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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An innovative kinome platform to accelerate small-molecule inhibitor discovery and optimization from hits to leads von Chaudhry, Charu, Tebben, Andrew, Tokarski, John S., Borzilleri, Robert, Pitts, William J., Lippy, Jonathan, Zhang, Litao

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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 of N-(4-(2-Amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a Selective and Orally Efficac... von Schroeder, Gretchen M, An, Yongmi, Cai, Zhen-Wei, Chen, Xiao-Tao, Clark, Cheryl, Cornelius, Lyndon A. M, Dai, Jun, Gullo-Brown, Johnni, Gupta, Ashok, Henley, Benjamin, Hunt, John T, Jeyaseelan, Robert, Kamath, Amrita, Kim, Kyoung, Lippy, Jonathan, Lombardo, Louis J, Manne, Veeraswamy, Oppenheimer, Simone, Sack, John S, Schmidt, Robert J, Shen, Guoxiang, Stefanski, Kevin, Tokarski, John S, Trainor, George L, Wautlet, Barri S, Wei, Donna, Williams, David K, Zhang, Yingru, Zhang, Yueping, Fargnoli, Joseph, Borzilleri, Robert M

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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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Construction of 3D-QSAR Models Using the 4D-QSAR Analysis Formalism von Hopfinger, A. J, Wang, Shen, Tokarski, John S, Jin, Baiqiang, Albuquerque, Magaly, Madhav, Prakash J, Duraiswami, Chaya

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Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors von Cai, Zhen-Wei, Wei, Donna, Schroeder, Gretchen M., Cornelius, Lyndon A.M., Kim, Kyoung, Chen, Xiao-Tao, Schmidt, Robert J., Williams, David K., Tokarski, John S., An, Yongmi, Sack, John S., Manne, Veeraswamy, Kamath, Amrita, Zhang, Yueping, Marathe, Punit, Hunt, John T., Lombardo, Louis J., Fargnoli, Joseph, Borzilleri, Robert M.

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Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2 von Liu, Chunjian, Lin, James, Langevine, Charles, Smith, Daniel, Li, Jianqing, Tokarski, John S., Khan, Javed, Ruzanov, Max, Strnad, Joann, Zupa-Fernandez, Adriana, Cheng, Lihong, Gillooly, Kathleen M., Shuster, David, Zhang, Yifan, Thankappan, Anil, McIntyre, Kim W., Chaudhry, Charu, Elzinga, Paul A., Chiney, Manoj, Chimalakonda, Anjaneya, Lombardo, Louis J., Macor, John E., Carter, Percy H., Burke, James R., Weinstein, David S.

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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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Discovery of 2‑(Anilino)pyrimidine-4-carboxamides as Highly Potent, Selective, and Orally Active Glycogen Synthase Kinase‑3 (GSK-3) Inhibitors von Hartz, Richard A., Ahuja, Vijay T., Luo, Guanglin, Chen, Ling, Sivaprakasam, Prasanna, Xiao, Hong, Krause, Carol M., Clarke, Wendy J., Xu, Songmei, Tokarski, John S., Kish, Kevin, Lewis, Hal, Szapiel, Nicolas, Ravirala, Ramu, Mutalik, Sayali, Nakmode, Deepa, Shah, Devang, Burton, Catherine R., Macor, John E., Dubowchik, Gene M.

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Discovery and Preclinical Pharmacology of an Oral Bromodomain and Extra-Terminal (BET) Inhibitor Using Scaffold-Hopping and Structure-Guided Drug Design von Gavai, Ashvinikumar V, Norris, Derek, Delucca, George, Tortolani, David, Tokarski, John S, Dodd, Dharmpal, O’Malley, Daniel, Zhao, Yufen, Quesnelle, Claude, Gill, Patrice, Vaccaro, Wayne, Huynh, Tram, Ahuja, Vijay, Han, Wen-Ching, Mussari, Christopher, Harikrishnan, Lalgudi, Kamau, Muthoni, Poss, Michael, Sheriff, Steven, Yan, Chunhong, Marsilio, Frank, Menard, Krista, Wen, Mei-Li, Rampulla, Richard, Wu, Dauh-Rurng, Li, Jianqing, Zhang, Huiping, Li, Peng, Sun, Dawn, Yip, Henry, Traeger, Sarah C, Zhang, Yingru, Mathur, Arvind, Zhang, Haiying, Huang, Christine, Yang, Zheng, Ranasinghe, Asoka, Everlof, Gerry, Raghavan, Nirmala, Tye, Ching Kim, Wee, Susan, Hunt, John T, Vite, Gregory, Westhouse, Richard, Lee, Francis Y

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Discovery and Synthesis of Heterobifunctional Degraders of Rearranged during Transfection (RET) Kinase von Qiao, Jennifer X., Williams, David, Gill, Patrice, Li, Ling, Norris, Derek, Tokarski, John S., Wong, Jessica, Qi, Huilin, Hafeji, Yamnah, Downes, Daniel P., Degnen, Bill, Wang, Ying-Kai, Locke, Gregory, Fang, Hua, Yu, Fei, Xu, Songmei, Naglich, Joseph, Zhang, Jun, Nanjappa, Purushothama, Dai, Chao, Chourb, Lisa, Napoline, Jonathan, Tester, Richland, Jorge, Christine, Li, Yi-Xin, Mathur, Arvind, Barbieri, Christopher, Soars, Matthew G., Venkatanarayan, Avinashnarayan, Lees, Emma, Borzilleri, Robert M., Gavai, Ashvinikumar V., Wichroski, Michael, Dhar, T. G. Murali

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New dual inhibitors of EGFR and HER2 protein tyrosine kinases von Fink, Brian E., Vite, Gregory D., Mastalerz, Harold, Kadow, John F., Kim, Soong-Hoon, Leavitt, Kenneth J., Du, Karen, Crews, Donald, Mitt, Toomas, Wong, Tai W., Hunt, John T., Vyas, Dolatrai M., Tokarski, John S.

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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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Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties von Hill, Matthew D., Fang, Haiquan, Norris, Derek, Delucca, George V., Huang, Hong, DeBenedetto, Mikkel, Quesnelle, Claude, Schmitz, William D., Tokarski, John S., Sheriff, Steven, Yan, Chunhong, Fanslau, Caroline, Haarhoff, Zuzana, Huang, Christine, Kramer, Melissa, Madari, Shilpa, Menard, Krista, Monereau, Laura, Morrison, John, Raghavan, Nirmala, Shields, Eric E., Simmermacher-Mayer, Jean, Sinz, Michael, Tye, Ching Kim, Westhouse, Richard, Xie, Chunshan, Zhang, Haiying, Zhang, Lisa, Zvyaga, Tatyana, Lee, Francis, Gavai, Ashvinikumar V., Degnan, Andrew P.

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Identification and characterization of TYK2 pseudokinase domain stabilizers that allosterically inhibit TYK2 signaling von Locke, Gregory A, Muckelbauer, Jodi, Tokarski, John S, Barbieri, Christopher M, Belić, Stefan, Falk, Bradley, Tredup, Jeffrey, Wang, Ying-Kai

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Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors von Hynes, John, Wu, Hong, Kempson, James, Duan, James J.-W., Lu, Zhonghui, Jiang, Bin, Stachura, Sylwia, Tokarski, John S., Sack, John S., Khan, Javed A., Lippy, Jonathan S., Zhang, Rosemary F., Pitt, Sidney, Shen, Guoxiang, Gillooly, Kate, McIntyre, Kim, Carter, Percy H., Barrish, Joel C., Nadler, Steven G., Salter-Cid, Luisa M., Fura, Aberra, Schieven, Gary L., Pitts, William J., Wrobleski, Stephen T.

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The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists von Balog, Aaron, Salvati, Mark E., Shan, Weifang, Mathur, Arvind, Leith, Leslie W., Wei, Donna D., Attar, Ricardo M., Geng, Jieping, Rizzo, Cheryl A., Wang, Chihuei, Krystek, Stanley R., Tokarski, John S., Hunt, John T., Gottardis, Marco, Weinmann, Roberto

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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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