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. 2016 Nov 15;8(1):202–210. doi: 10.1039/c6md00523c

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