ArticleBioorganic & medicinal chemistry letters2012
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
Article in Bioorganic & medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 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
25 citing papers in PubMed.
- Discovery of VU6066098: A Selective and CNS-Penetrant mGluACS chemical neuroscience · 2026Article
- Glutamate Metabotropic Receptors-Linked Postsynaptic Density Proteins: An Emergent Hub for Antipsychotics' Regulation of Synaptic Plasticity and Metaplasticity.Biomolecules · 2026Review
- Acetylenic Replacement of Albicidin's Methacrylamide Residue Circumvents Detrimental E/Z Photoisomerization and Preserves Antibacterial Activity.Chemistry (Weinheim an der Bergstrasse, Germany) · 2021Article
- Allosteric Molecular Switches in Metabotropic Glutamate Receptors.ChemMedChem · 2021Review
- The mGluJournal of neural transmission (Vienna, Austria : 1996) · 2020Article
- Evaluation of Synthetic Cytochrome PACS omega · 2019Article
- Design and Synthesis ofACS medicinal chemistry letters · 2017Article
- Design and Synthesis of mGluACS medicinal chemistry letters · 2017Article
- Recent advances in the medicinal chemistry of group II and group III mGlu receptors.MedChemComm · 2017Review
- Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.Chemical reviews · 2016Review
- Design of 4-Oxo-1-aryl-1,4-dihydroquinoline-3-carboxamides as Selective Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 2.Journal of medicinal chemistry · 2015Article
- Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents.Journal of medicinal chemistry · 2015Article
- Further optimization of the mGlu5 PAM clinical candidate VU0409551/JNJ-46778212: Progress and challenges towards a back-up compound.Bioorganic & medicinal chemistry letters · 2015Article
- Positive allosteric modulators of metabotropic glutamate 2 receptors in schizophrenia treatment.Trends in neurosciences · 2015Review
- Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation.Molecular pharmacology · 2015Article
- Progress toward advanced understanding of metabotropic glutamate receptors: structure, signaling and therapeutic indications.Cellular signalling · 2014Review
- 2013 Philip S. Portoghese Medicinal Chemistry Lectureship: drug discovery targeting allosteric sites.Journal of medicinal chemistry · 2014Article
- Identification of specific ligand-receptor interactions that govern binding and cooperativity of diverse modulators to a common metabotropic glutamate receptor 5 allosteric site.ACS chemical neuroscience · 2014Article
- Drugs for allosteric sites on receptors.Annual review of pharmacology and toxicology · 2014Review
- Development of allosteric modulators of GPCRs for treatment of CNS disorders.Neurobiology of disease · 2014Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
15 authors.
Funding
Abstract
Herein we report the discovery and SAR of a novel metabotropic glutamate receptor 3 (mGlu(3)) NAM probe (ML289) with 15-fold selectivity versus mGlu(2). The mGlu(3) NAM was discovered via a 'molecular switch' from a closely related, potent mGlu(5) positive allosteric modulator (PAM), VU0092273. This NAM (VU0463597, ML289) displays an IC(50) value of 0.66 μM and is inactive against mGlu(5).
Indexed as
Identifiers
What 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.