ArticleACS medicinal chemistry letters2016
The Added Value of Assessing Ligand-Receptor Binding Kinetics in Drug Discovery.
Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed.
- Protein-ligand binding kinetics are primarily controlled by the protein, not the ligand.bioRxiv : the preprint server for biology · 2026Article
- A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand-binding assay.Frontiers in pharmacology · 2025Article
- Agonist efficacy at the βFrontiers in pharmacology · 2025Article
- Unraveling the Mechanism of Epichaperome Modulation by Zelavespib: Biochemical Insights on Target Occupancy and Extended Residence Time at the Site of Action.Biomedicines · 2023Article
- Adenosine AExperimental and therapeutic medicine · 2023Article
- International Union of Basic and Clinical Pharmacology. CXII: Adenosine Receptors: A Further Update.Pharmacological reviews · 2022Review
- Two for the Price of One: Heterobivalent Ligand Design Targeting Two Binding Sites on Voltage-Gated Sodium Channels Slows Ligand Dissociation and Enhances Potency.Journal of medicinal chemistry · 2020Article
- Detailed In Vitro Pharmacological Characterization of Clinically Tested Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5.Molecular pharmacology · 2020Article
- Rapid Quantification of Protein-Ligand Binding viaBiophysical journal · 2020Article
- On Calculating Free Energy Differences Using Ensembles of Transition Paths.Frontiers in molecular biosciences · 2020Article
- Pharmacokinetic-pharmacodynamic models that incorporate drug-target binding kinetics.Current opinion in chemical biology · 2019Review
- Mapping the Ligand Binding Landscape.Biophysical journal · 2018Article
- Drug-Target Kinetics in Drug Discovery.ACS chemical neuroscience · 2018Article
- Potent Prearranged Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor.ChemistryOpen · 2017Article
- Systematic Dissociation Pathway Searches Guided by Principal Component Modes.Journal of chemical theory and computation · 2017Article
Corrections and comments
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Authors and funding
3 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In the past decade drug research community has started to appreciate the indispensable role of ligand-receptor binding kinetics (BK) in drug discovery. Next to the classical equilibrium-based drug evaluation process with affinity and potency values as outcomes, kinetic investigation of the ligand-receptor interaction can aid compound triage in the hit-to-lead campaign and provide additional information to understand the molecular mechanism of drug action. Translational models incorporating BK are emerging as well, which represent powerful tools for the prediction of in vivo effects. In this viewpoint we will summarize some recent findings and discuss and emphasize the added value of ligand-receptor binding kinetics in drug research.
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Registered trials
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