druggable

Druggable describes the likelihood that a biological target can be modulated by a drug to achieve a therapeutic effect with acceptable safety. In pharmacology and drug discovery, druggability assesses whether a target such as a protein or nucleic acid can be modulated with a medicinal agent, and whether such modulation can be accomplished with desirable potency, selectivity, and pharmacokinetic properties.

Druggability depends on features of the target and its biology: the presence of a binding site of suitable size and chemical characteristics; the target's role in disease; the ability to reach the site in the body; and the feasibility of achieving sufficient potency without unacceptable toxicity. Small molecules and biologics represent two broad modalities, with small molecules typically targeting enzymes, receptors, ion channels, and transporters, while antibodies and other biologics often target extracellular or cell-surface components.

Common druggable classes include G protein-coupled receptors, tyrosine kinase receptors, other kinases, ion channels, transporters, and proteases. Some targets historically considered undruggable, such as certain transcription factors and intracellular protein–protein interactions, are becoming more tractable thanks to new approaches like biologics, targeted protein degradation, and nucleic acid therapies. Despite advances, many targets remain challenging due to issues such as specificity, off-target effects, or poor pharmacokinetics.

In research and industry, druggability is evaluated early to prioritize targets. Assessments combine structural information, biological validation, and in silico predictions with experimental assays to gauge whether a target can be modulated safely and effectively by a drug.