ArticleJournal of medicinal chemistry2025
Comparative Profiling and Chemogenomics Application of Chemical Tools for NR4A Nuclear Receptors.
Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
What it found
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Who cites it
4 citing papers in PubMed.
- Development of a Brain-Penetrant Nurr1 Agonist Tool.ChemMedChem · 2026Article
- Structural Tuning of Vidofludimus for High-Efficacy NR4A Agonism.Journal of medicinal chemistry · 2026Article
- Systematic Optimization of Fragment TLX Ligands toward Agonism and Inverse Agonism.Journal of medicinal chemistry · 2026Article
- A Commentary on Dual Orphan Nuclear Receptor 4A1 (NR4A1) and NR4A2 Ligands.Journal of cellular immunology · 2026Article
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Authors and funding
4 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The ligand-activated transcription factors of the NR4A family are implicated as promising drug targets with neuroprotective and anticancer potential and attract strong attention in drug discovery. Several NR4A modulators have been described, but a validated set of direct ligands for biological studies is lacking. Here, we profiled the reported and commercially available agonists and inverse agonists under uniform conditions in several orthogonal test systems to establish a highly annotated tool and gain comprehensive insights into the NR4A modulator characteristics. This comparative profiling revealed a lack of on-target binding and modulation for several putative NR4A ligands and validated a set of chemically diverse compounds as direct NR4A modulators for chemogenomics-based target identification studies. Prospective applications unveiled roles of NR4A receptors in endoplasmic reticulum stress and adipocyte differentiation, demonstrating suitability of the set to link the orphan targets with phenotypic effects.
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Registered trials
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