Table 1. Receptor Activation of N^α-Modified Peptides^a.

Peptideb	pEC50 ± SEMc	EC50 (pM)c	nd
GLP1R
GLP1	11.6 ± 0.1	2.5	3
1-GLP1e	10.0 ± 0.2	115.9	3
2-GLP1	11.5 ± 0.1	2.8	3
3-GLP1	11.2 ± 0.1	6.7	3
4-GLP1	11.4 ± 0.3	6.9	3
5-GLP1	11.4 ± 0.07	3.8	3
6-GLP1	12.0 ± 0.2	1.1	2
7-GLP1	11.3 ± 0.2	6.5	3
8-GLP1	10.8 ± 0.2	17.6	2
9-GLP1	11.7 ± 0.4	2.8	3
10-GLP1	11.4 ± 0.02	4.4	3
11-GLP1	11.6 ± 0.7	4.7	3
12-GLP1	11.6 ± 0.1	2.7	2
13-GLP1	11.3 ± 0.2	5.3	2
14-GLP1	10.6 ± 0.1	25.3	2
15-GLP1	11.4 ± 0.1	3.8	2
16-GLP1	11.0 ± 0.03	9.6	2
17-GLP1	10.4 ± 0.05	41.6	3
18-GLP1	11.1 ± 0.06	8.4	4
19-GLP1	7.5 ± 0.1	3.3 × 104	2
Liraglutide	11.6 ± 0.2	3.2	3
2-Liraglutide	11.4 ± 0.03	4.0	3
Exenatide	11.6 ± 0.02	2.6	3
2-Exenatide	11.6 ± 0.06	2.9	3
2-Triagonist(Ala2)	11.2	6.9	1
GIP	6.92	1.2 × 105	1
Glucagon	9.31	490	1
GIPR
GIP	12.2 ± 0.04	0.6	3
1-GIP	10.3 ± 0.2	54.6	2
2-GIP	12.6 ± 0.02	0.3	3
Glucagon	8.07	8.6 × 103	1
GLP1	8.30	5.0 × 103	1
2-Triagonist(Ala2)	11.5	3.3	1
GCGR
Glucagon	11.5 ± 0.04	3.4	5
2-Glucagon	11.6 ± 0.1	2.3	5
7-Glucagon	9.49 ± 0.1	325	2
GLP1	6.18	6.6 × 105	1
GIP	6.30	5.1 × 105	1
2-Triagonist(Ala2)	11.4	4.5	1
GLP2R
GLP2	10.7 ± 0.1	21	3
2-GLP2	11.2 ± 0.1	7	3

^aPotency of synthesized peptides using HEK293 cells expressing GLP1R, GIPR, GCGR, or GLP2R and luciferase reporter system. Results are separated by target receptors.

^bSee Figure 2 for peptide structures.

^cEC₅₀ is the concentration of peptide required for half-maximal activity of the targeted receptor. pEC₅₀ = −log(EC₅₀) ± standard error of the mean (SEM) of independent experiments where applicable.

^dNumber of independent experiments that were run in triplicate or quadruplicate.

^ePeptides were incubated at 37 °C overnight before stimulating transfected cells.