An analysis of the attrition of drug candidates from four major pharmaceutical companies MJ Waring, J Arrowsmith, AR Leach, PD Leeson, S Mandrell, RM Owen, ... Nature reviews Drug discovery 14 (7), 475-486, 2015 | 1379 | 2015 |
Lipophilicity in drug discovery MJ Waring Expert Opinion on Drug Discovery 5 (3), 235-248, 2010 | 838 | 2010 |
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 | 558 | 2014 |
Crystallographic and electrophilic fragment screening of the SARS-CoV-2 main protease A Douangamath, D Fearon, P Gehrtz, T Krojer, P Lukacik, CD Owen, ... Nature communications 11 (1), 5047, 2020 | 448 | 2020 |
Defining optimum lipophilicity and molecular weight ranges for drug candidates—molecular weight dependent lower log D limits based on permeability MJ Waring Bioorganic & medicinal chemistry letters 19 (10), 2844-2851, 2009 | 362 | 2009 |
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 | 269 | 2013 |
Directed dihydroxylation of cyclic allylic alcohols and trichloroacetamides using OsO4/TMEDA TJ Donohoe, K Blades, PR Moore, MJ Waring, JJG Winter, M Helliwell, ... The Journal of organic chemistry 67 (23), 7946-7956, 2002 | 188 | 2002 |
A quantitative assessment of hERG liability as a function of lipophilicity MJ Waring, C Johnstone Bioorganic & medicinal chemistry letters 17 (6), 1759-1764, 2007 | 175 | 2007 |
AZD5153: a novel bivalent BET bromodomain inhibitor highly active against hematologic malignancies GW Rhyasen, MM Hattersley, Y Yao, A Dulak, W Wang, P Petteruti, ... Molecular cancer therapeutics 15 (11), 2563-2574, 2016 | 144 | 2016 |
Potent and selective bivalent inhibitors of BET bromodomains MJ Waring, H Chen, AA Rabow, G Walker, R Bobby, S Boiko, ... Nature chemical biology 12 (12), 1097-1104, 2016 | 140 | 2016 |
Conversion of α, β-unsaturated ketones into α-hydroxy ketones using an MnIII catalyst, phenylsilane and dioxygen: acceleration of conjugate hydride reduction by dioxygen P Magnus, AH Payne, MJ Waring, DA Scott, V Lynch Tetrahedron Letters 41 (50), 9725-9730, 2000 | 136 | 2000 |
The directed dihydroxylation of allylic alcohols TJ Donohoe, PR Moore, MJ Waring, NJ Newcombe Tetrahedron letters 38 (28), 5027-5030, 1997 | 135 | 1997 |
Development of a novel B-cell lymphoma 6 (BCL6) PROTAC to provide insight into small molecule targeting of BCL6 W McCoull, T Cheung, E Anderson, P Barton, J Burgess, K Byth, Q Cao, ... ACS Chemical Biology 13 (11), 3131-3141, 2018 | 134 | 2018 |
FragLites—minimal, halogenated fragments displaying pharmacophore doublets. An efficient approach to druggability assessment and hit generation DJ Wood, JD Lopez-Fernandez, LE Knight, I Al-Khawaldeh, C Gai, S Lin, ... Journal of Medicinal Chemistry 62 (7), 3741-3752, 2019 | 83 | 2019 |
Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3 R)-4-[2-[4-[1-(3-Methoxy-[1, 2, 4] triazolo [4, 3-b … RH Bradbury, R Callis, GR Carr, H Chen, E Clark, L Feron, S Glossop, ... Journal of medicinal chemistry 59 (17), 7801-7817, 2016 | 80 | 2016 |
Conjugate reduction of α, β-unsaturated ketones using an MnIII catalyst, phenylsilane and isopropyl alcohol P Magnus, MJ Waring, DA Scott Tetrahedron Letters 41 (50), 9731-9733, 2000 | 79 | 2000 |
Sequential Double α-Arylation of N-Allylureas by Asymmetric Deprotonation and N→C Aryl Migration DJ Tetlow, U Hennecke, J Raftery, MJ Waring, DS Clarke, J Clayden Organic Letters 12 (23), 5442-5445, 2010 | 70 | 2010 |
Stereoselective synthesis of the bicyclo [5.3. 0] decane portion of the diterpene antibiotic guanacastepene using a pyrylium-ylide [5+ 2] cycloaddition reaction P Magnus, MJ Waring, C Ollivier, V Lynch Tetrahedron Letters 42 (30), 4947-4950, 2001 | 70 | 2001 |
Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors W McCoull, RD Abrams, E Anderson, K Blades, P Barton, M Box, ... Journal of Medicinal Chemistry 60 (10), 4386-4402, 2017 | 69 | 2017 |
Strategies to improve in vivo toxicology outcomes for basic candidate drug molecules T Luker, L Alcaraz, KK Chohan, N Blomberg, DS Brown, RJ Butlin, ... Bioorganic & medicinal chemistry letters 21 (19), 5673-5679, 2011 | 67 | 2011 |