| AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer DAE Cross, SE Ashton, S Ghiorghiu, C Eberlein, CA Nebhan, PJ Spitzler, ... Cancer discovery 4 (9), 1046-1061, 2014 | 2221 | 2014 |
| Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor MRV Finlay, M Anderton, S Ashton, P Ballard, PA Bethel, MR Box, ... Journal of medicinal chemistry 57 (20), 8249-8267, 2014 | 583 | 2014 |
| Structure-based design of targeted covalent inhibitors R Lonsdale, RA Ward Chemical Society Reviews 47 (11), 3816-3830, 2018 | 322 | 2018 |
| Characterization of VPS34-IN1, a selective inhibitor of Vps34, reveals that the phosphatidylinositol 3-phosphate-binding SGK3 protein kinase is a downstream target of class III … R Bago, N Malik, MJ Munson, AR Prescott, P Davies, E Sommer, N Shpiro, ... Biochemical Journal 463 (3), 413-427, 2014 | 313 | 2014 |
| Challenges and opportunities in cancer drug resistance RA Ward, S Fawell, N Floc’h, V Flemington, D McKerrecher, PD Smith Chemical Reviews 121 (6), 3297-3351, 2020 | 312 | 2020 |
| Structure-and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR) RA Ward, MJ Anderton, S Ashton, PA Bethel, M Box, S Butterworth, ... Journal of medicinal chemistry 56 (17), 7025-7048, 2013 | 283 | 2013 |
| Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation RA Ward, C Brassington, AL Breeze, A Caputo, S Critchlow, G Davies, ... Journal of medicinal chemistry 55 (7), 3285-3306, 2012 | 187 | 2012 |
| Expanding the armory: predicting and tuning covalent warhead reactivity R Lonsdale, J Burgess, N Colclough, NL Davies, EM Lenz, AL Orton, ... Journal of Chemical Information and Modeling 57 (12), 3124-3137, 2017 | 159 | 2017 |
| Preclinical comparison of the blood–brain barrier permeability of osimertinib with other EGFR TKIs N Colclough, K Chen, P Johnström, N Strittmatter, Y Yan, GL Wrigley, ... Clinical Cancer Research 27 (1), 189-201, 2021 | 152 | 2021 |
| AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer. Cancer Discov. 2014; 4: 1046–1061. doi: 10.1158/2159-8290 DA Cross, SE Ashton, S Ghiorghiu, C Eberlein, CA Nebhan, PJ Spitzler, ... CD-14-0337.[Europe PMC free article][Abstract][CrossRef][Google Scholar], 0 | 135 | |
| Comparison of the EGFR resistance mutation profiles generated by EGFR-targeted tyrosine kinase inhibitors and the impact of drug combinations E Avizienyte, RA Ward, AP Garner Biochemical Journal 415 (2), 197-206, 2008 | 116 | 2008 |
| Antitumor activity of osimertinib, an irreversible mutant-selective EGFR tyrosine kinase inhibitor, in NSCLC harboring EGFR exon 20 insertions N Floc'h, MJ Martin, JW Riess, JP Orme, AD Staniszewska, L Ménard, ... Molecular cancer therapeutics 17 (5), 885-896, 2018 | 106 | 2018 |
| Structure-guided design of highly selective and potent covalent inhibitors of ERK1/2 RA Ward, N Colclough, M Challinor, JE Debreczeni, K Eckersley, ... Journal of medicinal chemistry 58 (11), 4790-4801, 2015 | 104 | 2015 |
| Identification and characterization of dual inhibitors of the USP25/28 deubiquitinating enzyme subfamily JD Wrigley, G Gavory, I Simpson, M Preston, H Plant, J Bradley, ... ACS chemical biology 12 (12), 3113-3125, 2017 | 83 | 2017 |
| Insight into the therapeutic selectivity of the irreversible EGFR tyrosine kinase inhibitor osimertinib through enzyme kinetic studies X Zhai, RA Ward, P Doig, A Argyrou Biochemistry 59 (14), 1428-1441, 2020 | 62 | 2020 |
| Alkynyl benzoxazines and dihydroquinazolines as cysteine targeting covalent warheads and their application in identification of selective irreversible kinase inhibitors K McAulay, EA Hoyt, M Thomas, M Schimpl, MS Bodnarchuk, HJ Lewis, ... Journal of the American Chemical Society 142 (23), 10358-10372, 2020 | 60 | 2020 |
| Discovery of a potent and selective oral inhibitor of ERK1/2 (AZD0364) that is efficacious in both monotherapy and combination therapy in models of nonsmall cell lung cancer … RA Ward, MJ Anderton, P Bethel, J Breed, C Cook, EJ Davies, A Dobson, ... Journal of medicinal chemistry 62 (24), 11004-11018, 2019 | 59 | 2019 |
| Structure-guided discovery of potent and selective inhibitors of ERK1/2 from a modestly active and promiscuous chemical start point RA Ward, P Bethel, C Cook, E Davies, JE Debreczeni, G Fairley, L Feron, ... Journal of medicinal chemistry 60 (8), 3438-3450, 2017 | 57 | 2017 |
| The structure-guided discovery of osimertinib: the first US FDA approved mutant selective inhibitor of EGFR T790M S Butterworth, DAE Cross, MRV Finlay, RA Ward, MJ Waring Medchemcomm 8 (5), 820-822, 2017 | 48 | 2017 |
| Systematic enumeration of heteroaromatic ring systems as reagents for use in medicinal chemistry RA Ward, JG Kettle Journal of medicinal chemistry 54 (13), 4670-4677, 2011 | 48 | 2011 |
