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J

Jason G. Kettle

GlaxoSmithKline
H指数:31
被引数:3,394

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Discovery and Optimization of Pyrazine Carboxamide AZ3246, a Selective HPK1 Inhibitor

吡嗪羧酰胺AZ3246的发现与优化：一种选择性HPK1抑制剂

JOURNAL OF MEDICINAL CHEMISTRY
IF6.8
2025-02-102
PRE
Shields, Jason D.; Baker, David; Balazs, Amber Y. S.; Bommakanti, Gayathri; Casella, Robert; Cao, Shenggen; Cook, Steve; Escobar, Randolph A.; Fawell, Stephen; Gibbons, Francis D.; Giblin, Kathryn A.; Goldberg, Frederick W.; Gosselin, Eric; Grebe, Tyler; Hariparsad, Niresh; Hatoum-Mokdad, Holia; Howells, Rachel; Hughes, Samantha J.; Jackson, Anne; Reddy, Iswarya Karapa; Kettle, Jason G.; Lamont, Gillian M.; Lamont, Scott; Li, Min; Lill, Sten O. Nilsson; Mele, Deanna A.; Metrano, Anthony J.; Mfuh, Adelphe M.; Morrill, Lucas A.; Peng, Bo; Pflug, Alexander; Proia, Theresa A.; Rezaei, Hadi; Richards, Ryan; Richter, Magdalena; Robbins, Kevin J.; San Martin, Maryann; Schimpl, Marianne; Schuller, Alwin G.; Sha, Li; Shen, Minhui; Sheppeck, James E.; Singh, Meha; Stokes, Stephen; Song, Kun; Sun, Yuanyuan; Tang, Haoran; Wagner, David J.; Wang, Jianyan; Wang, Yanjun; Wilson, David M.; Wu, Allan; Wu, Chengyan; Wu, Dedong; Wu, Ye; Xu, Kevin; Yang, Yue; Yao, Tieguang; Ye, Minwei; Zhang, Andrew X.; Zhang, Hui; Zhai, Xiang; Zhou, Yanxiao; Ziegler, Robert E.; Grimster, Neil P.
Design of a Lead-Like Cysteine-Targeting Covalent Library and the Identification of Hits to Cys55 of Bfl-1
JOURNAL OF MEDICINAL CHEMISTRY
IF6.8
2024-06-251
PRE
Lucas, Simon C. C.; Milbradt, Alexander G.; Blackwell, J. Henry; Bonomo, Silvia; Brierley, Andrew; Cassar, Doyle J.; Freeman, Jared; Hadfield, Thomas E.; Morrill, Lucas A.; Riemens, Rick; Sarda, Sunil; Schiesser, Stefan; Wiktelius, Daniel; Ahmed, Samiyah; Bostock, Mark J.; Borjesson, Ulf; De Fusco, Claudia; Guerot, Carine; Hargreaves, David; Hewitt, Sarah; Lamb, Michelle L.; Su, Nancy; Whatling, Ryan; Wheeler, Matthew; Kettle, Jason G.
Metabolism-driven in vitro/in vivo disconnect of an oral ERα VHL-PROTAC
COMMUNICATIONS BIOLOGY
IF5.1
2024-05-135
OAAI
Hayhow, Thomas G.; Williamson, Beth; Lawson, Mandy; Cureton, Natalie; Braybrooke, Erin L.; Campbell, Andrew; Carbajo, Rodrigo J.; Cheraghchi-Bashi, Azadeh; Chiarparin, Elisabetta; Diene, Coura R.; Fallan, Charlene; Fisher, David I.; Goldberg, Frederick W.; Hopcroft, Lorna; Hopcroft, Philip; Jackson, Anne; Kettle, Jason G.; Klinowska, Teresa; Kuenzel, Ulrike; Lamont, Gillian; Lewis, Hilary J.; Maglennon, Gareth; Martin, Scott; Gutierrez, Pablo Morentin; Morrow, Christopher J.; Nikolaou, Myria; Nissink, J. Willem M.; O'Shea, Patrick; Polanski, Radoslaw; Schade, Markus; Scott, James S.; Smith, Aaron; Weber, Judith; Wilson, Joanne; Yang, Bin; Crafter, Claire
Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization
JOURNAL OF MEDICINAL CHEMISTRY
IF6.8
2023-09-223
PRE
Nilsson, Magnus; Berggren, Kristina; Berglund, Susanne; Cerboni, Silvia; Collins, Mia; Dahl, Goran; Elmqvist, David; Grimster, Neil P.; Hendrickx, Ramon; Johansson, Johan R.; Kettle, Jason G.; Lepisto, Matti; Rhedin, Magdalena; Smailagic, Amir; Su, Qibin; Wennberg, Tiiu; Wu, Allan; Osterlund, Torben; Naessens, Thomas; Mitra, Suman
Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration

AZD4747的发现，这是一种有效且选择性的突变体GTPase KRASG12C抑制剂，具有明显的中枢神经系统穿透性

JOURNAL OF MEDICINAL CHEMISTRY
IF6.8
2023-07-0311
PRE
Kettle, Jason G.; Bagal, Sharan K.; Barratt, Derek; Bodnarchuk, Michael S.; Boyd, Scott; Braybrooke, Erin; Breed, Jason; Cassar, Doyle J.; Cosulich, Sabina; Davies, Michael; Davies, Nichola L.; Deng, Chao; Eatherton, Andrew; Evans, Laura; Feron, Lyman J.; Fillery, Shaun; Gleave, Emma S.; Goldberg, Frederick W.; Gonzalez, Miguel A. Cortes; Guerot, Carine; Haider, Afreen; Harlfinger, Stephanie; Howells, Rachel; Jackson, Anne; Johnstrom, Peter; Kemmitt, Paul D.; Koers, Alex; Kondrashov, Mikhail; Lamont, Gillian M.; Lamont, Scott; Lewis, Hilary J.; Liu, Libin; Mylrea, Megan; Nash, Samuel; Niedbala, Michael J.; Peter, Alison; Phillips, Christopher; Pike, Kurt; Raubo, Piotr; Robb, Graeme R.; Ross, Sarah; Sanders, Matthew G.; Schou, Magnus; Simpson, Iain; Steward, Oliver
Discovery of Clinical Candidate AZD0095, a Selective Inhibitor of Monocarboxylate Transporter 4 (MCT4) for Oncology

发现临床候选药物AZD0095，一种用于肿瘤学的单羧酸转运蛋白4 (MCT4) 的选择性抑制剂

JOURNAL OF MEDICINAL CHEMISTRY
IF6.8
2022-12-1623
PRE
Goldberg, Frederick W.; Kettle, Jason G.; Lamont, Gillian M.; Buttar, David; Ting, Attilla K. T.; McGuire, Thomas M.; Cook, Calum R.; Beattie, David; Gutierrez, Pablo Morentin; Kavanagh, Stefan L.; Komen, Jasper C.; Kawatkar, Aarti; Clark, Roger; Hopcroft, Lorna; Hughes, Gareth; Critchlow, Susan E.
AZD4625 is a Potent and Selective Inhibitor of KRASG12C
MOLECULAR CANCER THERAPEUTICS
IF5.5
2022-08-052
OAAI
Chakraborty, Atanu; Hanson, Lyndsey; Robinson, David; Lewis, Hilary; Bickerton, Sue; Davies, Michael; Polanski, Radoslaw; Whiteley, Rebecca; Koers, Alex; Atkinson, James; Baker, Tamara; Barrantes, Ivan del Barco; Ciotta, Giovanni; Kettle, Jason G.; Magiera, Lukasz; Martins, Carla P.; Peter, Alison; Wigmore, Eleanor; Underwood, Zoe; Cosulich, Sabina; Niedbala, Michael; Ross, Sarah
Discovery of AZD4625, a Covalent Allosteric Inhibitor of the MutantGTPase KRASG12C

突变gtpase KRASG12C的共价变构抑制剂AZD4625的发现

JOURNAL OF MEDICINAL CHEMISTRY
IF6.8
2022-04-2637
PRE
Kettle, Jason G.; Bagal, Sharan K.; Bickerton, Sue; Bodnarchuk, Michael S.; Boyd, Scott; Breed, Jason; Carbajo, Rodrigo J.; Cassar, Doyle J.; Chakraborty, Atanu; Cosulich, Sabina; Cumming, Iain; Davies, Michael; Davies, Nichola L.; Eatherton, Andrew; Evans, Laura; Feron, Lyman; Fillery, Shaun; Gleave, Emma S.; Goldberg, Frederick W.; Hanson, Lyndsey; Harlfinger, Stephanie; Howard, Martin; Howells, Rachel; Jackson, Anne; Kemmitt, Paul; Lamont, Gillian; Lamont, Scott; Lewis, Hilary J.; Liu, Libin; Niedbala, Michael J.; Phillips, Christopher; Polanski, Radek; Raubo, Piotr; Robb, Graeme; Robinson, David M.; Ross, Sarah; Sanders, Matthew G.; Tonge, Michael; Whiteley, Rebecca; Wilkinson, Stephen; Yang, Junsheng; Zhang, Wenman
Alkynyl Benzoxazines and Dihydroquinazolines as Cysteine Targeting Covalent Warheads and Their Application in Identification of Selective Irreversible Kinase Inhibitors
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
IF15.6
2020-05-1552
OAAI
McAulay, Kirsten; Hoyt, Emily A.; Thomas, Morgan; Schimpl, Marianne; Bodnarchuk, Michael S.; Lewis, Hilary J.; Barratt, Derek; Bhavsar, Deepa; Robinson, David M.; Deery, Michael J.; Ogg, Derek J.; Bernardes, Goncalo J. L.; Ward, Richard A.; Waring, Michael J.; Kettle, Jason G.
Discovery and pharmacological characterization of AZD3229, a potent KIT/PDGFRα inhibitor for treatment of gastrointestinal stromal tumors
SCIENCE TRANSLATIONAL MEDICINE
IF14.6
2020-04-2923
OAAI
Banks, Erica; Grondine, Michael; Bhavsar, Deepa; Barry, Evan; Kettle, Jason G.; Reddy, Venkatesh Pilla; Brown, Crystal; Wang, Haiyun; Mettetal, Jerome T.; Collins, Teresa; Adeyemi, Oladipupo; Overman, Ross; Lawson, Deborah; Harmer, Alexander R.; Reimer, Corinne; Drew, Lisa; Packer, Martin J.; Cosulich, Sabina; Jones, Rhys D. O.; Shao, Wenlin; Wilson, David; Guichard, Sylvie; Fawell, Stephen; Anjum, Rana
Discovery of (2R)-N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor

发现 (2R)-N-[3-[2-[(3-甲氧基-1-甲基-吡唑-4-基) 氨基] pyrimidin-4-yl]-1h-吲哚-7-基]-2-(4-甲基哌嗪-1-基) 丙烯酰胺 (AZD4205) 作为有效和选择性的Janus激酶1抑制剂

JOURNAL OF MEDICINAL CHEMISTRY
IF6.8
2020-04-1639
PREAI
Su, Qibin; Banks, Erica; Bebernitz, Geraldine; Bell, Kirsten; Borenstein, Cassandra F.; Chen, Huawei; Chuaqui, Claudio E.; Deng, Nanhua; Ferguson, Andrew D.; Kawatkar, Sameer; Grimster, Neil P.; Ruston, Linette; Lyne, Paul D.; Read, Jon A.; Peng, Xianyou; Pei, Xiaohui; Fawell, Stephen; Tang, Zhanlei; Throner, Scott; Vasbinder, Melissa M.; Wang, Haoyu; Winter-Holt, Jon; Woessner, Richard; Wu, Allan; Yang, Wenzhan; Zinda, Michael; Kettle, Jason G.
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRASG12C
JOURNAL OF MEDICINAL CHEMISTRY
IF6.8
2020-02-0560
PREAI
Kettle, Jason G.; Bagal, Sharan K.; Bickerton, Sue; Bodnarchuk, Michael S.; Breed, Jason; Carbajo, Rodrigo J.; Cassar, Doyle J.; Chakraborty, Atanu; Cosulich, Sabina; Cumming, Iain; Davies, Michael; Eatherton, Andrew; Evans, Laura; Feron, Lyman; Fillery, Shaun; Gleave, Emma S.; Goldberg, Frederick W.; Harlfinger, Stephanie; Hanson, Lyndsey; Howard, Martin; Howells, Rachel; Jackson, Anne; Kemmitt, Paul; Kingston, Jennifer K.; Lamont, Scott; Lewis, Hilary J.; Li, Songlei; Liu, Libin; Ogg, Derek; Phillips, Christopher; Polanski, Radek; Robb, Graeme; Robinson, David; Ross, Sarah; Smith, James M.; Tonge, Michael; Whiteley, Rebecca; Yang, Junsheng; Zhang, Longfei; Zhao, Xiliang

研究方向

暂未获取到该数据
F
Frederick W. Goldberg
H 指数:20论文数:71被引数:1,711
H
Hilary Lewis
H 指数:14论文数:63被引数:1,227
N
Neil P. Grimster
H 指数:21论文数:60被引数:3,930
S
Sabina Cosulich
H 指数:36论文数:293被引数:5,846
G
Gillian M. Lamont
H 指数:16论文数:58被引数:1,626
D
Doyle J. Cassar
H 指数:8论文数:25被引数:304
R
Richard A. Ward
H 指数:51论文数:308被引数:1.0万
S
Shaun Fillery
H 指数:18论文数:33被引数:1,188
Q
Qibin Su
H 指数:17论文数:38被引数:1,018
R
Richard Woessner
H 指数:28论文数:147被引数:3,436