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. Author manuscript; available in PMC: 2022 Dec 28.
Published in final edited form as: Trends Pharmacol Sci. 2021 Feb 10;42(4):283–299. doi: 10.1016/j.tips.2020.12.005

Figure 2. Analysis of endogenous receptor-ligand interactions suggests the need to look beyond the orthosteric pocket to develop biased GPCR ligands.

Figure 2.

An analysis of non-odorant, rhodopsin family GPCRs was completed to determine inherent informational entropy. For each receptor family, the number of endogenous ligands was divided by the number of receptor variants to yield a “Ligands/Receptor” value indicative of informational entropy. The percent of total receptor families with a given Ligands/Receptor value is shown. Results were fit to a sum of gaussians, indicating that receptors analyzed fall into two main categories with different mean entropies. Mean ± SD for peak 1 and peak 2 are 0.97 ± 0.55 and 3.93 ± 1.6 ligands/receptor, respectively.