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SAR of western amine substituent
| ||
|---|---|---|
| Cmp | R1 | IC50(μM)a |
| 1a |
|
0.46 |
| 2b |
|
0.26 |
| 2c |
|
>25 |
| 2d |
|
5.0 |
| 2e |
|
0.054 |
| 2f |
|
>25 |
| 2g |
|
2.1 |
| 2h |
|
10 |
| 2i |
|
>25 |
| 2l |
|
0.092 |
| 2m |
|
0.30 |
| 2n |
|
7.1 |
| 2o |
|
0.35 |
| 2p |
|
0.10 ± 0.02b |
| 2q |
|
1.6 |
| 2r |
|
3.2 |
| 2s |
|
14 |
| 2t |
|
0.19 |
Average of at least two measurements in DiI uptake assay with resynthesized or repurified compounds.
Standard error of mean, N = 3.
