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 | 265 | 2013 |
Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective A Pike, B Williamson, S Harlfinger, S Martin, DF McGinnity Drug Discovery Today 25 (10), 1793-1800, 2020 | 124 | 2020 |
Metabolic disposition of osimertinib in rats, dogs, and humans: insights into a drug designed to bind covalently to a cysteine residue of epidermal growth factor receptor PA Dickinson, MV Cantarini, J Collier, P Frewer, S Martin, K Pickup, ... Drug Metabolism and Disposition 44 (8), 1201-1212, 2016 | 106 | 2016 |
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 … JW Johannes, A Balazs, D Barratt, M Bista, MD Chuba, S Cosulich, ... Journal of Medicinal Chemistry 64 (19), 14498-14512, 2021 | 56 | 2021 |
Investigation of (E)-3-[4-(2-Oxo-3-aryl-chromen-4-yl)oxyphenyl]acrylic Acids as Oral Selective Estrogen Receptor Down-Regulators SL Degorce, A Bailey, R Callis, C De Savi, R Ducray, G Lamont, ... Journal of Medicinal Chemistry 58 (8), 3522-3533, 2015 | 52 | 2015 |
Identification of the thiophene ring of methapyrilene as a novel bioactivation-dependent hepatic toxicophore EE Graham, RJ Walsh, CM Hirst, JL Maggs, S Martin, MJ Wild, ID Wilson, ... Journal of Pharmacology and Experimental Therapeutics 326 (2), 657-671, 2008 | 45 | 2008 |
(1R,2R)-N-(1-Cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydropyrido[4,3-b]indole-2-carbonyl)cyclohexanecarboxamide (AZD4996): A Potent and Highly … AG Dossetter, H Beeley, J Bowyer, CR Cook, JJ Crawford, JE Finlayson, ... Journal of medicinal chemistry 55 (14), 6363-6374, 2012 | 37 | 2012 |
Pharmacokinetic benefits of 3, 4-dimethoxy substitution of a phenyl ring and design of isosteres yielding orally available cathepsin K inhibitors JJ Crawford, PW Kenny, J Bowyer, CR Cook, JE Finlayson, C Heyes, ... Journal of Medicinal Chemistry 55 (20), 8827-8837, 2012 | 25 | 2012 |
Reactive metabolite trapping screens and potential pitfalls: bioactivation of a homomorpholine and formation of an unstable thiazolidine adduct EM Lenz, S Martin, R Schmidt, PE Morin, R Smith, DJ Weston, ... Chemical Research in Toxicology 27 (6), 968-980, 2014 | 23 | 2014 |
In vitro exploration of potential mechanisms of toxicity of the human hepatotoxic drug fenclozic acid AVM Rodrigues, HE Rollison, S Martin, S Sarda, T Schulz-Utermoehl, ... Archives of toxicology 87, 1569-1579, 2013 | 22 | 2013 |
High‐throughput metabolic stability studies in drug discovery by orthogonal acceleration time‐of‐flight (OATOF) with analogue‐to‐digital signal capture (ADC) DG Temesi, S Martin, R Smith, C Jones, B Middleton Rapid Communications in Mass Spectrometry 24 (12), 1730-1736, 2010 | 14 | 2010 |
Drug metabolite identification using ultrahigh‐performance liquid chromatography–ultraviolet spectroscopy and parallelized scans on a tribrid Orbitrap mass spectrometer SD Wilkinson, S Martin, AL Orton, R Markandu, BC Jones Rapid Communications in Mass Spectrometry 34 (10), e8735, 2020 | 13 | 2020 |
The metabolism of [14C]-zibotentan (ZD4054) in rat, dog and human, the loss of the radiolabel and the identification of an anomalous peak, derived from the animal feed EM Lenz, A Kenyon, S Martin, D Temesi, J Clarkson-Jones, H Tomkinson Journal of pharmaceutical and biomedical analysis 55 (3), 500-517, 2011 | 12 | 2011 |
Identification of the reactive metabolites of fenclozic acid in bile duct cannulated rats S Martin, EM Lenz, W Keene, MR Clench Analytical chemistry 86 (22), 11281-11289, 2014 | 9 | 2014 |
The metabolic fate of [14C]-fenclozic acid in the hepatic reductase null (HRN) mouse K Pickup, J Wills, A Rodrigues, HB Jones, C Page, S Martin, S Sarda, ... Xenobiotica 44 (2), 164-173, 2014 | 9 | 2014 |
The disconnect in intrinsic clearance determined in human hepatocytes and liver microsomes results from divergent cytochrome P450 activities TE Bapiro, S Martin, SD Wilkinson, AL Orton, N Hariparsad, S Harlfinger, ... Drug Metabolism and Disposition 51 (7), 892-901, 2023 | 4 | 2023 |
Methanol adducts leading to the identification of a reactive aldehyde metabolite of CPAQOP in human liver microsomes by ultra‐high‐performance liquid chromatography/mass … S Martin, EM Lenz, R Smith, DG Temesi, AL Orton, MR Clench Rapid Communications in Mass Spectrometry 31 (1), 145-151, 2017 | 3 | 2017 |
Reaction of homopiperazine with endogenous formaldehyde: a carbon hydrogen addition metabolite/product identified in rat urine and blood S Martin, EM Lenz, D Temesi, M Wild, MR Clench Drug Metabolism and Disposition 40 (8), 1478-1486, 2012 | 3 | 2012 |
Acute liver effects, disposition and metabolic fate of [14C]-fenclozic acid following oral administration to normal and bile-cannulated male C57BL/6J mice K Pickup, S Martin, EA Partridge, HB Jones, J Wills, T Schulz-Utermoehl, ... Archives of Toxicology 91, 2643-2653, 2017 | 1 | 2017 |
The role of intramolecular reactions and chemical degradation in the apparent biotransformation pathways of a series of SYK inhibitors B Calle, B Barlaam, C Diene, E Lenz, S Martin, U Sarkar, S Wilkinson, ... Drug Metabolism and Disposition, 2024 | | 2024 |