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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Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain
Burke, James R, Cheng, Lihong, Gillooly, Kathleen M, Strnad, Joann, Zupa-Fernandez, Adriana, Catlett, Ian M, Zhang, Yifan, Heimrich, Elizabeth M, McIntyre, Kim W, Cunningham, Mark D, Carman, Julie A, Zhou, Xiadi, Banas, Dana, Chaudhry, Charu, Li, Sha, D'Arienzo, Celia, Chimalakonda, Anjaneya, Yang, XiaoXia, Xie, Jenny H, Pang, Jian, Zhao, Qihong, Rose, Shawn M, Huang, Jinwen, Moslin, Ryan M, Wrobleski, Stephen T, Weinstein, David S, Salter-Cid, Luisa M
Published in Science translational medicine (24.07.2019)
Published in Science translational medicine (24.07.2019)
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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-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton’s Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers
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
Published in Journal of medicinal chemistry (13.10.2016)
Published in Journal of medicinal chemistry (13.10.2016)
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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 Sphingosine-1-phosphate Receptor 1 (S1P1) Modulator Advanced into Clinical Trials
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
Published in Journal of medicinal chemistry (14.03.2019)
Published in Journal of medicinal chemistry (14.03.2019)
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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 Kinase (BTK)
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
Published in Journal of medicinal chemistry (11.04.2019)
Published in Journal of medicinal chemistry (11.04.2019)
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Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Attachment. 5. An Evolution from Indole to Azaindoles Leading to the Discovery of 1-(4-Benzoylpiperazin-1-yl)-2-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)ethane-1,2-dione (BMS-488043), a Drug Candidate That Demonstrates Antiviral Activity in HIV-1-Infected Subjects
Wang, Tao, Yin, Zhiwei, Zhang, Zhongxing, Bender, John A, Yang, Zhong, Johnson, Graham, Yang, Zheng, Zadjura, Lisa M, D’Arienzo, Celia J, DiGiugno Parker, Dawn, Gesenberg, Christophe, Yamanaka, Gregory A, Gong, Yi-Fei, Ho, Hsu-Tso, Fang, Hua, Zhou, Nannan, McAuliffe, Brian V, Eggers, Betsy J, Fan, Li, Nowicka-Sans, Beata, Dicker, Ira B, Gao, Qi, Colonno, Richard J, Lin, Pin-Fang, Meanwell, Nicholas A, Kadow, John F
Published in Journal of medicinal chemistry (10.12.2009)
Published in Journal of medicinal chemistry (10.12.2009)
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Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity
Gong, Hua, Weinstein, David S., Lu, Zhonghui, Duan, James J.-W., Stachura, Sylwia, Haque, Lauren, Karmakar, Ananta, Hemagiri, Hemalatha, Raut, Dhanya Kumar, Gupta, Arun Kumar, Khan, Javed, Camac, Dan, Sack, John S., Pudzianowski, Andrew, Wu, Dauh-Rurng, Yarde, Melissa, Shen, Ding-Ren, Borowski, Virna, Xie, Jenny H., Sun, Huadong, D'Arienzo, Celia, Dabros, Marta, Galella, Michael A., Wang, Faye, Weigelt, Carolyn A., Zhao, Qihong, Foster, William, Somerville, John E., Salter-Cid, Luisa M., Barrish, Joel C., Carter, Percy H., Dhar, T.G. Murali
Published in Bioorganic & medicinal chemistry letters (15.01.2018)
Published in Bioorganic & medicinal chemistry letters (15.01.2018)
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Conformational-Analysis-Guided Discovery of 2,3-Disubstituted Pyridine IDO1 Inhibitors
Cherney, Emily C, Zhang, Liping, Guo, Weiwei, Huang, Audris, Williams, David, Seitz, Steven, Shan, Weifang, Zhu, Xiao, Gullo-Brown, Johnni, Maley, Derrick, Lin, Tai-an, Hunt, John T, Huang, Christine, Yang, Zheng, D’Arienzo, Celia J, Discenza, Lorell N, Ranasinghe, Asoka, Grubb, Mary F, Traeger, Sarah C, Li, Xin, Johnston, Kathy A, Kopcho, Lisa, Fereshteh, Mark, Foster, Kimberly A, Stefanski, Kevin, Delpy, Diane, Dhar, Gopal, Anandam, Aravind, Mahankali, Sandeep, Padmanabhan, Shweta, Rajanna, Prabhakar, Murali, Venkata, Mariappan, T. Thanga, Pattasseri, Shabeerali, Nimje, Roshan Y, Hong, Zhenqiu, Kempson, James, Rampulla, Richard, Mathur, Arvind, Gupta, Anuradha, Borzilleri, Robert, Vite, Gregory, Balog, Aaron
Published in ACS medicinal chemistry letters (08.07.2021)
Published in ACS medicinal chemistry letters (08.07.2021)
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Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK
Srivastava, Anurag S, Ko, Soo, Watterson, Scott H, Pattoli, Mark A, Skala, Stacey, Cheng, Lihong, Obermeier, Mary T, Vickery, Rodney, Discenza, Lorell N, D’Arienzo, Celia J, Gillooly, Kathleen M, Taylor, Tracy L, Pulicicchio, Claudine, McIntyre, Kim W, Yip, Shiuhang, Li, Peng, Sun, Dawn, Wu, Dauh-Rurng, Dai, Jun, Wang, Chunlei, Zhang, Yingru, Wang, Bei, Pawluczyk, Joseph, Kempson, James, Zhao, Rulin, Hou, Xiaoping, Rampulla, Richard, Mathur, Arvind, Galella, Michael A, Salter-Cid, Luisa, Barrish, Joel C, Carter, Percy H, Fura, Aberra, Burke, James R, Tino, Joseph A
Published in ACS medicinal chemistry letters (12.11.2020)
Published in ACS medicinal chemistry letters (12.11.2020)
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Inhibitors of HIV-1 attachment. Part 9: An assessment of oral prodrug approaches to improve the plasma exposure of a tetrazole-containing derivative
Yeung, Kap-Sun, Qiu, Zhilei, Yang, Zheng, Zadjura, Lisa, D’Arienzo, Celia J., Browning, Marc R., Hansel, Steven, Huang, Xiaohua Stella, Eggers, Betsy J., Riccardi, Keith, Lin, Ping-Fang, Meanwell, Nicholas A., Kadow, John F.
Published in Bioorganic & medicinal chemistry letters (01.01.2013)
Published in Bioorganic & medicinal chemistry letters (01.01.2013)
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Discovery of Brivanib Alaninate ((S)-((R)-1-(4-(4-Fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-yl)2-aminopropanoate), A Novel Prodrug of Dual Vascular Endothelial Growth Factor Receptor-2 and Fibroblast Growth Factor Receptor-1 Kinase Inhibitor (BMS-540215)
Cai, Zhen-wei, Zhang, Yongzheng, Borzilleri, Robert M, Qian, Ligang, Barbosa, Stephanie, Wei, Donna, Zheng, Xiaoping, Wu, Lawrence, Fan, Junying, Shi, Zhongping, Wautlet, Barri S, Mortillo, Steve, Jeyaseelan, Robert, Kukral, Daniel W, Kamath, Amrita, Marathe, Punit, D’Arienzo, Celia, Derbin, George, Barrish, Joel C, Robl, Jeffrey A, Hunt, John T, Lombardo, Louis J, Fargnoli, Joseph, Bhide, Rajeev S
Published in Journal of medicinal chemistry (27.03.2008)
Published in Journal of medicinal chemistry (27.03.2008)
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Discovery of Clinical Candidate BMS-906024: A Potent Pan-Notch Inhibitor for the Treatment of Leukemia and Solid Tumors
Gavai, Ashvinikumar V, Quesnelle, Claude, Norris, Derek, Han, Wen-Ching, Gill, Patrice, Shan, Weifang, Balog, Aaron, Chen, Ke, Tebben, Andrew, Rampulla, Richard, Wu, Dauh-Rurng, Zhang, Yingru, Mathur, Arvind, White, Ronald, Rose, Anne, Wang, Haiqing, Yang, Zheng, Ranasinghe, Asoka, D’Arienzo, Celia, Guarino, Victor, Xiao, Lan, Su, Ching, Everlof, Gerry, Arora, Vinod, Shen, Ding Ren, Cvijic, Mary Ellen, Menard, Krista, Wen, Mei-Li, Meredith, Jere, Trainor, George, Lombardo, Louis J, Olson, Richard, Baran, Phil S, Hunt, John T, Vite, Gregory D, Fischer, Bruce S, Westhouse, Richard A, Lee, Francis Y
Published in ACS medicinal chemistry letters (14.05.2015)
Published in ACS medicinal chemistry letters (14.05.2015)
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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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Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials
Dhar, T. G. Murali, Xiao, Hai-Yun, Xie, Jenny, Lehman-McKeeman, Lois D, Wu, Dauh-Rurng, Dabros, Marta, Yang, Xiaoxia, Taylor, Tracy L, Zhou, Xia D, Heimrich, Elizabeth M, Thomas, Rochelle, McIntyre, Kim W, Warrack, Bethanne, Shi, Hong, Levesque, Paul C, Zhu, Jia L, Hennan, James, Balimane, Praveen, Yang, Zheng, Marino, Anthony M, Cornelius, Georgia, D’Arienzo, Celia J, Mathur, Arvind, Shen, Ding Ren, Cvijic, Mary Ellen, Salter-Cid, Luisa, Barrish, Joel C, Carter, Percy H, Dyckman, Alaric J
Published in ACS medicinal chemistry letters (10.03.2016)
Published in ACS medicinal chemistry letters (10.03.2016)
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Identification of Tricyclic Agonists of Sphingosine-1-phosphate Receptor 1 (S1P1) Employing Ligand-Based Drug Design
Xiao, Hai-Yun, Watterson, Scott H, Langevine, Charles M, Srivastava, Anurag S, Ko, Soo S, Zhang, Yanlei, Cherney, Robert J, Guo, Wei-Wei, Gilmore, John L, Sheppeck, James E, Wu, Dauh-Rurng, Li, Peng, Ramasamy, Duraisamy, Arunachalam, Piramanayagam, Mathur, Arvind, Taylor, Tracy L, Shuster, David J, McIntyre, Kim W, Shen, Ding-Ren, Yarde, Melissa, Cvijic, Mary Ellen, Marino, Anthony M, Balimane, Praveen V, Yang, Zheng, Banas, Dana M, Cornelius, Georgia, D’Arienzo, Celia J, Warrack, Bethanne M, Lehman-McKeeman, Lois, Salter-Cid, Luisa M, Xie, Jenny, Barrish, Joel C, Carter, Percy H, Dyckman, Alaric J, Dhar, T. G. Murali
Published in Journal of medicinal chemistry (10.11.2016)
Published in Journal of medicinal chemistry (10.11.2016)
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2017 White Paper on Recent Issues in Bioanalysis: Rise of Hybrid LBA/LCMS Immunogenicity Assays (Part 2: Hybrid LBA/LCMS Biotherapeutics, Biomarkers & Immunogenicity Assays and Regulatory Agencies’ Inputs)
Neubert, Hendrik, Song, An, Lee, Anita, Wei, Cong, Duggan, Jeff, Xu, Keyang, Woolf, Eric, Evans, Chris, Palandra, Joe, Laterza, Omar, Amur, Shashi, Berger, Isabella, Bustard, Mark, Cancilla, Mark, Chen, Shang-Chiung, Cho, Seongeun (Julia), Ciccimaro, Eugene, Cludts, Isabelle, Cocea, Laurent, D’Arienzo, Celia, Danan-Leon, Lieza, Donato, Lorella Di, Garofolo, Fabio, Haidar, Sam, Ishii-Watabe, Akiko, Jiang, Hao, Kadavil, John, Kassim, Sean, Kurki, Pekka, Blaye, Olivier Le, Liu, Kai, Mathews, Rod, Lima Santos, Gustavo Mendes, Niwa, Makoto, Pedras-Vasconcelos, João, Qian, Mark, Rago, Brian, Saad, Ola, Saito, Yoshiro, Savoie, Natasha, Su, Dian, Szapacs, Matthew, Tampal, Nilufer, Vinter, Stephen, Wang, Jian, Welink, Jan, Whale, Emma, Wilson, Amanda, Xue, Y-J
Published in Bioanalysis (01.12.2017)
Published in Bioanalysis (01.12.2017)
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Quantification of human mAbs in mouse tissues using generic affinity enrichment procedures and LC-MS detection
Sleczka, Bogdan G, Mehl, John T, Shuster, David J, Lewis, Katherine E, Moore, Robin, Vuppugalla, Ragini, Rajendran, Surendran, D'Arienzo, Celia J, Olah, Timothy V
Published in Bioanalysis (01.01.2014)
Published in Bioanalysis (01.01.2014)
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Ultrasensitive quantitative LC-MS/MS of an inhibitor of apoptosis protein's antagonist in plasma using protein target affinity extraction
Discenza, Lorell N, Cornelius, Georgia, Gan, Jinping, Szapiel, Nicolas, Talbott, Randy L, Chaudhry, Charu, Roy, Anirban, Borzilleri, Robert M, Vuppugalla, Ragini, Stefanski, Kevin, Moore, Robin, D'Arienzo, Celia J, Olah, Timothy V, Mehl, John T
Published in Bioanalysis (01.02.2016)
Published in Bioanalysis (01.02.2016)
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Utilization of in vitro Caco‐2 permeability and liver microsomal half‐life screens in discovering BMS‐488043, a novel HIV‐1 attachment inhibitor with improved pharmacokinetic properties
Yang, Zheng, Zadjura, Lisa M., Marino, Anthony M., D'Arienzo, Celia J., Malinowski, Jacek, Gesenberg, Christoph, Lin, Pin‐Fang, Colonno, Richard J., Wang, Tao, Kadow, John F., Meanwell, Nicholas A., Hansel, Steven B.
Published in Journal of pharmaceutical sciences (01.04.2010)
Published in Journal of pharmaceutical sciences (01.04.2010)
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Identification of potent tricyclic prodrug S1P1 receptor modulators
Marcoux, David, Xiao, Hai-Yun, Murali Dhar, TG, Xie, Jenny, Lehman-McKeeman, Lois D, Wu, Dauh-Rurng, Dabros, Marta, Yang, Xiaoxia, Taylor, Tracy L, Zhou, Xia D, Heimrich, Elizabeth M, Thomas, Rochelle, McIntyre, Kim W, Shi, Hong, Levesque, Paul C, Sun, Huadong, Yang, Zheng, Marino, Anthony M, Cornelius, Georgia, D'Arienzo, Celia J, Gupta, Anuradha, Pragalathan, Bala, Rampulla, Richard, Mathur, Arvind, Shen, Ding Ren, Cvijic, Mary Ellen, Salter-Cid, Luisa, Lombardo, Louis J, Carter, Percy H, Dyckman, Alaric J
Published in MedChemComm (01.04.2017)
Published in MedChemComm (01.04.2017)
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