Table 1.
SAR of substituents at N-1 of the imidazole ring.
![]() |
|||||
|---|---|---|---|---|---|
| Compound | R | FPA Kd(μM)* | Compound | R | FPA Kd (μM)* |
| 2a | ![]() |
1.0 ±0.3 | 2i | ![]() |
0.4 ±0.1 |
| 2b | ![]() |
3.2 ±0.5 | 2j | ![]() |
11 ±3 |
| 2c | ![]() |
4.0 ±0.7 | 2k | ![]() |
2.1 ±0.7 |
| 2d | ![]() |
5.2 ±0.9 | 2l | ![]() |
4.5 ±0.8 |
| 2e | ![]() |
1.2 ±0.2 | 2m | ![]() |
3.4 ±0.7 |
| 2f | ![]() |
5.5 ±0.7 | 2n | ![]() |
8 ± 2 |
| 2g | ![]() |
4.0 ±0.6 | 2o | ![]() |
38 ±3 |
| 2h | ![]() |
0.4 ±0.1 | 2p | ![]() |
>40 |
Data displayed is the average of at least 3 independent replicates ± standard deviation.
















