Antitumor Activity of Osimertinib, an Irreversible Mutant-Selective EGFR Tyrosine Kinase Inhibitor, in NSCLC Harboring EGFR Exon 20 Insertions
Floc'h, Nicolas, Martin, Matthew J, Riess, Jonathan W, Orme, Jonathan P, Staniszewska, Anna D, Ménard, Ludovic, Cuomo, Maria Emanuela, O'Neill, Daniel J, Ward, Richard A, Finlay, M Raymond V, McKerrecher, Darren, Cheng, Mingshan, Vang, Daniel P, Burich, Rebekah A, Keck, James G, Gandara, David R, Mack, Philip C, Cross, Darren A E
Published in Molecular cancer therapeutics (01.05.2018)
Published in Molecular cancer therapeutics (01.05.2018)
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Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD5305): A PARP1-DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs
Johannes, Jeffrey W., Balazs, Amber, Barratt, Derek, Bista, Michal, Chuba, Matthew D., Cosulich, Sabina, Critchlow, Susan E., Degorce, Sebastien L., Di Fruscia, Paolo, Edmondson, Scott D., Embrey, Kevin, Fawell, Stephen, Ghosh, Avipsa, Gill, Sonja J., Gunnarsson, Anders, Hande, Sudhir M., Heightman, Tom D., Hemsley, Paul, Illuzzi, Giuditta, Lane, Jordan, Larner, Carrie, Leo, Elisabetta, Liu, Lina, Madin, Andrew, Martin, Scott, McWilliams, Lisa, O'Connor, Mark J., Orme, Jonathan P., Pachl, Fiona, Packer, Martin J., Pei, Xiaohui, Pike, Andrew, Schimpl, Marianne, She, Hongyao, Staniszewska, Anna D., Talbot, Verity, Underwood, Elizabeth, Varnes, Jeffrey G., Xue, Lin, Yao, Tieguang, Zhang, Ke, Zhang, Andrew X., Zheng, Xiaolan
Published in Journal of medicinal chemistry (14.10.2021)
Published in Journal of medicinal chemistry (14.10.2021)
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Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations
Thomson, Clare, Barton, Peter, Braybrooke, Erin, Colclough, Nicola, Dong, Zhiqiang, Evans, Laura, Floc’h, Nicolas, Guérot, Carine, Hargreaves, David, Khurana, Puneet, Li, Songlei, Li, Xiuwei, Lister, Andrew, McCoull, William, McWilliams, Lisa, Orme, Jonathan P., Packer, Martin J., Swaih, Aisha M., Ward, Richard A., Winlow, Poppy, Ye, Yang
Published in Journal of medicinal chemistry (21.05.2024)
Published in Journal of medicinal chemistry (21.05.2024)
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Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance
Finlay, M. Raymond V, Barton, Peter, Bickerton, Sue, Bista, Michal, Colclough, Nicola, Cross, Darren A. E, Evans, Laura, Floc’h, Nicolas, Gregson, Clare, Guérot, Carine M, Hargreaves, David, Kang, Xiaoming, Lenz, Eva M, Li, Xu, Liu, Yi, Lorthioir, Olivier, Martin, Matthew J, McKerrecher, Darren, McWhirter, Claire, O’Neill, Daniel, Orme, Jonathan P, Mosallanejad, Arash, Rahi, Amar, Smith, Paul D, Talbot, Verity, Ward, Richard A, Wrigley, Gail, Wylot, Marta, Xue, Lin, Yao, Tieguang, Ye, Yang, Zhao, Xiliang
Published in Journal of medicinal chemistry (23.09.2021)
Published in Journal of medicinal chemistry (23.09.2021)
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Positioning High-Throughput CETSA in Early Drug Discovery through Screening against B-Raf and PARP1
Shaw, Joseph, Dale, Ian, Hemsley, Paul, Leach, Lindsey, Dekki, Nancy, Orme, Jonathan P., Talbot, Verity, Narvaez, Ana J., Bista, Michal, Martinez Molina, Daniel, Dabrowski, Michael, Main, Martin J., Gianni, Davide
Published in SLAS discovery (01.02.2019)
Published in SLAS discovery (01.02.2019)
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Utilization of Structure-Based Design to Identify Novel, Irreversible Inhibitors of EGFR Harboring the T790M Mutation
Hennessy, Edward J, Chuaqui, Claudio, Ashton, Susan, Colclough, Nicola, Cross, Darren A. E, Debreczeni, Judit É, Eberlein, Cath, Gingipalli, Lakshmaiah, Klinowska, Teresa C. M, Orme, Jonathan P, Sha, Li, Wu, Xiaoyun
Published in ACS medicinal chemistry letters (12.05.2016)
Published in ACS medicinal chemistry letters (12.05.2016)
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Cellular assay optimization: part I: the use of large-scale transiently transfected cryobanks and introduction of a c-Myc tag to design a standardized ELISA process
Macmillan, Marie A, Fisher, David I, Roberts, Karen, Orme, Jonathan P
Published in Journal of biomolecular screening (01.10.2011)
Published in Journal of biomolecular screening (01.10.2011)
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Discovery of 5‑{4-[(7-Ethyl-6-oxo‑5,6-dihydro‑1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}‑N‑methylpyridine-2-carboxamide (AZD5305): A PARP1–DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs
Johannes, Jeffrey W, Balazs, Amber, Barratt, Derek, Bista, Michal, Chuba, Matthew D, Cosulich, Sabina, Critchlow, Susan E, Degorce, Sébastien L, Di Fruscia, Paolo, Edmondson, Scott D, Embrey, Kevin, Fawell, Stephen, Ghosh, Avipsa, Gill, Sonja J, Gunnarsson, Anders, Hande, Sudhir M, Heightman, Tom D, Hemsley, Paul, Illuzzi, Giuditta, Lane, Jordan, Larner, Carrie, Leo, Elisabetta, Liu, Lina, Madin, Andrew, Martin, Scott, McWilliams, Lisa, O’Connor, Mark J, Orme, Jonathan P, Pachl, Fiona, Packer, Martin J, Pei, Xiaohui, Pike, Andrew, Schimpl, Marianne, She, Hongyao, Staniszewska, Anna D, Talbot, Verity, Underwood, Elizabeth, Varnes, Jeffrey G, Xue, Lin, Yao, Tieguang, Zhang, Ke, Zhang, Andrew X, Zheng, Xiaolan
Published in Journal of medicinal chemistry (14.10.2021)
Published in Journal of medicinal chemistry (14.10.2021)
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Abstract 4451: Evaluation of the therapeutic potential of phosphine oxide pyrazole inhibitors in tumors harboring EGFR C797S mutation
Floch, Nicolas, Finlay, M. Raymond V., Bianco, Ambra, Bickerton, Sue, Colclough, Nicola, Cross, Darren A., Cuomo, Emanuela M., Guerot, Carine M., Hargreaves, David, Martin, Matthew J., McKerrecher, Darren, O’Neill, Daniel J., Orme, Jonathan P., Rahi, Amar, Smith, Paul D., Ward, Richard A.
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Abstract 4813: Comparative activity profiling of tyrosine kinase inhibitors (TKIs) against exon 20 insertions and the wild-type form of epidermal growth factor receptor (EGFR)
Ward, Richard A., Bianco, Ambra, Colclough, Nicola, Cross, Darren, Cuomo, Emanuela M., Finlay, M. Raymond V., Fitzek, Martina, Floc’h, Nicolas, Gagrica, Sladjana, Hammond, Beverley, Martin, Matthew J., McKerrecher, Darren, O’Neill, Daniel J., Orme, Jonathan P., Smith, Paul D., Staniszewska, Anna D., Urosevic, Jelena, Whalley, Nicky, Yates, James W.
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Abstract LB-273: A head-to-head comparison of the properties of five clinical PARP inhibitors identifies new insights that can explain both the observed clinical efficacy and safety profiles
Leo, Elisabetta, Johannes, Jeffrey, Illuzzi, Giuditta, Zhang, Andrew, Hemsley, Paul, Bista, Michal J., Orme, Jonathan P., Talbot, Verity A., Narvaez, Ana J., Underwood, Elizabeth, Pike, Andrew, Nikkila, Jenni K., Riches, Lucy, Sweeney, Sinbad, Gustafsson, Frida, Cronin, Anna, Ricchiuto, Piero, Roaquin, Debora A., Pachl, Fiona, Miele, Eric, MacDonald, Ruth, Hawthorne, Glen, Mead, Andrew N., O'Connor, Mark J.
Published in Cancer research (Chicago, Ill.) (01.07.2018)
Published in Cancer research (Chicago, Ill.) (01.07.2018)
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Anti-tumor activity of osimertinib, an irreversible mutant-selective EGFR tyrosine kinase inhibitor, in NSCLC harboring EGFR Exon 20 Insertions
Floc’h, Nicolas, Martin, Matthew J., Riess, Jonathan W., Orme, Jonathan P., Staniszewska, Anna D., Menard, Ludovic, Cuomo, Maria Emanuela, O'Neill, Daniel J, Ward, Richard A., Finlay, M. Raymond V., McKerrecher, Darren, Cheng, Mingshan, Vang, Daniel P, Tsai, Rebekah A., Keck, James G., Gandara, David R., Mack, Philip C., Cross, Darren, AE
Published in Molecular cancer therapeutics (26.02.2018)
Published in Molecular cancer therapeutics (26.02.2018)
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Abstract 2079: Osimertinib, an irreversible mutant selective EGFR tyrosine kinase inhibitor, exerts anti tumor activity in NSCLC harbouring exon 20 insertion mutant-EGFR
Floc'h, Nicolas, Ashton, Susan, Bianco, Ambra, Colclough, Nicola, Cross, Darren AE, Cuomo, Maria Emanuela, Finlay, M. Raymond V., Martin, Matthew J, Menard, Ludovic, McKerrecher, Darren, O'Neill, Daniel J, Orme, Jonathan P, Staniszewska, Anna D, Ward, Richard A, Yates, James W T
Published in Cancer research (Chicago, Ill.) (01.07.2017)
Published in Cancer research (Chicago, Ill.) (01.07.2017)
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