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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Journal Article
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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Journal Article
An Efficient Scale-Up Synthesis of BMS-520, a Potent and Selective Isoxazole-Containing S1P1 Receptor Agonist
Hou, Xiaoping, Zhu, Juliang, Chen, Bang-Chi, Watterson, Scott H, Pitts, William J, Dyckman, Alaric J, Carter, Percy H, Mathur, Arvind, Zhang, Huiping
Published in Organic process research & development (20.05.2016)
Published in Organic process research & development (20.05.2016)
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Journal Article
Practical olefin hydroamination with nitroarenes
Gui, Jinghan, Pan, Chung-Mao, Jin, Ying, Qin, Tian, Lo, Julian C., Lee, Bryan J., Spergel, Steven H., Mertzman, Michael E., Pitts, William J., La Cruz, Thomas E., Schmidt, Michael A., Darvatkar, Nitin, Natarajan, Swaminathan R., Baran, Phil S.
Published in Science (American Association for the Advancement of Science) (22.05.2015)
Published in Science (American Association for the Advancement of Science) (22.05.2015)
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Journal Article
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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Journal Article
Comparison of percentile tables and algorithm‐based calculators for classification of blood pressures in children and adolescents with obesity: A secondary analysis of a clinical trial
Pitts, William J, Cave, Tami L, Cavadino, Alana, Shypailo, Roman J, Maessen, Sarah E, Hofman, Paul L, Wong, William, Anderson, Yvonne C
Published in Journal of paediatrics and child health (01.02.2023)
Published in Journal of paediatrics and child health (01.02.2023)
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Journal Article
Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage
Hart, Amy C, Abell, Lynn, Guo, Junqing, Mertzman, Michael E, Padmanabha, Ramesh, Macor, John E, Chaudhry, Charu, Lu, Hao, O’Malley, Kevin, Shaw, Patrick J, Weigelt, Carolyn, Pokross, Matthew, Kish, Kevin, Kim, Kyoung S, Cornelius, Lyndon, Douglas, Andrew E, Calambur, Deepa, Zhang, Ping, Carpenter, Brian, Pitts, William J
Published in ACS medicinal chemistry letters (12.03.2020)
Published in ACS medicinal chemistry letters (12.03.2020)
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Journal Article
Discovery and structure-based design of 4,6-diaminonicotinamides as potent and selective IRAK4 inhibitors
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.
Published in Bioorganic & medicinal chemistry letters (01.11.2017)
Published in Bioorganic & medicinal chemistry letters (01.11.2017)
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Journal Article
Discovery of highly potent, selective, covalent inhibitors of JAK3
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.
Published in Bioorganic & medicinal chemistry letters (15.10.2017)
Published in Bioorganic & medicinal chemistry letters (15.10.2017)
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Journal Article
Discovery and Structure–Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1)
Gilmore, John L, Sheppeck, James E, Watterson, Scott H, Haque, Lauren, Mukhopadhyay, Parag, Tebben, Andrew J, Galella, Michael A, Shen, Ding Ren, Yarde, Melissa, Cvijic, Mary Ellen, Borowski, Virna, Gillooly, Kathleen, Taylor, Tracy, McIntyre, Kim W, Warrack, Bethanne, Levesque, Paul C, Li, Julia P, Cornelius, Georgia, D’Arienzo, Celia, Marino, Anthony, Balimane, Praveen, Salter-Cid, Luisa, Barrish, Joel C, Pitts, William J, Carter, Percy H, Xie, Jenny, Dyckman, Alaric J
Published in Journal of medicinal chemistry (14.07.2016)
Published in Journal of medicinal chemistry (14.07.2016)
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Journal Article
Potent and Selective Agonists of Sphingosine 1‑Phosphate 1 (S1P1): Discovery and SAR of a Novel Isoxazole Based Series
Watterson, Scott H, Guo, Junqing, Spergel, Steve H, Langevine, Charles M, Moquin, Robert V, Shen, Ding Ren, Yarde, Melissa, Cvijic, Mary Ellen, Banas, Dana, Liu, Richard, Suchard, Suzanne J, Gillooly, Kathleen, Taylor, Tracy, Rex-Rabe, Sandra, Shuster, David J, McIntyre, Kim W, Cornelius, Georgia, D’Arienzo, Celia, Marino, Anthony, Balimane, Praveen, Warrack, Bethanne, Salter-Cid, Luisa, McKinnon, Murray, Barrish, Joel C, Carter, Percy H, Pitts, William J, Xie, Jenny, Dyckman, Alaric J
Published in Journal of medicinal chemistry (24.03.2016)
Published in Journal of medicinal chemistry (24.03.2016)
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Journal Article
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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Journal Article
Optimization of Nicotinamides as Potent and Selective IRAK4 Inhibitors with Efficacy in a Murine Model of Psoriasis
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
Published in ACS medicinal chemistry letters (09.07.2020)
Published in ACS medicinal chemistry letters (09.07.2020)
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Journal Article
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis
Spergel, Steven H, Mertzman, Michael E, Kempson, James, Guo, Junqing, Stachura, Sylwia, Haque, Lauren, Lippy, Jonathan S, Zhang, Rosemary F, Galella, Michael, Pitt, Sidney, Shen, Guoxiang, Fura, Aberra, Gillooly, Kathleen, McIntyre, Kim W, Tang, Vicky, Tokarski, John, Sack, John S, Khan, Javed, Carter, Percy H, Barrish, Joel C, Nadler, Steven G, Salter-Cid, Luisa M, Schieven, Gary L, Wrobleski, Stephen T, Pitts, William J
Published in ACS medicinal chemistry letters (14.03.2019)
Published in ACS medicinal chemistry letters (14.03.2019)
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Journal Article
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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Journal Article
Identification of a Novel Inhibitor of Mitogen-activated Protein Kinase Kinase
Favata, M F, Horiuchi, K Y, Manos, E J, Daulerio, A J, Stradley, D A, Feeser, W S, Van Dyk, D E, Pitts, W J, Earl, R A, Hobbs, F, Copeland, R A, Magolda, R L, Scherle, P A, Trzaskos, J M
Published in The Journal of biological chemistry (17.07.1998)
Published in The Journal of biological chemistry (17.07.1998)
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Journal Article
Identification and synthesis of potent and selective pyridyl-isoxazole based agonists of sphingosine-1-phosphate 1 (S1P1)
Guo, Junqing, Watterson, Scott H., Spergel, Steven H., Kempson, James, Langevine, Charles M., Shen, Ding Ren, Yarde, Melissa, Cvijic, Mary Ellen, Banas, Dana, Liu, Richard, Suchard, Suzanne J., Gillooly, Kathleen, Taylor, Tracy, Rex-Rabe, Sandra, Shuster, David J., McIntyre, Kim W., Cornelius, Georgia, D’Arienzo, Celia, Marino, Anthony, Balimane, Praveen, Salter-Cid, Luisa, McKinnon, Murray, Barrish, Joel C., Carter, Percy H., Pitts, William J., Xie, Jenny, Dyckman, Alaric J.
Published in Bioorganic & medicinal chemistry letters (15.05.2016)
Published in Bioorganic & medicinal chemistry letters (15.05.2016)
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Journal Article
Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5‑d]pyrrolo[2,3‑b]pyridine Inhibitors
Hart, Amy C, Schroeder, Gretchen M, Wan, Honghe, Grebinski, James, Inghrim, Jennifer, Kempson, James, Guo, Junqing, Pitts, William J, Tokarski, John S, Sack, John S, Khan, Javed A, Lippy, Jonathan, Lorenzi, Matthew V, You, Dan, McDevitt, Theresa, Vuppugalla, Ragini, Zhang, Yueping, Lombardo, Louis J, Trainor, George L, 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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