ArticleBioorganic & medicinal chemistry2009
Structure-based drug design identifies novel LPA3 antagonists.
Article in Bioorganic & medicinal chemistry, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 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.
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Who cites it
9 citing papers in PubMed.
- Multiple LPAInternational journal of molecular sciences · 2025Article
- Compensatory Upregulation of LPACells · 2022Article
- Review
- The LPAInternational journal of molecular sciences · 2021Review
- Lysophosphatidic acid acts on LPABritish journal of pharmacology · 2018Article
- Structural Characterization of an LPA1 Second Extracellular Loop Mimetic with a Self-Assembling Coiled-Coil Folding Constraint.International journal of molecular sciences · 2013Article
- Aiming drug discovery at lysophosphatidic acid targets.British journal of pharmacology · 2010Review
- Pharmacological tools for lysophospholipid GPCRs: development of agonists and antagonists for LPA and S1P receptors.Acta pharmacologica Sinica · 2010Review
- 2D binary QSAR modeling of LPA3 receptor antagonism.Journal of molecular graphics & modelling · 2010Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors.
Funding
Abstract
Compound 5 ([5-(3-nitrophenoxy)-1,3-dioxo-1,3-dihydro-2-isoindol-2-yl]acetic acid) was identified as a weak selective LPA(3) antagonist (IC(50)=4504 nM) in a virtual screening effort to optimize a dual LPA(2 and 3) antagonist. Structure-based drug design techniques were used to prioritize similarity search matches of compound 5. This strategy rapidly identified 10 novel antagonists. The two most efficacious compounds identified inhibit activation of the LPA(3) receptor by 200 nM LPA with IC(50) values of 752 nM and 2992 nM. These compounds additionally define changes to our previously reported pharmacophore that will improve its ability to identify more potent and selective LPA(3) receptor antagonists. The results of the combined computational and experimental screening are reported.
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Registered trials
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