Discovery of CC-90011: A Potent and Selective Reversible Inhibitor of Lysine Specific Demethylase 1 (LSD1) von 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

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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... von 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.

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KDM4 Inhibition Targets Breast Cancer Stem-like Cells von 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

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JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders von 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.

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Integration of taste and calorie sensing in Drosophila von Stafford, Jeffrey W, Lynd, Kaylea M, Jung, Aera Y, Gordon, Michael D

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Discovery of Alogliptin:  A Potent, Selective, Bioavailable, and Efficacious Inhibitor of Dipeptidyl Peptidase IV von 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

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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 Steatohepat... von 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

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Pharmacokinetic-pharmacodynamic correlation from mouse to human with pazopanib, a multikinase angiogenesis inhibitor with potent antitumor and antiangiogenic activity von 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

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Structure-based design and discovery of potent and selective KDM5 inhibitors von Nie, Zhe, Shi, Lihong, Lai, Chon, O'Connell, Shawn M., Xu, Jiangchun, Stansfield, Ryan K., Hosfield, David J., Veal, James M., Stafford, Jeffrey A.

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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 R... von 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

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Author Correction: JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders von 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.

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Design and Synthesis of Pyrimidinone and Pyrimidinedione Inhibitors of Dipeptidyl Peptidase IV von 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

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TACH101, a first-in-class pan-inhibitor of KDM4 for treatment of gastrointestinal cancers von Perabo, Frank, Chandhasin, Chandtip, Yoo, Sanghee, Dang, Van, Del Rosario, Joselyn, Chen, Young K, Stafford, Jeffrey, Quake, Stephen, Clarke, Michael F.

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CNS 7056: a novel ultra-short-acting Benzodiazepine von 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

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Structure-based design and discovery of potent and selective lysine-specific demethylase 1 (LSD1) inhibitors von 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.

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Design, synthesis and biological evaluation of novel 4-phenylisoquinolinone BET bromodomain inhibitors von 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.

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Design of KDM4 Inhibitors with Antiproliferative Effects in Cancer Models von 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

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Structure-based design and SAR development of 5,6-dihydroimidazolo[1,5-f]pteridine derivatives as novel Polo-like kinase-1 inhibitors von Kiryanov, Andre, Natala, Srinivasa, Jones, Benjamin, McBride, Christopher, Feher, Victoria, Lam, Betty, Liu, Yan, Honda, Kouhei, Uchiyama, Noriko, Kawamoto, Tomohiro, Hikichi, Yuichi, Zhang, Lilly, Hosfield, David, Skene, Robert, Zou, Hua, Stafford, Jeffrey, Cao, Xiaodong, Ichikawa, Takashi

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Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1) von Nie, Zhe, Feher, Victoria, Natala, Srinivasa, McBride, Christopher, Kiryanov, Andre, Jones, Benjamin, Lam, Betty, Liu, Yan, Kaldor, Stephen, Stafford, Jeffrey, Hikami, Kouki, Uchiyama, Noriko, Kawamoto, Tomohiro, Hikichi, Yuichi, Matsumoto, Shin-ichi, Amano, Nobuyuki, Zhang, Lilly, Hosfield, David, Skene, Robert, Zou, Hua, Cao, Xiaodong, Ichikawa, Takashi

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Discovery and Evaluation of 2-Anilino-5-aryloxazoles as a Novel Class of VEGFR2 Kinase Inhibitors von 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

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