Discovery of N‑Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo‑1H‑pyrrolo[2,3‑c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain
Sheppard, George S, Wang, Le, Fidanze, Steven D, Hasvold, Lisa A, Liu, Dachun, Pratt, John K, Park, Chang H, Longenecker, Kenton, Qiu, Wei, Torrent, Maricel, Kovar, Peter J, Bui, Mai, Faivre, Emily, Huang, Xiaoli, Lin, Xiaoyu, Wilcox, Denise, Zhang, Lu, Shen, Yu, Albert, Daniel H, Magoc, Terrance J, Rajaraman, Ganesh, Kati, Warren M, McDaniel, Keith F
Published in Journal of medicinal chemistry (28.05.2020)
Published in Journal of medicinal chemistry (28.05.2020)
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Journal Article
Discovery of N -Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1 H -pyrrolo[2,3- c ]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain
Sheppard, George S, Wang, Le, Fidanze, Steven D, Hasvold, Lisa A, Liu, Dachun, Pratt, John K, Park, Chang H, Longenecker, Kenton, Qiu, Wei, Torrent, Maricel, Kovar, Peter J, Bui, Mai, Faivre, Emily, Huang, Xiaoli, Lin, Xiaoyu, Wilcox, Denise, Zhang, Lu, Shen, Yu, Albert, Daniel H, Magoc, Terrance J, Rajaraman, Ganesh, Kati, Warren M, McDaniel, Keith F
Published in Journal of medicinal chemistry (28.05.2020)
Published in Journal of medicinal chemistry (28.05.2020)
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Discovery of N‑(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro‑1H‑pyrrolo[2,3‑c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor
McDaniel, Keith F, Wang, Le, Soltwedel, Todd, Fidanze, Steven D, Hasvold, Lisa A, Liu, Dachun, Mantei, Robert A, Pratt, John K, Sheppard, George S, Bui, Mai H, Faivre, Emily J, Huang, Xiaoli, Li, Leiming, Lin, Xiaoyu, Wang, Rongqi, Warder, Scott E, Wilcox, Denise, Albert, Daniel H, Magoc, Terrance J, Rajaraman, Ganesh, Park, Chang H, Hutchins, Charles W, Shen, Jianwei J, Edalji, Rohinton P, Sun, Chaohong C, Martin, Ruth, Gao, Wenqing, Wong, Shekman, Fang, Guowei, Elmore, Steven W, Shen, Yu, Kati, Warren M
Published in Journal of medicinal chemistry (26.10.2017)
Published in Journal of medicinal chemistry (26.10.2017)
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Structure-Guided Design of a Series of MCL‑1 Inhibitors with High Affinity and Selectivity
Bruncko, Milan, Wang, Le, Sheppard, George S, Phillips, Darren C, Tahir, Stephen K, Xue, John, Erickson, Scott, Fidanze, Steve, Fry, Elizabeth, Hasvold, Lisa, Jenkins, Gary J, Jin, Sha, Judge, Russell A, Kovar, Peter J, Madar, David, Nimmer, Paul, Park, Chang, Petros, Andrew M, Rosenberg, Saul H, Smith, Morey L, Song, Xiaohong, Sun, Chaohong, Tao, Zhi-Fu, Wang, Xilu, Xiao, Yu, Zhang, Haichao, Tse, Chris, Leverson, Joel D, Elmore, Steven W, Souers, Andrew J
Published in Journal of medicinal chemistry (12.03.2015)
Published in Journal of medicinal chemistry (12.03.2015)
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Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors
Wang, Le, Pratt, John K, Soltwedel, Todd, Sheppard, George S, Fidanze, Steven D, Liu, Dachun, Hasvold, Lisa A, Mantei, Robert A, Holms, James H, McClellan, William J, Wendt, Michael D, Wada, Carol, Frey, Robin, Hansen, T. Matthew, Hubbard, Robert, Park, Chang H, Li, Leiming, Magoc, Terrance J, Albert, Daniel H, Lin, Xiaoyu, Warder, Scott E, Kovar, Peter, Huang, Xiaoli, Wilcox, Denise, Wang, Rongqi, Rajaraman, Ganesh, Petros, Andrew M, Hutchins, Charles W, Panchal, Sanjay C, Sun, Chaohong, Elmore, Steven W, Shen, Yu, Kati, Warren M, McDaniel, Keith F
Published in Journal of medicinal chemistry (11.05.2017)
Published in Journal of medicinal chemistry (11.05.2017)
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Correction to Structure-Guided Design of a Series of MCL‑1 Inhibitors with High Affinity and Selectivity
Bruncko, Milan, Wang, Le, Sheppard, George S, Phillips, Darren C, Tahir, Stephen K, Xue, John, Erickson, Scott, Fidanze, Steve, Fry, Elizabeth, Hasvold, Lisa, Jenkins, Gary J, Jin, Sha, Judge, Russell A, Kovar, Peter J, Madar, David, Nimmer, Paul, Park, Chang, Petros, Andrew M, Rosenberg, Saul H, Smith, Morey L, Song, Xiaohong, Sun, Chaohong, Tao, Zhi-Fu, Wang, Xilu, Xiao, Yu, Zhang, Haichao, Tse, Chris, Leverson, Joel D, Elmore, Steven W, Souers, Andrew J
Published in Journal of medicinal chemistry (14.05.2015)
Published in Journal of medicinal chemistry (14.05.2015)
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Discovery and Optimization of Anthranilic Acid Sulfonamides as Inhibitors of Methionine Aminopeptidase-2: A Structural Basis for the Reduction of Albumin Binding
Sheppard, George S, Wang, Jieyi, Kawai, Megumi, Fidanze, Steve D, BaMaung, Nwe Y, Erickson, Scott A, Barnes, David M, Tedrow, Jason S, Kolaczkowski, Lawrence, Vasudevan, Anil, Park, David C, Wang, Gary T, Sanders, William J, Mantei, Robert A, Palazzo, Fabio, Tucker-Garcia, Lora, Lou, Pingping, Zhang, Qian, Park, Chang H, Kim, Ki H, Petros, Andrew, Olejniczak, Edward, Nettesheim, David, Hajduk, Phillip, Henkin, Jack, Lesniewski, Richard, Davidsen, Steven K, Bell, Randy L
Published in Journal of medicinal chemistry (29.06.2006)
Published in Journal of medicinal chemistry (29.06.2006)
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The Role of Platelet-Activating Factor (PAF) and the Efficacy of ABT-491, a Highly Potent and Selective PAF Antagonist, in Experimental Allergic Rhinitis
Albert, D H, Malo, P E, Tapang, P, Shaughnessy, T K, Morgan, D W, Wegner, C D, Curtin, M L, Sheppard, G S, Xu, L, Davidsen, S K, Summers, J B, Carter, G W
Published in The Journal of pharmacology and experimental therapeutics (01.01.1998)
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Published in The Journal of pharmacology and experimental therapeutics (01.01.1998)
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Pharmacology of ABT-491, a highly potent platelet-activating factor receptor antagonist
Albert, Daniel H., Magoc, Terrance J., Tapang, Paul, Luo, Gongjin, Morgan, Douglas W., Curtin, Michael, Sheppard, George S., Xu, Lianhong, Heyman, H.Robin, Davidsen, Steven K., Summers, James B., Carter, George W.
Published in European journal of pharmacology (23.04.1997)
Published in European journal of pharmacology (23.04.1997)
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3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a Novel Series of Platelet Activating Factor Antagonists
Sheppard, George S, Pireh, Daisy, Carrera, George M, Bures, Mark G, Heyman, H. Robin, Steinman, Douglas H, Davidsen, Steven K, Phillips, James G, Guinn, Denise E, May, Paul D, Conway, Richard D, Rhein, David A, Calhoun, William C, Albert, Daniel H, Magoc, Terrance J, Carter, George W, Summers, James B
Published in Journal of medicinal chemistry (01.06.1994)
Published in Journal of medicinal chemistry (01.06.1994)
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Why optimize cancer drugs for ADMET?
Sheppard, George S., Bouska, Jennifer J.
Published in Drug discovery today. Therapeutic strategies (2005)
Published in Drug discovery today. Therapeutic strategies (2005)
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