Related Experiment Video
Updated: Jul 2, 2026
08:21
Monitoring GPCR-β-arrestin1/2 Interactions in Real Time Living Systems to Accelerate Drug Discovery
Published on: June 28, 2019
An online GPCR drug discovery resource
Jimmy Caroli1, Søren N Andreassen1, Javier Sánchez Lorente1
1Department of Drug Design and Pharmacology, University of Copenhagen, Universitetsparken 2, 2100, Copenhagen, Denmark.
Npj Drug Discovery
|July 1, 2026
Summary
This study introduces GPCRdb, an online resource detailing G protein-coupled receptor (GPCR) drugs and clinical trial agents. It aids in identifying trends and prioritizing GPCR targets for future drug discovery efforts.
Area of Science:
- Pharmacology
- Biotechnology
- Drug Discovery
Background:
- G protein-coupled receptors (GPCRs) are crucial drug targets, involved in 516 approved drugs and 337 agents in clinical trials.
- Currently, 121 GPCRs are targeted by approved drugs, with 30 more in clinical trials, indicating a growing 'drugged GPCRome'.
Purpose of the Study:
- To present a comprehensive online resource for GPCR drugs, clinical trial agents, targets, and associated disease indications.
- To provide tools for analyzing GPCR drug discovery trends and prioritizing potential therapeutic targets.
Main Methods:
- Integration of a new 'Drugs and Agents in trial' section into the existing GPCR database, GPCRdb.
- Development of a target selection tool for prioritizing GPCRs in drug discovery.
Main Results:
- GPCRdb now offers curated data on GPCR-targeted drugs and clinical trial agents.
- The resource includes analysis, visualization, and a tool for receptor prioritization.
Conclusions:
- The updated GPCRdb serves as a valuable knowledge base for understanding GPCR drug discovery.
- It offers insights into current strategies, trends, and the therapeutic potential of both drugged and untapped GPCR targets for specific diseases.
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