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. Author manuscript; available in PMC: 2016 May 1.
Published in final edited form as: Bioorg Med Chem Lett. 2015 Mar 24;25(9):1849–1855. doi: 10.1016/j.bmcl.2015.03.051

TABLE 2.

Binding parameters of CCK1R-based chimeric constructs expressed in CHO cells.

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.