Adriaan p. Ijzerman

Adriaan p. Ijzerman's AcademicInfluence.com Rankings

Adriaan p. Ijzerman

Medical

#2032

World Rank

#2426

Historical Rank

Pharmacology

#206

World Rank

#246

Historical Rank

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Medical

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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)
Three “hotspots” important for adenosine A2B receptor activation: a mutational analysis of transmembrane domains 4 and 5 and the second extracellular loop (2011) (23)
Modelling of the pharmacodynamic interaction of an A1 adenosine receptor agonist and antagonist in vivo: N6‐cyclopentyladenosine and 8‐cyclopentyltheophylline (1995) (23)
Human G protein-coupled receptor studies in Saccharomyces cerevisiae. (2016) (22)
Interference of linoleic acid fraction in some receptor binding assays. (1999) (22)
Allosteric modulators of the hERG K(+) channel: radioligand binding assays reveal allosteric characteristics of dofetilide analogs. (2014) (22)
Adenosine A1 receptor and ligand molecular modeling (1993) (21)
High-performance liquid chromatography of the adenosine A1 agonist N6-cyclopentyladenosine and the A1 antagonist 8-cyclopentyltheophylline and its application in a pharmacokinetic study in rats. (1993) (21)
Scanning mutagenesis in a yeast system delineates the role of the NPxxY(x)(5,6)F motif and helix 8 of the adenosine A(2B) receptor in G protein coupling. (2015) (21)
Structure-Affinity Relationships (SARs) and Structure-Kinetics Relationships (SKRs) of Kv11.1 Blockers. (2015) (21)
The Added Value of Assessing Ligand-Receptor Binding Kinetics in Drug Discovery. (2016) (21)
A yeast screening method to decipher the interaction between the adenosine A2B receptor and the C-terminus of different G protein α-subunits (2014) (21)
Indanes—Properties, Preparation, and Presence in Ligands for G Protein Coupled Receptors (2015) (21)
The membrane stabilizing activity of beta-adrenoceptor ligands. Quantitative evaluation of the interaction of phenoxypropanolamines with the [3H]batrachotoxinin A 20-alpha-benzoate binding site on voltage-sensitive sodium channels in rat brain. (1987) (21)
A "locked-on," constitutively active mutant of the adenosine A1 receptor. (2005) (21)
Isoquinoline and Quinazoline Urea Analogues as Antagonists for the Human Adenosine A3 Receptor. (2000) (20)
Physiological Indirect Effect Modeling of the Antilipolytic Effects of Adenosine A1-Receptor Agonists (1997) (20)
Allosteric Modulation of Kv11.1 (hERG) Channels Protects Against Drug-Induced Ventricular Arrhythmias (2016) (20)
Data-driven approaches used for compound library design, hit triage and bioactivity modeling in high-throughput screening (2016) (20)
Molecular mechanism of allosteric modulation at GPCRs: insight from a binding kinetics study at the human A1 adenosine receptor (2014) (20)
The kinetics of the binding of warfarin to human serum albumin as studied by stopped-flow spectrophotometry (1982) (20)
Inhibition of nucleoside transport proteins by C8-alkylamine-substituted purines. (2005) (20)
Quantitative evaluation of the beta 2-adrenoceptor affinity of phenoxypropanolamines and phenylethanolamines. (1985) (19)
Non‐Xanthine Antagonists for the Adenosine A1 Receptor (2004) (19)
Melanosome binding and oxidation-reduction properties of synthetic L-dopa-melanin as in vitro tests for drug toxicity. (1988) (19)
Equilibrium and kinetic selectivity profiling on the human adenosine receptors. (2016) (19)
When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists. (2015) (19)
In search of novel ligands using a structure-based approach: a case study on the adenosine A2A receptor (2016) (19)
An Overview of Cell-Based Assay Platforms for the Solute Carrier Family of Transporters (2021) (19)
Pharmacokinetic‐pharmacodynamic modelling of the anti‐lipolytic and anti‐ketotic effects of the adenosine A1‐receptor agonist N6‐(p‐sulphophenyl)adenosine in rats (1997) (19)
Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene. (2014) (19)
Chemogenomics approaches for receptor deorphanization and extensions of the chemogenomics concept to phenotypic space. (2011) (19)
Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718. (1992) (18)
Modulation of agonist responses at the A(1) adenosine receptor by an irreversible antagonist, receptor-G protein uncoupling and by the G protein activation state. (2002) (18)
N6-cyclopentyl-3'-substituted-xylofuranosyladenosines: a new class of non-xanthine adenosine A1 receptor antagonists. (1997) (18)
Allosteric modulation of G protein‐coupled receptors by amiloride and its derivatives. Perspectives for drug discovery? (2019) (18)
2-Nitro analogues of adenosine and 1-deazaadenosine: synthesis and binding studies at the adenosine A1, A2A and A3 receptor subtypes. (2000) (18)
Mass spectrometry-based ligand binding assays on adenosine A1 and A2A receptors (2015) (18)
Structure-Activity Relationships of the Sustained Effects of Adenosine A2A Receptor Agonists Driven by Slow Dissociation Kinetics (2017) (18)
Functional selectivity of adenosine A1 receptor ligands? (2012) (18)
Mapping the turkey erythrocyte beta receptor: a distance geometry approach. (1986) (18)
The mouse brain adenosine A1 receptor: functional expression and pharmacology. (2004) (18)
Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A2A Receptor (2021) (17)
Covalent Allosteric Probe for the Metabotropic Glutamate Receptor 2: Design, Synthesis, and Pharmacological Characterization (2018) (17)
Understanding of Molecular Substructures that Contribute to hERG K+ Channel Blockade: Synthesis and Biological Evaluation of E‐4031 Analogues (2012) (17)
Blood-brain barrier transport of synthetic adenosine A1 receptor agonists in vitro: structure transport relationships. (2003) (17)
Partial agonism of theophylline-7-riboside on adenosine receptors (1994) (17)
Partial adenosine A(1) receptor agonists inhibit sarin-induced epileptiform activity in the hippocampal slice. (2003) (17)
Nucleoside transport inhibition and platelet aggregation in human blood: R75231 and its enantiomers, draflazine and R88016. (1994) (17)
Suramin analogs, divalent cations and ATPγS as inhibitors of ecto-ATPase (1995) (17)
The antiarrhythmic properties of β-adrenoceptor antagonists (1989) (17)
Chemical modification of adenosine A1 receptors. Implications for the interaction with R-PIA, DPCPX and amiloride. (1990) (16)
Affinity, binding kinetics and functional characterization of draflazine analogues for human Equilibrative Nucleoside Transporter 1 (SLC29A1). (2019) (16)
Proteochemometrics - recent developments in bioactivity and selectivity modeling. (2019) (16)
The adenosine A3 receptor and its ligands. (2001) (16)
Relative binding orientations of adenosine A1 receptor ligands — A test case for Distributed Multipole Analysis in medicinal chemistry (1995) (16)
Adenosine derivatives with N 6‐alkyl, ‐alkylamine or ‐alkyladenosine substituents as probes for the A1‐receptor (1987) (16)
Synthesis and biological evaluation of negative allosteric modulators of the Kv11.1(hERG) channel. (2015) (16)
Designing active template molecules by combining computational de novo design and human chemist's expertise. (2007) (16)
Receptor binding profiles of amiloride analogues provide no evidence for a link between receptors and the Na+/H+ exchanger, but indicate a common structure on receptor proteins. (1991) (16)
Binding of the radioligand [3Sadenosine 5'-O-(2-thiodiphosphate) and intracellular calcium response in rat liver parenchymal cells (1993) (16)
A two‐state model for the kinetics of competitive radioligand binding (2018) (15)
Getting from A to B—exploring the activation motifs of the class B adhesion G protein‐coupled receptor subfamily G member 4/GPR112 (2016) (15)
A Novel Selective Inverse Agonist of the CB2 Receptor as a Radiolabeled Tool Compound for Kinetic Binding Studies (2017) (15)
DrugEx v2: de novo design of drug molecules by Pareto-based multi-objective reinforcement learning in polypharmacology (2021) (15)
Selective Human Adenosine A3 Antagonists based on Pyrido[2,1‐f]purine‐2,4‐diones: Novel Features of hA3 Antagonist Binding (2008) (15)
Radical scavenging properties of adenosine and derivatives in vitro (1996) (15)
Inhibition of nucleoside transport by new analogues of 4-nitrobenzylthioinosine: replacement of the ribose moiety by substituted benzyl groups. (2004) (15)
Chemogenomics: Looking at biology through the lens of chemistry (2009) (14)
LUF7244, an allosteric modulator/activator of Kv11.1 channels, counteracts dofetilide‐induced torsades de pointes arrhythmia in the chronic atrioventricular block dog model (2019) (14)
Kinetic binding and activation profiles of endogenous tachykinins targeting the NK1 receptor. (2016) (14)
Computational Approaches for De Novo Drug Design: Past, Present, and Future (2021) (14)
Characterization of [3H]LUF5834: A novel non-ribose high-affinity agonist radioligand for the adenosine A1 receptor. (2010) (14)
Biological activities of N6,C8-disubstituted adenosine derivatives as partial agonists at rat brain adenosine A1 receptors. (1997) (14)
Phenyl‐substituted N6‐phenyladenosines and N6‐phenyl‐5′‐N‐ethylcarboxamidoadenosines with high activity at human adenosine A2B receptors (2000) (14)
Mining protein dynamics from sets of crystal structures using “consensus structures” (2010) (14)
Evolutionary algorithms for automated drug design towards target molecule properties (2008) (14)
Putative role of the adenosine A3 receptor in the antiproliferative action of N6-(2-isopentenyl)adenosine (2011) (14)
Structure-Affinity Relationships of Adenosine A2B Receptor Ligands (2006) (13)
A binding kinetics study of human adenosine A3 receptor agonists (2018) (13)
The structure of the adenosine receptors: implications for drug discovery. (2011) (13)
Factors controlling β1-adrenoceptor affinity and selectivity (1985) (13)
Molecular modeling of a putative antagonist binding site on helix III of the β-adrenoceptor (1989) (13)
Adenosine and ATP: from receptor structure to clinical applications. (1994) (13)
Metabolic and cardiovascular effects of the adenosine A1 receptor agonist N6-(p-sulfophenyl)adenosine in diabetic Zucker rats: influence of the disease on the selectivity of action. (1998) (13)
Heterodimers of G protein-coupled receptors as novel and distinct drug targets (2006) (13)
Interacting with GPCRs: Using Interaction Fingerprints for Virtual Screening (2016) (13)
Long residence time adenosine A1 receptor agonists produce sustained wash-resistant antilipolytic effect in rat adipocytes. (2019) (13)
Domains for activation and inactivation in G protein-coupled receptors--a mutational analysis of constitutive activity of the adenosine A2B receptor. (2014) (13)
Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core. (2008) (13)
Identification of novel small molecule inhibitors for solute carrier SGLT1 using proteochemometric modeling (2019) (13)
Inhibition of nucleoside uptake in human erythrocytes by a new series of compounds related to lidoflazine and mioflazine. (1990) (12)
Inhibition of nucleoside transport by new analogues of nitrobenzylthioinosine. (2003) (12)
Label-free detection of transporter activity via GPCR signalling in living cells: A case for SLC29A1, the equilibrative nucleoside transporter 1 (2019) (12)
Persistent GnRH receptor activation in pituitary αT3-1 cells analyzed with a label-free technology. (2016) (12)
A New Class of Fluorinated A2A Adenosine Receptor Agonist with Application to Last‐Step Enzymatic [18F]Fluorination for PET Imaging (2017) (12)
Data-Driven Derivation of an "Informer Compound Set" for Improved Selection of Active Compounds in High-Throughput Screening (2016) (12)
Squalene-Adenosine Nanoparticles: Ligands of Adenosine Receptors or Adenosine Prodrug? (2019) (12)
Constitutive activity of the metabotropic glutamate receptor 2 explored with a whole‐cell label‐free biosensor (2018) (12)
Pharmacokinetic/pharmacodynamic modelling of the anti-hyperalgesic and anti-nociceptive effect of adenosine A1 receptor partial agonists in neuropathic pain. (2005) (12)
Novel 3,6,7-substituted pyrazolopyrimidines as positive allosteric modulators for the hydroxycarboxylic acid receptor 2 (GPR109A). (2012) (12)
Characterization of cancer-related somatic mutations in the adenosine A2B receptor. (2020) (12)
Pyrrolone Derivatives as Intracellular Allosteric Modulators for Chemokine Receptors: Selective and Dual-Targeting Inhibitors of CC Chemokine Receptors 1 and 2 (2018) (11)
Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A). (2011) (11)
Quantitative evaluation of the beta 2-adrenoceptor intrinsic activity of N-tert-butylphenylethanolamines. (1986) (11)
Study of interaction between agonists and asn293 in helix VI of human beta(2)-adrenergic receptor. (1999) (11)
The relation between ionization and affinity of β-adrenoceptor ligands (1984) (11)
Species differences and mechanism of action of A3 adenosine receptor allosteric modulators (2018) (11)
Application of portfolio optimization to drug discovery (2019) (10)
Stereoselectivity of drug-receptor interactions. (2003) (10)
5'-Deoxy congeners of 9-(3-amido-3-deoxy-beta-D-xylofuranosyl)-N(6)-cyclopentyladenine: new adenosine A(1) receptor antagonists and inverse agonists. (2002) (10)
Mutational analysis of the putative devazepide binding site of the CCK(A) receptor. (1997) (10)
From receptor binding kinetics to signal transduction; a missing link in predicting in vivo drug-action (2017) (10)
Allosteric approaches to GPCR drug discovery. (2013) (10)
General T-cell receptor antagonists to immunomodulate HLA-A2-restricted minor histocompatibility antigen HA-1-specific T-cell responses. (2002) (10)
Novel natural and synthetic inhibitors of solute carriers SGLT1 and SGLT2 (2019) (10)
Synthesis and biological evaluation of a new series of 2-amino-3-aroyl thiophene derivatives as agonist allosteric modulators of the A1 adenosine receptor. A position-dependent effect study. (2015) (9)
Time course of action of three adenosine A1 receptor agonists with differing lipophilicity in rats: comparison of pharmacokinetic, haemodynamic and EEG effects (1997) (9)
Quantification of the in vivo potency of the adenosine A2 receptor antagonist 8-(3-chlorostyryl)caffeine. (1995) (9)
A molecular graphics study exploring a putative ligand binding site of theβ-adrenoceptor (1988) (9)
Allosteric modulation of the rat adenosine A1 receptor: Differential effects on agonist and antagonist binding (2000) (9)
Design and Pharmacological Profile of a Novel Covalent Partial Agonist for the Adenosine A1 Receptor. (2020) (9)
Pharmacokinetic‐haemodynamic relationships of 2‐chloroadenosine at adenosine A1 and A2a receptors in vivo (1996) (9)
Cover Picture: Understanding of Molecular Substructures that Contribute to hERG K+ Channel Blockade: Synthesis and Biological Evaluation of E‐4031 Analogues (ChemMedChem 1/2012) (2012) (9)
A model for the hydrogen-bonding interactions between adenosine receptor ligands and histidyl residues in the adenosine A1 receptor binding site, based on AMI calculations (1991) (9)
A study of the dopamine transporter using the TRACT assay, a novel in vitro tool for solute carrier drug discovery (2021) (8)
Partial agonists for adenosine receptors (1996) (8)
Correlation between human ether‐a‐go‐go‐related gene channel inhibition and action potential prolongation (2017) (8)
Pharmacokinetic-pharmacodynamic modelling of the cardiovascular effects of R- and S-N6-phenylisopropyladenosine in conscious normotensive rats. (1995) (8)
LUF7244 plus Dofetilide Rescues Aberrant Kv11.1 Trafficking and Produces Functional IKv11.1 (2020) (8)
Synthesis and evaluation of N-substituted 2-amino-4,5-diarylpyrimidines as selective adenosine A1 receptor antagonists. (2017) (8)
Mapping the xanthine C8-region of the adenosine A1 receptor with computer graphics☆ (1991) (8)
Substituted 4‐Phenyl‐2‐(phenylcarboxamido)‐1,3‐thiazole Derivatives as Antagonists for the Adenosine A1 Receptor (2001) (8)
Partial agonism of the nonselective adenosine receptor agonist 8-butylaminoadenosine at the A1 receptor in vivo. (1996) (8)
5′‐AMP impacts lymphocyte recirculation through activation of A2B receptors (2013) (8)
1H-Imidazo(4,5-c)quinolin-4-amines: Novel Non-Xanthine Adenosine Antagonists. (1991) (8)
Site-directed mutagenesis studies of human A2A adenosine receptors (2000) (8)
Kinetic Profile of Neuropeptide–Receptor Interactions (2016) (7)
The mode of interaction of amiloride and some of its analogues with the adenosine A1 receptor (1992) (7)
Affinity and kinetics study of anthranilic acids as HCA2 receptor agonists. (2015) (7)
In vitro analysis of QSAR in wanted and unwanted effects of azacycloheptanones as transdermal penetration enhancers (1993) (7)
Synthesis and Pharmacological Evaluation of Triazolopyrimidinone Derivatives as Noncompetitive, Intracellular Antagonists for CC Chemokine Receptors 2 and 5 (2019) (7)
Adenosine-A1 receptors are not coupled to Ca2+ uptake in rat brain synaptosomes. (1989) (7)
Effects of the adenosine A1 receptor allosteric modulators PD 81,723 and LUF 5484 on the striatal acetylcholine release. (2002) (7)
Kinetics of human cannabinoid 1 (CB1) receptor antagonists: Structure‐kinetics relationships (SKR) and implications for insurmountable antagonism (2017) (7)
Population Pharmacokinetic Modeling of Blood-Brain Barrier Transport of Synthetic Adenosine A1 Receptor Agonists (2004) (7)
Computational Approaches to Fragment and Substructure Discovery and Evaluation (2008) (7)
Intrinsic activity at adenosine A1 receptors: partial and inverse agonism. (2002) (7)
The role of the C-terminus of the human hydroxycarboxylic acid receptors 2 and 3 in G protein activation using Gα-engineered yeast cells. (2016) (6)
Targeting the Kv11.1 (hERG) channel with allosteric modulators. Synthesis and biological evaluation of three novel series of LUF7346 derivatives. (2020) (6)
Temperature dependence of the affinity enhancement of selective adenosine A1 receptor agonism: a thermodynamic analysis. (2002) (6)
Stochastic multidimensional hypercubes and inverse agonism. (2000) (6)
Determination of dexmedetomidine in rat plasma by a sensitive [3H]clonidine radioreceptor assay. (1997) (6)
Importance of Drug–Target Residence Time at G Protein‐Coupled Receptors – a Case for the Adenosine Receptors (2015) (6)
Reliable Hierarchical Clustering with the Self-organizing Map (2005) (6)
Characterization of the pharmacokinetics, brain distribution, and therapeutic efficacy of the adenosine A1 receptor partial agonist 2'-deoxy-N6-cyclopentyladenosine in sarin-poisoned rats. (2003) (6)
G Protein‐Coupled Receptors of the Hypothalamic—Pituitary—Gonadal Axis: A Case for GnRH, LH, FSH, and GPR54 Receptor Ligands (2009) (6)
Rollover Cyclometalation vs Nitrogen Coordination in Tetrapyridyl Anticancer Gold(III) Complexes: Effect on Protein Interaction and Toxicity (2021) (6)
Molecular modelling of CCK-A receptors. (1994) (6)
The molecule evoluator: an interactive evolutionary algorithm for designing drug molecules (2005) (6)
Structure–Affinity Relationships and Structure–Kinetic Relationships of 1,2-Diarylimidazol-4-carboxamide Derivatives as Human Cannabinoid 1 Receptor Antagonists (2017) (6)
Population pharmacokinetic-pharmacodynamic modelling of the anti-hyperalgesic effect of 5'deoxy-N6-cylopentyladenosine in the mononeuropathic rat. (2004) (5)
Design and synthesis of novel small molecule CCR2 antagonists: evaluation of 4-aminopiperidine derivatives. (2014) (5)
Getting personal: Endogenous adenosine receptor signaling in lymphoblastoid cell lines. (2016) (5)
Allosteric modulation of G protein-coupled receptors. (2001) (5)
Ligand Binding and Subtype Selectivity of the Human A2A Adenosine Receptor (2010) (5)
The relation between ionization and affinity of beta-adrenoceptor ligands. (1984) (5)
Allosteric modulation and constitutive activity of fusion proteins between the adenosine A1 receptor and different 351Cys-mutated Gi alpha-subunits. (2004) (5)
Analyzing molecular landscapes using random walks and information theory (2009) (5)
Principles of agonism: undressing efficacy. (1998) (5)
Low efficacy adenosine A1 agonists inhibit striatal acetylcholine release in rats improving central selectivity of action (2003) (5)
TLR-Induced IL-12 and CCL2 Production by Myeloid Cells Is Dependent on Adenosine A3 Receptor–Mediated Signaling (2019) (5)
Characteristic amino acid combinations in olfactory G protein‐coupled receptors (2007) (5)
Evaluation of (4‐Arylpiperidin‐1‐yl)cyclopentanecarboxamides As High‐Affinity and Long‐Residence‐Time Antagonists for the CCR2 Receptor (2015) (4)
A Novel Class of Adenosine A3 Receptor Ligands. Part 2. Structure Affinity Profile of a Series of Isoquinoline and Quinazoline Compounds. (1999) (4)
Synthesis of 1,5-anhydro-2-(N-6-cyclopentyladenin-9-yl)-2-deoxy-d-altrohexitol (1995) (4)
Design and Characterization of an Intracellular Covalent Ligand for CC Chemokine Receptor 2 (2021) (4)
A Novel Class of Adenosine A3 Receptor Ligands. Part 1. 3‐(2‐Pyridinyl)isoquinoline Derivatives. (1999) (4)
Identification of V6.51L as a selectivity hotspot in stereoselective A2B adenosine receptor antagonist recognition (2021) (4)
[3H]batrachotoxinin-A 20-alpha-benzoate binding to sodium channels in rat brain: sensitivity to tetrodotoxin and divalent cations. (1988) (4)
Chemical modification of cholecystokinin-A receptors in rat pancreatic membranes. (1992) (4)
Regulation of Second Messenger Systems and Intracellular Pathways (2010) (4)
Effects of pyrazole partial agonists on HCA2‐mediated flushing and VLDL‐triglyceride levels in mice (2012) (4)
QUANTITATIVE EVALUATION OF THE β2-ADRENOCEPTOR AFFINITY OF PHENOXYPROPANOLAMINES AND PHENYLETHANOLAMINES (1985) (4)
Quantitative prediction of selectivity between the A1 and A2A adenosine receptors (2020) (4)
N‐Cycloalkyl Derivatives of Adenosine and 1‐Deazaadenosine as Agonists and Partial Agonists of the A1 Adenosine Receptor. (2000) (4)
Suramin analogs, divalent cations and ATP gamma S as inhibitors of ecto-ATPase. (1995) (4)
Pharmacokinetic-pharmacodynamic modelling of the anti-lipolytic effects of the adenosine A1-receptor agonist N6-(P-sulfophenyl)adenosine (SPA) in rats (1995) (4)
Impact of allosteric modulation: Exploring the binding kinetics of glutamate and other orthosteric ligands of the metabotropic glutamate receptor 2 (2018) (4)
Molecular modelling of asperlicin derived cholecystokinin A receptor antagonists. (1992) (4)
Label-free high-throughput screening assay for the identification of norepinephrine transporter (NET/SLC6A2) inhibitors (2021) (4)
Successive Statistical and Structure-Based Modeling to Identify Chemically Novel Kinase Inhibitors (2020) (3)
Oncological drug discovery: AI meets structure-based computational research. (2022) (3)
G protein-coupled receptors expressed and studied in yeast. The adenosine receptor as a prime example. (2020) (3)
Cyclopentyladenosine and some of its low-efficacy derivatives inhibit striatal synaptosomal release of acetylcholine to a similar degree. (2003) (3)
ZM 241385 , DPCPX , MRS 1706 Are Inverse Agonists with Different Relative Intrinsic Efficacies on Constitutively Active Mutants of the Human Adenosine A 2 B Receptor (2007) (3)
Molecular Basis of Ligand Dissociation from G Protein-Coupled Receptors and Predicting Residence Time. (2018) (3)
Molecular probes for the human adenosine receptors (2020) (3)
Adenosine receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database (2019) (3)
Ionization constants of sparingly soluble substances from aqueous titration data (1988) (3)
2‐Nitro Analogues of Adenosine and 1‐Deazaadenosine: Synthesis and Binding Studies at the Adenosine A1, A2A, and A3 Receptor Subtypes. (2000) (3)
Thermodynamic In Vitro Studies as a Method to Investigate the Pharmacodynamic Behavior of Adenosine A1 Receptor Ligands (1999) (3)
Limiting Solubilities and lonization Constants of Sparingly Soluble Compounds: Determination from Aqueous Potentiometric Titration Data Only (1988) (3)
Phenotypic screening of cannabinoid receptor 2 ligands shows different sensitivity to genotype (2017) (3)
Molecular Modeling of Adenosine A1 and A2a Receptors (1995) (3)
Quantitative Evaluation of the β2-Adrenoceptor Intrinsic Activity of N-tert-Butylphenylethanolamines. (1986) (3)
Synthesis of 3′-Fluoro-3′-deoxy-N6-cyclopentyladenosine (1994) (2)
Functional selectivity of adenosine A1 receptor ligands? (2012) (2)
Papyrus: a large-scale curated dataset aimed at bioactivity predictions (2021) (2)
Activation of G Protein-Coupled Receptors (2007) (2)
Annotation of Allosteric Compounds to Enhance Bioactivity Modeling for Class A GPCRs (2020) (2)
Structure—Activity Relationships of Inverse Agonists for G-Protein-Couplet Receptors (2005) (2)
Abstracts of papers Medicinal chemistry meeting (2005) (2)
Enantioselectivity in Drug-Receptor Interactions (2003) (2)
Multiple binding sites for small molecule antagonists at the chemokine receptor CCR2 (2014) (2)
The relationship between ionization and affinity of nucleoside transport inhibitors (1990) (2)
Synthesis and Use of FSCPX, an Irreversible Adenosine A1 Antagonist, as a “Receptor Knock‐Down” Tool. (2001) (2)
3′-Amidated 3′-Deoxyxylofuranose Analogues of N 6-−Cyclopentyladenosines: a New Class of Non-Xanthine Antagonists at the Adenosine A1 Receptor. (1998) (2)
Combining and Comparing Cluster Methods in a Receptor Database (2003) (2)
Three “hotspots” important for adenosine A2B receptor activation: a mutational analysis of transmembrane domains 4 and 5 and the second extracellular loop (2011) (2)
MPP+-Induced Changes in Cellular Impedance as a Measure for Organic Cation Transporter (SLC22A1-3) Activity and Inhibition (2022) (2)
Adenosine receptors in GtoPdb v.2021.2 (2021) (2)
Liquid chromatographic determination of the adenosine receptor agonist CGS 21680 in blood using on-line solid-phase extraction on a phenylboronic acid support and fluorescence detection. (1994) (1)
11 2 Evolutionary Algorithms in Drug Design (2010) (1)
Crystal structure of the chimeric protein of A2aAR-BRIL in complex with ZM241385 at 1.8A resolution (2012) (1)
Synthesis and biological evaluation of lorglumide‐like hybrid cholecystokinin‐A receptor antagonists (1994) (1)
Hydroxycarboxylic acid receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database (2019) (1)
A platform for assessing pro- and anti-arrhythmic effects of drugs based on isogenic human iPSC-derived cardiomyocytes (2019) (1)
Assessment of the enantiomeric purity of R- and S-N6-phenylisopropyladenosine (PIA): Implications for adenosine receptor subclassification (1994) (1)
Mapping the xanthine C8-region of the adenosine A1 receptor with computer graphics. (1991) (1)
Cancer-Related Somatic Mutations in Transmembrane Helices Alter Adenosine A1 Receptor Pharmacology (2022) (1)
Medicinal chemistry of the human adenosine A3 receptor (1998) (1)
Reduced hepatitis B and D viral entry using novel clinically-applied inhibitors of the sodium taurocholate co-transporting polypeptide (2017) (1)
The role of adenosine receptors in IL-6-dependent neuroprotection (2006) (1)
Molecular bioactivity extrapolation to novel targets by support vector machines (2010) (1)
Recognition of Adenosine Receptors by Amiloride and Its Analogues (1991) (1)
DrugEx v3: scaffold-constrained drug design with graph transformer-based reinforcement learning (2021) (1)
Abstract 11581: Longer Receptor Residence Times Improve the Effectiveness of CCR2 Antagonists in the Prevention of Atherosclerosis (2015) (1)
The antiarrhythmic properties of beta-adrenoceptor antagonists. (1989) (1)
Radioligand binding studies on the nucleoside transport protein. (1991) (1)
Lymphoblast-derived hiPS cell lines generated from four individuals of a family of genetically unrelated parents and their female monozygotic twins. (2019) (1)
Pan-cancer in silico analysis of somatic mutations in G-protein coupled receptors: The effect of evolutionary conservation and natural variance (2021) (1)
Cancer‐related somatic mutations alter adenosine A1 receptor pharmacology—A focus on mutations in the loops and C‐terminus (2022) (1)
Pharmacology of purinergic receptors: implications for drug design: Noordwijk, Netherlands 6–8 July 1990 (1990) (1)
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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