Table 2.

Functional cooperativity (logαβ) estimates for the interactions between ACh and M₁ PAMs in IP₁ accumulation assays with or without pre-treatment with PBZ in CHO-hM₁ cells. The values were estimated by fitting the data to an operational model of allosterism (Eq. (3)), and represent the mean ± S.E.M. of at least four experiments performed in duplicate. The pK_B of each modulator was constrained to the values listed in Table 1. The β parameter was constrained to 1 to indicate lack of efficacy modulation. Logα β values were not significantly different between non-alkylated and alkylated experiments (p > 0.05, unpaired Student’s t-test, degree of freedom 6).

PAM	Logαβ (αβ)
	Non-alkylated	Alkylated with PBZ
BQCA	1.34 ± 0.10 (22)	1.79 ± 0.11 (62)
PF-06767832	1.92 ± 0.11 (83)	2.16 ± 0.11 (144)
VU6004256	1.78 ± 0.18 (60)	1.96 ± 0.22 (91)
MIPS1780	1.77 ± 0.14 (59)	2.07 ± 0.13 (117)