Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1)
Kanouni, Toufike, Severin, Christophe, Cho, Robert W, Yuen, Natalie Y.-Y, Xu, Jiangchun, Shi, Lihong, Lai, Chon, Del Rosario, Joselyn R, Stansfield, Ryan K, Lawton, Lee N, Hosfield, David, O’Connell, Shawn, Kreilein, Matt M, Tavares-Greco, Paula, Nie, Zhe, Kaldor, Stephen W, Veal, James M, Stafford, Jeffrey A, Chen, Young K
Published in Journal of medicinal chemistry (10.12.2020)
Published in Journal of medicinal chemistry (10.12.2020)
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Discovery of Alogliptin: A Potent, Selective, Bioavailable, and Efficacious Inhibitor of Dipeptidyl Peptidase IV
Feng, Jun, Zhang, Zhiyuan, Wallace, Michael B, Stafford, Jeffrey A, Kaldor, Stephen W, Kassel, Daniel B, Navre, Marc, Shi, Lihong, Skene, Robert J, Asakawa, Tomoko, Takeuchi, Koji, Xu, Rongda, Webb, David R, Gwaltney, Stephen L
Published in Journal of medicinal chemistry (17.05.2007)
Published in Journal of medicinal chemistry (17.05.2007)
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JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders
Ambrus-Aikelin, Geza, Takeda, Katsuyuki, Joetham, Anthony, Lazic, Milos, Povero, Davide, Santini, Angelina M, Pranadinata, Rama, Johnson, Casey D, McGeough, Matthew D, Beasley, Federico C, Stansfield, Ryan, McBride, Christopher, Trzoss, Lynnie, Hoffman, Hal M, Feldstein, Ariel E, Stafford, Jeffrey A, Veal, James M, Bain, Gretchen, Gelfand, Erwin W
Published in Scientific reports (19.08.2023)
Published in Scientific reports (19.08.2023)
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Pharmacokinetic-pharmacodynamic correlation from mouse to human with pazopanib, a multikinase angiogenesis inhibitor with potent antitumor and antiangiogenic activity
Kumar, Rakesh, Knick, Victoria B, Rudolph, Sharon K, Johnson, Jennifer H, Crosby, Renae M, Crouthamel, Ming-Chih, Hopper, Teresa M, Miller, Charles G, Harrington, Laura E, Onori, James A, Mullin, Robert J, Gilmer, Tona M, Truesdale, Anne T, Epperly, Andrea H, Boloor, Amogh, Stafford, Jeffrey A, Luttrell, Deirdre K, Cheung, Mui
Published in Molecular cancer therapeutics (01.07.2007)
Published in Molecular cancer therapeutics (01.07.2007)
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Discovery of 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a Novel and Potent Vascular Endothelial Growth Factor Receptor Inhibitor
Harris, Philip A, Boloor, Amogh, Cheung, Mui, Kumar, Rakesh, Crosby, Renae M, Davis-Ward, Ronda G, Epperly, Andrea H, Hinkle, Kevin W, Hunter, Robert N, Johnson, Jennifer H, Knick, Victoria B, Laudeman, Christopher P, Luttrell, Deirdre K, Mook, Robert A, Nolte, Robert T, Rudolph, Sharon K, Szewczyk, Jerzy R, Truesdale, Anne T, Veal, James M, Wang, Liping, Stafford, Jeffrey A
Published in Journal of medicinal chemistry (14.08.2008)
Published in Journal of medicinal chemistry (14.08.2008)
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Author Correction: JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders
Ambrus-Aikelin, Geza, Takeda, Katsuyuki, Joetham, Anthony, Lazic, Milos, Povero, Davide, Santini, Angelina M, Pranadinata, Rama, Johnson, Casey D, McGeough, Matthew D, Beasley, Federico C, Stansfield, Ryan, McBride, Christopher, Trzoss, Lynnie, Hoffman, Hal M, Feldstein, Ariel E, Stafford, Jeffrey A, Veal, James M, Bain, Gretchen, Gelfand, Erwin W
Published in Scientific reports (16.11.2023)
Published in Scientific reports (16.11.2023)
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Design and Synthesis of Pyrimidinone and Pyrimidinedione Inhibitors of Dipeptidyl Peptidase IV
Zhang, Zhiyuan, Wallace, Michael B, Feng, Jun, Stafford, Jeffrey A, Skene, Robert J, Shi, Lihong, Lee, Bumsup, Aertgeerts, Kathleen, Jennings, Andy, Xu, Rongda, Kassel, Daniel B, Kaldor, Stephen W, Navre, Marc, Webb, David R, Gwaltney, Stephen L
Published in Journal of medicinal chemistry (27.01.2011)
Published in Journal of medicinal chemistry (27.01.2011)
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Overcoming Preclinical Safety Obstacles to Discover (S)‑N‑((1,2,3,5,6,7-Hexahydro‑s‑indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro‑5H‑pyrazolo[5,1‑b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor
McBride, Christopher, Trzoss, Lynnie, Povero, Davide, Lazic, Milos, Ambrus-Aikelin, Geza, Santini, Angelina, Pranadinata, Rama, Bain, Gretchen, Stansfield, Ryan, Stafford, Jeffrey A., Veal, James, Takahashi, Ryan, Ly, Justin, Chen, Shu, Liu, Liling, Nespi, Marika, Blake, Robert, Katewa, Arna, Kleinheinz, Tracy, Sujatha-Bhaskar, Swathi, Ramamoorthi, Nandhini, Sims, Jessica, McKenzie, Brent, Chen, Mark, Ultsch, Mark, Johnson, Matthew, Murray, Jeremy, Ciferri, Claudio, Staben, Steven T., Townsend, Michael J., Stivala, Craig E.
Published in Journal of medicinal chemistry (10.11.2022)
Published in Journal of medicinal chemistry (10.11.2022)
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KDM4 Inhibition Targets Breast Cancer Stem-like Cells
Metzger, Eric, Stepputtis, Stella S, Strietz, Juliane, Preca, Bogdan-Tiberius, Urban, Sylvia, Willmann, Dominica, Allen, Anita, Zenk, Fides, Iovino, Nicola, Bronsert, Peter, Proske, Amelie, Follo, Marie, Boerries, Melanie, Stickeler, Elmar, Xu, Jiangchun, Wallace, Michael B, Stafford, Jeffrey A, Kanouni, Toufike, Maurer, Jochen, Schüle, Roland
Published in Cancer research (Chicago, Ill.) (01.11.2017)
Published in Cancer research (Chicago, Ill.) (01.11.2017)
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Pharmacology of a Potent and Novel Inhibitor of the NOD-Like Receptor Pyrin Domain-Containing Protein 3 (NLRP3) Inflammasome that Attenuates Development of Nonalcoholic Steatohepatitis and Liver Fibrosis
Povero, Davide, Lazic, Milos, McBride, Christopher, Ambrus-Aikelin, Geza, Stansfield, Ryan, Johnson, Casey D, Santini, Angelina M, Pranadinata, Rama F, McGeough, Matthew D, Stafford, Jeffrey A, Hoffman, Hal M, Feldstein, Ariel E, Veal, James M, Bain, Gretchen
Published in The Journal of pharmacology and experimental therapeutics (01.08.2023)
Published in The Journal of pharmacology and experimental therapeutics (01.08.2023)
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Structure-based design and discovery of potent and selective KDM5 inhibitors
Nie, Zhe, Shi, Lihong, Lai, Chon, O'Connell, Shawn M., Xu, Jiangchun, Stansfield, Ryan K., Hosfield, David J., Veal, James M., Stafford, Jeffrey A.
Published in Bioorganic & medicinal chemistry letters (15.05.2018)
Published in Bioorganic & medicinal chemistry letters (15.05.2018)
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Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase
Sammond, Douglas M., Nailor, Kristen E., Veal, James M., Nolte, Robert T., Wang, Liping, Knick, Victoria B., Rudolph, Sharon K., Truesdale, Anne T., Nartey, Eldridge N., Stafford, Jeffrey A., Kumar, Rakesh, Cheung, Mui
Published in Bioorganic & medicinal chemistry letters (01.08.2005)
Published in Bioorganic & medicinal chemistry letters (01.08.2005)
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Structure-based design and discovery of potent and selective lysine-specific demethylase 1 (LSD1) inhibitors
Nie, Zhe, Shi, Lihong, Lai, Chon, Severin, Christophe, Xu, Jiangchun, Del Rosario, Joselyn R., Stansfield, Ryan K., Cho, Robert W., Kanouni, Toufike, Veal, James M., Stafford, Jeffrey A., Chen, Young K.
Published in Bioorganic & medicinal chemistry letters (01.01.2019)
Published in Bioorganic & medicinal chemistry letters (01.01.2019)
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CNS 7056: a novel ultra-short-acting Benzodiazepine
Kilpatrick, Gavin J, McIntyre, Margaret S, Cox, Richard F, Stafford, Jeffrey A, Pacofsky, Gregory J, Lovell, Gwyer G, Wiard, Robert P, Feldman, Paul L, Collins, Holly, Waszczak, Barbara L, Tilbrook, Gary S
Published in Anesthesiology (Philadelphia) (01.07.2007)
Published in Anesthesiology (Philadelphia) (01.07.2007)
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Design, synthesis and biological evaluation of novel 4-phenylisoquinolinone BET bromodomain inhibitors
Bennett, Michael J., Wu, Yiqin, Boloor, Amogh, Matuszkiewicz, Jennifer, O'Connell, Shawn M., Shi, Lihong, Stansfield, Ryan K., Del Rosario, Joselyn R., Veal, James M., Hosfield, David J., Xu, Jiangchun, Kaldor, Stephen W., Stafford, Jeffrey A., Betancort, Juan M.
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
Published in Bioorganic & medicinal chemistry letters (01.06.2018)
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Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models
Chen, Young K, Bonaldi, Tiziana, Cuomo, Alessandro, Del Rosario, Joselyn R, Hosfield, David J, Kanouni, Toufike, Kao, Shih-chu, Lai, Chon, Lobo, Neethan A, Matuszkiewicz, Jennifer, McGeehan, Andrew, O’Connell, Shawn M, Shi, Lihong, Stafford, Jeffrey A, Stansfield, Ryan K, Veal, James M, Weiss, Michael S, Yuen, Natalie Y, Wallace, Michael B
Published in ACS medicinal chemistry letters (10.08.2017)
Published in ACS medicinal chemistry letters (10.08.2017)
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Discovery and Evaluation of 2-Anilino-5-aryloxazoles as a Novel Class of VEGFR2 Kinase Inhibitors
Harris, Philip A, Cheung, Mui, Hunter, Robert N, Brown, Matthew L, Veal, James M, Nolte, Robert T, Wang, Liping, Liu, Wendy, Crosby, Renae M, Johnson, Jennifer H, Epperly, Andrea H, Kumar, Rakesh, Luttrell, Deirdre K, Stafford, Jeffrey A
Published in Journal of medicinal chemistry (10.03.2005)
Published in Journal of medicinal chemistry (10.03.2005)
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Efficient and Regioselective Synthesis of 2-Alkyl-2H-indazoles
Cheung, Mui, Boloor, Amogh, Stafford, Jeffrey A
Published in Journal of organic chemistry (16.05.2003)
Published in Journal of organic chemistry (16.05.2003)
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Design and Synthesis of Conformationally Constrained Analogs of 4-(3-Butoxy-4-methoxybenzyl)imidazolidin-2-one (Ro 20-1724) as Potent Inhibitors of cAMP-Specific Phosphodiesterase
Brackeen, Marcus F, Stafford, Jeffrey A, Cowan, David J, Brown, Peter J, Domanico, Paul L, Feldman, Paul L, Rose, Dudley, Strickland, Alan B, Veal, James M, Verghese, Margrith
Published in Journal of medicinal chemistry (01.11.1995)
Published in Journal of medicinal chemistry (01.11.1995)
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Journal Article
Discovery of Alogliptin: A Potent, Selective, Bioavailable, and Efficacious Inhibitor of Dipeptidyl Peptidase IV
Feng, Jun, Zhang, Zhiyuan, Wallace, Michael B, Stafford, Jeffrey A, Kaldor, Stephen W, Kassel, Daniel B, Navre, Marc, Shi, Lihong, Skene, Robert J, Asakawa, Tomoko, Takeuchi, Koji, Xu, Rongda, Webb, David R, Gwaltney, Stephen L
Published in Journal of medicinal chemistry (24.07.2008)
Published in Journal of medicinal chemistry (24.07.2008)
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