Table 1. TSPO binding affinities (Ki) of carbazole derivatives using membranes from TSPO WT and A147T over-expressing 293T cells. Values represent the mean ± SEM from at least three independent experiments performed in duplicate.
Compound | TSPO WT Ki (nM) | TSPO A147T Ki (nM) | TSPO A147T Ki/TSPO WT Ki |
PK 11195 | 29.2 ± 7.3 | 36.0 ± 6.8 | 1.2 |
DPA-713 | 19.5 ± 3.5 | 98.8 ± 2.3 | 5.1 |
XBD-173 | 6.4 ± 1.4 | 31.3 ± 3.6 | 4.9 |
3a | 30.1 ± 3.6 | 176.6 ± 41.6 | 5.9 |
3b | 91.6 ± 0.9 | 459.6 ± 83.0 | 5.0 |
4a | 31.5 ± 5.4 | 160.9 ± 20.6 | 5.1 |
4b | 54.3 ± 8.4 | 123.4 ± 16.3 | 2.3 |
5a | 31.6 ± 1.9 | 159.8 ± 31.0 | 5.1 |
5b | 25.4 ± 0.2 | 137.3 ± 20.9 | 5.4 |
5c | 28.9 ± 3.6 | 93.4 ± 14.6 | 3.2 |