TABLE 2.
CCK1R-based chimeric receptors |
Receptor Abbreviations |
GR134056X, IC50 (nM) | GR135470X, IC50 (nM) | ||
---|---|---|---|---|---|
125I-BDZ-1 | 125I-CCK | 125I-BDZ-1 | 125I-CCK | ||
CCK1R WT | CCK1R | NDB | 541.0 ± 139.2 | NDB | 450.0 ± 104.1 |
N2.61T | CCK1R TM2 | NDB | 128.0 ± 13.3* | 875.0 ± 296.2 | 40.3 ± 5.7* |
T3.28V, T3.29S | CCK1R TM3 | 259.0 ± 60.0* | 1000 ± 115.5 | 50.2 ± 6.6* | 333.6 ± 33.1 |
I6.51V, F6.52Y | CCK1R TM6 | >1000 | 316.7 ± 60.0 | >1000 | 151.0 ± 26.8* |
L7.39H | CCK1R TM7 | 505.3 ± 97.4* | 303.3 ± 3.3 | 233.3 ± 66.6* | 153.3 ± 3.3* |
p < 0.05 values compared with wild type CCK1R; NDB - no detectable binding.