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. Author manuscript; available in PMC: 2018 Feb 19.
Published in final edited form as: Nat Rev Drug Discov. 2014 Jun 6;13(7):549–560. doi: 10.1038/nrd4295

Figure 1. Modes of targeting mAChRs (GPCRs) by different classes of ligands.

Figure 1

Orthosteric ligands (green) bind to the site recognized by the endogenous agonist (acetylcholine) for the receptor. Allosteric ligands (yellow) bind to a topographically distinct site. Bitopic ligands (blue) concomitantly interact with both orthosteric and allosteric sites. The key properties generally associated with each mode of receptor targeting are also indicated. GPCR, G protein-coupled receptor; mAChR, muscarinic acetylcholine receptor; SAR, structure–activity relationship.