A receptor modulator, or receptor ligand, is a general term for a substance, endogenous or exogenous, that binds to and regulates the activity of chemical receptors. They are ligands that can act on different parts of receptors and regulate activity in a positive, negative, or neutral direction with varying degrees of efficacy. Categories of these modulators include receptor agonists and receptor antagonists, as well as receptor partial agonists, inverse agonists, orthosteric modulators, and allosteric modulators, Examples of receptor modulators in modern medicine include CFTR modulators, selective androgen receptor modulators (SARMs), and muscarinic ACh receptor modulators.
- van Westen GJ, Gaulton A, Overington JP (April 2014). "Chemical, target, and bioactive properties of allosteric modulation". PLoS Computational Biology. 10 (4): e1003559. doi:10.1371/journal.pcbi.1003559. PMC 3974644. PMID 24699297.
- "CFTR Modulator Therapies". Cystic Fibrosis Foundation. Retrieved 2020-12-08.