Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases
Harris, Philip A, Berger, Scott B, Jeong, Jae U, Nagilla, Rakesh, Bandyopadhyay, Deepak, Campobasso, Nino, Capriotti, Carol A, Cox, Julie A, Dare, Lauren, Dong, Xiaoyang, Eidam, Patrick M, Finger, Joshua N, Hoffman, Sandra J, Kang, James, Kasparcova, Viera, King, Bryan W, Lehr, Ruth, Lan, Yunfeng, Leister, Lara K, Lich, John D, MacDonald, Thomas T, Miller, Nathan A, Ouellette, Michael T, Pao, Christina S, Rahman, Attiq, Reilly, Michael A, Rendina, Alan R, Rivera, Elizabeth J, Schaeffer, Michelle C, Sehon, Clark A, Singhaus, Robert R, Sun, Helen H, Swift, Barbara A, Totoritis, Rachel D, Vossenkämper, Anna, Ward, Paris, Wisnoski, David D, Zhang, Daohua, Marquis, Robert W, Gough, Peter J, Bertin, John
Published in Journal of medicinal chemistry (23.02.2017)
Published in Journal of medicinal chemistry (23.02.2017)
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DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors
Harris, Philip A, King, Bryan W, Bandyopadhyay, Deepak, Berger, Scott B, Campobasso, Nino, Capriotti, Carol A, Cox, Julie A, Dare, Lauren, Dong, Xiaoyang, Finger, Joshua N, Grady, LaShadric C, Hoffman, Sandra J, Jeong, Jae U, Kang, James, Kasparcova, Viera, Lakdawala, Ami S, Lehr, Ruth, McNulty, Dean E, Nagilla, Rakesh, Ouellette, Michael T, Pao, Christina S, Rendina, Alan R, Schaeffer, Michelle C, Summerfield, Jennifer D, Swift, Barbara A, Totoritis, Rachel D, Ward, Paris, Zhang, Aming, Zhang, Daohua, Marquis, Robert W, Bertin, John, Gough, Peter J
Published in Journal of medicinal chemistry (10.03.2016)
Published in Journal of medicinal chemistry (10.03.2016)
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New IDH1 mutant inhibitors for treatment of acute myeloid leukemia
Okoye-Okafor, Ujunwa C, Bartholdy, Boris, Cartier, Jessy, Gao, Enoch N, Pietrak, Beth, Rendina, Alan R, Rominger, Cynthia, Quinn, Chad, Smallwood, Angela, Wiggall, Kenneth J, Reif, Alexander J, Schmidt, Stanley J, Qi, Hongwei, Zhao, Huizhen, Joberty, Gerard, Faelth-Savitski, Maria, Bantscheff, Marcus, Drewes, Gerard, Duraiswami, Chaya, Brady, Pat, Groy, Arthur, Narayanagari, Swathi-Rao, Antony-Debre, Iléana, Mitchell, Kelly, Wang, Heng Rui, Kao, Yun-Ruei, Christopeit, Maximilian, Carvajal, Luis, Barreyro, Laura, Paietta, Elisabeth, Makishima, Hideki, Will, Britta, Concha, Nestor, Adams, Nicholas D, Schwartz, Benjamin, McCabe, Michael T, Maciejewski, Jaroslav, Verma, Amit, Steidl, Ulrich
Published in Nature chemical biology (01.11.2015)
Published in Nature chemical biology (01.11.2015)
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A highly selective, cell-permeable furin inhibitor BOS-318 rescues key features of cystic fibrosis airway disease
Douglas, Lisa E.J., Reihill, James A., Ho, Melisa W.Y., Axten, Jeffrey M., Campobasso, Nino, Schneck, Jessica L., Rendina, Alan R., Wilcoxen, Keith M., Martin, S. Lorraine
Published in Cell chemical biology (16.06.2022)
Published in Cell chemical biology (16.06.2022)
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Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa
Pinto, Donald J. P, Orwat, Michael J, Koch, Stephanie, Rossi, Karen A, Alexander, Richard S, Smallwood, Angela, Wong, Pancras C, Rendina, Alan R, Luettgen, Joseph M, Knabb, Robert M, He, Kan, Xin, Baomin, Wexler, Ruth R, Lam, Patrick Y. S
Published in Journal of medicinal chemistry (01.11.2007)
Published in Journal of medicinal chemistry (01.11.2007)
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A human fatty acid synthase inhibitor binds β-ketoacyl reductase in the keto-substrate site
Hardwicke, Mary Ann, Rendina, Alan R, Williams, Shawn P, Moore, Michael L, Wang, Liping, Krueger, Julie A, Plant, Ramona N, Totoritis, Rachel D, Zhang, Guofeng, Briand, Jacques, Burkhart, William A, Brown, Kristin K, Parrish, Cynthia A
Published in Nature chemical biology (01.09.2014)
Published in Nature chemical biology (01.09.2014)
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Mutant IDH1 Enhances the Production of 2‑Hydroxyglutarate Due to Its Kinetic Mechanism
Rendina, Alan R, Pietrak, Beth, Smallwood, Angela, Zhao, Huizhen, Qi, Hongwei, Quinn, Chad, Adams, Nicholas D, Concha, Nestor, Duraiswami, Chaya, Thrall, Sara H, Sweitzer, Sharon, Schwartz, Benjamin
Published in Biochemistry (Easton) (02.07.2013)
Published in Biochemistry (Easton) (02.07.2013)
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Exploration of the P1 residue in 3CL protease inhibitors leading to the discovery of a 2-tetrahydrofuran P1 replacement
Barton, Linda S., Callahan, James F., Cantizani, Juan, Concha, Nestor O., Cotillo Torrejon, Ignacio, Goodwin, Nicole C., Joshi-Pangu, Amruta, Kiesow, Terry J., McAtee, Jeff J., Mellinger, Mark, Nixon, Christopher J., Padrón-Barthe, Laura, Patterson, Jaclyn R., Pearson, Neil D., Pouliot, Jeffrey J., Rendina, Alan R., Buitrago Santanilla, Alexander, Schneck, Jessica L., Sanz, Olalla, Thalji, Reema K., Ward, Paris, Williams, Shawn P., King, Bryan W.
Published in Bioorganic & medicinal chemistry (15.02.2024)
Published in Bioorganic & medicinal chemistry (15.02.2024)
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Tetrahydroquinoline Derivatives as Potent and Selective Factor XIa Inhibitors
Quan, Mimi L, Wong, Pancras C, Wang, Cailan, Woerner, Francis, Smallheer, Joanne M, Barbera, Frank A, Bozarth, Jeffrey M, Brown, Randi L, Harpel, Mark R, Luettgen, Joseph M, Morin, Paul E, Peterson, Tara, Ramamurthy, Vidhyashankar, Rendina, Alan R, Rossi, Karen A, Watson, Carol A, Wei, Anzhi, Zhang, Ge, Seiffert, Dietmar, Wexler, Ruth R
Published in Journal of medicinal chemistry (13.02.2014)
Published in Journal of medicinal chemistry (13.02.2014)
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Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer
Harris, Philip A, Marinis, Jill M, Lich, John D, Berger, Scott B, Chirala, Anirudh, Cox, Julie A, Eidam, Patrick M, Finger, Joshua N, Gough, Peter J, Jeong, Jae U, Kang, James, Kasparcova, Viera, Leister, Lara K, Mahajan, Mukesh K, Miller, George, Nagilla, Rakesh, Ouellette, Michael T, Reilly, Michael A, Rendina, Alan R, Rivera, Elizabeth J, Sun, Helen H, Thorpe, James H, Totoritis, Rachel D, Wang, Wei, Wu, Dongling, Zhang, Daohua, Bertin, John, Marquis, Robert W
Published in ACS medicinal chemistry letters (13.06.2019)
Published in ACS medicinal chemistry letters (13.06.2019)
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In vitro, antithrombotic and bleeding time studies of BMS-654457, a small-molecule, reversible and direct inhibitor of factor XIa
Wong, Pancras C., Quan, Mimi L., Watson, Carol A., Crain, Earl J., Harpel, Mark R., Rendina, Alan R., Luettgen, Joseph M., Wexler, Ruth R., Schumacher, William A., Seiffert, Dietmar A.
Published in Journal of thrombosis and thrombolysis (01.11.2015)
Published in Journal of thrombosis and thrombolysis (01.11.2015)
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The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors
Deaton, David N., Do, Young, Holt, Jason, Jeune, Michael R., Kramer, H. Fritz, Larkin, Andrew L., Orband-Miller, Lisa A., Peckham, Gregory E., Poole, Chuck, Price, Daniel J., Schaller, Lee T., Shen, Ying, Shewchuk, Lisa M., Stewart, Eugene L., Stuart, J. Darren, Thomson, Stephen A., Ward, Paris, Wilson, Joseph W., Xu, Tianshun, Guss, Jeffrey H., Musetti, Caterina, Rendina, Alan R., Affleck, Karen, Anders, David, Hancock, Ashley P., Hobbs, Heather, Hodgson, Simon T., Hutchinson, Jonathan, Leveridge, Melanie V., Nicholls, Harry, Smith, Ian E.D., Somers, Don O., Sneddon, Helen F., Uddin, Sorif, Cleasby, Anne, Mortenson, Paul N., Richardson, Caroline, Saxty, Gordon
Published in Bioorganic & medicinal chemistry (15.04.2019)
Published in Bioorganic & medicinal chemistry (15.04.2019)
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Journal Article
Phenylimidazoles as Potent and Selective Inhibitors of Coagulation Factor XIa with in Vivo Antithrombotic Activity
Hangeland, Jon J, Friends, Todd J, Rossi, Karen A, Smallheer, Joanne M, Wang, Cailan, Sun, Zhong, Corte, James R, Fang, Tianan, Wong, Pancras C, Rendina, Alan R, Barbera, Frank A, Bozarth, Jeffrey M, Luettgen, Joseph M, Watson, Carol A, Zhang, Ge, Wei, Anzhi, Ramamurthy, Vidhyashankar, Morin, Paul E, Bisacchi, Gregory S, Subramaniam, Srinath, Arunachalam, Piramanayagam, Mathur, Arvind, Seiffert, Dietmar A, Wexler, Ruth R, Quan, Mimi L
Published in Journal of medicinal chemistry (11.12.2014)
Published in Journal of medicinal chemistry (11.12.2014)
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Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa–Tissue Factor Complex
Zhang, Xiaojun, Glunz, Peter W, Johnson, James A, Jiang, Wen, Jacutin-Porte, Swanee, Ladziata, Vladimir, Zou, Yan, Phillips, Monique S, Wurtz, Nicholas R, Parkhurst, Brandon, Rendina, Alan R, Harper, Timothy M, Cheney, Daniel L, Luettgen, Joseph M, Wong, Pancras C, Seiffert, Dietmar, Wexler, Ruth R, Priestley, E. Scott
Published in Journal of medicinal chemistry (11.08.2016)
Published in Journal of medicinal chemistry (11.08.2016)
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Journal Article
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group
Corte, James R., Fang, Tianan, Pinto, Donald J.P., Orwat, Michael J., Rendina, Alan R., Luettgen, Joseph M., Rossi, Karen A., Wei, Anzhi, Ramamurthy, Vidhyashankar, Myers, Joseph E., Sheriff, Steven, Narayanan, Rangaraj, Harper, Timothy W., Zheng, Joanna J., Li, Yi-Xin, Seiffert, Dietmar A., Wexler, Ruth R., Quan, Mimi L.
Published in Bioorganic & medicinal chemistry (15.05.2016)
Published in Bioorganic & medicinal chemistry (15.05.2016)
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Journal Article
Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors
Lin, Hong, Zeng, Jin, Xie, Ren, Schulz, Mark J, Tedesco, Rosanna, Qu, Junya, Erhard, Karl F, Mack, James F, Raha, Kaushik, Rendina, Alan R, Szewczuk, Lawrence M, Kratz, Patricia M, Jurewicz, Anthony J, Cecconie, Ted, Martens, Stan, McDevitt, Patrick J, Martin, John D, Chen, Stephenie B, Jiang, Yong, Nickels, Leng, Schwartz, Benjamin J, Smallwood, Angela, Zhao, Baoguang, Campobasso, Nino, Qian, Yanqiu, Briand, Jacques, Rominger, Cynthia M, Oleykowski, Catherine, Hardwicke, Mary Ann, Luengo, Juan I
Published in ACS medicinal chemistry letters (10.03.2016)
Published in ACS medicinal chemistry letters (10.03.2016)
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Journal Article
Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties
Pinto, Donald J.P., Smallheer, Joanne M., Corte, James R., Austin, Erin J.D., Wang, Cailan, Fang, Tianan, Smith, Leon M., Rossi, Karen A., Rendina, Alan R., Bozarth, Jeffrey M., Zhang, Ge, Wei, Anzhi, Ramamurthy, Vidhyashankar, Sheriff, Steven, Myers, Joseph E., Morin, Paul E., Luettgen, Joseph M., Seiffert, Dietmar A., Quan, Mimi L., Wexler, Ruth R.
Published in Bioorganic & medicinal chemistry letters (01.04.2015)
Published in Bioorganic & medicinal chemistry letters (01.04.2015)
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