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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The structure of dasatinib (BMS-354825) bound to activated ABL kinase domain elucidates its inhibitory activity against imatinib-resistant ABL mutants von TOKARSKI, John S, NEWITT, John A, DIANLIN XIE, YAQUN ZHANG, KLEI, Herbert E, CHANG, Chieh Ying J, CHENG, Janet D, WITTEKIND, Michael, KIEFER, Susan E, KISH, Kevin, LEE, Francis Y. F, BORZILLERRI, Robert, LOMBARDO, Louis J

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Discovery and Preclinical Characterization of the Cyclopropylindolobenzazepine BMS-791325, A Potent Allosteric Inhibitor of the Hepatitis C Virus NS5B Polymerase von Gentles, Robert G., Ding, Min, Bender, John A., Bergstrom, Carl P., Grant-Young, Katharine, Hewawasam, Piyasena, Hudyma, Thomas, Martin, Scott, Nickel, Andrew, Regueiro-Ren, Alicia, Tu, Yong, Yang, Zhong, Yeung, Kap-Sun, Zheng, Xiaofan, Chao, Sam, Sun, Jung-Hui, Beno, Brett R., Camac, Daniel M., Chang, Chong-Hwan, Gao, Mian, Morin, Paul E., Sheriff, Steven, Tredup, Jeff, Wan, John, Witmer, Mark R., Xie, Dianlin, Hanumegowda, Umesh, Knipe, Jay, Mosure, Kathy, Santone, Kenneth S., Parker, Dawn D., Zhuo, Xiaoliang, Lemm, Julie, Liu, Mengping, Pelosi, Lenore, Rigat, Karen, Voss, Stacey, Wang, Yi, Wang, Ying-Kai, Colonno, Richard J., Gao, Min, Roberts, Susan B., Gao, Qi, Ng, Alicia, Meanwell, Nicholas A, Kadow, John F.

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Discovery of Pyrrolopyridine−Pyridone Based Inhibitors of Met Kinase: Synthesis, X-ray Crystallographic Analysis, and Biological Activities von Kim, Kyoung Soon, Zhang, Liping, Schmidt, Robert, Cai, Zhen-Wei, Wei, Donna, Williams, David K, Lombardo, Louis J, Trainor, George L, Xie, Dianlin, Zhang, Yaquan, An, Yongmi, Sack, John S, Tokarski, John S, Darienzo, Celia, Kamath, Amrita, Marathe, Punit, Zhang, Yueping, Lippy, Jonathan, Jeyaseelan, Robert, Wautlet, Barri, Henley, Benjamin, Gullo-Brown, Johnni, Manne, Veeraswamy, Hunt, John T, Fargnoli, Joseph, Borzilleri, Robert M

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Involvement of DPP‐IV catalytic residues in enzyme–saxagliptin complex formation von Metzler, William J., Yanchunas, Joseph, Weigelt, Carolyn, Kish, Kevin, Klei, Herbert E., Xie, Dianlin, Zhang, Yaqun, Corbett, Martin, Tamura, James K., He, Bin, Hamann, Lawrence G., Kirby, Mark S., Marcinkeviciene, Jovita

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Correlation of High-Throughput Pregnane X Receptor (PXR) Transactivation and Binding Assays von Zhu, Zhengrong, Kim, Sean, Chen, Taosheng, Lin, Jun-Hsiang, Bell, Aneka, Bryson, James, Dubaquie, Yves, Yan, Ning, Yanchunas, Joseph, Xie, Dianlin, Stoffel, Robert, Sinz, Michael, Dickinson, Kenneth

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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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Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain von Tokarski, John S., Zupa-Fernandez, Adriana, Tredup, Jeffrey A., Pike, Kristen, Chang, ChiehYing, Xie, Dianlin, Cheng, Lihong, Pedicord, Donna, Muckelbauer, Jodi, Johnson, Stephen R., Wu, Sophie, Edavettal, Suzanne C., Hong, Yang, Witmer, Mark R., Elkin, Lisa L., Blat, Yuval, Pitts, William J., Weinstein, David S., Burke, James R.

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Time-Resolved Limited Proteolysis of Mitogen-Activated Protein Kinase-Activated Protein Kinase-2 Determined by LC/MS Only von Tao, Li, Kiefer, Susan E., Xie, Dianlin, Bryson, James W., Hefta, Stanley A., Doyle, Michael L.

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Crystal structures of apo and inhibitor-bound TGFβR2 kinase domain: insights into TGFβR isoform selectivity von Tebben, Andrew J., Ruzanov, Maxim, Gao, Mian, Xie, Dianlin, Kiefer, Susan E., Yan, Chunhong, Newitt, John A., Zhang, Liping, Kim, Kyoung, Lu, Hao, Kopcho, Lisa M., Sheriff, Steven

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Structural basis for CARM1 inhibition by indole and pyrazole inhibitors von Sack, John S, Thieffine, Sandrine, Bandiera, Tiziano, Fasolini, Marina, Duke, Gerald J, Jayaraman, Lata, Kish, Kevin F, Klei, Herbert E, Purandare, Ashok V, Rosettani, Pamela, Troiani, Sonia, Xie, Dianlin, Bertrand, Jay A

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TGFbR1 ATP binding site: a magnet for fragments von Sheriff, Steven, Ruzanov, Maxim, O'Malley, Kevin, Kiefer, Susan, Yan, Chunhong, Xie, Dianlin

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Development of a RapidFire mass spectrometry assay and a fluorescence assay for the discovery of kynurenine aminotransferase II inhibitors to treat central nervous system disorders von Lu, Hao, Kopcho, Lisa, Ghosh, Kaushik, Witmer, Mark, Parker, Michael, Gupta, Sumit, Paul, Marilyn, Krishnamurthy, Prasad, Laksmaiah, Basanth, Xie, Dianlin, Tredup, Jeffrey, Zhang, Litao, Abell, Lynn M.

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Identification of Imidazo[1,2‑b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors von Liu, Chunjian, Lin, James, Moslin, Ryan, Tokarski, John S, Muckelbauer, Jodi, Chang, ChiehYing, Tredup, Jeffrey, Xie, Dianlin, Park, Hyunsoo, Li, Peng, Wu, Dauh-Rurng, Strnad, Joann, Zupa-Fernandez, Adriana, Cheng, Lihong, Chaudhry, Charu, Chen, Jing, Chen, Cliff, Sun, Huadong, Elzinga, Paul, D’arienzo, Celia, Gillooly, Kathleen, Taylor, Tracy L, McIntyre, Kim W, Salter-Cid, Luisa, Lombardo, Louis J, Carter, Percy H, Aranibar, Nelly, Burke, James R, Weinstein, David S

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Discovery of Pyridazinone and Pyrazolo[1,5‑a]pyridine Inhibitors of C‑Terminal Src Kinase von O’Malley, Daniel P, Ahuja, Vijay, Fink, Brian, Cao, Carolyn, Wang, Cindy, Swanson, Jesse, Wee, Susan, Gavai, Ashvinikumar V, Tokarski, John, Critton, David, Paiva, Anthony A, Johnson, Benjamin M, Szapiel, Nicolas, Xie, Dianlin

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An improved protocol for amino acid type-selective isotope labeling in insect cells von Zhang, Yaqun, Wei, Hui, Xie, Dianlin, Calambur, Deepa, Douglas, Andrew, Gao, Mian, Marsilio, Frank, Metzler, William J., Szapiel, Nicolas, Zhang, Ping, Witmer, Mark R., Mueller, Luciano, Hedin, David

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Using yeast surface display to engineer a soluble and crystallizable construct of hematopoietic progenitor kinase 1 (HPK1) von Lau, Wai L., Pearce, Bradley, Malakian, Heather, Rodrigo, Iyoncy, Xie, Dianlin, Gao, Mian, Marsilio, Frank, Chang, Chiehying, Ruzanov, Max, Muckelbauer, Jodi K., Newitt, John A., Lipovšek, Daša, Sheriff, Steven

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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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The Influence of Adnectin Binding on the Extracellular Domain of Epidermal Growth Factor Receptor von Iacob, Roxana E., Chen, Guodong, Ahn, Joomi, Houel, Stephane, Wei, Hui, Mo, Jingjie, Tao, Li, Cohen, Daniel, Xie, Dianlin, Lin, Zheng, Morin, Paul E., Doyle, Michael L., Tymiak, Adrienne A., Engen, John R.

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Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis von Nair, Satheesh, Kumar, Sreekantha Ratna, Paidi, Venkatram Reddy, Sistla, Ramesh, Kantheti, Durgarao, Polimera, Subba Rao, Thangavel, Soodamani, Mukherjee, Amrita Jha, Das, Mitalee, Bhide, Rajeev S, Pitts, William J, Murugesan, Natesan, Dudhgoankar, Shailesh, Nagar, Jignesh, Subramani, Siva, Mazumder, Debarati, Carman, Julie A, Holloway, Deborah A, Li, Xin, Fereshteh, Mark P, Ruepp, Stefan, Palanisamy, Kamalavenkatesh, Mariappan, T. Thanga, Maddi, Srinivas, Saxena, Ajay, Elzinga, Paul, Chimalakonda, Anjaneya, Ruan, Qian, Ghosh, Kaushik, Bose, Sucharita, Sack, John, Yan, Chunhong, Kiefer, Susan E, Xie, Dianlin, Newitt, John A, Saravanakumar, S. Pon, Rampulla, Richard A, Barrish, Joel C, Carter, Percy H, Hynes, John

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