ReviewCurrent opinion in chemical biology2010
Drug-target residence time: critical information for lead optimization.
Review in Current opinion in chemical biology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 182 papers.
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
182 citing papers in PubMed.
- Mutant-Selective Binding ofInternational journal of molecular sciences · 2026Article
- Identification of potential inhibitors of dengue virus ns5 methyltransferase and polymerase domains through virtual screening and molecular dynamics studies.Journal of molecular modeling · 2026Article
- Biophysical Sensing Tools in Drug Discovery: Integrating Kinetics, Thermodynamics, Cellular Target Engagement and Structure.Sensors (Basel, Switzerland) · 2026Review
- Altered residence time as a cause of drug resistance.Current opinion in structural biology · 2026Review
- A pothole-filling strategy for selective targeting of rCUG-repeats associated with myotonic dystrophy type 1.Proceedings of the National Academy of Sciences of the United States of America · 2026Article
- Article
- Exploiting the Cryptic αD Pocket of Casein Kinase 2α (CK2α) to Deliver Highly Potent and Selective Type 1 Inhibitors.Journal of medicinal chemistry · 2025Article
- Kinetic Modeling of Covalent Inhibition: Effects of Rapidly Fluctuating Intermediate States.Journal of chemical information and modeling · 2025Article
- Symmetric Ligand Binding Pathways and Dual-State Bottleneck in [NiFe] Hydrogenases from Unbiased Molecular Dynamics.The journal of physical chemistry letters · 2025Article
- Modulating the Binding Kinetics of Bruton's Tyrosine Kinase Inhibitors through Transition-State Effects.Journal of the American Chemical Society · 2025Article
- FAP inhibitors: are we really using the best method to evaluate the residence time?European journal of nuclear medicine and molecular imaging · 2025Article
- Is Mycobacterial InhA a Suitable Target for Rational Drug Design?ChemMedChem · 2025Review
- High-Throughput Ligand Dissociation Kinetics Predictions Using Site Identification by Ligand Competitive Saturation.Journal of chemical theory and computation · 2025Article
- Discovery of ATX968: An Orally Available Allosteric Inhibitor of DHX9.Journal of medicinal chemistry · 2025Article
- Human plasma protein bindings of neonicotinoid insecticides and metabolites.Scientific reports · 2025Article
- ModBind, a Rapid Simulation-Based Predictor of Ligand Binding and Off-Rates.Journal of chemical information and modeling · 2025Article
- Targeting chromosomally unstable tumors with a selective KIF18A inhibitor.Nature communications · 2025Article
- SRC is a potential target of Arctigenin in treating triple-negative breast cancer: based on machine learning algorithms, molecular modeling andFrontiers in molecular biosciences · 2025Article
- Advances and Challenges in Milestoning Simulations for Drug-Target Kinetics.Journal of chemical theory and computation · 2024Article
- Chemoselective Reagents for the Traceless Bioreversible Modification of Native Proteins.Bioconjugate chemistry · 2024Article
122 more citing papers are in PubMed but not listed here.
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
2 authors.
Funding
Abstract
Failure due to poor in vivo efficacy is a primary contributor to attrition during the development of new chemotherapeutics. Lead optimization programs that in their quest for efficacy focus solely on improving the affinity of drug-target binding are flawed, since this approach ignores the fluctuations in drug concentration that occur in vivo. Instead the lifetime of the drug-target complex must also be considered, since drugs only act when they are bound to their targets. Consequently, to improve the correlation between the in vitro and in vivo activity of drugs, measurements of drug-target residence time must be incorporated into the drug discovery process.
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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.