Table 3.

Pharmacological properties of CaS receptor modulators at the naturally occurring G⁶⁷⁰E mutant receptor

	Cell surface expression (% WT)			Ca2+i mobilization
	0 modulator	0.3 μM	3 μM	pKB ± SEM (n)	Logαβ ± SEM (αβ)
Cinacalcet	12 ± 2	74 ± 12	152 ± 39	6.00 ± 0.19 (7)a	0.59 ± 0.06 (3.9)a
NPS-R568		33 ± 9	126 ± 37	6.61 ± 0.14 (4)	0.74 ± 0.14 (5.5)
Calindol		36 ± 7	112 ± 28	6.33 ± 0.31 (3)	0.53 ± 0.10 (3.4)
R,R-calcimimetic B		62 ± 11	152 ± 40	5.27 ± 0.37 (4)	0.51 ± 0.12 (3.2)
S,R-calcimimetic B		12 ± 3	14 ± 5	Not performed	Not performed
nor-calcimimetic B		28 ± 6	91 ± 27	6.21 ± 0.23 (3)	0.42 ± 0.06 (2.6)
AC-265347		14 ± 3	18 ± 5	6.62 ± 0.23 (3)	0.72 ± 0.10 (5.2)

Cell surface expression of the mutant following overnight treatment with modulator was determined by FACS analysis. The potency of Ca²⁺_o in Ca²⁺_i mobilization assays in the presence of increasing concentrations of modulator was fitted to an allosteric ternary complex model (Equation 2013a) to quantify the equilibrium dissociation constant (pK_B) and cooperativity (αβ) of the modulators at the G⁶⁷⁰E mutant.

^aDatasets taken from those used in (Leach et al., 2013).