ArticleJournal of medicinal chemistry2016
Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s).
Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 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
24 citing papers in PubMed, 60 citations in OpenAlex.
- Charge Transfer-Induced Complexation of Urea Confined Within 1,4-Dimethoxypillar[5]arene.ChemPlusChem · 2026Article
- Development of Squaramides as Allosteric Modulators of the CBJournal of medicinal chemistry · 2025Article
- Specific pupylation as IDEntity reporter (SPIDER) for the identification of protein-biomolecule interactions.Science China. Life sciences · 2023Article
- Covalent cannabinoid receptor ligands - structural insight and selectivity challenges.RSC medicinal chemistry · 2022Review
- Covalent allosteric modulation: An emerging strategy for GPCRs drug discovery.European journal of medicinal chemistry · 2020Review
- Impact of Allosteric Modulation in Drug Discovery: Innovation in Emerging Chemical Modalities.ACS medicinal chemistry letters · 2020Article
- Structure of an allosteric modulator bound to the CB1 cannabinoid receptor.Nature chemical biology · 2019Article
- Allosteric Modulation of Cannabinoid Receptor 1-Current Challenges and Future Opportunities.International journal of molecular sciences · 2019Review
- Identification of CB1 Receptor Allosteric Sites Using Force-Biased MMC Simulated Annealing and Validation by Structure-Activity Relationship Studies.ACS medicinal chemistry letters · 2019Article
- Translational potential of allosteric modulators targeting the cannabinoid CBActa pharmacologica Sinica · 2019Review
- Allosteric Modulation of Class A GPCRs: Targets, Agents, and Emerging Concepts.Journal of medicinal chemistry · 2019Review
- Allosteric modulators of cannabinoid receptor 1: developing compounds for improved specificity.Drug metabolism reviews · 2018Review
- Preclinical Studies of Cannabinoid Reward, Treatments for Cannabis Use Disorder, and Addiction-Related Effects of Cannabinoid Exposure.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2018Review
- Cannabinoid Receptor 1 Positive Allosteric Modulators for Posttraumatic Stress Disorder.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2018Article
- Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.Bioorganic & medicinal chemistry · 2017Article
- The great divide: Separation between in vitro and in vivo effects of PSNCBAM-based CBNeuropharmacology · 2017Article
- Enantiospecific Allosteric Modulation of Cannabinoid 1 Receptor.ACS chemical neuroscience · 2017Article
- Microwave-accelerated conjugate addition of 2-arylindoles to substituted β-nitrostyrenes in the presence of ammonium trifluoroacetate: an efficient approach for the synthesis of a novel class of CB1 cannabinoid receptor allosteric modulators.Journal of heterocyclic chemistry · 2017Article
- Allosteric Modulation: An Alternate Approach Targeting the Cannabinoid CB1 Receptor.Medicinal research reviews · 2017Review
- Functional selectivity at G-protein coupled receptors: Advancing cannabinoid receptors as drug targets.Biochemical pharmacology · 2017Review
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 4 countries.
Funding
Abstract
Undesirable side effects associated with orthosteric agonists/antagonists of cannabinoid 1 receptor (CB1R), a tractable target for treating several pathologies affecting humans, have greatly limited their translational potential. Recent discovery of CB1R negative allosteric modulators (NAMs) has renewed interest in CB1R by offering a potentially safer therapeutic avenue. To elucidate the CB1R allosteric binding motif and thereby facilitate rational drug discovery, we report the synthesis and biochemical characterization of first covalent ligands designed to bind irreversibly to the CB1R allosteric site. Either an electrophilic or a photoactivatable group was introduced at key positions of two classical CB1R NAMs: Org27569 (1) and PSNCBAM-1 (2). Among these, 20 (GAT100) emerged as the most potent NAM in functional assays, did not exhibit inverse agonism, and behaved as a robust positive allosteric modulator of binding of orthosteric agonist CP55,940. This novel covalent probe can serve as a useful tool for characterizing CB1R allosteric ligand-binding motifs.
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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.