Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors
McTigue, Michele, Murray, Brion William, Chen, Jeffrey H, Deng, Ya-Li, Solowiej, James, Kania, Robert S
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Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19
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Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal–Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Kinase (ALK)
Cui, J. Jean, Tran-Dubé, Michelle, Shen, Hong, Nambu, Mitchell, Kung, Pei-Pei, Pairish, Mason, Jia, Lei, Meng, Jerry, Funk, Lee, Botrous, Iriny, McTigue, Michele, Grodsky, Neil, Ryan, Kevin, Padrique, Ellen, Alton, Gordon, Timofeevski, Sergei, Yamazaki, Shinji, Li, Qiuhua, Zou, Helen, Christensen, James, Mroczkowski, Barbara, Bender, Steve, Kania, Robert S, Edwards, Martin P
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Nonclinical Antiangiogenesis and Antitumor Activities of Axitinib (AG-013736), an Oral, Potent, and Selective Inhibitor of Vascular Endothelial Growth Factor Receptor Tyrosine Kinases 1, 2, 3
HU-LOWE, Dana D, ZOU, Helen Y, MCTIGUE, Michele A, MURRAY, Brion W, KANIA, Robert S, O'CONNOR, Patrick, SHALINSKY, David R, BENDER, Steve L, GRAZZINI, Maren L, HALLIN, Max E, WICKMAN, Grant R, AMUNDSON, Karin, CHEN, Jeffrey H, REWOLINSKI, David A, YAMAZAKI, Shinji, WU, Ellen Y
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Published in Journal of the American Chemical Society (25.09.1996)
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Discovery of (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations
Johnson, Ted W., Richardson, Paul F., Bailey, Simon, Brooun, Alexei, Burke, Benjamin J., Collins, Michael R., Cui, J. Jean, Deal, Judith G., Deng, Ya-Li, Dinh, Dac, Engstrom, Lars D., He, Mingying, Hoffman, Jacqui, Hoffman, Robert L., Huang, Qinhua, Kania, Robert S., Kath, John C., Lam, Hieu, Lam, Justine L., Le, Phuong T., Lingardo, Laura, Liu, Wei, McTigue, Michele, Palmer, Cynthia L., Sach, Neal W., Smeal, Tod, Smith, Graham L., Stewart, Albert E., Timofeevski, Sergei, Zhu, Huichun, Zhu, Jinjiang, Zou, Helen Y., Edwards, Martin P.
Published in Journal of medicinal chemistry (12.06.2014)
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Design and Synthesis of Functionally Active 5‑Amino-6-Aryl Pyrrolopyrimidine Inhibitors of Hematopoietic Progenitor Kinase 1
Gallego, Rebecca A., Bernier, Louise, Chen, Hui, Cho-Schultz, Sujin, Chung, Loanne, Collins, Michael, Del Bel, Matthew, Elleraas, Jeff, Costa Jones, Cinthia, Cronin, Ciaran N., Edwards, Martin, Fang, Xu, Fisher, Timothy, He, Mingying, Hoffman, Jacqui, Huo, Ruiduan, Jalaie, Mehran, Johnson, Eric, Johnson, Ted W., Kania, Robert S., Kraus, Manfred, Lafontaine, Jennifer, Le, Phuong, Liu, Tongnan, Maestre, Michael, Matthews, Jean, McTigue, Michele, Miller, Nichol, Mu, Qiming, Qin, Xulong, Ren, Shijian, Richardson, Paul, Rohner, Allison, Sach, Neal, Shao, Li, Smith, Graham, Su, Ruirui, Sun, Bin, Timofeevski, Sergei, Tran, Phuong, Wang, Shuiwang, Wang, Wei, Zhou, Ru, Zhu, Jinjiang, Nair, Sajiv K.
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The Discovery of Exarafenib (KIN-2787): Overcoming the Challenges of Pan-RAF Kinase Inhibition
Chen, Young K., Kanouni, Toufike, Arnold, Lee D., Cox, Jason M., Gardiner, Elisabeth, Grandinetti, Kathryn, Jiang, Ping, Kaldor, Stephen W., Lee, Catherine, Li, Chun, Martin, Eric S., Miller, Nichol, Murphy, Eric A., Timple, Noel, Tyhonas, John S., Vassar, Angie, Wang, Tim S., Williams, Richard, Yuan, Ding, Kania, Robert S.
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Discovery of N‑((3R,4R)‑4-Fluoro-1-(6-((3-methoxy-1-methyl‑1H‑pyrazol-4-yl)amino)-9-methyl‑9H‑purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR
Planken, Simon, Behenna, Douglas C, Nair, Sajiv K, Johnson, Theodore O, Nagata, Asako, Almaden, Chau, Bailey, Simon, Ballard, T. Eric, Bernier, Louise, Cheng, Hengmiao, Cho-Schultz, Sujin, Dalvie, Deepak, Deal, Judith G, Dinh, Dac M, Edwards, Martin P, Ferre, Rose Ann, Gajiwala, Ketan S, Hemkens, Michelle, Kania, Robert S, Kath, John C, Matthews, Jean, Murray, Brion W, Niessen, Sherry, Orr, Suvi T. M, Pairish, Mason, Sach, Neal W, Shen, Hong, Shi, Manli, Solowiej, James, Tran, Khanh, Tseng, Elaine, Vicini, Paolo, Wang, Yuli, Weinrich, Scott L, Zhou, Ru, Zientek, Michael, Liu, Longqing, Luo, Yiqin, Xin, Shuibo, Zhang, Chengyi, Lafontaine, Jennifer
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Structure-Based Drug Design and Synthesis of PI3K alpha-Selective Inhibitor (PF-06843195)
Cheng, Hengmiao, Orr, Suvi T. M., Bailey, Simon, Brooun, Alexei, Chen, Ping, Deal, Judith G., Deng, Yali L., Edwards, Martin P., Gallego, Gary M., Grodsky, Neil, Huang, Buwen, Jalaie, Mehran, Kaiser, Stephen, Kania, Robert S., Kephart, Susan E., Lafontaine, Jennifer, Ornelas, Martha A., Pairish, Mason, Planken, Simon, Shen, Hong, Sutton, Scott, Zehnder, Luke, Almaden, Chau D., Bagrodia, Shubha, Falk, Matthew D., Gukasyan, Hovhannes J., Ho, Caroline, Kang, Xiaolin, Kosa, Rachel E., Liu, Ling, Spilker, Mary E., Timofeevski, Sergei, Visswanathan, Ravi, Wang, Zhenxiong, Meng, Fanxiu, Ren, Shijian, Shao, Li, Xu, Feng, Kath, John C.
Published in Journal of medicinal chemistry (14.01.2021)
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Discovery of 1‑{(3R,4R)‑3-[({5-Chloro-2-[(1-methyl‑1H‑pyrazol-4-yl)amino]‑7H‑pyrrolo[2,3‑d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants
Cheng, Hengmiao, Nair, Sajiv K, Murray, Brion W, Almaden, Chau, Bailey, Simon, Baxi, Sangita, Behenna, Doug, Cho-Schultz, Sujin, Dalvie, Deepak, Dinh, Dac M, Edwards, Martin P, Feng, Jun Li, Ferre, Rose Ann, Gajiwala, Ketan S, Hemkens, Michelle D, Jackson-Fisher, Amy, Jalaie, Mehran, Johnson, Ted O, Kania, Robert S, Kephart, Susan, Lafontaine, Jennifer, Lunney, Beth, Liu, Kevin K.-C, Liu, Zhengyu, Matthews, Jean, Nagata, Asako, Niessen, Sherry, Ornelas, Martha A, Orr, Suvi T. M, Pairish, Mason, Planken, Simon, Ren, Shijian, Richter, Daniel, Ryan, Kevin, Sach, Neal, Shen, Hong, Smeal, Tod, Solowiej, Jim, Sutton, Scott, Tran, Khanh, Tseng, Elaine, Vernier, William, Walls, Marlena, Wang, Shuiwang, Weinrich, Scott L, Xin, Shuibo, Xu, Haiwei, Yin, Min-Jean, Zientek, Michael, Zhou, Ru, Kath, John C
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Characterizing the Effects of the Juxtamembrane Domain on Vascular Endothelial Growth Factor Receptor-2 Enzymatic Activity, Autophosphorylation, and Inhibition by Axitinib
Solowiej, James, Bergqvist, Simon, McTigue, Michele A, Marrone, Tami, Quenzer, Terri, Cobbs, Morena, Ryan, Kevin, Kania, Robert S, Diehl, Wade, Murray, Brion W
Published in Biochemistry (Easton) (28.07.2009)
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Structure-Based Design of (5-Arylamino-2H-pyrazol-3-yl)-biphenyl-2‘,4‘-diols as Novel and Potent Human CHK1 Inhibitors
Teng, Min, Zhu, Jinjiang, Johnson, Michael D, Chen, Ping, Kornmann, Jill, Chen, Enhong, Blasina, Alessandra, Register, James, Anderes, Kenna, Rogers, Caroline, Deng, Yali, Ninkovic, Sacha, Grant, Stephan, Hu, Qiyue, Lundgren, Karen, Peng, Zhengwei, Kania, Robert S
Published in Journal of medicinal chemistry (01.11.2007)
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Peptoids: A Modular Approach to Drug Discovery
Simon, Reyna J., Kania, Robert S., Zuckermann, Ronald N., Huebner, Verena D., Jewell, David A., Banville, Steven, Ng, Simon, Wang, Liang, Rosenberg, Steven, Marlowe, Charles K., Spellmeyer, David C., Tan, Ruoying, Frankel, Alan D., Santi, Daniel V., Cohen, Fred E., Bartlett, Paul A.
Published in Proceedings of the National Academy of Sciences - PNAS (15.10.1992)
Published in Proceedings of the National Academy of Sciences - PNAS (15.10.1992)
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Design of Potent and Selective Inhibitors to Overcome Clinical Anaplastic Lymphoma Kinase Mutations Resistant to Crizotinib
Huang, Qinhua, Johnson, Ted W, Bailey, Simon, Brooun, Alexei, Bunker, Kevin D, Burke, Benjamin J, Collins, Michael R, Cook, Andrew S, Cui, J. Jean, Dack, Kevin N, Deal, Judith G, Deng, Ya-Li, Dinh, Dac, Engstrom, Lars D, He, Mingying, Hoffman, Jacqui, Hoffman, Robert L, Johnson, Patrick S, Kania, Robert S, Lam, Hieu, Lam, Justine L, Le, Phuong T, Li, Qiuhua, Lingardo, Laura, Liu, Wei, Lu, Melissa West, McTigue, Michele, Palmer, Cynthia L, Richardson, Paul F, Sach, Neal W, Shen, Hong, Smeal, Tod, Smith, Graham L, Stewart, Albert E, Timofeevski, Sergei, Tsaparikos, Konstantinos, Wang, Hui, Zhu, Huichun, Zhu, Jinjiang, Zou, Helen Y, Edwards, Martin P
Published in Journal of medicinal chemistry (27.02.2014)
Published in Journal of medicinal chemistry (27.02.2014)
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Discovery of N -((3 R ,4 R )-4-Fluoro-1-(6-((3-methoxy-1-methyl-1 H -pyrazol-4-yl)amino)-9-methyl-9 H -purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR
Planken, Simon, Behenna, Douglas C., Nair, Sajiv K., Johnson, Theodore O., Nagata, Asako, Almaden, Chau, Bailey, Simon, Ballard, T. Eric, Bernier, Louise, Cheng, Hengmiao, Cho-Schultz, Sujin, Dalvie, Deepak, Deal, Judith G., Dinh, Dac M., Edwards, Martin P., Ferre, Rose Ann, Gajiwala, Ketan S., Hemkens, Michelle, Kania, Robert S., Kath, John C., Matthews, Jean, Murray, Brion W., Niessen, Sherry, Orr, Suvi T. M., Pairish, Mason, Sach, Neal W., Shen, Hong, Shi, Manli, Solowiej, James, Tran, Khanh, Tseng, Elaine, Vicini, Paolo, Wang, Yuli, Weinrich, Scott L., Zhou, Ru, Zientek, Michael, Liu, Longqing, Luo, Yiqin, Xin, Shuibo, Zhang, Chengyi, Lafontaine, Jennifer
Published in Journal of medicinal chemistry (13.04.2017)
Published in Journal of medicinal chemistry (13.04.2017)
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Abstract PR10: Is CNS availability for oncology a no-brainer? Discovery of PF-06463922, a novel small molecule inhibitor of ALK/ROS1 with preclinical brain availability and broad spectrum potency against ALK-resistant mutations
Johnson, Ted W., Bailey, Simon, Burke, Benjamin J., Collins, Michael R., Cui, J. Jean, Deal, Judy, Deng, Ya-Li, Edwards, Martin P., He, Mingying, Hoffman, Jacqui, Hoffman, Robert L., Huang, Qinhua, Kania, Robert S., Le, Phuong, McTigue, Michele, Palmer, Cynthia L., Richardson, Paul F., Sach, Neal W., Smith, Graham L., Engstrom, Lars, Hu, Wenyue, Lam, Hieu, Lam, Justine L., Smeal, Tod, Zou, Helen Y.
Published in Molecular cancer therapeutics (01.11.2013)
Published in Molecular cancer therapeutics (01.11.2013)
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