Table 1. Equilibrium Dissociation Constants (pKd values) of the Fluorescent Y1R Ligand 1 Obtained from BRET Saturation Binding Experiments.
| compound | receptor (construct) | pKd (BRET)a | N |
|---|---|---|---|
| 1 | Nluc-Y1R(Nterm) | n.a. | – |
| Nluc-Y1R(Δ1–31) | 8.54 ± 0.05 | 3 | |
| Nluc-Y1R(Y192) | 9.62 ± 0.05 | 4 | |
| Nluc-Y1R(Q291) | 9.54 ± 0.07 | 4 |
Determined by BRET saturation binding experiments at intact HEK293T cells stably expressing the respective receptor construct. Data are shown as means ± SEM of N independent experiments performed in triplicate. n.a.: not applicable.