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Detailed information on affinity experiments is provided in the SI. In brief, competitive binding studies were determined on HEK293-hGLP-1R cells (1.50 × 105 cells in 1 mL/well) after incubation at 4 °C for 2 hours, using [125I]Tyr(3-I)40–3 (0.41 nM/well) as reference radioligand (n = 3). IC50 values of GLP-1 were determined in parallel on the same day to ensure assay validity. Only IC50 values of the new compounds, for which the IC50 of the corresponding GLP-1 control experiment lied in a range of 23.2 ± 12.2 nM (n = 11), were considered.
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