2D-structures of (A) co-crystallized ligands in the crystal structures (Figure 2) and (B) ligands shown in Table 1 or mentioned in the text. Most of the ligands in panel B are ordered according to their primary aminergic GPCR target: histamine receptors H1R (8, 11–20), H2R (8), H3R/H4R (8–10, 20–34), dopamine receptor D3R (35–41), muscarinic receptors M2R/M3R (42–49), beta-adrenergic receptors β1AR/β2AR (50–60), but it should be noted that many of the ligands bind to multiple aminergic GPCR subfamilies (e.g. 48, 61, 62, 63).