Table 3 SAR of aryl group on CMKLR1 inhibition.
From: Novel CMKLR1 Inhibitors for Application in Demyelinating Disease
Cmpd ID | Ar | β-arrestin IC50 µM mean ± SEM (n) | Chemotaxis IC50 µM mean ± SEM (n) |
|---|---|---|---|
22(α-NETA) |
| 4.9 ± 1.5 (18) | 37.0 ± 8.9 (6) |
23 |
| 2.5 ± 0.9 (5) | 24.1 (1) |
24 |
| 5.6 ± 0.7 (6) | >100 (1) |
25 |
| 11.9 (1) | >100 (1) |
26 |
| 2.9 ± 1.6 (5) | 7.2 (1) |
27 |
| 1.9 ± 0.2 (8) n.s. | 4.5 ± 1.5 (3)* |
28 |
| 3.8 ± 1.7 (4) | 14.6 ± 4.8 (2) |
29 |
| 4.8 ± 1.6 (8) | 17.4 ± 2.2 (4) |
30 |
| 2.1 ± 1.1 (7) | 6.8 (1) |
31 |
| 6.0 ± 2.2 (6) | >100 (4) |
32 |
| 1.5 ± 0.3 (3) | 20 ± 6.2 (3) |
33 |
| 0.6 ± 0.3 (3) | 10.7 (1) |
