Table 4.
β-Arrestin Recruitment EC50 and Emax and Bias Factors of Selected Compounds
| compound | EC50 (nM)a | Emax (%)a | G protein bias factor | β-arrestin bias factor |
|---|---|---|---|---|
| 4a | 22 ± 5 | 100 ± 10 | 1.00 | 1.00 |
| 10a | 483 ± 46 | 70 ± 6 | 25.8 | 0.039 |
| 10g | 1585 ± 250 | 125 ± 12 | 66.3 | 0.015 |
| 10l | 1582 ± 149 | 127 ± 7 | 63.2 | 0.016 |
| 15b | 110 ± 11 | 109 ± 3 | 16.4 | 0.061 |
| 15c | 247 ± 62 | 100 ± 7 | 31.2 | 0.032 |
| 15d | 14 ± 4 | 92 ± 2 | 4.10 | 0.244 |
| 15e | 335 ± 69 | 118 ± 5 | 26.9 | 0.037 |
| 24b | 17 ± 3 | 109 ± 6 | 2.41 | 0.415 |
| 24e | 89 ± 12 | 120 ± 3 | 11.7 | 0.085 |
| 24f | 1036 ± 136 | 172 ± 7 | 81.9 | 0.012 |
| 24j | 563 ± 28 | 142 ± 6 | 34.7 | 0.029 |
| 24k | 349 ± 25 | 131 ± 4 | 64.9 | 0.015 |
a
Values are mean ± SEM from n ≥ 3 independent experiments.
Emax (%) is the efficacy maximum of the compounds in the β-arrestin recruitment assay relative to compound 4a as 100% and DMSO as 0%.