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. Author manuscript; available in PMC: 2019 Dec 28.
Published in final edited form as: Curr Top Med Chem. 2018;18(23):2002–2006. doi: 10.2174/1568026619999190101151837

Fig. 1.

Fig. 1.

GPCR-targeted orthosteric small molecules may exhibit disadvantages such as difficulty binding diffuse orthosteric sites with high affinity, unintended kinetic or physiological effects from exclusively occupying the orthosteric site, and off-target effects through poor selectivity between highly homologous receptor subtypes.