Lipophilic Efficiency as an Important Metric in Drug Design
Johnson, Ted W, Gallego, Rebecca A, Edwards, Martin P
Published in Journal of medicinal chemistry (09.08.2018)
Published in Journal of medicinal chemistry (09.08.2018)
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Journal Article
Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound ALK Mutations in ALK-Positive Lung Cancer
Yoda, Satoshi, Lin, Jessica J, Lawrence, Michael S, Burke, Benjamin J, Friboulet, Luc, Langenbucher, Adam, Dardaei, Leila, Prutisto-Chang, Kylie, Dagogo-Jack, Ibiayi, Timofeevski, Sergei, Hubbeling, Harper, Gainor, Justin F, Ferris, Lorin A, Riley, Amanda K, Kattermann, Krystina E, Timonina, Daria, Heist, Rebecca S, Iafrate, A John, Benes, Cyril H, Lennerz, Jochen K, Mino-Kenudson, Mari, Engelman, Jeffrey A, Johnson, Ted W, Hata, Aaron N, Shaw, Alice T
Published in Cancer discovery (01.06.2018)
Published in Cancer discovery (01.06.2018)
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Using the Golden Triangle to optimize clearance and oral absorption
Johnson, Ted W., Dress, Klaus R., Edwards, Martin
Published in Bioorganic & medicinal chemistry letters (01.10.2009)
Published in Bioorganic & medicinal chemistry letters (01.10.2009)
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Journal Article
PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models
Zou, Helen Y., Friboulet, Luc, Kodack, David P., Engstrom, Lars D., Li, Qiuhua, West, Melissa, Tang, Ruth W., Wang, Hui, Tsaparikos, Konstantinos, Wang, Jinwei, Timofeevski, Sergei, Katayama, Ryohei, Dinh, Dac M., Lam, Hieu, Lam, Justine L., Yamazaki, Shinji, Hu, Wenyue, Patel, Bhushankumar, Bezwada, Divya, Frias, Rosa L., Lifshits, Eugene, Mahmood, Sidra, Gainor, Justin F., Affolter, Timothy, Lappin, Patrick B., Gukasyan, Hovhannes, Lee, Nathan, Deng, Shibing, Jain, Rakesh K., Johnson, Ted W., Shaw, Alice T., Fantin, Valeria R., Smeal, Tod
Published in Cancer cell (13.07.2015)
Published in Cancer cell (13.07.2015)
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PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations
Zou, Helen Y., Li, Qiuhua, Engstrom, Lars D., West, Melissa, Appleman, Vicky, Wong, Katy A., McTigue, Michele, Deng, Ya-Li, Liu, Wei, Brooun, Alexei, Timofeevski, Sergei, McDonnell, Scott R. P., Jiang, Ping, Falk, Matthew D., Lappin, Patrick B., Affolter, Timothy, Nichols, Tim, Hu, Wenyue, Lam, Justine, Johnson, Ted W., Smeal, Tod, Charest, Al, Fantin, Valeria R.
Published in Proceedings of the National Academy of Sciences - PNAS (17.03.2015)
Published in Proceedings of the National Academy of Sciences - PNAS (17.03.2015)
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Journal Article
Spectrum of Mechanisms of Resistance to Crizotinib and Lorlatinib in ROS1 Fusion-Positive Lung Cancer
Lin, Jessica J, Choudhury, Noura J, Yoda, Satoshi, Zhu, Viola W, Johnson, Ted W, Sakhtemani, Ramin, Dagogo-Jack, Ibiayi, Digumarthy, Subba R, Lee, Charlotte, Do, Andrew, Peterson, Jennifer, Prutisto-Chang, Kylie, Malik, Wafa, Hubbeling, Harper G, Langenbucher, Adam, Schoenfeld, Adam J, Falcon, Christina J, Temel, Jennifer S, Sequist, Lecia V, Yeap, Beow Y, Lennerz, Jochen K, Shaw, Alice T, Lawrence, Michael S, Ou, Sai-Hong Ignatius, Hata, Aaron N, Drilon, Alexander, Gainor, Justin F
Published in Clinical cancer research (15.05.2021)
Published in Clinical cancer research (15.05.2021)
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Journal Article
Reviving B‑Factors: Activating ALK Mutations Increase Protein Dynamics of the Unphosphorylated Kinase
Johnson, Ted W, Bolanos, Ben, Brooun, Alexei, Gallego, Rebecca A, Gehlhaar, Dan, Jalaie, Mehran, McTigue, Michele, Timofeevski, Sergei
Published in ACS medicinal chemistry letters (13.09.2018)
Published in ACS medicinal chemistry letters (13.09.2018)
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Journal Article
Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F
Shaw, Alice T, Friboulet, Luc, Leshchiner, Ignaty, Gainor, Justin F, Bergqvist, Simon, Brooun, Alexei, Burke, Benjamin J, Deng, Ya-Li, Liu, Wei, Dardaei, Leila, Frias, Rosa L, Schultz, Kate R, Logan, Jennifer, James, Leonard P, Smeal, Tod, Timofeevski, Sergei, Katayama, Ryohei, Iafrate, A. John, Le, Long, McTigue, Michele, Getz, Gad, Johnson, Ted W, Engelman, Jeffrey A
Published in The New England journal of medicine (07.01.2016)
Published in The New England journal of medicine (07.01.2016)
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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)
Published in Journal of medicinal chemistry (12.06.2014)
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Journal Article
LTK fusions: A new target emerges in non-small cell lung cancer
Cooper, Alissa J., Sequist, Lecia V., Johnson, Ted W., Lin, Jessica J.
Published in Cancer cell (10.01.2022)
Published in Cancer cell (10.01.2022)
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Journal Article
Conformational Studies and Atropisomerism Kinetics of the ALK Clinical Candidate Lorlatinib (PF-06463922) and Desmethyl Congeners
Elleraas, Jeff, Ewanicki, Jason, Johnson, Ted W., Sach, Neal W., Collins, Michael R., Richardson, Paul F.
Published in Angewandte Chemie International Edition (07.03.2016)
Published in Angewandte Chemie International Edition (07.03.2016)
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Journal Article
Multiple conformational states of the HPK1 kinase domain in complex with sunitinib reveal the structural changes accompanying HPK1 trans-regulation
Johnson, Eric, McTigue, Michele, Gallego, Rebecca A., Johnson, Ted W., Timofeevski, Sergei, Maestre, Michael, Fisher, Timothy S., Kania, Robert, Sawasdikosol, Sansana, Burakoff, Steven, Cronin, Ciarán N.
Published in The Journal of biological chemistry (07.06.2019)
Published in The Journal of biological chemistry (07.06.2019)
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Journal Article
Lipophilic efficiency: the most important efficiency metric in medicinal chemistry
Freeman-Cook, Kevin D, Hoffman, Robert L, Johnson, Ted W
Published in Future medicinal chemistry (01.02.2013)
Published in Future medicinal chemistry (01.02.2013)
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The Axl kinase domain in complex with a macrocyclic inhibitor offers first structural insights into an active TAM receptor kinase
Gajiwala, Ketan S., Grodsky, Neil, Bolaños, Ben, Feng, Junli, Ferre, RoseAnn, Timofeevski, Sergei, Xu, Meirong, Murray, Brion W., Johnson, Ted W., Stewart, Al
Published in The Journal of biological chemistry (22.09.2017)
Published in The Journal of biological chemistry (22.09.2017)
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Journal Article
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.
Published in Journal of medicinal chemistry (13.04.2023)
Published in Journal of medicinal chemistry (13.04.2023)
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Reviving B‑Factors: Retrospective Normalized B‑Factor Analysis of c‑ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib
Johnson, Ted W, Gallego, Rebecca A, Brooun, Alexei, Gehlhaar, Dan, McTigue, Michele
Published in ACS medicinal chemistry letters (13.09.2018)
Published in ACS medicinal chemistry letters (13.09.2018)
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Journal Article
Analysis of lorlatinib analogs reveals a roadmap for targeting diverse compound resistance mutations in ALK-positive lung cancer
Shiba-Ishii, Aya, Johnson, Ted W, Dagogo-Jack, Ibiayi, Mino-Kenudson, Mari, Johnson, Theodore R, Wei, Ping, Weinrich, Scott L, McTigue, Michele A, Walcott, Makeba A, Nguyen-Phuong, Linh, Dionne, Kristin, Acker, Adam, Kiedrowski, Lesli A, Do, Andrew, Peterson, Jennifer L, Barth, Jaimie L, Yeap, Beow Y, Gainor, Justin F, Lin, Jessica J, Yoda, Satoshi, Hata, Aaron N
Published in Nature cancer (01.06.2022)
Published in Nature cancer (01.06.2022)
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Journal Article
CNS Anticancer Drug Discovery and Development Conference White Paper
Levin, Victor A, Tonge, Peter J, Gallo, James M, Birtwistle, Marc R, Dar, Arvin C, Iavarone, Antonio, Paddison, Patrick J, Heffron, Timothy P, Elmquist, William F, Lachowicz, Jean E, Johnson, Ted W, White, Forest M, Sul, Joohee, Smith, Quentin R, Shen, Wang, Sarkaria, Jann N, Samala, Ramakrishna, Wen, Patrick Y, Berry, Donald A, Petter, Russell C
Published in Neuro-oncology (01.11.2015)
Published in Neuro-oncology (01.11.2015)
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Conference Proceeding
Effect of water solvation on the lipophilicity of isomeric pyrimidine-carboxamides
Linton, Maria Angelica, Burke, Benjamin J., Johnson, Ted W., Ninkovic, Sacha, Gajiwala, Ketan S., Richardson, Paul, Le, Phuong T.
Published in Bioorganic & medicinal chemistry (01.07.2015)
Published in Bioorganic & medicinal chemistry (01.07.2015)
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