Jonathan P. Orme

biopharmaceutical r&d

H指数:10

被引数:785

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AZ14289671 is a highly selective and blood-brain barrier penetrant irreversible TKI that targets EGFRExon20 insertions

AZ14289671 是一种高选择性的血脑屏障穿透性不可逆TKI，可靶向EGFRExon20插入突变。

Cell Reports Medicine

IF10.6

2025-08-250

OAAI

Discovery of 6-Fluoro-5-{4-[(5-fluoro-2-methyl-3-oxo-3,4-dihydroquinoxalin-6-yl)methyl]piperazin-1-yl}-N-methylpyridine-2-carboxamide (AZD9574): A CNS-Penetrant, PARP1-Selective Inhibitor

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2024-12-100

PRE

Johannes, Jeffrey W.; Balazs, Amber Y. S.; Barratt, Derek; Bista, Michal; Chuba, Matthew D.; Cosulich, Sabina; Critchlow, Susan E.; Degorce, SebastienL.; Di Fruscia, Paolo; Edmondson, Scott D.; Embrey, Kevin J.; Fawell, Stephen; Ghosh, Avipsa; Gill, Sonja J.; Gunnarsson, Anders; Hande, Sudhir M.; Heightman, Tom D.; Hemsley, Paul; Illuzzi, Giuditta; Lane, Jordan; Larner, Carrie J. B.; Leo, Elisabetta; Liu, Lina; Madin, Andrew; Mcwilliams, Lisa; O'Connor, Mark J.; Orme, Jonathan P.; Pachl, Fiona; Packer, Martin J.; Pei, Xiaohui; Pike, Andy; 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

Optimization of Potent, Efficacious, Selective and Blood-Brain Barrier Penetrating Inhibitors Targeting EGFR Exon20 Insertion Mutations

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2024-09-280

PRE

Thomson, Clare; Braybrooke, Erin; Colclough, Nicola; Davies, Nichola L.; Floc'h, Nicolas; Greenwood, Ryan; Guerot, Carine; Hargreaves, David; Johnstrom, Peter; Khurana, Puneet; Kostomiris, Demetrios H.; Li, Songlei; Lister, Andrew; Lorthioir, Olivier; Martin, Scott; Mccoull, William; Mclean, Neville J.; Mcwilliams, Lisa; Orme, Jonathan P.; Packer, Martin J.; Pearson, Stuart; Swaih, Aisha M.; Tentarelli, Sharon; Tucker, Michael J.; Ward, Richard A.; Wilkinson, Stephen; Winlow, Poppy; Wood, Isabel L.

Discovery and Optimization of Potent, Efficacious and Selective Inhibitors Targeting EGFR Exon20 Insertion Mutations

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2024-05-212

PRE

CLANet: A comprehensive framework for cross-batch cell line identification using brightfield images

MEDICAL IMAGE ANALYSIS

IF11.8

2024-05-010

Vinylpyridine as a Tunable Covalent Warhead Targeting C797 in EGFR

ACS MEDICINAL CHEMISTRY LETTERS

IF4

2024-04-050

PRE

An automated cell line authentication method for AstraZeneca global cell bank using deep neural networks on brightfield images

SCIENTIFIC REPORTS

IF3.9

2022-05-123

OAAI

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

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2021-09-2781

PREAI

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

Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance

JOURNAL OF MEDICINAL CHEMISTRY

IF6.8

2021-09-0721

PRE

Finlay, M. Raymond, V; Barton, Peter; Bickerton, Sue; Bista, Michal; Colclough, Nicola; Cross, Darren A. E.; Evans, Laura; Floc'h, Nicolas; Gregson, Clare; Guerot, 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

Osimertinib, an Irreversible Next-Generation EGFR Tyrosine Kinase Inhibitor, Exerts Antitumor Activity in Various Preclinical NSCLC Models Harboring the Uncommon EGFR Mutations G719X or L861Q or S768I

MOLECULAR CANCER THERAPEUTICS

IF5.5

2020-11-0337

OAAI

Evaluation of the therapeutic potential of phosphine oxide pyrazole inhibitors in tumors harboring EGFR C797S mutation

CANCER RESEARCH

IF16.6

2019-07-019

PRE

Comparative activity profiling of tyrosine kinase inhibitors (TKIs) against exon 20 insertions and the wild-type form of epidermal growth factor receptor (EGFR)

CANCER RESEARCH

IF16.6

2019-07-011

PRE

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

CANCER RESEARCH

IF16.6

2018-07-0120

PRE

The brain-penetrant clinical ATM inhibitor AZD1390 radiosensitizes and improves survival of preclinical brain tumor models

SCIENCE ADVANCES

IF12.5

2018-06-01221

OAAI

Durant, Stephen T.; Zheng, Li; Wang, Yingchun; Chen, Kan; Zhang, Lingli; Zhang, Tianwei; Yang, Zhenfan; Riches, Lucy; Trinidad, Antonio G.; Fok, Jacqueline H. L.; Hunt, Tom; Pike, Kurt G.; Wilson, Joanne; Smith, Aaron; Colclough, Nicola; Reddy, Venkatesh Pilla; Sykes, Andrew; Janefeldt, Annika; Johnstrom, Peter; Varnas, Katarina; Takano, Akihiro; Ling, Stephanie; Orme, Jonathan; Stott, Jonathan; Roberts, Caroline; Barrett, Ian; Jones, Gemma; Roudier, Martine; Pierce, Andrew; Allen, Jasmine; Kahn, Jenna; Sule, Amrita; Karlin, Jeremy; Cronin, Anna; Chapman, Melissa; Valerie, Kristoffer; Illingworth, Ruth; Pass, Martin

Antitumor Activity of Osimertinib, an Irreversible Mutant-Selective EGFR Tyrosine Kinase Inhibitor, in NSCLC Harboring EGFR Exon 20 Insertions

MOLECULAR CANCER THERAPEUTICS

IF5.5

2018-04-3084

OAAI

Osimertinib, an irreversible mutant selective EGFR tyrosine kinase inhibitor, exerts anti tumor activity in NSCLC harbouring exon 20 insertion mutant-EGFR

CANCER RESEARCH

IF16.6

2017-07-010

PRE

Osimertinib (AZD9291), an irreversible 3rd generation TKI, induces tumor growth inhibition in NSCLC pre-clinical models harboring the most prevalent EGFR Ex20Ins (in vitro and in vivo)

EUROPEAN JOURNAL OF CANCER