Table 2 SAR of tertiary amines on CMKLR1 inhibition.
From: Novel CMKLR1 Inhibitors for Application in Demyelinating Disease
Cmpd ID | Ar | R1 | R2 | β-arrestin IC50 µM mean ± SEM (n) |
|---|---|---|---|---|
α-NETA | 4.9 ± 1.5 (18) | |||
3 |
| Me | Me | 18.8 (1) |
4 |
| Me | Et | 17.9 (1) |
5 |
| Et | Et | 8.9 ± 2.4 (4) |
6 |
| Me | Me | 6.2 ± 2.5 (3) n.s. |
7 |
| Me | Me | 18.5 (1) |
8 |
| Et | Et | 71.3 (1) |
9 |
| Me | Et | 39.6 (1) |
10 |
| Me | Bu | 44.5 (1) |
11 |
| Me | Me | >100 (2) |
12 |
| Me | Me | >100 (1) |
13 |
| Me | Et | 16.8 ± 8.3 (3) |
14 |
| Et | Et | 77.8 (1) |
15 |
| Me | Bu | >100 (4) |
16 |
| Me | Me | >100 (1) |
17 |
| Me | Me | >100 (1) |
18 |
| Me | Me | 64 (1) |
19 |
| Me | Me | 10.3 ± 4.5 (4) |
20 |
| Me | Me | >100 (1) |
