The target groups currently included on the Guide to PHARMACOLOGY are:
* Catalytic receptors
* Enzymes
* G protein-coupled receptors
* Ion channels
* Kinases
* Nuclear receptors
* Transporters
* Other protein targets including fatty acid-binding proteins, sigma receptors and adiponectin receptors
Information for each target group is subdivided into families based on classification, with a separate data page for each family. Within each page, targets are arranged into lists of tables, with each table including the protein and gene nomenclature for the target with links to gene nomenclature databases, and listing selected ligands with activity at the target, including agonists, antagonists, inhibitors and radioligands. Pharmacological data and references are given and each ligand is hyperlinked to a ligand page displaying nomenclature and a chemical structure or peptide sequence, along with synonyms and relevant database links. The Guide to PHARMACOLOGY also includes a list of all ligand molecules included on the site, subdivided into categories including small organic molecules (including mammalian metabolites, hormones and neurotransmitters), synthetic organic molecules, natural products, peptides, inorganic molecules and antibodies. A complete list of all the approved drugs included on the website is also available via the ligand list. The Guide to PHARMACOLOGY is being expanded to include clinical information on targets and ligands, in addition to educational resources. 
Search features on the website include quick and advanced search options, and receptor and ligand searches, including support for ligand structures using chemical structures. Other features include Hot topic news items and a recent receptor-ligand pairing list.