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. Author manuscript; available in PMC: 2015 Aug 13.
Published in final edited form as: J Biomol Screen. 2014 Feb 13;19(6):847–858. doi: 10.1177/1087057114520971

Figure 5.

Figure 5

Glucagon-like peptide 1 (GLP-1) receptor (GLP-1R) allosteric modulators potentiate intracellular calcium in GLP-1R cells, glucagon R cells, and cyclic adenosine monophosphate (cAMP) accumulation in GLP-1R insulinoma (INS-1) cells. Compounds were added in triplicate in an 11-point concentration-response curve prior to adding an 20% maximal effective concentration (EC20) concentration of either GLP-1 or glucagon. Concentration-response curves of compound hits are shown (A) in the presence of EC20 GLP-1 in the calcium assay using GLP-1R cells, (B) in the presence of EC20 glucagon in the calcium assay using glucagon R cells, and (C) in the presence of EC20 GLP-1 in the secondary GloSensor™ assay using GLP-1R INS-1 cells. A sigmoidal dose–response equation was fit to the data, and potencies and efficacies were calculated for comparison (D). All compounds classified as potentiators increase the calcium and cAMP signals, as reflected in the percentage of EMAX for the respective peptide and cells. Notably, VU0089276 exhibits the greatest increase at 93% and 70% for GLP-1R and glucagon R, respectively. Each compound was more efficacious for GLP-1R than glucagon R. Error bars represent ±SEM.