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G Protein-coupled Receptors01:15

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G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
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The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
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Drug Discovery: Overview01:26

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Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
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Updated: Jan 7, 2026

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The Concise Guide to PHARMACOLOGY 2025/26: Catalytic receptors.

Stephen P H Alexander1, Doriano Fabbro2, Chloe J Peach3

  • 1Division of Physiology, Pharmacology & Neuroscience, School of Life Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK.

British Journal of Pharmacology
|December 29, 2025
PubMed
Summary
This summary is machine-generated.

The Concise Guide to Pharmacology 2025/26 offers a comprehensive overview of human drug targets and their interactions. This biennial publication provides expert-curated recommendations for pharmacological tools, serving as a stable, citable record.

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Area of Science:

  • Pharmacology
  • Drug Discovery
  • Biomedical Sciences

Background:

  • The British Journal of Pharmacology publishes the biennial Concise Guide to Pharmacology.
  • This guide provides a comparative overview of drug target families' pharmacology.
  • The 2025/26 edition is the seventh in this series.

Purpose of the Study:

  • To provide a clear, accessible, and well-structured summary of human drug targets and their interactions.
  • To offer expert-curated recommendations for selective pharmacological tools.
  • To serve as a permanent, citable, point-in-time record of pharmacological information.

Main Methods:

  • Summarization of key pharmacological properties for approximately 1900 human drug targets.
  • Inclusion of nearly 7000 interactions involving around 4400 ligands.
  • Expert curation of 'Gold Standard' selective pharmacological tools.

Main Results:

  • The guide covers six major pharmacological target families: catalytic receptors, G protein-coupled receptors, ion channels, nuclear hormone receptors, enzymes, and transporters.
  • It includes nomenclature guidance, concise summaries, and information on available pharmacological tools.
  • Content is based on material current as of mid-2025.

Conclusions:

  • The Concise Guide to Pharmacology 2025/26 supersedes all previous editions.
  • It provides official IUPHAR classification and nomenclature for human drug targets.
  • The guide complements the comprehensive online database at www.guidetopharmacology.org.