Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165
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
Published in Journal of medicinal chemistry (24.10.2019)
Published in Journal of medicinal chemistry (24.10.2019)
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An innovative kinome platform to accelerate small-molecule inhibitor discovery and optimization from hits to leads
Chaudhry, Charu, Tebben, Andrew, Tokarski, John S., Borzilleri, Robert, Pitts, William J., Lippy, Jonathan, Zhang, Litao
Published in Drug discovery today (01.05.2021)
Published in Drug discovery today (01.05.2021)
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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
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
Published in Cancer research (Chicago, Ill.) (01.06.2006)
Published in Cancer research (Chicago, Ill.) (01.06.2006)
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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 Efficacious Inhibitor of the Met Kinase Superfamily
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
Published in Journal of medicinal chemistry (12.03.2009)
Published in Journal of medicinal chemistry (12.03.2009)
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Discovery of Pyrrolopyridine−Pyridone Based Inhibitors of Met Kinase: Synthesis, X-ray Crystallographic Analysis, and Biological Activities
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
Published in Journal of medicinal chemistry (11.09.2008)
Published in Journal of medicinal chemistry (11.09.2008)
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Discovery of orally active pyrrolopyridine- and aminopyridine-based Met kinase inhibitors
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.
Published in Bioorganic & medicinal chemistry (01.06.2008)
Published in Bioorganic & medicinal chemistry (01.06.2008)
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Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2
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.
Published in Journal of medicinal chemistry (14.01.2021)
Published in Journal of medicinal chemistry (14.01.2021)
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Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain
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.
Published in The Journal of biological chemistry (24.04.2015)
Published in The Journal of biological chemistry (24.04.2015)
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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
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.
Published in Journal of medicinal chemistry (08.06.2023)
Published in Journal of medicinal chemistry (08.06.2023)
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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
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
Published in Journal of medicinal chemistry (14.10.2021)
Published in Journal of medicinal chemistry (14.10.2021)
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New dual inhibitors of EGFR and HER2 protein tyrosine kinases
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.
Published in Bioorganic & medicinal chemistry letters (01.11.2005)
Published in Bioorganic & medicinal chemistry letters (01.11.2005)
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Identification of Imidazo[1,2‑b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors
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
Published in ACS medicinal chemistry letters (14.03.2019)
Published in ACS medicinal chemistry letters (14.03.2019)
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Development of BET Inhibitors as Potential Treatments for Cancer: Optimization of Pharmacokinetic Properties
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.
Published in ACS medicinal chemistry letters (14.07.2022)
Published in ACS medicinal chemistry letters (14.07.2022)
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Identification and characterization of TYK2 pseudokinase domain stabilizers that allosterically inhibit TYK2 signaling
Locke, Gregory A, Muckelbauer, Jodi, Tokarski, John S, Barbieri, Christopher M, Belić, Stefan, Falk, Bradley, Tredup, Jeffrey, Wang, Ying-Kai
Published in Methods in enzymology (2022)
Published in Methods in enzymology (2022)
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Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors
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.
Published in Bioorganic & medicinal chemistry letters (15.07.2017)
Published in Bioorganic & medicinal chemistry letters (15.07.2017)
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Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors
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, 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.
Published in Bioorganic & medicinal chemistry letters (15.12.2014)
Published in Bioorganic & medicinal chemistry letters (15.12.2014)
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9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors
Zimmermann, Kurt, Sang, Xiaopeng, Mastalerz, Harold A., Johnson, Walter L., Zhang, Guifen, Liu, Qingjie, Batt, Douglas, Lombardo, Louis J., Vyas, Dinesh, Trainor, George L., Tokarski, John S., Lorenzi, Matthew V., You, Dan, Gottardis, Marco M., Lippy, Jonathan, Khan, Javed, Sack, John S., Purandare, Ashok V.
Published in Bioorganic & medicinal chemistry letters (15.07.2015)
Published in Bioorganic & medicinal chemistry letters (15.07.2015)
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N-(Cycloalkylamino)acyl-2-aminothiazole Inhibitors of Cyclin-Dependent Kinase 2. N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4- piperidinecarboxamide (BMS-387032), a Highly Efficacious and Selective Antitumor Agent
Misra, Raj N, Xiao, Hai-yun, Kim, Kyoung S, Lu, Songfeng, Han, Wen-Ching, Barbosa, Stephanie A, Hunt, John T, Rawlins, David B, Shan, Weifang, Ahmed, Syed Z, Qian, Ligang, Chen, Bang-Chi, Zhao, Rulin, Bednarz, Mark S, Kellar, Kristen A, Mulheron, Janet G, Batorsky, Roberta, Roongta, Urvashi, Kamath, Amrita, Marathe, Punit, Ranadive, Sunanda A, Sack, John S, Tokarski, John S, Pavletich, Nikola P, Lee, Francis Y. F, Webster, Kevin R, Kimball, S. David
Published in Journal of medicinal chemistry (25.03.2004)
Published in Journal of medicinal chemistry (25.03.2004)
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Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms
Wan, Honghe, Schroeder, Gretchen M, Hart, Amy C, Inghrim, Jennifer, Grebinski, James, Tokarski, John S, Lorenzi, Matthew V, You, Dan, Mcdevitt, Theresa, Penhallow, Becky, Vuppugalla, Ragini, Zhang, Yueping, Gu, Xiaomei, Iyer, Ramaswamy, Lombardo, Louis J, Trainor, George L, Ruepp, Stefan, Lippy, Jonathan, Blat, Yuval, Sack, John S, Khan, Javed A, Stefanski, Kevin, Sleczka, Bogdan, Mathur, Arvind, Sun, Jung-Hui, Wong, Michael K, Wu, Dauh-Rurng, Li, Peng, Gupta, Anuradha, Arunachalam, P. N, Pragalathan, Bala, Narayanan, Sankara, K.C, Nanjundaswamy, Kuppusamy, Prakasam, Purandare, Ashok V
Published in ACS medicinal chemistry letters (13.08.2015)
Published in ACS medicinal chemistry letters (13.08.2015)
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