmange, Jean-Christophe, Dominguez, Celia, Kim, Tae-Seong, Dussault, Isabelle
Published in Journal of medicinal chemistry (08.03.2012)
Published in Journal of medicinal chemistry (08.03.2012)
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Journal Article
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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c-Met Inhibitors with Novel Binding Mode Show Activity against Several Hereditary Papillary Renal Cell Carcinoma-related Mutations
Bellon, Steven F., Kaplan-Lefko, Paula, Yang, Yajing, Zhang, Yihong, Moriguchi, Jodi, Rex, Karen, Johnson, Carol W., Rose, Paul E., Long, Alexander M., O'Connor, Anne B., Gu, Yan, Coxon, Angela, Kim, Tae-Seong, Tasker, Andrew, Burgess, Teresa L., Dussault, Isabelle
Published in The Journal of biological chemistry (01.02.2008)
Published in The Journal of biological chemistry (01.02.2008)
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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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The Structure of Dimeric ROCK I Reveals the Mechanism for Ligand Selectivity
Jacobs, Marc, Hayakawa, Koto, Swenson, Lora, Bellon, Steven, Fleming, Mark, Taslimi, Paul, Doran, John
Published in The Journal of biological chemistry (06.01.2006)
Published in The Journal of biological chemistry (06.01.2006)
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Journal Article
Discovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase
Albrecht, Brian K, Harmange, Jean-Christophe, Bauer, David, Berry, Loren, Bode, Christiane, Boezio, Alessandro A, Chen, April, Choquette, Deborah, Dussault, Isabelle, Fridrich, Cary, Hirai, Satoko, Hoffman, Doug, Larrow, Jay F, Kaplan-Lefko, Paula, Lin, Jasmine, Lohman, Julia, Long, Alexander M, Moriguchi, Jodi, O’Connor, Anne, Potashman, Michele H, Reese, Monica, Rex, Karen, Siegmund, Aaron, Shah, Kavita, Shimanovich, Roman, Springer, Stephanie K, Teffera, Yohannes, Yang, Yajing, Zhang, Yihong, Bellon, Steven F
Published in Journal of medicinal chemistry (22.05.2008)
Published in Journal of medicinal chemistry (22.05.2008)
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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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Journal Article
Design and Synthesis of Styrenylcyclopropylamine LSD1 Inhibitors
Gehling, Victor S., Mcgrath, John P., Duplessis, Martin, Khanna, Avinash, Brucelle, Francois, Vaswani, Rishi G., Cote, Alexandre, Stuckey, Jacob, Watson, Venita, Cummings, Richard T., Balasubramanian, Srividya, Iyer, Priya, Sawant, Priyanka, Good, Andrew C., Albrecht, Brian K., Harmange, Jean-Christophe, Audia, James E., Bellon, Steven F., Trojer, Patrick, Levell, Julian R.
Published in ACS medicinal chemistry letters (11.06.2020)
Published in ACS medicinal chemistry letters (11.06.2020)
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Discovery of a Potent, Selective, and Orally Bioavailable c-Met Inhibitor: 1-(2-Hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458)
Liu, Longbin, Siegmund, Aaron, Xi, Ning, Kaplan-Lefko, Paula, Rex, Karen, Chen, April, Lin, Jasmine, Moriguchi, Jodi, Berry, Loren, Huang, Liyue, Teffera, Yohannes, Yang, Yajing, Zhang, Yihong, Bellon, Steven F, Lee, Matthew, Shimanovich, Roman, Bak, Annette, Dominguez, Celia, Norman, Mark H, Harmange, Jean-Christophe, Dussault, Isabelle, Kim, Tae-Seong
Published in Journal of medicinal chemistry (10.07.2008)
Published in Journal of medicinal chemistry (10.07.2008)
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Journal Article
Design, Synthesis, and Biological Evaluation of Potent c-Met Inhibitors
D’Angelo, Noel D, Bellon, Steven F, Booker, Shon K, Cheng, Yuan, Coxon, Angela, Dominguez, Celia, Fellows, Ingrid, Hoffman, Douglas, Hungate, Randall, Kaplan-Lefko, Paula, Lee, Matthew R, Li, Chun, Liu, Longbin, Rainbeau, Elizabeth, Reider, Paul J, Rex, Karen, Siegmund, Aaron, Sun, Yaxiong, Tasker, Andrew S, Xi, Ning, Xu, Shimin, Yang, Yajing, Zhang, Yihong, Burgess, Teresa L, Dussault, Isabelle, Kim, Tae-Seong
Published in Journal of medicinal chemistry (25.09.2008)
Published in Journal of medicinal chemistry (25.09.2008)
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Journal Article
The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor
Duffy, John P, Harrington, Edmund M, Salituro, Francesco G, Cochran, John E, Green, Jeremy, Gao, Huai, Bemis, Guy W, Evindar, Ghotas, Galullo, Vincent P, Ford, Pamella J, Germann, Ursula A, Wilson, Keith P, Bellon, Steven F, Chen, Guanging, Taslimi, Paul, Jones, Peter, Huang, Cassey, Pazhanisamy, S, Wang, Yow-Ming, Murcko, Mark A, Su, Michael S.S
Published in ACS medicinal chemistry letters (13.10.2011)
Published in ACS medicinal chemistry letters (13.10.2011)
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Journal Article
Correction to 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 (14.05.2015)
Published in Journal of medicinal chemistry (14.05.2015)
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Journal Article
Crystal Structures of Escherichia coli Topoisomerase IV ParE Subunit (24 and 43 Kilodaltons): a Single Residue Dictates Differences in Novobiocin Potency against Topoisomerase IV and DNA Gyrase
BELLON, Steven, PARSONS, Jonathan D, YUNYI WEI, HAYAKAWA, Koto, SWENSON, Lora L, CHARIFSON, Paul S, LIPPKE, Judith A, ALDAPE, Robert, GROSS, Christian H
Published in Antimicrobial Agents and Chemotherapy (01.05.2004)
Published in Antimicrobial Agents and Chemotherapy (01.05.2004)
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Journal Article
Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors
Boezio, Alessandro A., Berry, Loren, Albrecht, Brian K., Bauer, David, Bellon, Steven F., Bode, Christiane, Chen, April, Choquette, Deborah, Dussault, Isabelle, Hirai, Satoko, Kaplan-Lefko, Paula, Larrow, Jay F., Lin, Min-Hwa Jasmine, Lohman, Julia, Potashman, Michele H., Rex, Karen, Santostefano, Michael, Shah, Kavita, Shimanovich, Roman, Springer, Stephanie K., Teffera, Yohannes, Yang, Yajing, Zhang, Yihong, Harmange, Jean-Christophe
Published in Bioorganic & medicinal chemistry letters (15.11.2009)
Published in Bioorganic & medicinal chemistry letters (15.11.2009)
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