Table 2. Binding affinities (Ki) of indole and benzimidazole carboxamides to wild type and A147T TSPO-expressing HEK-293 membranes. The affinity of all compounds was indexed by the displacement of [3H]PK-11195 (10 nM) in radioligand binding assays. Values represent the mean ± SD from at least three independent experiments performed in duplicate.
| Compound |
K
i (nM) |
A147T : wild type | |
| A147T | Wild type | ||
| 4 | >10 000 | >10 000 | N/A |
| 5 | >10 000 | 3061.3 ± 1380.2 | >3.3 |
| 6 | 2570.0 ± 731.3 | >10 000 | <0.3 |
| 7 | >10 000 | >10 000 | N/A |
| 8 | >10 000 | ∼10 000 a | N/A |
| 9 | >10 000 | 3282.4 ± 1842.0 | >3.0 |
| 10 | >10 000 | >10 000 | N/A |
| 11 | >10 000 | >10 000 | N/A |
| 12 | >10 000 | >10 000 | N/A |
| 13 | >10 000 | >10 000 | N/A |
| 14 | 2861.4 ± 892.3 | 2073.3 ± 683.8 | 1.4 |
| 15 | 760.9 ± 149.4 | 1496.3 ± 176.9 | 0.5 |
| 16 | 982.7 ± 233.9 | >10 000 | 0.1 |
aAffinity not high enough to give accurate fit (mean 47% inhibition of [3H]PK-11195 binding at 10 μM).