Adriaan p. Ijzerman
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(Suggest an Edit or Addition)Adriaan p. Ijzerman's Published Works
Number of citations in a given year to any of this author's works
Total number of citations to an author for the works they published in a given year. This highlights publication of the most important work(s) by the author
Published Works
- International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors. (2001) (2602)
- The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist (2008) (1695)
- International Union of Basic and Clinical Pharmacology. LXXXI. Nomenclature and Classification of Adenosine Receptors—An Update (2011) (1147)
- Structural Basis for Allosteric Regulation of GPCRs by Sodium Ions (2012) (829)
- International Union of Basic and Clinical Pharmacology. LXXXII: Nomenclature and Classification of Hydroxy-carboxylic Acid Receptors (GPR81, GPR109A, and GPR109B) (2011) (545)
- Allosteric modulation of G-protein-coupled receptors (2001) (538)
- Role of ceramide 1 in the molecular organization of the stratum corneum lipids. (1998) (265)
- Small molecule absorption by PDMS in the context of drug response bioassays (2017) (250)
- Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery. (2006) (230)
- THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors (2021) (212)
- Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation. (2011) (209)
- Beyond the hype: deep neural networks outperform established methods using a ChEMBL bioactivity benchmark set (2017) (204)
- Structure-based discovery of novel chemotypes for adenosine A(2A) receptor antagonists. (2010) (204)
- Structure of CC Chemokine Receptor 2 with Orthosteric and Allosteric Antagonists (2016) (195)
- Inverse agonism at G protein‐coupled receptors: (patho)physiological relevance and implications for drug discovery (2000) (187)
- Involvement of Asn-293 in stereospecific agonist recognition and in activation of the beta 2-adrenergic receptor. (1996) (178)
- A binding site model and structure-activity relationships for the rat A3 adenosine receptor. (1994) (164)
- Drug‐Target Residence Time—A Case for G Protein‐Coupled Receptors (2014) (150)
- Proteochemometric modeling as a tool to design selective compounds and for extrapolating to novel targets (2011) (147)
- Suramin analogues as subtype-selective G protein inhibitors. (1996) (147)
- Functional efficacy of adenosine A2A receptor agonists is positively correlated to their receptor residence time (2012) (146)
- Kinetics for Drug Discovery: an industry-driven effort to target drug residence time. (2017) (145)
- Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength. (2016) (140)
- New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine. (2004) (135)
- Inhibition of receptor/G protein coupling by suramin analogues. (1996) (129)
- Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists. (2001) (128)
- 2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. (2008) (124)
- The role of a sodium ion binding site in the allosteric modulation of the A(2A) adenosine G protein-coupled receptor. (2013) (118)
- Internalization and desensitization of adenosine receptors (2007) (113)
- Structure-Based Identification of OATP1B1/3 Inhibitors (2013) (110)
- Allosteric modulation of A(2A) adenosine receptors by amiloride analogues and sodium ions. (2000) (100)
- A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor. (2005) (99)
- Pyrazole derivatives as partial agonists for the nicotinic acid receptor. (2003) (97)
- Pharmacological analysis of ecto‐ATPase inhibition: evidence for combined enzyme inhibition and receptor antagonism in P2X‐purinoceptor ligands (1994) (95)
- Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor. (2000) (91)
- The Molecule Evoluator. An Interactive Evolutionary Algorithm for the Design of Drug-Like Molecules (2006) (91)
- Polypharmacology modelling using proteochemometrics (PCM): recent methodological developments, applications to target families, and future prospects (2015) (90)
- 2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists. (2004) (89)
- Allosteric modulation of the adenosine A(1) receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding. (1999) (88)
- G Protein-Coupled Receptor Heteromerization: A Role in Allosteric Modulation of Ligand Binding (2011) (88)
- Predicting Binding Affinities for GPCR Ligands Using Free-Energy Perturbation (2016) (87)
- Substructure Mining Using Elaborate Chemical Representation (2006) (86)
- Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. (1998) (85)
- How to catch a membrane protein in action: a review of functional membrane protein immobilization strategies and their applications. (2011) (85)
- Optogenetic activation of intracellular adenosine A2A receptor signaling in hippocampus is sufficient to trigger CREB phosphorylation and impair memory (2014) (84)
- Multi-RELIEF: a method to recognize specificity determining residues from multiple sequence alignments using a Machine-Learning approach for feature weighting (2008) (83)
- Ligand binding and subtype selectivity of the human A(2A) adenosine receptor: identification and characterization of essential amino acid residues. (2010) (82)
- Bias in chemokine receptor signalling. (2014) (81)
- Benchmarking of protein descriptor sets in proteochemometric modeling (part 1): comparative study of 13 amino acid descriptor sets (2013) (81)
- Nicotinic acid receptor subtypes and their ligands (2007) (80)
- Allosteric modulation of G protein-coupled receptors: perspectives and recent developments. (2004) (79)
- A new hERG allosteric modulator rescues genetic and drug‐induced long‐QT syndrome phenotypes in cardiomyocytes from isogenic pairs of patient induced pluripotent stem cells (2016) (79)
- Allosteric modulation of A(3) adenosine receptors by a series of 3-(2-pyridinyl)isoquinoline derivatives. (2001) (78)
- Hybrid ortho/allosteric ligands for the adenosine A(1) receptor. (2010) (78)
- Fragment screening of GPCRs using biophysical methods: identification of ligands of the adenosine A(2A) receptor with novel biological activity. (2012) (77)
- Coupling of the human A1 adenosine receptor to different heterotrimeric G proteins: evidence for agonist‐specific G protein activation (2004) (77)
- Kinetics, ultrastructural aspects and molecular modelling of transdermal peptide flux enhancement by N-alkylazacycloheptanones (1991) (77)
- Prospective Validation of a Comprehensive In silico hERG Model and its Applications to Commercial Compound and Drug Databases (2010) (77)
- Mechanism-based pharmacokinetic-pharmacodynamic modeling of antilipolytic effects of adenosine A(1) receptor agonists in rats: prediction of tissue-dependent efficacy in vivo. (1999) (76)
- Sodium Ion Binding Pocket Mutations and Adenosine A2A Receptor Function (2015) (73)
- Molecular Basis of Ligand Dissociation from the Adenosine A2A Receptor (2016) (73)
- Adenosine A1 receptor binding activity of methoxy flavonoids from Orthosiphon stamineus. (2009) (71)
- Molecular modeling of adenosine receptors. I. The ligand binding site on the A1 receptor. (1992) (70)
- Site-directed mutagenesis of the human A1 adenosine receptor: influences of acidic and hydroxy residues in the first four transmembrane domains on ligand binding. (1996) (70)
- Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors. (2004) (70)
- Differential Expression of Adenosine A3 Receptors Controls Adenosine A2A Receptor-Mediated Inhibition of TLR Responses in Microglia (2009) (69)
- Allosteric modulation of the adenosine family of receptors. (2005) (65)
- How Diverse Are Diversity Assessment Methods? A Comparative Analysis and Benchmarking of Molecular Descriptor Space (2014) (64)
- Complementarity between in Silico and Biophysical Screening Approaches in Fragment-Based Lead Discovery against the A2A Adenosine Receptor (2013) (64)
- Mechanism-based pharmacokinetic-pharmacodynamic modeling of the effects of N6-cyclopentyladenosine analogs on heart rate in rat: estimation of in vivo operational affinity and efficacy at adenosine A1 receptors. (1997) (63)
- Hemodynamic effects and histamine release elicited by the selective adenosine A3 receptor agonist 2-Cl-IB-MECA in conscious rats. (1996) (63)
- Why are A(2B) receptors low-affinity adenosine receptors? Mutation of Asn273 to Tyr increases affinity of human A(2B) receptor for 2-(1-Hexynyl)adenosine. (2000) (63)
- Benchmarking of protein descriptor sets in proteochemometric modeling (part 2): modeling performance of 13 amino acid descriptor sets (2013) (63)
- Reduced hepatitis B and D viral entry using clinically applied drugs as novel inhibitors of the bile acid transporter NTCP (2017) (62)
- Site-directed mutagenesis studies of human A(2A) adenosine receptors: involvement of glu(13) and his(278) in ligand binding and sodium modulation. (2000) (62)
- Allosteric modulation of adenosine receptors (2000) (62)
- TinyGRAP database: a bioinformatics tool to mine G-protein-coupled receptor mutant data. (1999) (62)
- Selective allosteric enhancement of agonist binding and function at human A3 adenosine receptors by a series of imidazoquinoline derivatives. (2002) (61)
- 1,3‐dialkylxanthine derivatives having high potency as antagonists at human A2B adenosine receptors (1999) (61)
- Extracellular adenosine-induced apoptosis in mouse neuroblastoma cells: studies on involvement of adenosine receptors and adenosine uptake. (2001) (60)
- Structure-kinetic relationships--an overlooked parameter in hit-to-lead optimization: a case of cyclopentylamines as chemokine receptor 2 antagonists. (2013) (59)
- Advances and Challenges in Computational Target Prediction (2019) (59)
- False positives in a reporter gene assay: identification and synthesis of substituted N-pyridin-2-ylbenzamides as competitive inhibitors of firefly luciferase. (2008) (58)
- Ribose-modified adenosine analogues as potential partial agonists for the adenosine receptor. (1995) (58)
- Functionally biased modulation of A(3) adenosine receptor agonist efficacy and potency by imidazoquinolinamine allosteric enhancers. (2011) (57)
- Pharmacokinetic-pharmacodynamic relationship of the cardiovascular effects of adenosine A1 receptor agonist N6-cyclopentyladenosine in the rat. (1994) (56)
- The role of the second and third extracellular loops of the adenosine A1 receptor in activation and allosteric modulation. (2012) (56)
- Donated chemical probes for open science (2018) (56)
- A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor. (2009) (55)
- Random mutagenesis of the human adenosine A2B receptor followed by growth selection in yeast. Identification of constitutively active and gain of function mutations. (2004) (55)
- The 2.6 A Crystal Structure of a Human A2A Adenosine Receptor bound to ZM241385. (2008) (54)
- Receptors coupling to G proteins: Is there a signal behind the sequence? (2000) (54)
- Kinetic Aspects of the Interaction between Ligand and G Protein-Coupled Receptor: The Case of the Adenosine Receptors. (2017) (54)
- 5-HT1A-versus D2-receptor selectivity of flesinoxan and analogous N4-substituted N1-arylpiperazines. (1997) (54)
- Which Compound to Select in Lead Optimization? Prospectively Validated Proteochemometric Models Guide Preclinical Development (2011) (53)
- Selecting an Optimal Number of Binding Site Waters To Improve Virtual Screening Enrichments Against the Adenosine A2A Receptor (2014) (52)
- Thermodynamics of full agonist, partial agonist, and antagonist binding to wild-type and mutant adenosine A1 receptors. (1998) (52)
- GPCR structure and activation: an essential role for the first extracellular loop in activating the adenosine A2B receptor (2011) (52)
- 1H-imidazo[4,5-c]quinolin-4-amines: novel non-xanthine adenosine antagonists. (1991) (52)
- Selective Photoaffinity Probe That Enables Assessment of Cannabinoid CB2 Receptor Expression and Ligand Engagement in Human Cells (2018) (52)
- Functional selectivity of adenosine receptor ligands (2011) (51)
- A novel class of adenosine A3 receptor ligands. 2. Structure affinity profile of a series of isoquinoline and quinazoline compounds. (1998) (51)
- Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists. (2002) (51)
- Biological and pharmacological roles of HCA receptors. (2011) (50)
- Caffeine increases light responsiveness of the mouse circadian pacemaker (2014) (50)
- Agonists for the adenosine A1 receptor with tunable residence time. A Case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines. (2014) (50)
- A novel chemogenomics analysis of G protein-coupled receptors (GPCRs) and their ligands: a potential strategy for receptor de-orphanization (2010) (49)
- Interleukin-6 Upregulates Neuronal Adenosine A1 Receptors: Implications for Neuromodulation and Neuroprotection (2008) (49)
- Synthesis and evaluation of homo-bivalent GnRHR ligands. (2007) (49)
- GPCR NaVa database: natural variants in human G protein‐coupled receptors (2008) (49)
- Identifying novel adenosine receptor ligands by simultaneous proteochemometric modeling of rat and human bioactivity data. (2012) (49)
- The adhesion G protein-coupled receptor G2 (ADGRG2/GPR64) constitutively activates SRE and NFκB and is involved in cell adhesion and migration. (2015) (48)
- N6,C8-distributed adenosine derivatives as partial agonists for adenosine A1 receptors. (1996) (48)
- Differential effects of the allosteric enhancer (2-amino-4,5-dimethyl-trienyl)[3-trifluoromethyl) phenyl]methanone (PD81,723) on agonist and antagonist binding and function at the human wild-type and a mutant (T277A) adenosine A1 receptor. (2001) (48)
- Evolutionary Algorithms in Drug Design (2005) (48)
- An exploration strategy improves the diversity of de novo ligands using deep reinforcement learning: a case for the adenosine A2A receptor (2018) (47)
- Small molecule antagonists for chemokine CCR3 receptors (2009) (47)
- The crystallographic structure of the human adenosine A2A receptor in a high-affinity antagonist-bound state: implications for GPCR drug screening and design. (2010) (47)
- A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy (2017) (46)
- Potent antagonists for the human adenosine A2B receptor. Derivatives of the triazolotriazine adenosine receptor antagonist ZM241385 with high affinity (1999) (46)
- Dual-Point Competition Association Assay (2013) (46)
- N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor. (2003) (46)
- Binding Kinetics of ZM241385 Derivatives at the Human Adenosine A2A Receptor (2014) (45)
- Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor. (2006) (45)
- Study of the interaction between aryloxypropanolamines and Asn386 in helix VII of the human 5-hydroxytryptamine1A receptor. (1997) (45)
- Multiple Binding Sites for Small-Molecule Antagonists at the CC Chemokine Receptor 2 (2013) (44)
- A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives. (1998) (44)
- 2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor. (2002) (43)
- Significantly Improved HIV Inhibitor Efficacy Prediction Employing Proteochemometric Models Generated From Antivirogram Data (2013) (43)
- The endocannabinoid 2-arachidonylglycerol is a negative allosteric modulator of the human A3 adenosine receptor. (2010) (43)
- A model for the antagonist binding site on the adenosine A1 receptor, based on steric, electrostatic, and hydrophobic properties. (1990) (43)
- A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines. (2008) (43)
- [3H]Org 43553, the First Low-Molecular-Weight Agonistic and Allosteric Radioligand for the Human Luteinizing Hormone Receptor (2008) (43)
- G protein‐coupled receptors of the hypothalamic–pituitary–gonadal axis: A case for gnrh, LH, FSH, and GPR54 receptor ligands (2008) (43)
- Lys 199 mutation of the human angiotensin type 1 receptor differentially affects the binding of surmountable and insurmountable non-peptide antagonists (2000) (42)
- Selectivity of action of 8‐alkylamino analogues of N6‐cyclopentyladenosine in vivo: haemodynamic versus anti‐lipolytic responses in rats (1998) (42)
- Luteolin, a compound with adenosine A(1) receptor-binding activity, and chromone and dihydronaphthalenone constituents from Senna siamea. (2000) (42)
- Mining a Chemical Database for Fragment Co-occurrence: Discovery of "Chemical Clichés" (2006) (42)
- Molecular modeling of adenosine receptors. The ligand binding site on the rat adenosine A2A receptor. (1994) (42)
- Differential allosteric modulation by amiloride analogues of agonist and antagonist binding at A(1) and A(3) adenosine receptors. (2003) (41)
- The RESOLUTE consortium: unlocking SLC transporters for drug discovery (2020) (41)
- Characterization of ecto-ATPase on human blood cells. A physiological role in platelet aggregation? (1993) (40)
- The Role of Target Binding Kinetics in Drug Discovery (2015) (40)
- A functional screening of adenosine analogues at the adenosine A2B receptor: a search for potent agonists. (1998) (39)
- N-cycloalkyl derivatives of adenosine and 1-deazaadenosine as agonists and partial agonists of the A(1) adenosine receptor. (2000) (39)
- Synthesis and biological evaluation of a new series of 2,3,5-substituted [1,2,4]-thiadiazoles as modulators of adenosine A1 receptors and their molecular mechanism of action. (2005) (39)
- A two‐entropies analysis to identify functional positions in the transmembrane region of class A G protein‐coupled receptors (2006) (39)
- 5'-substituted adenosine analogs as new high-affinity partial agonists for the adenosine A1 receptor. (1998) (38)
- Processing of adenosine receptor agonists in rat and human whole blood. (1998) (38)
- 2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. (2006) (38)
- Scintillation proximity assay (SPA) as a new approach to determine a ligand’s kinetic profile. A case in point for the adenosine A1 receptor (2015) (38)
- N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor. (1999) (38)
- Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000 (2008) (38)
- Deoxyribose analogues of N6‐cyclopentyladenosine (CPA): partial agonists at the adenosine A1 receptor in vivo (1995) (37)
- Tracing evolutionary pressure (2008) (37)
- TreeSOM: Cluster analysis in the self-organizing map (2006) (37)
- A Novel Nonribose Agonist, LUF5834, Engages Residues That Are Distinct from Those of Adenosine-Like Ligands to Activate the Adenosine A2a Receptor (2011) (36)
- Molecular mechanism of positive allosteric modulation of the metabotropic glutamate receptor 2 by JNJ‐46281222 (2016) (36)
- Inhibition of nucleoside transport by a new series of compounds related to lidoflazine and mioflazine. (1989) (36)
- Interleukin-6 Upregulates Neuronal Adenosine A1 Receptors: Implications for Neuromodulation and Neuroprotection (2008) (36)
- Interaction of amiloride and its analogues with adenosine A1 receptors in calf brain. (1990) (36)
- N4-unsubstituted N1-arylpiperazines as high-affinity 5-HT1A receptor ligands. (1995) (35)
- Influence of the molecular structure of N6-(omega-aminoalkyl)adenosines on adenosine receptor affinity and intrinsic activity. (1989) (35)
- Substructure Mining of GPCR Ligands Reveals Activity-Class Specific Functional Groups in an Unbiased Manner (2009) (35)
- Novel competitive antagonists for P2 purinoceptors. (1994) (35)
- Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor. (2009) (35)
- Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists. (2015) (34)
- Substituted terphenyl compounds as the first class of low molecular weight allosteric inhibitors of the luteinizing hormone receptor. (2009) (34)
- Site-directed mutagenesis of the human adenosine A2A receptor. Critical involvement of Glu13 in agonist recognition. (1996) (34)
- Combining Aggregation with Pareto Optimization: A Case Study in Evolutionary Molecular Design (2009) (34)
- Medicinal chemistry of adenosine A1 receptor ligands. (2003) (34)
- Structure‐affinity relationships of adenosine A2B receptor ligands (2006) (34)
- Allosteric modulation, thermodynamics and binding to wild‐type and mutant (T277A) adenosine A1 receptors of LUF5831, a novel nonadenosine‐like agonist (2006) (34)
- 5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors. (1999) (34)
- ZM241385, DPCPX, MRS1706 Are Inverse Agonists with Different Relative Intrinsic Efficacies on Constitutively Active Mutants of the Human Adenosine A2B Receptor (2007) (33)
- Analysis of Iterative Screening with Stepwise Compound Selection Based on Novartis In-house HTS Data. (2016) (33)
- Whole-cell biosensor for label-free detection of GPCR-mediated drug responses in personal cell lines. (2015) (33)
- 8-substituted adenosine and theophylline-7-riboside analogues as potential partial agonists for the adenosine A1 receptor. (1995) (33)
- 5'-O-alkyl ethers of N,2-substituted adenosine derivatives: partial agonists for the adenosine A1 and A3 receptors. (2001) (33)
- A steric and electrostatic comparison of three models for the agonist/antagonist binding site on the adenosine A1 receptor. (1992) (33)
- Allosteric modulation of purine and pyrimidine receptors. (2011) (32)
- Kv11.1 (hERG)‐induced cardiotoxicity: a molecular insight from a binding kinetics study of prototypical Kv11.1 (hERG) inhibitors (2015) (32)
- Functional role of adenosine receptor subtypes in the regulation of blood-brain barrier permeability: possible implications for the design of synthetic adenosine derivatives. (2003) (32)
- Drug-Target Association Kinetics in Drug Discovery. (2019) (32)
- Characterization of 12 GnRH peptide agonists – a kinetic perspective (2016) (31)
- Proteochemometric modelling coupled to in silico target prediction: an integrated approach for the simultaneous prediction of polypharmacology and binding affinity/potency of small molecules (2015) (31)
- Amiloride Derivatives and a Nonpeptidic Antagonist Bind at Two Distinct Allosteric Sites in the Human Gonadotropin-Releasing Hormone Receptor (2008) (31)
- Therapeutic efficacy of the adenosine A1 receptor agonist N6-cyclopentyladenosine (CPA) against organophosphate intoxication (2002) (31)
- Allosteric modulation of adenosine receptors. (2011) (31)
- Structure-Based Discovery of Novel Chemotypes for Adenosine A 2 A Receptor Antagonists (2010) (30)
- International Union of Basic and Clinical Pharmacology. CXII: Adenosine Receptors: A Further Update (2022) (30)
- Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor. (2001) (30)
- A prospective cross-screening study on G-protein-coupled receptors: lessons learned in virtual compound library design. (2012) (30)
- Determination of different putative allosteric binding pockets at the lutropin receptor by using diverse drug-like low molecular weight ligands (2012) (30)
- Synthesis and biological evaluation of 2-aminothiazoles and their amide derivatives on human adenosine receptors. Lack of effect of 2-aminothiazoles as allosteric enhancers. (2005) (30)
- Apoptosis induced by extracellular ATP in the mouse neuroblastoma cell line N1E-115: studies on involvement of P2 receptors and adenosine. (2002) (30)
- Techniques: how to boost GPCR mutagenesis studies using yeast. (2005) (30)
- Strategies to reduce HERG K+ channel blockade. Exploring heteroaromaticity and rigidity in novel pyridine analogues of dofetilide. (2013) (29)
- Isolation of Opioid‐active Compounds from Tabernaemontana pachysiphon leaves (1999) (29)
- 2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. (2007) (29)
- Discovery and Mapping of an Intracellular Antagonist Binding Site at the Chemokine Receptor CCR2 (2014) (28)
- Xanthine-7-Ribosides as Adenosine Al Receptor Antagonists: Further Evidence for Adenosine's Anti Mode of Binding (1990) (28)
- Multi-Objective Evolutionary Design of Adenosine Receptor Ligands (2012) (28)
- Intracellular Receptor Modulation: Novel Approach to Target GPCRs. (2018) (28)
- Elucidation of structure–activity relationships of 2‐amino‐3‐benzoylthiophenes: Study of their allosteric enhancing vs. antagonistic activity on adenosine A1 receptors (2000) (28)
- 5'-Substituted Amiloride Derivatives as Allosteric Modulators Binding in the Sodium Ion Pocket of the Adenosine A2A Receptor. (2016) (28)
- Discovery and Kinetic Profiling of 7-Aryl-1,2,4-triazolo[4,3-a]pyridines: Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 2. (2017) (28)
- A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor (2019) (27)
- Mapping the N6-region of the adenosine A1 receptor with computer graphics. (1989) (27)
- Structural aspects of bile acids involved in the regulation of cholesterol 7 alpha-hydroxylase and sterol 27-hydroxylase. (1995) (27)
- Synthesis and biological evaluation of disubstituted N6-cyclopentyladenine analogues: the search for a neutral antagonist with high affinity for the adenosine A1 receptor. (2004) (26)
- 2,8-Disubstituted adenosine derivatives as partial agonists for the adenosine A2A receptor. (2003) (26)
- Enhancing search space diversity in multi-objective evolutionary drug molecule design using niching (2009) (26)
- Exploring Chemical Substructures Essential for hERG K+ Channel Blockade by Synthesis and Biological Evaluation of Dofetilide Analogues (2009) (26)
- Full and partial agonistic behaviour and thermodynamic binding parameters of adenosine A1 receptor ligands. (1994) (26)
- A model of the serotonin 5-HT1A receptor: agonist and antagonist binding sites. (1994) (26)
- Shallow agonist competition binding curves for beta-adrenergic receptors: the role of tight agonist binding. (1987) (25)
- Removal of human ether-à-go-go related gene (hERG) K+ channel affinity through rigidity: a case of clofilium analogues. (2013) (25)
- Adenosine A1 Receptor AgonistN 6-Cyclopentyladenosine Affects the Inactivation of Acetylcholinesterase in Blood and Brain by Sarin (2003) (25)
- An efficient, versatile and scalable pattern growth approach to mine frequent patterns in unaligned protein sequences (2007) (25)
- A3 Adenosine Receptor Allosteric Modulator Induces an Anti-Inflammatory Effect: In Vivo Studies and Molecular Mechanism of Action (2014) (25)
- An Affinity-Based Probe for the Human Adenosine A2A Receptor (2018) (24)
- Allosteric modulators affect the internalization of human adenosine A1 receptors. (2005) (24)
- Protection from Myocardial Ischemia/Reperfusion Injury by a Positive Allosteric Modulator of the A3 Adenosine Receptor (2012) (24)
- A covalent antagonist for the human adenosine A2A receptor (2016) (24)
- Substructure‐Based Virtual Screening for Adenosine A2A Receptor Ligands (2011) (24)
- Structure–activity relationships of inverse agonists for G‐protein‐coupled receptors (2005) (24)
- Pharmacokinetic-Pharmacodynamic Analysis of the EEG Effect of Alfentanil in Rats Followingβ-Funaltrexamine-Induced μOpioid Receptor “Knockdown”In Vivo (2000) (24)
- Structure–Affinity Relationships and Structure–Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A3 Receptor Antagonists (2017) (24)
- Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A3 Receptor (2019) (24)
- Identification of class-determining residues in G protein-coupled receptors by sequence analysis. (1997) (24)
- Medicinal chemistry of P2 and adenosine receptors: Common scaffolds adapted for multiple targets. (2020) (24)
- Adenosine A2B Receptor Agonism Inhibits Neointimal Lesion Development After Arterial Injury in Apolipoprotein E–Deficient Mice (2012) (24)
- Mutations inducing divergent shifts of constitutive activity reveal different modes of binding among catecholamine analogues to the β2‐adrenergic receptor (2002) (24)
- Brain penetration of synthetic adenosine A1 receptor agonists in situ: role of the rENT1 nucleoside transporter and binding to blood constituents. (2005) (23)
- Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'receptor knock-down' tool. (2001) (23)
- Label-free technology and patient cells: from early drug development to precision medicine. (2017) (23)
- 8-Alkylamino-substituted analogs of N6-cyclopentyladenosine are partial agonists for the cardiovascular adenosine A1 receptors in vivo. (1997) (23)
- Pharmacokinetic modelling of the haemodynamic effects of the A2a adenosine receptor agonist CGS 21680C in conscious normotensive rats (1995) (23)
- Study of Interaction between Agonists and Asn293 in Helix VI of Human β2-Adrenergic Receptor (1999) (23)
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- Deciphering conformational selectivity in the A2A adenosine G protein-coupled receptor by free energy simulations (2021) (1)
- Species differences and mechanism of action of A3 adenosine receptor allosteric modulators (2017) (1)
- [3H]R75231 — a new radioligand for the nitrobenzylthioinosine sensitive nucleoside transport proteins Characterization of (±)-[3H]R75231 binding to calf lung membranes, stereospecificity of its two stereoisomers, and comparison with [3H]nitrobenzylthioinosine binding (1992) (1)
- Allosteric modulation of the chemokine receptor CCR2 by amiloride analogues and sodium ions (2014) (1)
- POPULATION PHARMACOKINETIC MODELLING OF BLOOD-BRAIN BARRIER TRANSPORT OF SYNTHETIC ADENOSINE A 1 RECEPTOR AGONISTS (2004) (1)
- G protein-coupled receptor heteromerization : A role in allosteric modulation of ligand-mediated receptor binding (2011) (1)
- Novel algorithms for protein sequence analysis (2005) (0)
- Binding characteristics of the regulatory guanine nucleotide binding protein, and the activation of the enzyme adenylate cyclase, present in a bovine skeletal muscle membrane preparation. (1986) (0)
- Identification of OATP1B1 and OATP1B3 inhibitors by in silico modeling of in vitro data (2012) (0)
- Evolutionary algorithms in de novo molecule design : comparing atom-based and fragment-based optimization (2010) (0)
- Inverse agonism at adenosine A1 receptors (2003) (0)
- The RESOLUTE consortium: unlocking SLC transporters for drug discovery (2020) (0)
- Impact of cancer-associated mutations in CC chemokine receptor 2 on receptor function and antagonism. (2022) (0)
- Inverse agonism : proceedings of the Esteve Foundation Symposium X, S'Agaró (Girona), Spain, 2-5 October 2002 (2003) (0)
- Scintillation proximity assay (SPA) as a new approach to determine a ligand’s kinetic profile. A case in point for the adenosine A1 receptor (2015) (0)
- Deja Vu - Reja Vu; On knowledge-based approaches linking ligand and target information to bioactivity (2007) (0)
- Author response: Donated chemical probes for open science (2018) (0)
- A yeast screening method to decipher the interaction between the adenosine A2B receptor and the C-terminus of different G protein α-subunits (2014) (0)
- Abstracts Dutch Pharmacological Society Meeting Lunteren, The Netherlands, February 2627, 1998 Edited by AF Roffel, AD Kraneveld, AL Frankhuijzen (2009) (0)
- A novel CCR2 antagonist inhibits atherogenesis in apoE deficient mice by achieving high receptor occupancy (2017) (0)
- K v 11.1 (hERG)-induced cardiotoxicity: a molecular insight from a binding kinetics study of prototypic K v 11.1 inhibitors (2015) (0)
- Computers and drug discovery (2001) (0)
- Pan-cancer functional analysis of somatic mutations in G protein-coupled receptors (2022) (0)
- A covalent antagonist for the human adenosine A2A receptor (2016) (0)
- Therapeutic efficacy in organophosphate poisoning by inhibiting central release of acetylcholine (2004) (0)
- Chemogenomics Approaches for the Discovery of New Medicines against Malaria (2012) (0)
- Using data mining to improve mutation in a tool for molecular evolution (2005) (0)
- Binding of the radioligand [35S]adenosine 5'-O-(2-thiodiphosphate) and intracellular calcium response in rat liver parenchymal cells. (1993) (0)
- Abstracts of Dutch Ph.D. Theses (2005) (0)
- Mapping the Turkey Erythrocyte β Receptor: A Distance Geometry Approach. (1986) (0)
- 3′‐Amidated 3′‐Deoxyxylofuranose Analogues of N6‐Cyclopentyladenosines: A New Class of Non‐Xanthine Antagonists at the Adenosine A1 Receptor. (1999) (0)
- Abstracts of papers pharmacological meeting (2005) (0)
- Synthesis of 3′‐Fluoro‐3′‐deoxy‐N6‐cyclopentyladenosine. (1995) (0)
- Effects of pyrazole partial agonists on HCA 2-mediated flushing and hepatic VLDL production in mice (2011) (0)
- Design, Synthesis and Pharmacological Profile of LUF7746, a Novel Covalent Partial Agonist for the Adenosine A1 Receptor (2020) (0)
- Abstracts of papers medicinal chemical meeting (1988) (0)
- [3H]R75231; A New Radiolabelled Nucleoside Transporter Probe Related to Mioflazine and Lidoflazine (1991) (0)
- Interleukin-6 is involved in upregulation of adenosine A1 receptor expression after seizures (2004) (0)
- Pharmacokinetic and pharmacodynamic studies of full and partial agonists of adenosine A1 receptors (1998) (0)
- Transforming Data into Knowledge for Intelligent Decision-making in Early Drug Discovery (2012) (0)
- Radioligand binding assays reveal allosteric characteristics of dofetilide analogues (2015) (0)
- Study of Interaction between Agonists and Asn293 in Helix VI of Human b 2 -Adrenergic Receptor (1999) (0)
- Abstracts of papers medicinal chemistry meeting (2005) (0)
- Proteochemometric Modeling Identifies Chemically Diverse Norepinephrine Transporter Inhibitors (2023) (0)
- Mass spectrometry-based ligand binding assays on adenosine A1 and A2A receptors (2015) (0)
- On the Relation between HERG Channel Block in Cell Line and Action Potential Prolongation in Human iPSC Cardiomyocytes (2016) (0)
- Crystal structure of stabilized A2A adenosine receptor A2AR-StaR2-bRIL in complex with compound 12b at 2.2A resolution (2016) (0)
- Responses in Microglia Receptor-Mediated Inhibition of TLR 2 AReceptors Controls Adenosine A 3 Differential Expression of Adenosine (2009) (0)
- Modelling ofthepharmacodynamic interaction ofan Al adenosine receptor agonist andantagonist invivo: N6-cyclopentyladenosine and8-cyclopentylthe ophylline (1995) (0)
- Activation of the human adenosine A2B receptor (2005) (0)
- COMPUTATIONAL CHEMISTRY IN RECEPTOR-BASED DRUG DESIGN (1998) (0)
- The Inhibition of Nucleoside Transport in Human Erythrocytes by Mioflazine Analogues (1991) (0)
- P2-Purinoceptor Mediated Inhibition of Adenylate Cyclase Activity (1991) (0)
- Purinoceptor mediated inhibition of adenylate cyciase activity (1990) (0)
- A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine A3 receptor (2019) (0)
- Pharmacokinetics and cardiovascular pharmaco-dynamics in rats of three adenosine A1-receptor agonists with differing lipophilicity (1995) (0)
- Allosteric Modulation of G- Protein- Coupled Receptors: IMPLICATIONS FOR DRUG ACTION (2003) (0)
- Abstracts of papers (2005) (0)
- From receptor binding kinetics to signal transduction; a missing link in predicting in vivo drug-action (2017) (0)
- Data Citation: Giving Credit where Credit is Due (2018) (0)
- Drug-induced loss of cell-cell and cell-extracellular matrix interactions: implications for apoptosis (2000) (0)
- Gonadotrophin-releasing hormone receptors in GtoPdb v.2021.3 (2021) (0)
- Structure-Activity Relationships of the Sustained Effects of Adenosine A 2 A Receptor Agonists Driven by Slow Dissociation Kinetics s (2016) (0)
- Molecular mechanisms and drug design (2001) (0)
- Impedance-Based Phenotypic Readout of Transporter Function: A Case for Glutamate Transporters (2022) (0)
- Reduced hepatitis B and D viral entry using clinically applied drugs as novel inhibitors of the bile acid transporter NTCP (2017) (0)
- Corrections to Substituted Terphenyl Compounds as the First Class of Low Molecular Weight Allosteric Inhibitors of the Luteinizing Hormone Receptor (2010) (0)
- Adenosine A2B receptor agonism inhibits vascular smooth muscle cell proliferation and intimal hyperplasia in ApoE deficient mice (2012) (0)
- Targeting solute carriers to modulate receptor-ligand interactions. (2022) (0)
- Predicting conformational selectivity in a prototypical GPCR (2020) (0)
- The beta-adrenoceptor-adenylate cyclase complex (1986) (0)
- Development of subtype-selective covalent ligands for the adenosine A2B receptor by tuning the reactive group. (2022) (0)
- Gonadotrophin-releasing hormone receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database (2019) (0)
- Kinetic profiling and functional characterization of 8-phenylxanthine derivatives as A2B adenosine receptor antagonists. (2022) (0)
- In vitro and in silico screening of OATP1B1 and OATP1B3 modulators (2012) (0)
- Kinetics of drug effects to optimise delivery to the brain (2001) (0)
- Evolutionary design of selective adenosine receptor ligands (2010) (0)
- Corrigendum to "Impact of cancer-associated mutations in CC chemokine receptor 2 on receptor function and antagonism" [Biochem. Pharmacol. 208 (2023) 115399]. (2023) (0)
- 5'-Deoxy congeners of 9-(3-amido-3-deoxy-β-D-xylofuranosyl)- N 6 -cyclopentyladenine: New adenosine A 1 receptor antagonists (1999) (0)
- Crystal structure of the non-ribose partial agonist LUF5833 bound to the adenosine A2A receptor (2021) (0)
- Adenosine-induced caspase activity in N1E-115 cells. (2000) (0)
- Brazilian Amazon Extinction Debt and Windows of Conservation Opportunity in the (2012) (0)
- Abstracts of papers (1971) (0)
- Activity of LUF6000 and LUF6096 as positive allosteric modulators (PAMs) for the A3 adenosine receptor (AR) is species‐dependent (2012) (0)
- Allosteric modulation of 'reproductive' GPCRs (2004) (0)
- Abstracts of papers (2005) (0)
- Chapter 3 Adenosine A 1 receptor binding activity of methoxy flavonoids from Orthosiphon stamineus Benth (2011) (0)
- ASSOCIATE EDITOR: ELIOT OHLSTEIN International Union of Basic andClinical Pharmacology. CXII: Adenosine Receptors: A Further Update (2022) (0)
- Target Residence Time (2010) (0)
- Structural analysis of κ-opioid receptor agonists (2010) (0)
- Adenosine delivery via squalene-adenosine nanoparticles to treat ischemic diseases: liver versus brain (2018) (0)
- Kinetic studies of the Kv11.1 (hERG) channel (2015) (0)
- Abstracts of papers Pharmacological Meeting (2005) (0)
- New insights into the molecular mechanisms of A1 adenosine receptor action (1998) (0)
- Substituted pyrazolo as analgesics and thiazolopyrimidiner (2002) (0)
- A Chemical Biological Approach to Study G Protein-Coupled Receptors: Labeling the Adenosine A1 Receptor Using an Electrophilic Covalent Probe (2022) (0)
- Structural Analysis of ϰ-Opioid Receptor Agonists. (1993) (0)
- Molecular probes for the human adenosine receptors (2020) (0)
- Factors controlling beta 1-adrenoceptor affinity and selectivity. (1985) (0)
- Insights into Molecular Basis of hERG Inhibition by Studying a Library of Dofetilide Derivatives (2014) (0)
- Abstracts of papers (2005) (0)
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