ReviewNature reviews. Drug discovery2009
Cellular assays as portals to seven-transmembrane receptor-based drug discovery.
Review in Nature reviews. Drug discovery, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 55 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
55 citing papers in PubMed.
- A label-free cell-based screening identifies enhydrin as a novel natural antagonist of the histamine H1 receptor.Molecular diversity · 2026Article
- Know your molecule: pharmacological characterization of drug candidates to enhance efficacy and reduce late-stage attrition.Nature reviews. Drug discovery · 2024Review
- Probing Activation and Conformational Dynamics of the Vesicle-Reconstituted βThe journal of physical chemistry. B · 2024Article
- Comparative Saturation Binding Analysis ofACS omega · 2023Article
- Investigating the ligand agonism and antagonism at the DScientific reports · 2022Article
- Receptor-Receptor Interactions and Glial Cell Functions with a Special Focus on G Protein-Coupled Receptors.International journal of molecular sciences · 2021Review
- Receptor-Receptor Interactions as a Widespread Phenomenon: Novel Targets for Drug Development?Frontiers in endocrinology · 2019Review
- Characterisation of small molecule ligands 4CMTB and 2CTAP as modulators of human FFA2 receptor signalling.Scientific reports · 2018Article
- Lack of beta-arrestin signaling in the absence of active G proteins.Nature communications · 2018Article
- Distinct Signaling Patterns of Allosteric Antagonism at the P2YMolecular pharmacology · 2017Article
- On the different experimental manifestations of two-state 'induced-fit' binding of drugs to their cellular targets.British journal of pharmacology · 2016Review
- Review
- A High-Throughput Drug Screening Strategy for Detecting Rhodopsin P23H Mutant Rescue and Degradation.Investigative ophthalmology & visual science · 2015Article
- Discovery and Development of Small Molecule Allosteric Modulators of Glycoprotein Hormone Receptors.Frontiers in endocrinology · 2015Review
- Receptor, Ligand and Transducer Contributions to Dopamine D2 Receptor Functional Selectivity.PloS one · 2015Article
- Label-free cell phenotypic profiling decodes the composition and signaling of an endogenous ATP-sensitive potassium channel.Scientific reports · 2014Article
- Divergent label-free cell phenotypic pharmacology of ligands at the overexpressed β₂-adrenergic receptors.Scientific reports · 2014Article
- Label-free drug discovery.Frontiers in pharmacology · 2014Review
- Decoding signaling and function of the orphan G protein-coupled receptor GPR17 with a small-molecule agonist.Science signaling · 2013Article
- Regulation of G protein subunit composition in cardiomyocytes: pharmacological implications.Naunyn-Schmiedeberg's archives of pharmacology · 2013Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
1 author.
Funding
No grant is acknowledged in the PubMed record.
Abstract
As technology advances to the point at which various behaviours of seven-transmembrane (7TM) receptors (also known as G protein-coupled receptors (GPCRs)) can be observed individually, it is clear that, rather than being 'on-off' switches, 7TM receptors are more akin to 'microprocessors' of information. This has introduced the phenomenon of functional selectivity, whereby certain ligands initiate only portions of the signalling mechanisms mediated by a given receptor, which has opened new horizons for drug discovery. The need to discover new 7TM receptor-ligand behaviours and quantify the effect of the drug on these complex systems, to guide medicinal chemistry, puts the pharmacological assay into the spotlight. This Perspective outlines the return to whole-system assays from reductionist recombinant systems, and discusses how the efficacy of a drug is linked to the particular assay used to observe its effects. It also highlights how these new assays are adding value to the drug discovery process.
Indexed as
Identifiers
19609267What 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.