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. 2021 Jan 19;4(1):296–313. doi: 10.1021/acsptsci.0c00193

Table 2. Quantification of Biased Agonism (ΔΔlog(τ/KA)) on GLP-1Ra.

ligand cAMP:β-arrestin 2 cAMP:calcium mobilization cAMP:internalization calcium mobilization:β-arrestin 2 calcium mobilization:internalization β-arrestin 2:internalization
GLP-1 0.00 ± 0.03 0.00 ± 0.05 0.00 ± 0.05 0.00 ± 0.06 0.00 ± 0.07 0.00 ± 0.05
GLP-1 Val8 0.10 ± 0.05 –0.14 ± 0.05 0.65 ± 0.04**** 0.24 ± 0.07 0.79 ± 0.06**** 0.55 ± 0.06****
a

ΔΔlog(τ/KA) values determined for GLP-1 and GLP-1 Val8 across different functional outcomes. Data represent the mean ± s.e.m. of 18 independent experiments performed in duplicate for cAMP production and β-arrestin 2 recruitment, 4 independent experiments in duplicate for calcium mobilization, and 6 independent experiments performed in duplicate and triplicate for internalization. Statistical significance was assessed using a repeated measures two-way ANOVA (****P < 0.0001; between GLP-1 and GLP-1 Val8).