Implications of the Conformationally Flexible, Macrocyclic Structure of the First-Generation, Direct-Acting Anti-Viral Paritaprevir on Its Solid Form Complexity and Chameleonic Behavior
Sheikh, Ahmad Y., Mattei, Alessandra, Miglani Bhardwaj, Rajni, Hong, Richard S., Abraham, Nathan S., Schneider-Rauber, Gabriela, Engstrom, Kenneth M., Diwan, Moiz, Henry, Rodger F., Gao, Yi, Juarez, Vivian, Jordan, Erin, DeGoey, David A., Hutchins, Charles W.
Published in Journal of the American Chemical Society (27.10.2021)
Published in Journal of the American Chemical Society (27.10.2021)
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Journal Article
CRISPR Screen Reveals BRD2/4 Molecular Glue-like Degrader via Recruitment of DCAF16
Shergalis, Andrea G., Marin, Violeta L., Rhee, David Y., Senaweera, Sameera, McCloud, Rebecca L., Ronau, Judith A., Hutchins, Charles W., McLoughlin, Shaun, Woller, Kevin R., Warder, Scott E., Vasudevan, Anil, Reitsma, Justin M.
Published in ACS chemical biology (17.02.2023)
Published in ACS chemical biology (17.02.2023)
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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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Journal Article
Discovery of Novel and Highly Selective Inhibitors of Calpain for the Treatment of Alzheimer’s Disease: 2‑(3-Phenyl‑1H‑pyrazol-1-yl)-nicotinamides
Kling, Andreas, Jantos, Katja, Mack, Helmut, Hornberger, Wilfried, Drescher, Karla, Nimmrich, Volker, Relo, Ana, Wicke, Karsten, Hutchins, Charles W, Lao, Yanbin, Marsh, Kennan, Moeller, Achim
Published in Journal of medicinal chemistry (24.08.2017)
Published in Journal of medicinal chemistry (24.08.2017)
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Journal Article
Discovery of a Potent Chloroacetamide GPX4 Inhibitor with Bioavailability to Enable Target Engagement in Mice, a Potential Tool Compound for Inducing Ferroptosis In Vivo
Randolph, John T., O’Connor, Matthew J., Han, Fei, Hutchins, Charles W., Siu, Y. Amy, Cho, Min, Zheng, Yunan, Hickson, Jonathan A., Markley, Jana L., Manaves, Vlasios, Algire, Mikkel, Baker, Kenton A., Chapman, Alex M., Gopalakrishnan, Sujatha M., Panchal, Sanjay C., Foster-Duke, Kelly, Stolarik, DeAnne F., Kempf-Grote, Anita, Dammeier, Darby, Fossey, Stacey, Sun, Qi, Sun, Chaohong, Shen, Yu, Dart, Michael J., Kati, Warren M., Lai, Albert, Firestone, Ari J., Kort, Michael E.
Published in Journal of medicinal chemistry (23.03.2023)
Published in Journal of medicinal chemistry (23.03.2023)
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Journal Article
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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Journal Article
Discovery of ABT-267, a Pan-Genotypic Inhibitor of HCV NS5A
DeGoey, David A., Randolph, John T., Liu, Dachun, Pratt, John, Hutchins, Charles, Donner, Pamela, Krueger, A. Chris, Matulenko, Mark, Patel, Sachin, Motter, Christopher E., Nelson, Lissa, Keddy, Ryan, Tufano, Michael, Caspi, Daniel D., Krishnan, Preethi, Mistry, Neeta, Koev, Gennadiy, Reisch, Thomas J., Mondal, Rubina, Pilot-Matias, Tami, Gao, Yi, Beno, David W. A., Maring, Clarence J., Molla, Akhter, Dumas, Emily, Campbell, Andrew, Williams, Laura, Collins, Christine, Wagner, Rolf, Kati, Warren M.
Published in Journal of medicinal chemistry (13.03.2014)
Published in Journal of medicinal chemistry (13.03.2014)
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Journal Article
Novel, potent, selective and brain penetrant vasopressin 1b receptor antagonists
Geneste, Hervé, Bhowmik, Swati, van Gaalen, Marcel M., Hornberger, Wilfried, Hutchins, Charles W., Netz, Astrid, Oost, Thorsten, Unger, Liliane
Published in Bioorganic & medicinal chemistry letters (15.10.2018)
Published in Bioorganic & medicinal chemistry letters (15.10.2018)
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Journal Article
Discovery of Small Molecule Interleukin 17A Inhibitors with Novel Binding Mode and Stoichiometry: Optimization of DNA-Encoded Chemical Library Hits to In Vivo Active Compounds
Ramos, Ashley L., Goedken, Eric R., Frank, Kristine E., Argiriadi, Maria A., Bazzaz, Sana, Bian, Zhiguo, Brown, Jesse T. C., Centrella, Paolo A., Chen, Hui-Ju, Disch, Jeremy S., Donner, Pamela L., Duignan, David B., Gikunju, Diana, Greszler, Stephen N., Guié, Marie-Aude, Habeshian, Sevan, Hartl, Hajnalka E., Hein, Christopher D., Hutchins, Charles W., Jetson, Rachael, Keefe, Anthony D., Khan, Hasan, Li, Huan-Qiu, Olszewski, Allison, Ortiz Cardona, Benjamin J., Osuma, Augustine, Panchal, Sanjay C., Phelan, Ryan, Qiu, Wei, Shotwell, J. Brad, Shrestha, Anurupa, Srikumaran, Myron, Su, Zhi, Sun, Chaohong, Upadhyay, Anup K., Wood, Michael D., Wu, Haihong, Zhang, Ruijie, Zhang, Ying, Zhao, Gang, Zhu, Haizhong, Webster, Matthew P.
Published in Journal of medicinal chemistry (25.04.2024)
Published in Journal of medicinal chemistry (25.04.2024)
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Journal Article
Analgesic potential of TRPV1 antagonists
Kym, Philip R., Kort, Michael E., Hutchins, Charles W.
Published in Biochemical pharmacology (01.08.2009)
Published in Biochemical pharmacology (01.08.2009)
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Journal Article
Mechanistic insights into a heterobifunctional degrader-induced PTPN2/N1 complex
Hao, Qi, Rathinaswamy, Manoj K., Klinge, Kelly L., Bratkowski, Matthew, Mafi, Amirhossein, Baumgartner, Christina K., Hamel, Keith M., Veits, Gesine K., Jain, Rinku, Catalano, Claudio, Fitzgerald, Mark, Hird, Alexander W., Park, Eunice, Vora, Harit U., Henderson, James A., Longenecker, Kenton, Hutchins, Charles W., Qiu, Wei, Scapin, Giovanna, Sun, Qi, Stoll, Vincent S., Sun, Chaohong, Li, Ping, Eaton, Dan, Stokoe, David, Fisher, Stewart L., Nasveschuk, Christopher G., Paddock, Marcia, Kort, Michael E.
Published in Communications chemistry (16.08.2024)
Published in Communications chemistry (16.08.2024)
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Journal Article
Molecular Determinants of Species-Specific Activation or Blockade of TRPA1 Channels
Chen, Jun, Zhang, Xu-Feng, Kort, Michael E, Huth, Jeffrey R, Sun, Chaohong, Miesbauer, Laura J, Cassar, Steven C, Neelands, Torben, Scott, Victoria E, Moreland, Robert B, Reilly, Regina M, Hajduk, Philip J, Kym, Philip R, Hutchins, Charles W, Faltynek, Connie R
Published in The Journal of neuroscience (07.05.2008)
Published in The Journal of neuroscience (07.05.2008)
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Journal Article
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
Discovery of a Potent, Selective Protein Tyrosine Phosphatase 1B Inhibitor Using a Linked-Fragment Strategy
Szczepankiewicz, Bruce G, Liu, Gang, Hajduk, Philip J, Abad-Zapatero, Cele, Pei, Zhonghua, Xin, Zhili, Lubben, Thomas H, Trevillyan, James M, Stashko, Michael A, Ballaron, Stephen J, Liang, Heng, Huang, Flora, Hutchins, Charles W, Fesik, Stephen W, Jirousek, Michael R
Published in Journal of the American Chemical Society (09.04.2003)
Published in Journal of the American Chemical Society (09.04.2003)
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Journal Article
Fragment Screening and Assembly: A Highly Efficient Approach to a Selective and Cell Active Protein Tyrosine Phosphatase 1B Inhibitor
Liu, Gang, Xin, Zhili, Pei, Zhonghua, Hajduk, Philip J, Abad-Zapatero, Cele, Hutchins, Charles W, Zhao, Hongyu, Lubben, Thomas H, Ballaron, Stephen J, Haasch, Deanna L, Kaszubska, Wiweka, Rondinone, Cristina M, Trevillyan, James M, Jirousek, Michael R
Published in Journal of medicinal chemistry (25.09.2003)
Published in Journal of medicinal chemistry (25.09.2003)
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Journal Article
Aminopyridine-Based c-Jun N-Terminal Kinase Inhibitors with Cellular Activity and Minimal Cross-Kinase Activity
Szczepankiewicz, Bruce G, Kosogof, Christi, Nelson, Lissa T. J, Liu, Gang, Liu, Bo, Zhao, Hongyu, Serby, Michael D, Xin, Zhili, Liu, Mei, Gum, Rebecca J, Haasch, Deanna L, Wang, Sanyi, Clampit, Jill E, Johnson, Eric F, Lubben, Thomas H, Stashko, Michael A, Olejniczak, Edward T, Sun, Chaohong, Dorwin, Sarah A, Haskins, Kristi, Abad-Zapatero, Cele, Fry, Elizabeth H, Hutchins, Charles W, Sham, Hing L, Rondinone, Cristina M, Trevillyan, James M
Published in Journal of medicinal chemistry (15.06.2006)
Published in Journal of medicinal chemistry (15.06.2006)
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Journal Article
Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8
Judge, Russell A, Zhu, Haizhong, Upadhyay, Anup K, Bodelle, Pierre M, Hutchins, Charles W, Torrent, Maricel, Marin, Violeta L, Yu, Wenyu, Vedadi, Masoud, Li, Fengling, Brown, Peter J, Pappano, William N, Sun, Chaohong, Petros, Andrew M
Published in ACS medicinal chemistry letters (08.12.2016)
Published in ACS medicinal chemistry letters (08.12.2016)
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Journal Article
Potent and conditional redirected T cell killing of tumor cells using Half DVD-Ig
Bardwell, Philip D., Staron, Matthew M., Liu, Junjian, Tao, Qingfeng, Scesney, Susanne, Bukofzer, Gail, Rodriguez, Luis E., Choi, Chee-Ho, Wang, Jennifer, Chang, Qing, Dong, Feng, Donawho, Cherrie, Wang, Jieyi, Grinnell, Christine M., Tarcsa, Edit, Hutchins, Charles, Ghayur, Tariq, Gu, Jijie
Published in Protein & cell (01.01.2018)
Published in Protein & cell (01.01.2018)
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Journal Article
Ligand association rates to the inner-variable-domain of a dual-variable-domain immunoglobulin are significantly impacted by linker design
DiGiammarino, Enrico L., Harlan, John E., Walter, Karl A., Ladror, Uri S., Edalji, Rohinton P., Hutchins, Charles W., Lake, Marc R., Greischar, Amy J., Liu, Junjian, Ghayur, Tariq, Jakob, Clarissa G.
Published in mAbs (01.09.2011)
Published in mAbs (01.09.2011)
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