Ternary complex model binding parameters for various allosteric modulators against [3H]NMS at human M2 mAChRs expressed in intact CHO cells
Modulator | log KBa | log αb |
|---|---|---|
| Gallamine | −5.70 ± 0.04 | −1.30 ± 0.12 |
| (0.05) | ||
| Alcuronium | −6.10 ± 0.07 | 0.23 ± 0.07 |
| (1.7) | ||
| C7/3-phth | −5.70 ± 0.23 | −1.02 ± 0.06 |
|
|
| (0.1) |
↵ a Logarithm of the equilibrium dissociation constant for the allosteric modulator at the free receptor, determined from a nonequilibrium binding assay using nonlinear regression according to eqs. 6 through 9 under Materials and Methods. Values represent the mean ± standard error of the mean of three experiments conducted in triplicate.
↵ b Logarithm of the cooperativity factor. Antilogarithm (geometric mean) is given in parentheses. All other details as in footnote a.