TABLE 3.
Functional affinity (pKB) and efficacy (logτB) parameters for NPS R568 and AC265347 determined in Ca2+i mobilization assays in the absence of ambient divalent cations
Data are mean ± S.E.M. and 95% confidence intervals from the indicated number of independent experiments (n).
| NPS R568 |
AC265347 |
|||||
|---|---|---|---|---|---|---|
| pKB (95% CI) | LogτB (95% CI) (τB) | n | pKB (95% CI) | LogτB (95% CI) (τB) | n | |
| WT | ND | ND | 8 | 5.43 ± 0.10a (5.23–5.63) | 0.05 ± 0.10 (0.01–0.11) (1.1) | 8 |
| G670ECL1A | 5.71 ± 0.18a (5.28–6.13) | −0.19 ± 0.04 (−0.27 to −0.11) (0.6) | 7 | 6.13 ± 0.08b (5.96–6.31) | 0.07 ± 0.03 (0.04–0.11) (1.2) | 7 |
| E8377.32D | ND | ND | 8 | 5.90 ± 0.14a,b (5.60–6.19) | −0.03 ± 0.03 (−0.10 to 0.03) (0.9) | 8 |
| A8407.35V | ND | ND | 7 | ND | ND | 7 |
| A8447.39V | 6.48 ± 0.32 (5.78–7.21) | −0.27 ± 0.06 (−0.42 to −0.17) (0.5) | 6 | 6.89 ± 0.20b (6.51–7.31) | −0.16 ± 0.04b (−0.25 to −0.09) (0.7) | 6 |
CI, confidence interval; ND, not determined due to negligible efficacy and/or low affinity.
a
Significantly lower than in the presence of ambient divalent cations (P < 0.05, two-way ANOVA with Sidak’s comparisons post-test).
b
Significantly different from WT (P < 0.05, one-way ANOVA with Dunnett’s multiple comparisons post-test).