HEXIM1 as a Robust Pharmacodynamic Marker for Monitoring Target Engagement of BET Family Bromodomain Inhibitors in Tumors and Surrogate Tissues von Lin, Xiaoyu, Huang, Xiaoli, Uziel, Tamar, Hessler, Paul, Albert, Daniel H, Roberts-Rapp, Lisa A, McDaniel, Keith F, Kati, Warren M, Shen, Yu

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Identification of Highly Potent Human Immunodeficiency Virus Type‑1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomim... von Hidaka, Koushi, Kimura, Tooru, Sankaranarayanan, Rajesh, Wang, Jun, McDaniel, Keith F, Kempf, Dale J, Kameoka, Masanori, Adachi, Motoyasu, Kuroki, Ryota, Nguyen, Jeffrey-Tri, Hayashi, Yoshio, Kiso, Yoshiaki

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Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer von 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

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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 I... von 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

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In Vitro Antiviral Activity and Resistance Profile of the Next-Generation Hepatitis C Virus NS3/4A Protease Inhibitor Glecaprevir von Ng, Teresa I, Tripathi, Rakesh, Reisch, Thomas, Lu, Liangjun, Middleton, Timothy, Hopkins, Todd A, Pithawalla, Ron, Irvin, Michelle, Dekhtyar, Tatyana, Krishnan, Preethi, Schnell, Gretja, Beyer, Jill, McDaniel, Keith F, Ma, Jun, Wang, Guoqiang, Jiang, Li-Juan, Or, Yat Sun, Kempf, Dale, Pilot-Matias, Tami, Collins, Christine

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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 Bromodom... von 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

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Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies von 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

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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 Br... von 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

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Selective Inhibition of the Second Bromodomain of BET Family Proteins Results in Robust Antitumor Activity in Preclinical Models of Acute Myeloid Leukemia von Zhang, Lu, Cai, Tianyu, Lin, Xiaoyu, Huang, Xiaoli, Bui, Mai H, Plotnik, Joshua P, Bellin, Richard J, Faivre, Emily J, Kuruvilla, Vinitha M, Lam, Lloyd T, Lu, Xin, Zha, Zheng, Feng, Weiguo, Hessler, Paul, Uziel, Tamar, Zhang, Qi, Cavazos, Antonio, Han, Lina, Ferguson, Debra C, Mehta, Gaurav, Shanmugavelandy, Sriram S, Magoc, Terrance J, Rowe, Jenny, Goodwin, Neal C, Dorritie, Kathleen A, Boyiadzis, Michael, Albert, Daniel H, McDaniel, Keith F, Kati, Warren M, Konopleva, Marina, Shen, Yu

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Novel Physics-Based Ensemble Modeling Approach That Utilizes 3D Molecular Conformation and Packing to Access Aqueous Thermodynamic Solubility: A Case Study of Orally Available Brom... von Hong, Richard S, Mattei, Alessandra, Sheikh, Ahmad Y, Bhardwaj, Rajni Miglani, Bellucci, Michael A, McDaniel, Keith F, Pierce, M. Olivia, Sun, Guangxu, Li, Sizhu, Wang, Lingle, Mondal, Sayan, Ji, Jianguo, Borchardt, Thomas B

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Small-Sized Human Immunodeficiency Virus Type-1 Protease Inhibitors Containing Allophenylnorstatine to Explore the S2′ Pocket von Hidaka, Koushi, Kimura, Tooru, Abdel-Rahman, Hamdy M, Nguyen, Jeffrey-Tri, McDaniel, Keith F, Kohlbrenner, William E, Molla, Akhteruzzaman, Adachi, Motoyasu, Tamada, Taro, Kuroki, Ryota, Katsuki, Noriko, Tanaka, Yoshiaki, Matsumoto, Hikaru, Wang, Jun, Hayashi, Yoshio, Kempf, Dale J, Kiso, Yoshiaki

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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 von 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

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Co-clinical Modeling of the Activity of the BET Inhibitor Mivebresib (ABBV-075) in AML von ALBERT, DANIEL H., GOODWIN, NEAL C., DAVIES, ANGELA M., ROWE, JENNY, FEUER, GEROLD, BOYIADZIS, MICHAEL, DORRITIE, KATHLEEN A., MANCINI, MARIA, GANDOUR-EDWARDS, REGINA, JONAS, BRIAN A., BORTHAKUR, GAUTAM, ALDOSS, IBRAHIM, RIZZIERI, DAVID A., ODENIKE, OLATOYOSI, PREBET, THOMAS, SINGH, SANJANA, POPOVIC, RELJA, SHEN, YU, MCDANIEL, KEITH F., KATI, WARREN M., MODI, DIMPLE A., MOTWANI, MONICA, WOLFF, JOHANNES E., FROST, DAVID J.

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Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors von 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.

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Methylpyrrole inhibitors of BET bromodomains von 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.

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Novel Hepatitis C virus replicon inhibitors: Synthesis and structure–activity relationships of fused pyrimidine derivatives von Chris Krueger, A., Madigan, Darold L., Beno, David W., Betebenner, David A., Carrick, Robert, Green, Brian E., He, Wenping, Liu, Dachun, Maring, Clarence J., McDaniel, Keith F., Mo, Hongmei, Molla, Akhteruzzaman, Motter, Christopher E., Pilot-Matias, Tami J., Tufano, Michael D., Kempf, Dale J.

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Water-Soluble Prodrugs of the Human Immunodeficiency Virus Protease Inhibitors Lopinavir and Ritonavir von DeGoey, David A, Grampovnik, David J, Flosi, William J, Marsh, Kennan C, Wang, Xiu C, Klein, Larry L, McDaniel, Keith F, Liu, Yaya, Long, Michelle A, Kati, Warren M, Molla, Akhteruzzaman, Kempf, Dale J

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Design and synthesis of pseudo-Symmetric HIV protease inhibitors containing a novel hydroxymethylcarbonyl (HMC)-Hydrazide isostere von Hidaka, Koushi, Kimura, Tooru, Hayashi, Yoshio, McDaniel, Keith F, Dekhtyar, Tatyana, Colletti, Lynn, Kiso, Yoshiaki

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Inhibitors of HCV NS5B polymerase: synthesis and structure–activity relationships of N-1-heteroalkyl-4-hydroxyquinolon-3-yl-benzothiadiazines von 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

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Palladium-catalyzed reactions in the synthesis of 3- and 4-substituted indoles. 2. Total synthesis of the N-acetyl methyl ester of (.+-.)-clavicipitic acids von Harrington, Peter J, Hegedus, Louis S, McDaniel, Keith F

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