. 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 4.

Binding and biological activity parameters of CCK, CE-326597 and PF-04756956 at CCK1R-based mutants derived from the best fitting models.

CCK1R- based chimeric receptors	Receptor abbreviations	CCK, pIC₅₀	CCK binding, B_max (pmol/mg)	CE-326597, pIC₅₀		PF-04756956, pIC₅₀		CCK, pEC₅₀	CE- 326597, pEC₅₀	PF- 04756956, pEC₅₀
CCK1R- based chimeric receptors	Receptor abbreviations	CCK, pIC₅₀	CCK binding, B_max (pmol/mg)	¹²⁵I- BDZ- 1	¹²⁵I-CCK	¹²⁵I- BDZ- 1	¹²⁵I- CCK	CCK, pEC₅₀	CE- 326597, pEC₅₀	PF- 04756956, pEC₅₀
CCK1R WT	CCK1R	8.93 ± 0.12	5.0 ± 1.0	6.29 ± 0.21	7.52 ± 0.04	>6.00	7.41 ± 0.10	10.66 ± 0.08	8.75 ± 0.08	9.38 ± 0.10
M3.32A	CCK1R M121A	7.78 ± 0.10^**	151 ± 63^**	7.82 ± 0.04^**	6.78 ± 0.09^**	>6.00	>6.00^**	9.89 ± 0.05^**	NR	NR
V3.36A	CCK1R V125A	9.86 ± 0.21^*	0.9 ± 0.4^*	6.10 ± 0.19	7.78 ± 0.04	6.02 ± 0.11	8.00 ± 0.16^*	10.32 ± 0.10^*	8.51 ± 0.03^**	8.48 ± 0.03^**
W6.48A	CCK1R W326A	9.33 ± 0.18	0.8 ± 0.2^*	6.57 ± 0.21	7.38 ± 0.07	7.21 ± 0.08^**	8.85 ± 0.05^**	10.36 ± 0.06^*	>7.00^**	8.30 ± 0.11^**

p < 0.05;

^**

p < 0.01 compared with wild type CCK1 receptor. NR, no detectable response.