Design, Synthesis, and Anti-inflammatory Properties of Orally Active 4-(Phenylamino)-pyrrolo[2,1-f][1,2,4]triazine p38α Mitogen-Activated Protein Kinase Inhibitors von Hynes, John, Dyckman, Alaric J, Lin, Shuqun, Wrobleski, Stephen T, Wu, Hong, Gillooly, Kathleen M, Kanner, Steven B, Lonial, Herinder, Loo, Derek, McIntyre, Kim W, Pitt, Sidney, Shen, Ding Ren, Shuster, David J, Yang, XiaoXia, Zhang, Rosemary, Behnia, Kamelia, Zhang, Hongjian, Marathe, Punit H, Doweyko, Arthur M, Tokarski, John S, Sack, John S, Pokross, Matthew, Kiefer, Susan E, Newitt, John A, Barrish, Joel C, Dodd, John, Schieven, Gary L, Leftheris, Katerina

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Utilization of a nitrogen–sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors von Lin, Shuqun, Wrobleski, Stephen T., Hynes, John, Pitt, Sidney, Zhang, Rosemary, Fan, Yi, Doweyko, Arthur M., Kish, Kevin F., Sack, John S., Malley, Mary F., Kiefer, Susan E., Newitt, John A., McKinnon, Murray, Trzaskos, James, Barrish, Joel C., Dodd, John H., Schieven, Gary L., Leftheris, Katerina

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Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165 von Wrobleski, Stephen T, Moslin, Ryan, Lin, Shuqun, Zhang, Yanlei, Spergel, Steven, Kempson, James, Tokarski, John S, Strnad, Joann, Zupa-Fernandez, Adriana, Cheng, Lihong, Shuster, David, Gillooly, Kathleen, Yang, Xiaoxia, Heimrich, Elizabeth, McIntyre, Kim W, Chaudhry, Charu, Khan, Javed, Ruzanov, Max, Tredup, Jeffrey, Mulligan, Dawn, Xie, Dianlin, Sun, Huadong, Huang, Christine, D’Arienzo, Celia, Aranibar, Nelly, Chiney, Manoj, Chimalakonda, Anjaneya, Pitts, William J, Lombardo, Louis, Carter, Percy H, Burke, James R, Weinstein, David S

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Synthesis and SAR of new pyrrolo[2,1- f][1,2,4]triazines as potent p38α MAP kinase inhibitors von Wrobleski, Stephen T., Lin, Shuqun, Hynes, John, Wu, Hong, Pitt, Sidney, Shen, Ding Ren, Zhang, Rosemary, Gillooly, Kathleen M., Shuster, David J., McIntyre, Kim W., Doweyko, Arthur M., Kish, Kevin F., Tredup, Jeffrey A., Duke, Gerald J., Sack, John S., McKinnon, Murray, Dodd, John, Barrish, Joel C., Schieven, Gary L., Leftheris, Katerina

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The Discovery of Orally Active Triaminotriazine Aniline Amides as Inhibitors of p38 MAP Kinase von Leftheris, Katerina, Ahmed, Gulzar, Chan, Ran, Dyckman, Alaric J, Hussain, Zahid, Ho, Kan, Hynes, John, Letourneau, Jeffrey, Li, Wei, Lin, Shuqun, Metzger, Axel, Moriarty, Kevin J, Riviello, Chris, Shimshock, Yvonne, Wen, James, Wityak, John, Wrobleski, Stephen T, Wu, Hong, Wu, Junjun, Desai, Madhuri, Gillooly, Kathleen M, Lin, Tsung H, Loo, Derek, McIntyre, Kim W, Pitt, Sidney, Shen, Ding Ren, Shuster, David J, Zhang, Rosemary, Diller, David, Doweyko, Arthur, Sack, John, Baldwin, Jack, Barrish, Joel, Dodd, John, Henderson, Ian, Kanner, Steve, Schieven, Gary L, Webb, Maria

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Synthesis and SAR of p38α MAP kinase inhibitors based on heterobicyclic scaffolds von Murali Dhar, T.G., Wrobleski, Stephen T., Lin, Shuqun, Furch, Joseph A., Nirschl, David S., Fan, Yi, Todderud, Gordon, Pitt, Sidney, Doweyko, Arthur M., Sack, John S., Mathur, Arvind, McKinnon, Murray, Barrish, Joel C., Dodd, John H., Schieven, Gary L., Leftheris, Katerina

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Identification of N‑Methyl Nicotinamide and N‑Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2) von Moslin, Ryan, Zhang, Yanlei, Wrobleski, Stephen T, Lin, Shuqun, Mertzman, Michael, Spergel, Steven, Tokarski, John S, Strnad, Joann, Gillooly, Kathleen, McIntyre, Kim W, Zupa-Fernandez, Adriana, Cheng, Lihong, Sun, Huadong, Chaudhry, Charu, Huang, Christine, D’Arienzo, Celia, Heimrich, Elizabeth, Yang, Xiaoxia, Muckelbauer, Jodi K, Chang, ChiehYing, Tredup, Jeffrey, Mulligan, Dawn, Xie, Dianlin, Aranibar, Nelly, Chiney, Manoj, Burke, James R, Lombardo, Louis, Carter, Percy H, Weinstein, David S

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Rational Design and Synthesis of an Orally Active Indolopyridone as a Novel Conformationally Constrained Cannabinoid Ligand Possessing Antiinflammatory Properties von Wrobleski, Stephen T, Chen, Ping, Hynes, John, Lin, Shuqun, Norris, Derek J, Pandit, Chennagiri R, Spergel, Steven, Wu, Hong, Tokarski, John S, Chen, Xiaorong, Gillooly, Kathleen M, Kiener, Peter A, McIntyre, Kim W, Patil-koota, Vina, Shuster, David J, Turk, Lori A, Yang, Guchen, Leftheris, Katerina

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Synthesis and activity of N-acyl azacyclic urea HIV-1 protease inhibitors with high potency against multiple drug resistant viral strains von Zhao, Chen, Sham, Hing L., Sun, Minghua, Stoll, Vincent S., Stewart, Kent D., Lin, Shuqun, Mo, Hongmei, Vasavanonda, Sudthida, Saldivar, Ayda, Park, Chang, McDonald, Edith J., Marsh, Kennan C., Klein, Larry L., Kempf, Dale J., Norbeck, Daniel W.

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Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors von Bhide, Rajeev S., Keon, Alec, Weigelt, Carolyn, Sack, John S., Schmidt, Robert J., Lin, Shuqun, Xiao, Hai-Yun, Spergel, Steven H., Kempson, James, Pitts, William J., Carman, Julie, Poss, Michael A.

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Discovery of highly potent, selective, covalent inhibitors of JAK3 von Kempson, James, Ovalle, Damaso, Guo, Junqing, Wrobleski, Stephen T., Lin, Shuqun, Spergel, Steven H., Duan, James J.-W., Jiang, Bin, Lu, Zhonghui, Das, Jagabandhu, Yang, Bingwei V., Hynes, John, Wu, Hong, Tokarski, John, Sack, John S., Khan, Javed, Schieven, Gary, Blatt, Yuval, Chaudhry, Charu, Salter-Cid, Luisa M., Fura, Aberra, Barrish, Joel C., Carter, Percy H., Pitts, William J.

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Novel advances in biotransformation and bioactivation research-2020 year in review von Khojasteh, S. Cyrus, Argikar, Upendra A, Driscoll, James P, Heck, Carley J.S, King, Lloyd, Jackson, Klarissa D, Jian, Wenying, Kalgutkar, Amit S, Miller, Grover P, Kramlinger, Valerie, Rietjens, Ivonne M.C.M, Teitelbaum, Aaron M, Wang, Kai, Wei, Cong, Johnson, Benjamin M, Shu, Yue-Zhong, Zhuo, Xiaoliang, Meanwell, Nicholas A, Cerny, Matthew A, Obach, R. Scott, Sharma, Raman, Spracklin, Douglas K, Walker, Gregory S, Goracci, Laura, Desantis, Jenny, Valeri, Aurora, Castellani, Beatrice, Eleuteri, Michela, Cruciani, Gabriele, Lall, Manjinder S, Bassyouni, Asser, Bradow, James, Brown, Maria, Bundesmann, Mark, Chen, Jinshan, Ciszewski, Gregory, Hagen, Anne E, Hyek, Dennis, Jenkinson, Stephen, Liu, Bo, Pan, Senliang, Reilly, Usa, Sach, Neal, Smaltz, Daniel J, Starr, Jeremy, Wagenaar, Melissa, de Bruyn Kops, Christina, Sicho, Martin, Mazzolari, Angelica, Kirchmair, Johannes, Korprasertthaworn, Porntipa, Chau, Nuy, Nair, Pramod C, Rowland, Andrew, Miners, John O, Wrobleski, Stephen T, Moslin, Ryan, Lin, Shuqun, Zhang, Yanlei, Spergel, Steven, Kempson, James, Tokarski, John S, Strnad, Joann, Zupa-Fernandez, Adriana, Cheng, Lihong, Shuster, David, Gillooly, Kathleen, Yang, Xiaoxia, Heimrich, Elizabeth, McIntyre, Kim W, Chaudhry, Charu, Khan, Javed, Ruzanov, Max, Tredup, Jeffrey, Mulligan, Dawn, Xie, Dianlin, Sun, Huadong, Huang, Christine, D'Arienzo, Celia, Aranibar, Nelly, Chiney, Manoj, Chimalakonda, Anjaneya, Pitts, William J, Lombardo, Louis, Carter, Percy H, Burke, James R, Weinstein, David S, Li, Jing, Liu, Ju, Enders, Jennifer, Arciprete, Michael, Tran, Chris, Aluri, Krishna, Guan, Li-Hua, O'Shea, Jonathan, Bisbe, Anna, Charisse, Klaus, Zlatev, Ivan, Najarian, Diana, Xu, Yuanxin

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Discovery of 4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a Clinical p38α MAP Kinase Inhibitor for th... von Liu, Chunjian, Lin, James, Wrobleski, Stephen T, Lin, Shuqun, Hynes, John, Wu, Hong, Dyckman, Alaric J, Li, Tianle, Wityak, John, Gillooly, Kathleen M, Pitt, Sidney, Shen, Ding Ren, Zhang, Rosemary F, McIntyre, Kim W, Salter-Cid, Luisa, Shuster, David J, Zhang, Hongjian, Marathe, Punit H, Doweyko, Arthur M, Sack, John S, Kiefer, Susan E, Kish, Kevin F, Newitt, John A, McKinnon, Murray, Dodd, John H, Barrish, Joel C, Schieven, Gary L, Leftheris, Katerina

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Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyloxy)methyl-2-(4-(phosphonooxy)phenyl)acetate (BMS-... von Liu, Chunjian, Lin, James, Hynes, John, Wu, Hong, Wrobleski, Stephen T, Lin, Shuqun, Dhar, T G Murali, Vrudhula, Vivekananda M, Sun, Jung-Hui, Chao, Sam, Zhao, Rulin, Wang, Bei, Chen, Bang-Chi, Everlof, Gerry, Gesenberg, Christoph, Zhang, Hongjian, Marathe, Punit H, McIntyre, Kim W, Taylor, Tracy L, Gillooly, Kathleen, Shuster, David J, McKinnon, Murray, Dodd, John H, Barrish, Joel C, Schieven, Gary L, Leftheris, Katerina

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Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors von Duan, James J-W, Lu, Zhonghui, Jiang, Bin, Yang, Bingwei V, Doweyko, Lidia M, Nirschl, David S, Haque, Lauren E, Lin, Shuqun, Brown, Gregory, Hynes, Jr, John, Tokarski, John S, Sack, John S, Khan, Javed, Lippy, Jonathan S, Zhang, Rosemary F, Pitt, Sidney, Shen, Guoxiang, Pitts, William J, Carter, Percy H, Barrish, Joel C, Nadler, Steven G, Salter-Cid, Luisa M, McKinnon, Murray, Fura, Aberra, Schieven, Gary L, Wrobleski, Stephen T

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Discovery of ((4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methylpyrrolo[1,2‑f][1,2,4]triazine-6-carbonyl)­(propyl)­carba­moyl­oxy)­methyl-2-(4-(phos­pho­no­oxy)­phenyl)­ace... von Liu, Chunjian, Lin, James, Hynes, John, Wu, Hong, Wrobleski, Stephen T., Lin, Shuqun, Dhar, T. G. Murali, Vrudhula, Vivekananda M., Sun, Jung-Hui, Chao, Sam, Zhao, Rulin, Wang, Bei, Chen, Bang-Chi, Everlof, Gerry, Gesenberg, Christoph, Zhang, Hongjian, Marathe, Punit H., McIntyre, Kim W., Taylor, Tracy L., Gillooly, Kathleen, Shuster, David J., McKinnon, Murray, Dodd, John H., Barrish, Joel C., Schieven, Gary L., Leftheris, Katerina

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A Novel, Picomolar Inhibitor of Human Immunodeficiency Virus Type 1 Protease von Sham, Hing L, Zhao, Chen, Stewart, Kent D, Betebenner, David A, Lin, Shuqun, Park, Chang H, Kong, Xiang-P, Rosenbrook, William, Herrin, Thomas, Madigan, Darold, Vasavanonda, Suthida, Lyons, Nicholas, Molla, Akhter, Saldivar, Ayda, Marsh, Kennan C, McDonald, Edith, Wideburg, Norman E, Denissen, Jon F, Robins, Terrel, Kempf, Dale J, Plattner, Jacob J, Norbeck, Daniel W

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The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode von Wrobleski, Stephen T., Lin, Shuqun, Murali Dhar, T.G., Dyckman, Alaric J., Li, Tianle, Pitt, Sidney, Zhang, Rosemary, Fan, Yi, Doweyko, Arthur M., Tokarski, John S., Kish, Kevin F., Kiefer, Susan E., Sack, John S., Newitt, John A., Witmer, Mark R., McKinnon, Murray, Barrish, Joel C., Dodd, John H., Schieven, Gary L., Leftheris, Katerina

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The identification of novel p38I- isoform selective kinase inhibitors having an unprecedented p38I- binding mode von Wrobleski, Stephen, Lin, Shuqun, Dhar, T G, Dyckman, Alaric, Li, Tianle, Pitt, Sidney, Zhang, Rosemary, Fan, Yi, Doweyko, Arthur, Tokarski, John, Kish, Kevin, Kiefer, Susan, Sack, John, Newitt, John, Witmer, Mark, McKinnon, Murray, Barrish, Joel, Dodd, John, Schieven, Gary, Leftheris, Katerina

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Discovery of 4-(5-(Cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a Clinical p38[alpha] MAP Kinase Inhibitor... von Liu, Chunjian, Lin, James, Wrobleski, Stephen T., Lin, Shuqun, Hynes, Jr., John, Wu, Hong, Dyckman, Alaric J., Li, Tianle, Wityak, John, Gillooly, Kathleen M., Pitt, Sidney, Shen, Ding Ren, Zhang, Rosemary F., McIntyre, Kim W., Salter-Cid, Luisa, Shuster, David J., Zhang, Hongjian, Marathe, Punit H., Doweyko, Arthur M., Sack, John S., Kiefer, Susan E., Kish, Kevin F., Newitt, John A., McKinnon, Murray, Dodd, John H., Barrish, Joel C., Schieven, Gary L., Leftheris, Katerina

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