The role of kinetic context in apparent biased agonism at GPCRs C Klein Herenbrink, DA Sykes, P Donthamsetti, M Canals, T Coudrat, ... Nature communications 7 (1), 10842, 2016 | 284 | 2016 |
Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors DA Sykes, H Moore, L Stott, N Holliday, JA Javitch, JR Lane, SJ Charlton Nature communications 8 (1), 763, 2017 | 155 | 2017 |
The influence of receptor kinetics on the onset and duration of action and the therapeutic index of NVA237 and tiotropium DA Sykes, MR Dowling, J Leighton-Davies, TC Kent, L Fawcett, E Renard, ... Journal of Pharmacology and Experimental Therapeutics 343 (2), 520-528, 2012 | 134 | 2012 |
Exploring the mechanism of agonist efficacy: a relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor DA Sykes, MR Dowling, SJ Charlton Molecular pharmacology 76 (3), 543-551, 2009 | 126 | 2009 |
The Identification of Indacaterol as an Ultralong-Acting Inhaled β2-Adrenoceptor Agonist F Baur, D Beattie, D Beer, D Bentley, M Bradley, I Bruce, SJ Charlton, ... Journal of medicinal chemistry 53 (9), 3675-3684, 2010 | 105 | 2010 |
Observed drug-receptor association rates are governed by membrane affinity: the importance of establishing “micro-pharmacokinetic/pharmacodynamic relationships” at the β2 … DA Sykes, C Parry, J Reilly, P Wright, RA Fairhurst, SJ Charlton Molecular pharmacology 85 (4), 608-617, 2014 | 91 | 2014 |
Binding kinetics of ligands acting at GPCRs DA Sykes, LA Stoddart, LE Kilpatrick, SJ Hill Molecular and cellular endocrinology 485, 9-19, 2019 | 82 | 2019 |
Slow receptor dissociation is not a key factor in the duration of action of inhaled long‐acting β2‐adrenoceptor agonists DA Sykes, SJ Charlton British journal of pharmacology 165 (8), 2672-2683, 2012 | 77 | 2012 |
Fevipiprant (QAW039), a slowly dissociating CRTh2 antagonist with the potential for improved clinical efficacy DA Sykes, ME Bradley, DM Riddy, E Willard, J Reilly, A Miah, C Bauer, ... Molecular pharmacology 89 (5), 593-605, 2016 | 63 | 2016 |
Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists IM McDonald, C Austin, IM Buck, DJ Dunstone, J Gaffen, E Griffin, ... Journal of medicinal chemistry 50 (20), 4789-4792, 2007 | 63 | 2007 |
Investigating the molecular mechanisms through which FTY720‐P causes persistent S1P1 receptor internalization DA Sykes, DM Riddy, C Stamp, ME Bradley, N McGuiness, A Sattikar, ... British journal of pharmacology 171 (21), 4797-4807, 2014 | 50 | 2014 |
Optimization of 1, 3, 4-benzotriazepine-based CCK2 antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion IM McDonald, JW Black, IM Buck, DJ Dunstone, EP Griffin, EA Harper, ... Journal of medicinal chemistry 50 (13), 3101-3112, 2007 | 43 | 2007 |
Biased M1-muscarinic-receptor-mutant mice inform the design of next-generation drugs SJ Bradley, C Molloy, P Valuskova, L Dwomoh, M Scarpa, M Rossi, ... Nature chemical biology 16 (3), 240-249, 2020 | 35 | 2020 |
Uncoupling the structure–activity relationships of β2 adrenergic receptor ligands from membrane binding CJ Dickson, V Hornak, C Velez-Vega, DJJ McKay, J Reilly, DA Sandham, ... Journal of medicinal chemistry 59 (12), 5780-5789, 2016 | 29 | 2016 |
Discovery of Fevipiprant (NVP-QAW039), a Potent and Selective DP2 Receptor Antagonist for Treatment of Asthma DA Sandham, L Barker, L Brown, Z Brown, D Budd, SJ Charlton, ... ACS Medicinal Chemistry Letters 8 (5), 582-586, 2017 | 28 | 2017 |
An investigation into the structure–activity relationships associated with the systematic modification of the β2-adrenoceptor agonist indacaterol D Beattie, D Beer, ME Bradley, I Bruce, SJ Charlton, BM Cuenoud, ... Bioorganic & medicinal chemistry letters 22 (19), 6280-6285, 2012 | 28 | 2012 |
Optimization of the in vitro and in vivo properties of a novel series of 2, 4, 5-trisubstituted imidazoles as potent cholecystokinin-2 (CCK2) antagonists IM Buck, JW Black, T Cooke, DJ Dunstone, JD Gaffen, EP Griffin, ... Journal of medicinal chemistry 48 (22), 6803-6812, 2005 | 26 | 2005 |
Development of high-specificity fluorescent probes to enable cannabinoid type 2 receptor studies in living cells RC Sarott, MV Westphal, P Pfaff, C Korn, DA Sykes, T Gazzi, B Brennecke, ... Journal of the American Chemical Society 142 (40), 16953-16964, 2020 | 22 | 2020 |
Ligand specific efficiency (LSE) index for PET tracer optimization YP Auberson, E Briard, D Sykes, J Reilly, M Healy ChemMedChem 11 (13), 1415-1427, 2016 | 22 | 2016 |
Measuring receptor target coverage: a radioligand competition binding protocol for assessing the association and dissociation rates of unlabeled compounds DA Sykes, MR Dowling, SJ Charlton Current protocols in pharmacology 50 (1), 9.14. 1-9.14. 30, 2010 | 19 | 2010 |