| Structural basis for allosteric regulation of GPCRs by sodium ions W Liu, E Chun, AA Thompson, P Chubukov, F Xu, V Katritch, GW Han, ... Science 337 (6091), 232-236, 2012 | 1002 | 2012 |
| Cannabinoid CB2 receptor ligand profiling reveals biased signalling and off-target activity M Soethoudt, U Grether, J Fingerle, TW Grim, F Fezza, L De Petrocellis, ... Nature communications 8 (1), 13958, 2017 | 308 | 2017 |
| Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists Y Zheng, L Qin, NVO Zacarías, H de Vries, GW Han, M Gustavsson, ... Nature 540 (7633), 458-461, 2016 | 270 | 2016 |
| Functional efficacy of adenosine A2A receptor agonists is positively correlated to their receptor residence time D Guo, T Mulder‐Krieger, AP IJzerman, LH Heitman British journal of pharmacology 166 (6), 1846-1859, 2012 | 194 | 2012 |
| Kinetics for Drug Discovery: an industry-driven effort to target drug residence time DA Schuetz, WEA de Witte, YC Wong, B Knasmueller, L Richter, DB Kokh, ... Drug Discovery Today 22 (6), 896-911, 2017 | 187 | 2017 |
| Drug‐target residence time—a case for G protein‐coupled receptors D Guo, JM Hillger, AP IJzerman, LH Heitman Medicinal research reviews 34 (4), 856-892, 2014 | 184 | 2014 |
| Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength E Segala, D Guo, RKY Cheng, A Bortolato, F Deflorian, AS Doré, JC Errey, ... Journal of medicinal chemistry 59 (13), 6470-6479, 2016 | 183 | 2016 |
| The role of a sodium ion binding site in the allosteric modulation of the A2A adenosine G protein-coupled receptor H Gutiérrez-de-Terán, A Massink, D Rodríguez, W Liu, GW Han, ... Structure 21 (12), 2175-2185, 2013 | 135 | 2013 |
| Synthesis and evaluation of homo-bivalent GnRHR ligands KM Bonger, RJ van den Berg, LH Heitman, AP IJzerman, J Oosterom, ... Bioorganic & medicinal chemistry 15 (14), 4841-4856, 2007 | 112 | 2007 |
| Bias in chemokine receptor signalling AJM Zweemer, J Toraskar, LH Heitman, AP IJzerman Trends in immunology 35 (6), 243-252, 2014 | 102 | 2014 |
| Synthesis and biological evaluation of 2, 3, 5-substituted [1, 2, 4] thiadiazoles as allosteric modulators of adenosine receptors AMCH van den Nieuwendijk, D Pietra, L Heitman, A Göblyös, ... Journal of medicinal chemistry 47 (3), 663-672, 2004 | 100 | 2004 |
| Sodium ion binding pocket mutations and adenosine A2A receptor function A Massink, H Gutiérrez-de-Terán, EB Lenselink, NVO Zacarías, L Xia, ... Molecular pharmacology 87 (2), 305-313, 2015 | 96 | 2015 |
| Fragment Screening of GPCRs Using Biophysical Methods: Identification of Ligands of the Adenosine A2A Receptor with Novel Biological Activity D Chen, JC Errey, LH Heitman, FH Marshall, AP IJzerman, G Siegal ACS chemical biology 7 (12), 2064-2073, 2012 | 94 | 2012 |
| Molecular basis of ligand dissociation from the adenosine A2A receptor D Guo, AC Pan, RO Dror, T Mocking, R Liu, LH Heitman, DE Shaw, ... Molecular pharmacology 89 (5), 485-491, 2016 | 88 | 2016 |
| Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CB2 Receptor Expression and Ligand Engagement in Human Cells M Soethoudt, SC Stolze, MV Westphal, L Van Stralen, A Martella, ... Journal of the American Chemical Society 140 (19), 6067-6075, 2018 | 86 | 2018 |
| Structural mapping of adenosine receptor mutations: ligand binding and signaling mechanisms W Jespers, AC Schiedel, LH Heitman, RM Cooke, L Kleene, ... Trends in Pharmacological Sciences 39 (1), 75-89, 2018 | 83 | 2018 |
| Dual-point competition association assay: a fast and high-throughput kinetic screening method for assessing ligand-receptor binding kinetics D Guo, EJH van Dorp, T Mulder-Krieger, JPD van Veldhoven, J Brussee, ... Journal of biomolecular screening 18 (3), 309-320, 2013 | 80 | 2013 |
| The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI‐101 prevents cisplatin‐induced nephrotoxicity P Mukhopadhyay, M Baggelaar, K Erdelyi, Z Cao, R Cinar, F Fezza, ... British journal of pharmacology 173 (3), 446-458, 2016 | 76 | 2016 |
| G protein‐coupled receptors of the hypothalamic–pituitary–gonadal axis: A case for gnrh, LH, FSH, and GPR54 receptor ligands LH Heitman, AP IJzerman Medicinal research reviews 28 (6), 975-1011, 2008 | 76 | 2008 |
| Structure–kinetic relationships an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists M Vilums, AJM Zweemer, Z Yu, H de Vries, JM Hillger, H Wapenaar, ... Journal of medicinal chemistry 56 (19), 7706-7714, 2013 | 75 | 2013 |
