Receptors | Receptor Abbreviations | pIC50 | pEC50 | pKb | Log α |
---|---|---|---|---|---|
CCK1R WT | CCK1R | 8.10 ± 0.09 | 10.59 ± 0.11 | 8.20 ± 0.08 | −1.20 ± 0.10 |
CCK1R-Based Chimeric Receptorsa | |||||
N2.61T | CCK1R TM2 | 6.85 ± 0.04** | 9.70 ± 0.11** | 7.30 ± 0.11** | −0.50 ± 0.04** |
T3.28V, T3.29S | CCK1R TM3 | 9.13 ± 0.07** | 10.13 ± 0.09* | 9.14 ± 0.08** | (α is close to 0)** |
I6.51V, F6.52Y | CCK1R TM6 | 7.26 ± 0.04** | 10.12 ± 0.06* | 7.60 ± 01** | −0.64 ± 0.08** |
L7.39H | CCK1R TM7 | 6.33 ± 0.20** | 8.00 ± 0.10** | 7.24 ± 0.11** | −0.40 ± 0.05** |
CCK2R-Based Chimeric Receptorsb | |||||
CCK2R WT | CCK2R | 6.23 ± 0.13 | NR | 7.20 ± 0.17 | −0.36 ± 0.07 |
T2.61N | CCK2R TM2 | NDB | NR | NDB | NDB |
V3.28T, S3.29T | CCK2R TM3 | 5.94 ± 0.09 | NR | 7.06 ± 0.28 | −0.24 ± 0.08 |
V6.51I, Y6.52F | CCK2R TM6 | 7.03 ± 0.13** | <6.0 | 7.40 ± 0.12 | −0.61 ± 0.05* |
H7.39L | CCK2R TM7 | 8.03 ± 0.09** | <6.0 | 8.11 ± 0.08** | −1.11 ± 0.06** |
NDB, no detectable binding; NR, no response.
↵a Equilibrium binding was established using the CCK1R-selective small-molecule radioligand, 125I-BDZ-1.
↵b Equilibrium binding was established using the CCK2R-selective small-molecule radioligand, 125I-BDZ-2.
↵* P < 0.05; **P < 0.01, relative values compared with WT receptor.