|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
|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
|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
|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
|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
|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
|Binding kinetics of ligands acting at GPCRs|
DA Sykes, LA Stoddart, LE Kilpatrick, SJ Hill
Molecular and cellular endocrinology 485, 9-19, 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
|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
|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
|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
|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
|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
|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
|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
|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
|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
|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
|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
|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