. Author manuscript; available in PMC: 2024 Sep 20.

Published in final edited form as: J Am Chem Soc. 2023 Sep 11;145(37):20539–20550. doi: 10.1021/jacs.3c06703

Table 3.

GLP-1R cAMP Production and β-arrestin-1 and −2 Recruitment for GLP-1(7-36) and α/β/γ-Analogues 7 and 8.

	cAMP Production				β-arrestin-1 Recruitment				β-arrestin-2 Recruitment
Peptide	pEC₅₀	EC₅₀ (nM)	EC₅₀ relative	% Max	pEC₅₀	EC₅₀ (nM)	EC₅₀ relative	% Max	pEC₅₀	EC₅₀ (nM)	EC₅₀ relative	% Max
GLP-1(7-36)	10.0 ± 0.1	0.096	1	96 ± 4	7.6 ± 0.1	25	1	100 ± 2	7.5 ± 0.1	29	1	97 ± 6
7	10.2 ± 0.1	0.065	0.7	114 ± 5	7.3 ± 0.1	46	2	110 ± 7	7.8 ± 0.1	16	0.6	97 ± 6
8	9.5 ± 0.1	0.34	4	109 ± 3	6.2 ± 0.2	710	28	40^[#]	6.7 ± 0.2	220	8	61^[#]

For GLP-1R cAMP production, pEC₅₀, EC₅₀ and maximal response (% Max) values are derived from ≥3 independent experiments. For β-arrestin-1 and −2 recruitment to the GLP-1R, pEC₅₀, EC₅₀ and % Max represent ≥2 and ≥3 independent experiments, respectively. pEC₅₀ indicates the negative logarithm of the half-maximal effective concentration (EC₅₀). EC₅₀ relative indicates cAMP or β-arrestin recruitment potency normalized to GLP-1(7-36) by the quotient (α/β/γ-analogue/GLP-1(7-36)). pEC₅₀ and % Max uncertainties are expressed as SEM. Symbol ^[#] describes % Max measured at the highest concentration (1 μM) for 8 because the dose-response curve failed to reach saturation.