Structure-Based Drug Design of RN486, a Potent and Selective Bruton’s Tyrosine Kinase (BTK) Inhibitor, for the Treatment of Rheumatoid Arthritis
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.
Published in Journal of medicinal chemistry (08.01.2015)
Published in Journal of medicinal chemistry (08.01.2015)
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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 Polymerase
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.
Published in Journal of medicinal chemistry (13.03.2014)
Published in Journal of medicinal chemistry (13.03.2014)
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Design and Synthesis of 4-Azaindoles as Inhibitors of p38 MAP Kinase
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
Published in Journal of medicinal chemistry (23.10.2003)
Published in Journal of medicinal chemistry (23.10.2003)
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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 Cell Malignancies
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
Published in Journal of medicinal chemistry (22.02.2024)
Published in Journal of medicinal chemistry (22.02.2024)
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NRX-0492 degrades wild-type and C481 mutant BTK and demonstrates in vivo activity in CLL patient-derived xenografts
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
Published in Blood (30.03.2023)
Published in Blood (30.03.2023)
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Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2–p53 Inhibitor in Clinical Development
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
Published in Journal of medicinal chemistry (27.02.2014)
Published in Journal of medicinal chemistry (27.02.2014)
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Dual antagonists of alpha 5 beta 1/alpha v beta 1 integrin for airway hyperresponsiveness
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
Published in Bioorganic & medicinal chemistry letters (15.11.2020)
Published in Bioorganic & medicinal chemistry letters (15.11.2020)
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Journal Article
Nx-2127, a Degrader of BTK and IMiD Neosubstrates, for the Treatment of B-Cell Malignancies
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
Published in Blood (05.11.2020)
Published in Blood (05.11.2020)
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Selective and Potent Morpholinone Inhibitors of the MDM2–p53 Protein–Protein Interaction
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
Published in Journal of medicinal chemistry (27.03.2014)
Published in Journal of medicinal chemistry (27.03.2014)
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Journal Article
Dual antagonists of α5β1/αvβ1 integrin for airway hyperresponsiveness
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
Published in Bioorganic & medicinal chemistry letters (15.11.2020)
Published in Bioorganic & medicinal chemistry letters (15.11.2020)
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Journal Article
Targeted Protein Degradation of BTK As a Unique Therapeutic Approach for B Cell Malignancies
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
Published in Blood (13.11.2019)
Published in Blood (13.11.2019)
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Journal Article
Discovery of AM-7209, a Potent and Selective 4‑Amidobenzoic Acid Inhibitor of the MDM2–p53 Interaction
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
Published in Journal of medicinal chemistry (26.12.2014)
Published in Journal of medicinal chemistry (26.12.2014)
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Novel Inhibitors of the MDM2-p53 Interaction Featuring Hydrogen Bond Acceptors as Carboxylic Acid Isosteres
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
Published in Journal of medicinal chemistry (10.04.2014)
Published in Journal of medicinal chemistry (10.04.2014)
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Journal Article
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
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.
Published in Bioorganic & medicinal chemistry letters (15.01.2015)
Published in Bioorganic & medicinal chemistry letters (15.01.2015)
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Journal Article
Exploring N-Arylsulfonyl-L-proline Scaffold as a Platform for Potent and Selective alpha v beta 1 Integrin Inhibitors
Reed, Nilgun Isik, Tang, You-Zhi, McIntosh, Joel, Wu, Yibing, Molnar, Kathleen S., Civitavecchia, Annafelicia, Sheppard, Dean, DeGrado, William F., Jo, Hyunil
Published in ACS medicinal chemistry letters (01.10.2016)
Published in ACS medicinal chemistry letters (01.10.2016)
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Journal Article
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
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
Published in Cancer research (Chicago, Ill.) (04.04.2023)
Published in Cancer research (Chicago, Ill.) (04.04.2023)
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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-(tetrahydro-2 H -pyran-4-ylamino)pyrido[2,3- d ]pyrimidin-7(8 H )-one (R1487) as Orally Bioavailable and Highly Selective Inhibitors of p38α Mitogen-Activated Protein Kinase
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
Published in Journal of medicinal chemistry (14.04.2011)
Published in Journal of medicinal chemistry (14.04.2011)
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Journal Article
Exploring N‑Arylsulfonyl‑l‑proline Scaffold as a Platform for Potent and Selective αvβ1 Integrin Inhibitors
Reed, Nilgun Isik, Tang, You-Zhi, McIntosh, Joel, Wu, Yibing, Molnar, Kathleen S, Civitavecchia, Annafelicia, Sheppard, Dean, DeGrado, William F, Jo, Hyunil
Published in ACS medicinal chemistry letters (13.10.2016)
Published in ACS medicinal chemistry letters (13.10.2016)
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Journal Article
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-(tetrahydro-2H-pyran-4-ylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (R1487) as Orally Bioavailable and Highly Selective Inhibitors of p38α Mitogen-Activated Protein Kinase
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
Published in Journal of medicinal chemistry (14.04.2011)
Published in Journal of medicinal chemistry (14.04.2011)
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