Table 5.
Allosteric Parameters of Selected PAMs at Mouse GPR68a
| compd | Log(α) | Log(β) | −Log(KB) | Log(αβ/KB) | Δ |
|---|---|---|---|---|---|
| 1 | 0.80 ± 0.11 | 0.04 ± 0.05 | 4.13 ± 0.09 | 4.97 ± 0.02 | −0.34 |
| 46 | 1.41 ± 0.08 | −0.0 2 ± 0.06 | 4.30 ± 0.03 | 5.68 ± 0.05 | −0.43 |
| 63 | 0.91 ± 0.18 | 0.08 ± 0.03 | 4.91 ± 0.17 | 5.89 ± 0.02 | −0.40 |
| 71 | 1.26 ± 0.14 | 0.09 ± 0.03 | 5.12 ± 0.19 | 6.46 ± 0.05 | −0.43 |
| 77 | 1.06 ± 0.12 | 0.13 ± 0.09 | 4.72 ± 0.02 | 5.92 ± 0.02 | −0.34 |
| 78 | 0.99 ± 0.06 | 0.13 ± 0.06 | 4.86 ± 0.08 | 5.98 ± 0.04 | −0.40 |
a
Values represent means ± SEM from a minimum of three independent assays, each in quadruplicate. Δ stands for the difference of Log(αβ/KB) from the corresponding values at human GPR68 (Tables 1–4); positive values indicate increased allosteric activity, and negative values indicate reduced allosteric activity. Proton concentration-response curves are presented in Figure 3 and Supporting Figure 7.