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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Bruton's tyrosine kinase inhibitor BMS-986142 in experimental models of rheumatoid arthritis enhances efficacy of agents representing clinical standard-of-care von Gillooly, Kathleen M, Pulicicchio, Claudine, Pattoli, Mark A, Cheng, Lihong, Skala, Stacey, Heimrich, Elizabeth M, McIntyre, Kim W, Taylor, Tracy L, Kukral, Daniel W, Dudhgaonkar, Shailesh, Nagar, Jignesh, Banas, Dana, Watterson, Scott H, Tino, Joseph A, Fura, Aberra, Burke, James R

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2-Aminothiazole as a Novel Kinase Inhibitor Template. Structure−Activity Relationship Studies toward the Discovery of N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piper... von Das, Jagabandhu, Chen, Ping, Norris, Derek, Padmanabha, Ramesh, Lin, James, Moquin, Robert V, Shen, Zhongqi, Cook, Lynda S, Doweyko, Arthur M, Pitt, Sidney, Pang, Suhong, Shen, Ding Ren, Fang, Qiong, de Fex, Henry F, McIntyre, Kim W, Shuster, David J, Gillooly, Kathleen M, Behnia, Kamelia, Schieven, Gary L, Wityak, John, Barrish, Joel C

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Dual Inhibition of Interleukin-23 and Interleukin-17 Offers Superior Efficacy in Mouse Models of Autoimmunity von Mangan, Paul R, Su, Linhui Julie, Jenny, Victoria, Tatum, Andrea L, Picarillo, Caryn, Skala, Stacey, Ditto, Noah, Lin, Zheng, Yang, XiaoXia, Cotter, Pete Z, Shuster, David J, Song, Yunling, Borowski, Virna, Thomas, Rochelle L, Heimrich, Elizabeth M, Devaux, Brigitte, Das Gupta, Ruchira, Carvajal, Irvith, McIntyre, Kim W, Xie, Jenny, Zhao, Qihong, Struthers, Mary, Salter-Cid, Luisa 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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Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton’s Tyrosine Kinas... von Watterson, Scott H, Liu, Qingjie, Beaudoin Bertrand, Myra, Batt, Douglas G, Li, Ling, Pattoli, Mark A, Skala, Stacey, Cheng, Lihong, Obermeier, Mary T, Moore, Robin, Yang, Zheng, Vickery, Rodney, Elzinga, Paul A, Discenza, Lorell, D’Arienzo, Celia, Gillooly, Kathleen M, Taylor, Tracy L, Pulicicchio, Claudine, Zhang, Yifan, Heimrich, Elizabeth, McIntyre, Kim W, Ruan, Qian, Westhouse, Richard A, Catlett, Ian M, Zheng, Naiyu, Chaudhry, Charu, Dai, Jun, Galella, Michael A, Tebben, Andrew J, Pokross, Matt, Li, Jianqing, Zhao, Rulin, Smith, Daniel, Rampulla, Richard, Allentoff, Alban, Wallace, Michael A, Mathur, Arvind, Salter-Cid, Luisa, Macor, John E, Carter, Percy H, Fura, Aberra, Burke, James R, Tino, Joseph A

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Discovery of 6‑Fluoro-5‑(R)‑(3‑(S)‑(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)‑yl)-2-methylphenyl)-2‑(S)‑(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro‑1H‑carbazole-8-carbo... von Watterson, Scott H, De Lucca, George V, Shi, Qing, Langevine, Charles M, Liu, Qingjie, Batt, Douglas G, Beaudoin Bertrand, Myra, Gong, Hua, Dai, Jun, Yip, Shiuhang, Li, Peng, Sun, Dawn, Wu, Dauh-Rurng, Wang, Chunlei, Zhang, Yingru, Traeger, Sarah C, Pattoli, Mark A, Skala, Stacey, Cheng, Lihong, Obermeier, Mary T, Vickery, Rodney, Discenza, Lorell N, D’Arienzo, Celia J, Zhang, Yifan, Heimrich, Elizabeth, Gillooly, Kathleen M, Taylor, Tracy L, Pulicicchio, Claudine, McIntyre, Kim W, Galella, Michael A, Tebben, Andy J, Muckelbauer, Jodi K, Chang, ChiehYing, Rampulla, Richard, Mathur, Arvind, Salter-Cid, Luisa, Barrish, Joel C, Carter, Percy H, Fura, Aberra, Burke, James R, Tino, Joseph A

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Selective IRAK4 Inhibition Attenuates Disease in Murine Lupus Models and Demonstrates Steroid Sparing Activity von Dudhgaonkar, Shailesh, Ranade, Sourabh, Nagar, Jignesh, Subramani, Siva, Prasad, Durga Shiv, Karunanithi, Preethi, Srivastava, Ratika, Venkatesh, Kamala, Selvam, Sabariya, Krishnamurthy, Prasad, Mariappan, T Thanga, Saxena, Ajay, Fan, Li, Stetsko, Dawn K, Holloway, Deborah A, Li, Xin, Zhu, Jun, Yang, Wen-Pin, Ruepp, Stefan, Nair, Satheesh, Santella, Joseph, Duncia, John, Hynes, John, McIntyre, Kim W, Carman, Julie A

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Core exploration in optimization of chemokine receptor CCR4 antagonists von Purandare, Ashok V., Wan, Honghe, Somerville, John E., Burke, Christine, Vaccaro, Wayne, Yang, XiaoXia, McIntyre, Kim W., Poss, Michael A.

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Rationally Designed, Conformationally Constrained Inverse Agonists of RORγtIdentification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy von Marcoux, David, Duan, James J.-W, Shi, Qing, Cherney, Robert J, Srivastava, Anurag S, Cornelius, Lyndon, Batt, Douglas G, Liu, Qingjie, Beaudoin-Bertrand, Myra, Weigelt, Carolyn A, Khandelwal, Purnima, Vishwakrishnan, Sureshbabu, Selvakumar, Kumaravel, Karmakar, Ananta, Gupta, Arun Kumar, Basha, Mushkin, Ramlingam, Sridharan, Manjunath, Naveen, Vanteru, Sridhar, Karmakar, Sukhen, Maddala, Nageswara, Vetrichelvan, Muthalagu, Gupta, Anuradha, Rampulla, Richard A, Mathur, Arvind, Yip, Shiuhang, Li, Peng, Wu, Dauh-Rurng, Khan, Javed, Ruzanov, Max, Sack, John S, Wang, Jinhong, Yarde, Melissa, Cvijic, Mary Ellen, Li, Sha, Shuster, David J, Borowski, Virna, Xie, Jenny H, McIntyre, Kim W, Obermeier, Mary T, Fura, Aberra, Stefanski, Kevin, Cornelius, Georgia, Hynes, John, Tino, Joseph A, Macor, John E, Salter-Cid, Luisa, Denton, Rex, Zhao, Qihong, Carter, Percy H, Dhar, T. G. Murali

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Acridone-Based Inhibitors of Inosine 5‘-Monophosphate Dehydrogenase:  Discovery and SAR Leading to the Identification of N-(2-(6-(4-Ethylpiperazin-1-yl)pyridin-3-yl)propan-2-yl)-2-... von Watterson, Scott H, Chen, Ping, Zhao, Yufen, Gu, Henry H, Dhar, T. G. Murali, Xiao, Zili, Ballentine, Shelley K, Shen, Zhongqi, Fleener, Catherine A, Rouleau, Katherine A, Obermeier, Mary, Yang, Zheng, McIntyre, Kim W, Shuster, David J, Witmer, Mark, Dambach, Donna, Chao, Sam, Mathur, Arvind, Chen, Bang-Chi, Barrish, Joel C, Robl, Jeffrey A, Townsend, Robert, Iwanowicz, Edwin J

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Small Molecule Reversible Inhibitors of Bruton’s Tyrosine Kinase (BTK): Structure–Activity Relationships Leading to the Identification of 7‑(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-... von De Lucca, George V, Shi, Qing, Liu, Qingjie, Batt, Douglas G, Beaudoin Bertrand, Myra, Rampulla, Rick, Mathur, Arvind, Discenza, Lorell, D’Arienzo, Celia, Dai, Jun, Obermeier, Mary, Vickery, Rodney, Zhang, Yingru, Yang, Zheng, Marathe, Punit, Tebben, Andrew J, Muckelbauer, Jodi K, Chang, ChiehYing J, Zhang, Huiping, Gillooly, Kathleen, Taylor, Tracy, Pattoli, Mark A, Skala, Stacey, Kukral, Daniel W, McIntyre, Kim W, Salter-Cid, Luisa, Fura, Aberra, Burke, James R, Barrish, Joel C, Carter, Percy H, Tino, Joseph A

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IL-1 Receptor Accessory Protein Is an Essential Component of the IL-1 Receptor von Cullinan, Emily B, Kwee, Lia, Nunes, Perla, Shuster, David J, Ju, Grace, McIntyre, Kim W, Chizzonite, Richard A, Labow, Mark A

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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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BMS-345541 Is a Highly Selective Inhibitor of IκB Kinase That Binds at an Allosteric Site of the Enzyme and Blocks NF-κB-dependent Transcription in Mice von Burke, James R., Pattoli, Mark A., Gregor, Kurt R., Brassil, Patrick J., MacMaster, John F., McIntyre, Kim W., Yang, Xiaoxia, Iotzova, Violetta S., Clarke, Wendy, Strnad, Joann, Qiu, Yuping, Zusi, F. Christopher

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Bicyclic Ligand-Biased Agonists of S1P 1 : Exploring Side Chain Modifications to Modulate the PK, PD, and Safety Profiles von Gilmore, John L, Xiao, Hai-Yun, Dhar, T G Murali, Yang, Michael, Xiao, Zili, Yang, Xiaoxia, Taylor, Tracy L, McIntyre, Kim W, Warrack, Bethanne M, Shi, Hong, Levesque, Paul C, Marino, Anthony M, Cornelius, Georgia, Mathur, Arvind, Shen, Ding Ren, Pang, Jian, Cvijic, Mary Ellen, Lehman-McKeeman, Lois D, Sun, Huadong, Xie, Jenny, Salter-Cid, Luisa, Carter, Percy H, Dyckman, Alaric J

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Bicyclic Ligand-Biased Agonists of S1P1: Exploring Side Chain Modifications to Modulate the PK, PD, and Safety Profiles von Gilmore, John L, Xiao, Hai-Yun, Dhar, T. G. Murali, Yang, Michael, Xiao, Zili, Yang, Xiaoxia, Taylor, Tracy L, McIntyre, Kim W, Warrack, Bethanne M, Shi, Hong, Levesque, Paul C, Marino, Anthony M, Cornelius, Georgia, Mathur, Arvind, Shen, Ding Ren, Pang, Jian, Cvijic, Mary Ellen, Lehman-McKeeman, Lois D, Sun, Huadong, Xie, Jenny, Salter-Cid, Luisa, Carter, Percy H, Dyckman, Alaric J

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A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice von Kang, Liya, McIntyre, Kim W., Gillooly, Kathleen M., Yang, Yifan, Haycock, John, Roberts, Stephen, Khanna, Ashish, Herpin, Timothy F., Yu, Guixue, Wu, Ximao, Morton, George C., Tuerdi, Huji, Koplowitz, Barry, Walker, Stephen G., Wardwell‐Swanson, Judy, Macor, John E., Lawrence, R. Michael, Carlson, Kenneth E.

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Identification and Preclinical Pharmacology of ((1R,3S)‑1-Amino-3-((S)‑6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated... von Gilmore, John L, Xiao, Hai-Yun, Dhar, T. G. Murali, Yang, Michael G, Xiao, Zili, Xie, Jenny, Lehman-McKeeman, Lois D, Gong, Lei, Sun, Huadong, Lecureux, Lloyd, Chen, Cliff, Wu, Dauh-Rurng, Dabros, Marta, Yang, Xiaoxia, Taylor, Tracy L, Zhou, Xia D, Heimrich, Elizabeth M, Thomas, Rochelle, McIntyre, Kim W, Borowski, Virna, Warrack, Bethanne M, Li, Yuwen, Shi, Hong, Levesque, Paul C, Yang, Zheng, Marino, Anthony M, Cornelius, Georgia, D’Arienzo, Celia J, Mathur, Arvind, Rampulla, Richard, Gupta, Anuradha, Pragalathan, Bala, Shen, Ding Ren, Cvijic, Mary Ellen, Salter-Cid, Luisa M, Carter, Percy H, Dyckman, Alaric J

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