Evidence map›Paper›PMID 40271066›Full record

ArticleFrontiers in pharmacology2025

A universal cannabinoid CB1 and CB2 receptor TR-FRET kinetic ligand-binding assay.

Leire Borrega-Roman, Bradley L Hoare, Miroslav Kosar, Roman C Sarott, Kacper J Patej, Jara Bouma, Morgan Scott-Dennis, Eline J Koers, Thais Gazzi, Leonard Mach and 11 more

Abstract read
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In one paragraph

Article in Frontiers in pharmacology, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

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.

2 · The registry

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.

3 · Its place in the literature

Who cites it

1 citing paper in PubMed.

  1. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

21 authors.

Leire Borrega-RomanDivision of Physiology, Pharmacology & Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom.
Bradley L HoareDivision of Physiology, Pharmacology & Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom.
Miroslav KosarLaboratorium für Organische Chemie, Eidgenössische Technische Hochschule Zürich, Zürich, Switzerland.
Roman C SarottLaboratorium für Organische Chemie, Eidgenössische Technische Hochschule Zürich, Zürich, Switzerland.
Kacper J PatejLaboratorium für Organische Chemie, Eidgenössische Technische Hochschule Zürich, Zürich, Switzerland.
Jara BoumaDivision of Drug Discovery and Safety, Leiden Academic Center for Drug Research, Leiden University and Oncode Institute, Leiden, Netherlands.
Morgan Scott-DennisDivision of Physiology, Pharmacology & Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom.
Eline J KoersDivision of Physiology, Pharmacology & Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom.
Thais GazziLeibniz-Forschungsinstitut für Molekulare Pharmakologie FMP, Campus BerlinBuch, Berlin, Germany.
Leonard MachLeibniz-Forschungsinstitut für Molekulare Pharmakologie FMP, Campus BerlinBuch, Berlin, Germany.
Sergio BarrondoDepartment of Pharmacology, Faculty of Pharmacy, University of the Basque Country UPV/EHU, Vitoria-Gasteiz, Spain.
Joan SallésDepartment of Pharmacology, Faculty of Pharmacy, University of the Basque Country UPV/EHU, Vitoria-Gasteiz, Spain.
Wolfgang GubaRoche Pharma Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
Eric KusznirRoche Pharma Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
Marc NazaréLeibniz-Forschungsinstitut für Molekulare Pharmakologie FMP, Campus BerlinBuch, Berlin, Germany.
Arne C RuferRoche Pharma Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
Uwe GretherRoche Pharma Research and Early Development, Roche Innovation Center Basel, F. Hoffmann-La Roche Ltd., Basel, Switzerland.
Laura H HeitmanDivision of Drug Discovery and Safety, Leiden Academic Center for Drug Research, Leiden University and Oncode Institute, Leiden, Netherlands.
Erick M CarreiraLaboratorium für Organische Chemie, Eidgenössische Technische Hochschule Zürich, Zürich, Switzerland.
David A SykesDivision of Physiology, Pharmacology & Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom.
Dmitry B VeprintsevDivision of Physiology, Pharmacology & Neuroscience, School of Life Sciences, University of Nottingham, Nottingham, United Kingdom.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Introduction: The kinetics of ligand binding to G protein-coupled receptors (GPCRs) is an important optimization parameter in drug discovery. Traditional radioligand assays are labor-intensive, preventing their application at the early stages of drug discovery. Fluorescence-based assays offer several advantages, including a possibility to develop a homogeneous format, continuous data collection, and higher throughput. This study sought to develop a fluorescence-based binding assay to investigate ligand-binding kinetics at human cannabinoid type 1 and 2 receptors (CB1R and CB2R). Methods: We synthesized D77, a novel tracer derived from the non-selective cannabinoid Δ Results: The D77 tracer showed nanomolar-range affinity for truncated CB1R (CB1R Discussion: The

Indexed as

cannabinoid receptorscannabinoid type 1cannabinoid type 2fluorescent ligandkinetic ligand binding assayrebinding, ligand depletiontime-resolved Forster resonance energy transfer- based binding assay

Identifiers

PMID40271066
PMCPMC12015242

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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.