ReviewNature reviews. Drug discovery2012
Finding the sweet spot: the role of nature and nurture in medicinal chemistry.
Review in Nature reviews. Drug discovery, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 125 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
125 citing papers in PubMed.
- Molecular Striptease of a Thiadiazolopyrimidine Hit Yields a Streamlined, Artifact-Free NADPH Mimic for NOX Inhibition.ACS medicinal chemistry letters · 2026Article
- Interpretable QSAR modelling for PPAR-γ agonist prediction by integrating a stacking strategy, docking, and MD simulations.Molecular diversity · 2026Article
- Multi-Target Neuroprotective Effects of Cordycepin and Adenosine fromBiomedicines · 2026Article
- Bioactive Natural and Synthetic Chalcones: Brazil as a Research Powerhouse in Discovery and Innovation.ChemMedChem · 2026Review
- Counteranion-mediated dynamic kinetic asymmetric fluorination to access sulfur-stereogenic center.Nature communications · 2026Article
- The Evolution of Machine Learning in Medicinal Chemistry: A Comprehensive Bibliometric Analysis.Current neuropharmacology · 2026Review
- The changing landscape of medicinal chemistry optimization.Nature reviews. Drug discovery · 2025Review
- Unraveling the therapeutic landscape of approved non-peptide macrocycles.Acta pharmaceutica Sinica. B · 2025Review
- Electrostatic Anchoring in RNA-Ligand Design─Dissecting the Effects of Positive Charges on Affinity, Selectivity, Binding Kinetics, and Thermodynamics.Journal of medicinal chemistry · 2025Article
- Skeletal Modification via Activation of Relatively Unstrained C-C Bonds.Accounts of chemical research · 2025Article
- Synthesis and in vitro antitrypanosomatid activity of novel 5-nitroindole-rhodanine conjugates.Future medicinal chemistry · 2025Article
- Rapid Affinity and Microsomal Stability Ranking of Crude Mixture Libraries of Histone Deacetylase Inhibitors.ACS medicinal chemistry letters · 2024Article
- Sol-moiety: Discovery of a water-soluble prodrug technology for enhanced oral bioavailability of insoluble therapeutics.Nature communications · 2024Article
- Pharmacoinformatic approach to identify potential phytochemicals against SARS-CoV-2 spike receptor-binding domain in native and variants of concern.Molecular diversity · 2023Article
- Towards Symmetric Thioamides: Microwave-Aided Synthesis of Terephthalic Acid Derivatives.Pharmaceuticals (Basel, Switzerland) · 2023Article
- The Chemical Space of Marine Antibacterials: Diphenyl Ethers, Benzophenones, Xanthones, and Anthraquinones.Molecules (Basel, Switzerland) · 2023Article
- The evolving role of investigative toxicology in the pharmaceutical industry.Nature reviews. Drug discovery · 2023Review
- Mining the Protein Data Bank to inspire fragment library design.Frontiers in chemistry · 2023Article
- Discovery of small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- The Time and Place for Nature in Drug Discovery.JACS Au · 2022Review
65 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
No grant is acknowledged in the PubMed record.
Abstract
Given its position at the heart of small-molecule drug discovery, medicinal chemistry has an important role in tackling the well-known productivity challenges in pharmaceutical research and development. In recent years, extensive analyses of successful and failed discovery compounds and drug candidates have improved our understanding of the role of physicochemical properties in drug attrition. Based on the clarified challenges in finding the 'sweet spot' in medicinal chemistry programmes, we suggest that this goal can be achieved through a combination of first identifying chemical starting points with appropriate 'nature' and then rigorously 'nurturing' them during lead optimization. Here, we discuss scientific, strategic, organizational and cultural considerations for medicinal chemistry practices, with the aim of promoting more effective use of what is already known, as well as a wider appreciation of the risks of pursuing suboptimal compounds.
Indexed as
Identifiers
22543468What 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.