Structure-Based Drug Design of RN486, a Potent and Selective Bruton’s Tyrosine Kinase (BTK) Inhibitor, for the Treatment of Rheumatoid Arthritis von Lou, Yan, Han, Xiaochun, Kuglstatter, Andreas, Kondru, Rama K., Sweeney, Zachary K., Soth, Michael, McIntosh, Joel, Litman, Renee, Suh, Judy, Kocer, Buelent, Davis, Dana, Park, Jaehyeon, Frauchiger, Sandra, Dewdney, Nolan, Zecic, Hasim, Taygerly, Joshua P., Sarma, Keshab, Hong, Junbae, Hill, Ronald J., Gabriel, Tobias, Goldstein, David M., Owens, Timothy D.

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Discovery of N‑[4-[6-tert-Butyl-5-methoxy-8-(6-methoxy-2-oxo‑1H‑pyridin-3-yl)-3-quinolyl]phenyl]­methanesulfonamide (RG7109), a Potent Inhibitor of the Hepatitis C Virus NS5B Polym... von Talamas, Francisco X., Abbot, Sarah C., Anand, Shalini, Brameld, Ken A., Carter, David S., Chen, Jun, Davis, Dana, de Vicente, Javier, Fung, Amy D., Gong, Leyi, Harris, Seth F., Inbar, Petra, Labadie, Sharada S., Lee, Eun K., Lemoine, Remy, Le Pogam, Sophie, Leveque, Vincent, Li, Jim, McIntosh, Joel, Nájera, Isabel, Park, Jaehyeon, Railkar, Aruna, Rajyaguru, Sonal, Sangi, Michael, Schoenfeld, Ryan C., Staben, Leanna R., Tan, Yunchou, Taygerly, Joshua P., Villaseñor, Armando G., Weller, Paul E.

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Design and Synthesis of 4-Azaindoles as Inhibitors of p38 MAP Kinase von Trejo, Alejandra, Arzeno, Humberto, Browner, Michelle, Chanda, Sushmita, Cheng, Soan, Comer, Daniel D, Dalrymple, Stacie A, Dunten, Pete, Lafargue, JoAnn, Lovejoy, Brett, Freire-Moar, Jose, Lim, Julie, Mcintosh, Joel, Miller, Jennifer, Papp, Eva, Reuter, Deborah, Roberts, Rick, Sanpablo, Florentino, Saunders, John, Song, Kyung, Villasenor, Armando, Warren, Stephen D, Welch, Mary, Weller, Paul, Whiteley, Phyllis E, Zeng, Lu, Goldstein, David M

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Discovery and Preclinical Pharmacology of NX-2127, an Orally Bioavailable Degrader of Bruton’s Tyrosine Kinase with Immunomodulatory Activity for the Treatment of Patients with B C... von Robbins, Daniel W., Noviski, Mark A., Tan, Ying Siow, Konst, Zef A., Kelly, Aileen, Auger, Paul, Brathaban, Nivetha, Cass, Robert, Chan, Ming Liang, Cherala, Ganesh, Clifton, Matthew C., Gajewski, Stefan, Ingallinera, Timothy G., Karr, Dane, Kato, Daisuke, Ma, Jun, McKinnell, Jenny, McIntosh, Joel, Mihalic, Jeff, Murphy, Brent, Panga, Jaipal Reddy, Peng, Ge, Powers, Janine, Perez, Luz, Rountree, Ryan, Tenn-McClellan, Austin, Sands, Arthur T., Weiss, Dahlia R., Wu, Jeffrey, Ye, Jordan, Guiducci, Cristiana, Hansen, Gwenn, Cohen, Frederick

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NRX-0492 degrades wild-type and C481 mutant BTK and demonstrates in vivo activity in CLL patient-derived xenografts von Zhang, Deyi, Harris, Hailey M., Chen, Jonathan, Judy, Jen, James, Gabriella, Kelly, Aileen, McIntosh, Joel, Tenn-McClellan, Austin, Ambing, Eileen, Tan, Ying Siow, Lu, Hao, Gajewski, Stefan, Clifton, Matthew C., Yung, Stephanie, Robbins, Daniel W., Pirooznia, Mehdi, Skånland, Sigrid S., Gaglione, Erika, Mhibik, Maissa, Underbayev, Chingiz, Ahn, Inhye E., Sun, Clare, Herman, Sarah E. M., Noviski, Mark, Wiestner, Adrian

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Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2–p53 Inhibitor in Clinical Development von Sun, Daqing, Li, Zhihong, Rew, Yosup, Gribble, Michael, Bartberger, Michael D, Beck, Hilary P, Canon, Jude, Chen, Ada, Chen, Xiaoqi, Chow, David, Deignan, Jeffrey, Duquette, Jason, Eksterowicz, John, Fisher, Benjamin, Fox, Brian M, Fu, Jiasheng, Gonzalez, Ana Z, Gonzalez-Lopez De Turiso, Felix, Houze, Jonathan B, Huang, Xin, Jiang, Min, Jin, Lixia, Kayser, Frank, Liu, Jiwen (Jim), Lo, Mei-Chu, Long, Alexander M, Lucas, Brian, McGee, Lawrence R, McIntosh, Joel, Mihalic, Jeff, Oliner, Jonathan D, Osgood, Tao, Peterson, Matthew L, Roveto, Philip, Saiki, Anne Y, Shaffer, Paul, Toteva, Maria, Wang, Yingcai, Wang, Yu Chung, Wortman, Sarah, Yakowec, Peter, Yan, Xuelei, Ye, Qiuping, Yu, Dongyin, Yu, Ming, Zhao, Xiaoning, Zhou, Jing, Zhu, Jiang, Olson, Steven H, Medina, Julio C

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Dual antagonists of alpha 5 beta 1/alpha v beta 1 integrin for airway hyperresponsiveness von Sundaram, Aparna, Chen, Chun, Reed, Nilgun Isik, Liu, Sean, Yeon, Seul Ki, McIntosh, Joel, Tang, You-Zhi, Yang, Hyunjun, Adler, Marc, Beresis, Richard, Seiple, Ian B., Sheppard, Dean, DeGrado, William F., Jo, Hyunil

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Nx-2127, a Degrader of BTK and IMiD Neosubstrates, for the Treatment of B-Cell Malignancies von Robbins, Daniel W, Kelly, Aileen, Tan, May, McIntosh, Joel, Wu, Jeffrey, Konst, Zef, Kato, Daisuke, Peng, Ge, Mihalic, Jeff, Weiss, Dahlia, Perez, Luz, Tung, Jennifer, Kolobova, Anna, Borodovsky, Sasha, Rountree, Ryan, Tenn-McClellan, Austin, Noviski, Mark, Ye, Jordan, Basham, Steve, Ingallinera, Timothy, McKinnell, Jenny, Karr, Dane E, Powers, Janine, Guiducci, Cristiana, Sands, Arthur

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Selective and Potent Morpholinone Inhibitors of the MDM2–p53 Protein–Protein Interaction von Gonzalez, Ana Z, Eksterowicz, John, Bartberger, Michael D, Beck, Hilary P, Canon, Jude, Chen, Ada, Chow, David, Duquette, Jason, Fox, Brian M, Fu, Jiasheng, Huang, Xin, Houze, Jonathan B, Jin, Lixia, Li, Yihong, Li, Zhihong, Ling, Yun, Lo, Mei-Chu, Long, Alexander M, McGee, Lawrence R, McIntosh, Joel, McMinn, Dustin L, Oliner, Jonathan D, Osgood, Tao, Rew, Yosup, Saiki, Anne Y, Shaffer, Paul, Wortman, Sarah, Yakowec, Peter, Yan, Xuelei, Ye, Qiuping, Yu, Dongyin, Zhao, Xiaoning, Zhou, Jing, Olson, Steven H, Medina, Julio C, Sun, Daqing

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Dual antagonists of α5β1/αvβ1 integrin for airway hyperresponsiveness von Sundaram, Aparna, Chen, Chun, Isik Reed, Nilgun, Liu, Sean, Ki Yeon, Seul, McIntosh, Joel, Tang, You-Zhi, Yang, Hyunjun, Adler, Marc, Beresis, Richard, Seiple, Ian B., Sheppard, Dean, DeGrado, William F., Jo, Hyunil

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Targeted Protein Degradation of BTK As a Unique Therapeutic Approach for B Cell Malignancies von Kelly, Aileen, Robbins, Daniel W, Tan, May, Tenn-McClellan, Austin, McIntosh, Joel, Wu, Jeffrey, Konst, Zef, Kato, Daisuke, Perez, Luz, Tung, Jennifer, Kolobova, Anna, Ingallinera, Timothy, McKinnell, Jenny, Weiss, Dahlia, Noviski, Mark, Ye, Jordan, Peng, Ge, Cardozo, Mario, Mihalic, Jeff, Basham, Steve, Rountree, Ryan, Karr, Dane E, Bence, Neil, Zapf, Christoph W, Sands, Arthur T

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Discovery of AM-7209, a Potent and Selective 4‑Amidobenzoic Acid Inhibitor of the MDM2–p53 Interaction von Rew, Yosup, Sun, Daqing, Yan, Xuelei, Beck, Hilary P, Canon, Jude, Chen, Ada, Duquette, Jason, Eksterowicz, John, Fox, Brian M, Fu, Jiasheng, Gonzalez, Ana Z, Houze, Jonathan, Huang, Xin, Jiang, Min, Jin, Lixia, Li, Yihong, Li, Zhihong, Ling, Yun, Lo, Mei-Chu, Long, Alexander M, McGee, Lawrence R, McIntosh, Joel, Oliner, Jonathan D, Osgood, Tao, Saiki, Anne Y, Shaffer, Paul, Wang, Yu Chung, Wortman, Sarah, Yakowec, Peter, Ye, Qiuping, Yu, Dongyin, Zhao, Xiaoning, Zhou, Jing, Medina, Julio C, Olson, Steven H

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Novel Inhibitors of the MDM2-p53 Interaction Featuring Hydrogen Bond Acceptors as Carboxylic Acid Isosteres von Gonzalez, Ana Z, Li, Zhihong, Beck, Hilary P, Canon, Jude, Chen, Ada, Chow, David, Duquette, Jason, Eksterowicz, John, Fox, Brian M, Fu, Jiasheng, Huang, Xin, Houze, Jonathan, Jin, Lixia, Li, Yihong, Ling, Yun, Lo, Mei-Chu, Long, Alexander M, McGee, Lawrence R, McIntosh, Joel, Oliner, Jonathan D, Osgood, Tao, Rew, Yosup, Saiki, Anne Y, Shaffer, Paul, Wortman, Sarah, Yakowec, Peter, Yan, Xuelei, Ye, Qiuping, Yu, Dongyin, Zhao, Xiaoning, Zhou, Jing, Olson, Steven H, Sun, Daqing, Medina, Julio C

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Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold von Lou, Yan, Sweeney, Zachary K, Kuglstatter, Andreas, Davis, Dana, Goldstein, David M, Han, Xiaochun, Hong, Junbae, Kocer, Buelent, Kondru, Rama K, Litman, Renee, McIntosh, Joel, Sarma, Keshab, Suh, Judy, Taygerly, Joshua, Owens, Timothy D

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Abstract 3423: NX-2127: A first-in-class clinical stage degrader of BTK and IKZF1/3 for the treatment of patients with B cell malignancies von Mihalic, Jeffrey T., Brathaban, Nivetha, Bravo, Brandon, Ingallinera, Timothy, Kato, Daisuke, Lu, Hao, Ma, Jun, McIntosh, Joel, Tenn-McClellan, Austin, Mukerji, Ratul, Noviski, Mark A., Peng, Ge, Perez, Luz, Rountree, Ryan, Tan, May, Wu, Jeffrey, Ye, Jordan, Yung, Stephanie

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Discovery of 6-(2,4-Difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8 H -pyrido[2,3- d ]pyrimidin-7-one (Pamapimod) and 6-(2,4-Difluorophenoxy)-8-methyl-2-(te... von Goldstein, David M., Soth, Michael, Gabriel, Tobias, Dewdney, Nolan, Kuglstatter, Andreas, Arzeno, Humberto, Chen, Jeffrey, Bingenheimer, William, Dalrymple, Stacie A., Dunn, James, Farrell, Robert, Frauchiger, Sandra, La Fargue, JoAnn, Ghate, Manjiri, Graves, Bradford, Hill, Ronald J., Li, Fujun, Litman, Renee, Loe, Brad, McIntosh, Joel, McWeeney, Daniel, Papp, Eva, Park, Jaehyeon, Reese, Harlan F., Roberts, Richard T., Rotstein, David, San Pablo, Bong, Sarma, Keshab, Stahl, Martin, Sung, Man-Ling, Suttman, Rebecca T., Sjogren, Eric B., Tan, Yunchou, Trejo, Alejandra, Welch, Mary, Weller, Paul, Wong, Brian R., Zecic, Hasim

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Exploring N‑Arylsulfonyl‑l‑proline Scaffold as a Platform for Potent and Selective αvβ1 Integrin Inhibitors von Reed, Nilgun Isik, Tang, You-Zhi, McIntosh, Joel, Wu, Yibing, Molnar, Kathleen S, Civitavecchia, Annafelicia, Sheppard, Dean, DeGrado, William F, Jo, Hyunil

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Discovery of 6-(2,4-Difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidin-7-one (Pamapimod) and 6-(2,4-Difluorophenoxy)-8-methyl-2-(tetrah... von Goldstein, David M, Soth, Michael, Gabriel, Tobias, Dewdney, Nolan, Kuglstatter, Andreas, Arzeno, Humberto, Chen, Jeffrey, Bingenheimer, William, Dalrymple, Stacie A, Dunn, James, Farrell, Robert, Frauchiger, Sandra, La Fargue, JoAnn, Ghate, Manjiri, Graves, Bradford, Hill, Ronald J, Li, Fujun, Litman, Renee, Loe, Brad, McIntosh, Joel, McWeeney, Daniel, Papp, Eva, Park, Jaehyeon, Reese, Harlan F, Roberts, Richard T, Rotstein, David, San Pablo, Bong, Sarma, Keshab, Stahl, Martin, Sung, Man-Ling, Suttman, Rebecca T, Sjogren, Eric B, Tan, Yunchou, Trejo, Alejandra, Welch, Mary, Weller, Paul, Wong, Brian R, Zecic, Hasim

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Synthesis of Vinyl Sulfonamides Using the Horner Reaction von Reuter, Deborah C., McIntosh, Joel E., Guinn, Ashley C., Madera, Ann Marie

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3-Amino-pyrazolo[3,4-d]pyrimidines as p38α kinase inhibitors: Design and development to a highly selective lead von Soth, Michael, Abbot, Sarah, Abubakari, Allassan, Arora, Nidhi, Arzeno, Humberto, Billedeau, Roland, Dewdney, Nolan, Durkin, Kieran, Frauchiger, Sandra, Ghate, Manjiri, Goldstein, David M., Hill, Ronald J., Kuglstatter, Andreas, Li, Fujun, Loe, Brad, McCaleb, Kristen, McIntosh, Joel, Papp, Eva, Park, Jaehyeon, Stahl, Martin, Sung, Man-Ling, Suttman, Rebecca, Swinney, David C., Weller, Paul, Wong, Brian, Zecic, Hasim, Gabriel, Tobias

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