ReviewNature reviews. Drug discovery2025
The changing landscape of medicinal chemistry optimization.
Review in Nature reviews. Drug discovery, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
What it found
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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
14 citing papers in PubMed.
- Design, synthesis, and biological evaluation of tyrcinnamine derivatives as bactericides.Journal of enzyme inhibition and medicinal chemistry · 2026Article
- Multi-objective optimization in the context of generative chemistry.Nature communications · 2026Review
- Article
- Advancing Biochemical Molecule Registration, Representation and Search for New Drug Modalities.Journal of chemical information and modeling · 2026Article
- Discovery of Small Molecule Ligands Targeting Orphan G Protein-Coupled Receptors GPR3, GPR6, and GPR12.Journal of medicinal chemistry · 2026Review
- The expanding role of formulations to enable oral delivery of poorly water-soluble drugs.Nature reviews. Drug discovery · 2026Review
- More protein-ligand data are needed for AlphaFold-like models to enable drug discovery.Current opinion in structural biology · 2026Review
- Fragment-Based Design of Targeted Covalent Inhibitors: The Scope and Limitation of Linking Approaches.ChemMedChem · 2026Article
- Design, Synthesis and Biological Evaluation of Medicinal Potential Compounds.Molecules (Basel, Switzerland) · 2026Article
- Developments and challenges in hit progression within fragment-based drug discovery.Nature communications · 2026Review
- Therapeutic target database 2026: facilitating targeted therapies and precision medicine.Nucleic acids research · 2026Article
- TRAIL of Hope: Bioactive Dietary Component-Driven Carrier-Free Nanoplatforms for Synergistically Enhanced Tumor Multimodal Therapy.International journal of nanomedicine · 2026Review
- Phytochemical Profiling and Structure-Based Computational Characterization ofInternational journal of molecular sciences · 2025Article
- How many crystal structures do you need to trust your docking results?bioRxiv : the preprint server for biology · 2025Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The goal of a small-molecule drug discovery campaign is the development of chemical entities that fulfil the criteria of the target product profile for progression into clinical trials. This objective is realized through multiparameter medicinal chemistry optimization, typically by identifying the compounds at the hit stage with molecular properties that provide a high chance of subsequent success, and then iteratively optimizing the properties, often in parallel, to identify leads and, ultimately, drug candidates. To assess the impact of medicinal chemistry optimizations on molecular properties, a set of new drug candidates reported in the literature between 2015 and 2022, and their corresponding hit and lead compounds, were analysed, and compared with a set of drug candidates identified between 2000 and 2010, and their corresponding hits and leads. This analysis was complemented by similar analyses of the internal medicinal chemistry programmes pursued at AstraZeneca and Novartis. Here, we highlight and discuss the implications of the observed trends, which include shifts in key physicochemical properties and strategic changes in medicinal chemistry programmes.
Indexed as
Identifiers
40624317What 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.