. Author manuscript; available in PMC: 2016 Mar 14.

Published in final edited form as: J Med Chem. 2015 Dec 10;58(24):9562–9577. doi: 10.1021/acs.jmedchem.5b01110

Table 3.

Binding parameters of CE-326597 and PF-04756956 at CCK1R- or CCK2R-based chimeric receptor constructs.

CCK1R-based chimeric receptors	Receptor abbreviations	CE-326597, pIC₅₀		PF-04756956, pIC₅₀
CCK1R-based chimeric receptors	Receptor abbreviations	¹²⁵I-BDZ-1	¹²⁵I-CCK	¹²⁵I-BDZ-1	¹²⁵I-CCK
CCK1R WT	CCK1R	6.21 ± 0.14	7.65 ± 0.04	>6.00	7.56 ± 0.08
N2.61T	CCK1R TM2	7.03 ± 0.10^**	8.70 ± 0.12^**	6.98 ± 0.18^**	9.09 ± 0.14^**
T3.28V, T3.29S	CCK1R TM3	8.35 ± 0.08^**	7.43 ± 0.05	8.14 ± 0.08^**	7.37 ± 0.03
I6.51V, F6.52Y	CCK1R TM6	6.00 ± 0.10	7.37 ± 0.12	6.00 ± 0.18	7.15 ± 0.10
L7.39H	CCK1R TM7	>6.00^*	6.17 ± 0.12^**	>6.00^*	6.10 ± 0.10^**
CCK2R-based chimeric receptors	Receptor abbreviations	CE-326597, pIC₅₀		PF-04756956, pIC₅₀
CCK2R-based chimeric receptors	Receptor abbreviations	¹²⁵I-BDZ-2	¹²⁵I-CCK	¹²⁵I-BDZ-2	¹²⁵I-CCK
CCK2R WT	CCK2R	6.85 ± 0.13	6.56 ± 0.22	>6.00	6.16 ± 0.14
T2.61N	CCK2R TM2	NDB	>6.00^**	NDB	>6.00^**
V3.28T, S3.29T	CCK2R TM3	>6.00^*	6.68 ± 0.26	>6.00^*	6.52 ± 0.17
V6.51I, Y6.52F	CCK2R TM6	>6.00	>6.00	>6.00	>6.00
H7.39L	CCK2R TM7	8.70 ± 0.21^**	8.77 ± 0.19^**	8.00 ± 0.11^**	8.12 ± 0.21^**

p < 0.05;

^**

p < 0.01 compared with wild type CCK receptor. NDB no detectable binding.