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. Author manuscript; available in PMC: 2024 Jun 7.
Published in final edited form as: J Am Chem Soc. 2023 May 26;145(22):12105–12114. doi: 10.1021/jacs.3c01628

Table 3.

GLP-1R activation and nLuc-GLP-1R affinity for GLE and analogues.

GLP-1R cAMP Production nLuc-GLP-1R Affinity
Peptide EC50 (nM) EC50 relative % Max IC50 (nM) IC50 relative
GLE 5.1 1 95 ± 2 290 1
GLE L-Ala >1000 >200 NR 390 1
GLE D-Ala 21 4 21 ± 2 250 0.9
GLE (S,S)-ACPC >1000 >200 NR 15 0.05
GLE (R,R)-ACPC >1000 >200 NR 160 0.6
GLE β-hGly >1000 >200 NR 120 0.4

EC50 and maximal response (% Max) values were derived from ≥4 independent experiments. EC50 relative indicates potency normalized to GLE (GLE analogue/GLE). For nLuc-GLP-1R competition binding experiments, IC50 values represent the average of 4 independent experiments. IC50 relative indicates affinity normalized to GLE (GLE analogue/GLE). NR = No Response.