. 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 3.

Binding parameters of CCK2R-based chimeric constructs expressed in CHO cells.

CCK2R-based chimeric receptors	Receptor abbreviations	GR134056X, IC₅₀ (nM)		GR135470X, IC₅₀ (nM)
CCK2R-based chimeric receptors	Receptor abbreviations	¹²⁵I-BDZ-2	¹²⁵I-CCK	¹²⁵I-BDZ-2	¹²⁵I-CCK
CCK2R WT	CCK2R	31.7 ± 8.6	46.3 ± 10.6	20.3 ± 5.3	48.6 ± 13.3
T2.61N	CCK2R TM2	NDB	188.0 ± 31.2^*	NDB	519.3 ± 138.2^*
V3.28T, S3.29T	CCK2R TM3	135.0 ± 12.5^**	51.0 ± 2.8	26.2 ± 5.4	10.1 ± 1.6^*
V6.51I, Y6.52F	CCK2R TM6	33.1 ± 2.6	68.3 ± 9.3	36.0 ± 5.5	164.7 ± 38.0^*
H7.39L	CCK2R TM7	6.3 ± 2.0^*	11.5 ± 2.7^*	14.4 ± 1.8	24.6 ± 6.4

p < 0.05,

^**

p < 0.001 values compared with wild type CCK2R using unpaired t-test; NDB - no detectable binding.