ReviewMolecular and cellular endocrinology2019
Binding kinetics of ligands acting at GPCRs.
Review in Molecular and cellular endocrinology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 48 papers, 1 of them a synthesis that pooled it.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
48 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Synergistic, multi-level understanding of psychedelics: three systematic reviews and meta-analyses of their pharmacology, neuroimaging and phenomenology.Translational psychiatry · 2024Pooled it
- VEGFR2 dimerization kinetics on the cell surface determined by microscopy and mathematical modeling.Biophysical journal · 2026Article
- On the structural identifiability of nonlinear models of ligand binding dynamics.Journal of pharmacokinetics and pharmacodynamics · 2026Article
- Graph neural network modeling of receptor interaction kinetics from single-molecule imaging data.bioRxiv : the preprint server for biology · 2026Article
- Binding affinities for histamine receptors 1 to 4: Systematic comparison of ligands from the Psychoactive Drug Screening Program KMolecular pharmacology · 2026Review
- Accelerating GPCR drug discovery through computation and experiment integrated with direct detection of ligand binding events.npj drug discovery · 2026Review
- Modulation of Aging Diseases via RAGE Targets: A Dietary Intervention Review.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Review
- Residence time in drug discovery: current insights and future perspectives.Pharmacological reports : PR · 2025Review
- Ligand binding kinetics to evaluate the function and stability of ABiophysical journal · 2025Article
- A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand-binding assay.Frontiers in pharmacology · 2025Article
- Redefining Roles: A Paradigm Shift in Tryptophan-Kynurenine Metabolism for Innovative Clinical Applications.International journal of molecular sciences · 2024Review
- IS4-FAM, a fluorescent tool to study CXCR4 affinity and competitive antagonism in native cancer cells.Pharmacology research & perspectives · 2024Article
- Collagen-targeted protein nanomicelles for the imaging of non-alcoholic steatohepatitis.Acta biomaterialia · 2024Article
- Highly Selective Drug-Derived Fluorescent Probes for the Cannabinoid Receptor Type 1 (CBJournal of medicinal chemistry · 2024Article
- Discovery of a brain penetrant small molecule antagonist targeting LPA1 receptors to reduce neuroinflammation and promote remyelination in multiple sclerosis.Scientific reports · 2024Article
- Subtle Structural Modification of a Synthetic Cannabinoid Receptor Agonist Drastically Increases its Efficacy at the CB1 Receptor.ACS chemical neuroscience · 2023Article
- Comparative Saturation Binding Analysis ofACS omega · 2023Article
- Novel Cannabinoid Receptor 2 (CB2) Low Lipophilicity Agonists Produce Distinct cAMP and Arrestin Signalling Kinetics without Bias.International journal of molecular sciences · 2023Article
- A Single Point Mutation Blocks the Entrance of Ligands to the Cannabinoid CBJournal of chemical information and modeling · 2022Article
- Discovery and Structure-Activity Relationship Studies of Novel Adenosine AJournal of medicinal chemistry · 2022Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors.
Funding
Abstract
The influence of drug-receptor binding kinetics has often been overlooked during the development of new therapeutics that target G protein-coupled receptors (GPCRs). Over the last decade there has been a growing understanding that an in-depth knowledge of binding kinetics at GPCRs is required to successfully target this class of proteins. Ligand binding to a GPCR is often not a simple single step process with ligand freely diffusing in solution. This review will discuss the experiments and equations that are commonly used to measure binding kinetics and how factors such as allosteric regulation, rebinding and ligand interaction with the plasma membrane may influence these measurements. We will then consider the molecular characteristics of a ligand and if these can be linked to association and dissociation rates.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.