cAMP dose-response curves of (A) Sec-FL, (B) Sec(1–23), (C)
Sec(3–27) on SCTRs treated with DMSO or six increasing concentrations of
compounds (from left to right: A1, A2,
B1, B2, C4 and C9) ranging
from 0.8 to 25 μM; TR-FRET ratios converted to cAMP concentrations and
normalized to corresponding orthosteric ligand; allosteric activity parameters
KB, α and β were determined using the complete
operational model of allosterism in GraphPad Prism; experiments were performed
in duplicate in three independent experiments and data points are shown as mean
± SEM. For select compound concentrations only below error bars are shown
for illustrative purposes.