Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer
Faivre, Emily J., McDaniel, Keith F., Albert, Daniel H., Mantena, Srinivasa R., Plotnik, Joshua P., Wilcox, Denise, Zhang, Lu, Bui, Mai H., Sheppard, George S., Wang, Le, Sehgal, Vasudha, Lin, Xiaoyu, Huang, Xiaoli, Lu, Xin, Uziel, Tamar, Hessler, Paul, Lam, Lloyd T., Bellin, Richard J., Mehta, Gaurav, Fidanze, Steve, Pratt, John K., Liu, Dachun, Hasvold, Lisa A., Sun, Chaohong, Panchal, Sanjay C., Nicolette, John J., Fossey, Stacey L., Park, Chang H., Longenecker, Kenton, Bigelow, Lance, Torrent, Maricel, Rosenberg, Saul H., Kati, Warren M., Shen, Yu
Published in Nature (London) (13.02.2020)
Published in Nature (London) (13.02.2020)
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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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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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Nonsteroidal Selective Glucocorticoid Modulators: The Effect of C-10 Substitution on Receptor Selectivity and Functional Potency of 5-Allyl-2,5-dihydro-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines
Kym, Philip R, Kort, Michael E, Coghlan, Michael J, Moore, Jimmie L, Tang, Rui, Ratajczyk, James D, Larson, Daniel P, Elmore, Steven W, Pratt, John K, Stashko, Michael A, Falls, H. Douglass, Lin, Chun W, Nakane, Masake, Miller, Loan, Tyree, Curtis M, Miner, Jeffery N, Jacobson, Peer B, Wilcox, Denise M, Nguyen, Phong, Lane, Benjamin C
Published in Journal of medicinal chemistry (13.03.2003)
Published in Journal of medicinal chemistry (13.03.2003)
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Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies
Bui, Mai H, Lin, Xiaoyu, Albert, Daniel H, Li, Leiming, Lam, Lloyd T, Faivre, Emily J, Warder, Scott E, Huang, Xiaoli, Wilcox, Denise, Donawho, Cherrie K, Sheppard, George S, Wang, Le, Fidanze, Steve, Pratt, John K, Liu, Dachun, Hasvold, Lisa, Uziel, Tamar, Lu, Xin, Kohlhapp, Fred, Fang, Guowei, Elmore, Steven W, Rosenberg, Saul H, McDaniel, Keith F, Kati, Warren M, Shen, Yu
Published in Cancer research (Chicago, Ill.) (01.06.2017)
Published in Cancer research (Chicago, Ill.) (01.06.2017)
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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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Highlights of the Structure–Activity Relationships of Benzimidazole Linked Pyrrolidines Leading to the Discovery of the Hepatitis C Virus NS5A Inhibitor Pibrentasvir (ABT-530)
Wagner, Rolf, Randolph, John T, Patel, Sachin V, Nelson, Lissa, Matulenko, Mark A, Keddy, Ryan, Pratt, John K, Liu, Dachun, Krueger, A. Chris, Donner, Pamela L, Hutchinson, Douglas K, Flentge, Charles, Betebenner, David, Rockway, Todd, Maring, Clarence J, Ng, Teresa I, Krishnan, Preethi, Pilot-Matias, Tami, Collins, Christine, Panchal, Neeta, Reisch, Thomas, Dekhtyar, Tatyana, Mondal, Rubina, Stolarik, DeAnne F, Gao, Yi, Gao, Wenqing, Beno, David A, Kati, Warren M
Published in Journal of medicinal chemistry (10.05.2018)
Published in Journal of medicinal chemistry (10.05.2018)
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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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Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators
Elmore, Steven W, Pratt, John K, Coghlan, Michael J, Mao, Yue, Green, Brian E, Anderson, David D, Stashko, Michael A, Lin, Chun W, Falls, Douglas, Nakane, Masaki, Miller, Loan, Tyree, Curtis M, Miner, Jeffrey N, Lane, Ben
Published in Bioorganic & medicinal chemistry letters (05.04.2004)
Published in Bioorganic & medicinal chemistry letters (05.04.2004)
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Discovery of pyrido[2,3-d]pyrimidine-based inhibitors of HCV NS5A
DeGoey, David A., Betebenner, David A., Grampovnik, David J., Liu, Dachun, Pratt, John K., Tufano, Michael D., He, Wenping, Krishnan, Preethi, Pilot-Matias, Tami J., Marsh, Kennan C., Molla, Akhteruzzaman, Kempf, Dale J., Maring, Clarence J.
Published in Bioorganic & medicinal chemistry letters (15.06.2013)
Published in Bioorganic & medicinal chemistry letters (15.06.2013)
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Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors
Fidanze, Steven D., Liu, Dachun, Mantei, Robert A., Hasvold, Lisa A., Pratt, John K., Sheppard, George S., Wang, Le, Holms, James H., Dai, Yujia, Aguirre, Ana, Bogdan, Andrew, Dietrich, Justin D., Marjanovic, Jasmina, Park, Chang H., Hutchins, Charles W., Lin, Xiaoyu, Bui, Mai H., Huang, Xiaoli, Wilcox, Denise, Li, Leiming, Wang, Rongqi, Kovar, Peter, Magoc, Terrance J., Rajaraman, Ganesh, Albert, Daniel H., Shen, Yu, Kati, Warren M., McDaniel, Keith F.
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
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Journal Article
Synthesis and Biological Characterization of Aryl Uracil Inhibitors of Hepatitis C Virus NS5B Polymerase: Discovery of ABT-072, a trans-Stilbene Analog with Good Oral Bioavailability
Randolph, John T, Krueger, A. Chris, Donner, Pamela L, Pratt, John K, Liu, Dachun, Motter, Christopher E, Rockway, Todd W, Tufano, Michael D, Wagner, Rolf, Lim, Hock B, Beyer, Jill M, Mondal, Rubina, Panchal, Neeta S, Colletti, Lynn, Liu, Yaya, Koev, Gennadiy, Kati, Warren M, Hernandez, Lisa E, Beno, David W. A, Longenecker, Kenton L, Stewart, Kent D, Dumas, Emily O, Molla, Akhteruzzaman, Maring, Clarence J
Published in Journal of medicinal chemistry (08.02.2018)
Published in Journal of medicinal chemistry (08.02.2018)
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Journal Article
Methylpyrrole inhibitors of BET bromodomains
Hasvold, Lisa A., Sheppard, George S., Wang, Le, Fidanze, Steven D., Liu, Dachun, Pratt, John K., Mantei, Robert A., Wada, Carol K., Hubbard, Robbert, Shen, Yu, Lin, Xiaoyu, Huang, Xiaoli, Warder, Scott E., Wilcox, Denise, Li, Leiming, Buchanan, F. Greg, Smithee, Lauren, Albert, Daniel H., Magoc, Terrance J., Park, Chang H., Petros, Andrew M., Panchal, Sanjay C., Sun, Chaohong, Kovar, Peter, Soni, Nirupama B., Elmore, Steven W., Kati, Warren M., McDaniel, Keith F.
Published in Bioorganic & medicinal chemistry letters (15.05.2017)
Published in Bioorganic & medicinal chemistry letters (15.05.2017)
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Des-A-ring benzothiadiazines: Inhibitors of HCV genotype 1 NS5B RNA-dependent RNA polymerase
Donner, Pamela L., Xie, Qinghua, Pratt, John K., Maring, Clarence J., Kati, Warren, Jiang, Wen, Liu, Yaya, Koev, Gennadiy, Masse, Sherie, Montgomery, Debra, Molla, Akhter, Kempf, Dale J.
Published in Bioorganic & medicinal chemistry (15.04.2008)
Published in Bioorganic & medicinal chemistry (15.04.2008)
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Journal Article
Inhibitors of HCV NS5B polymerase: synthesis and structure–activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines
Pratt, John K., Donner, Pamela, McDaniel, Keith F., Maring, Clarence J., Kati, Warren M., Mo, Hongmei, Middleton, Tim, Liu, Yaya, Ng, Teresa, Xie, Qinghua, Zhang, Rong, Montgomery, Debra, Molla, Akhteruzzaman, Kempf, Dale J., Kohlbrenner, William
Published in Bioorganic & medicinal chemistry letters (15.03.2005)
Published in Bioorganic & medicinal chemistry letters (15.03.2005)
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Inhibitors of HCV NS5B polymerase: Synthesis and structure–activity relationships of N-1-benzyl and N-1-[3-methylbutyl]-4-hydroxy-1,8-naphthyridon-3-yl benzothiadiazine analogs containing substituents on the aromatic ring
Rockway, Todd W., Zhang, Rong, Liu, Dachun, Betebenner, David A., McDaniel, Keith F., Pratt, John K., Beno, David, Montgomery, Debra, Jiang, Wen W., Masse, Sherie, Kati, Warren M., Middleton, Tim, Molla, Akhteruzzaman, Maring, Clarence J., Kempf, Dale J.
Published in Bioorganic & medicinal chemistry letters (15.07.2006)
Published in Bioorganic & medicinal chemistry letters (15.07.2006)
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Journal Article
Inhibitors of Hepatitis C Virus Polymerase: Synthesis and Biological Characterization of Unsymmetrical Dialkyl-Hydroxynaphthalenoyl-benzothiadiazines
Wagner, Rolf, Larson, Daniel P, Beno, David W. A, Bosse, Todd D, Darbyshire, John F, Gao, Yi, Gates, Bradley D, He, Wenping, Henry, Rodger F, Hernandez, Lisa E, Hutchinson, Douglas K, Jiang, Wen W, Kati, Warren M, Klein, Larry L, Koev, Gennadiy, Kohlbrenner, William, Krueger, A. Chris, Liu, Jinrong, Liu, Yaya, Long, Michelle A, Maring, Clarence J, Masse, Sherie V, Middleton, Tim, Montgomery, Debra A, Pratt, John K, Stuart, Patricia, Molla, Akhteruzzaman, Kempf, Dale J
Published in Journal of medicinal chemistry (26.03.2009)
Published in Journal of medicinal chemistry (26.03.2009)
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Identification of halosalicylamide derivatives as a novel class of allosteric inhibitors of HCV NS5B polymerase
Liu, Yaya, Donner, Pamela L., Pratt, John K., Jiang, Wen W., Ng, Teresa, Gracias, Vijaya, Baumeister, Steve, Wiedeman, Paul E., Traphagen, Linda, Warrior, Usha, Maring, Clarence, Kati, Warren M., Djuric, Stevan W., Molla, Akhteruzzaman
Published in Bioorganic & medicinal chemistry letters (01.06.2008)
Published in Bioorganic & medicinal chemistry letters (01.06.2008)
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Journal Article
Nonsteroidal Selective Glucocorticoid Modulators: the Effect of C-5 Alkyl Substitution on the Transcriptional Activation/Repression Profile of 2,5-Dihydro-10-methoxy-2,2,4-trimethyl-1H-[1]benzopyrano[3,4-f]quinolines
Elmore, Steven W, Coghlan, Michael J, Anderson, David D, Pratt, John K, Green, Brian E, Wang, Alan X, Stashko, Michael A, Lin, Chun W, Tyree, Curtis M, Miner, Jeffery N, Jacobson, Peer B, Wilcox, Denise M, Lane, Benjamin C
Published in Journal of medicinal chemistry (06.12.2001)
Published in Journal of medicinal chemistry (06.12.2001)
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