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. 2020 Mar 12;11(4):511–517. doi: 10.1039/c9md00580c

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).