Table 3.
Cmpd | Structure | β-arrestin | cAMP | ||
---|---|---|---|---|---|
Emax (%) | EC50 (nM) | Emax (%) | EC50 (nM) | ||
46 | <20 | N/C | 43 | 98 | |
47 | <20 | N/C | 33 | 72 | |
48 | <20 | N/C | 33 | 62 | |
49 | <20 | N/C | 32 | 8.3 | |
50 | 33 | 6.4 | 41 | 1.0 | |
51 | 36 | 16 | 48 | 2.8 | |
52 | N/A | N/A | N/A | N/A | |
53 | <20 | N/C | 37 | 5.5 | |
54 | <20 | N/C | 47 | 50 | |
55 | <20 | N/C | 31 | 28 | |
56 | 29 | 6.5 | 49 | 1.1 | |
57 | N/A | N/A | N/A | N/A | |
58 | 24 | 460 | 56 | 88 |
EC50 and Emax values are the average of at least three independent experiments performed in triplicate. SEM: < ± 20%.
N/C. not calculated. N/A. no activity.