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. 2014 Oct 27;171(22):5059–5075. doi: 10.1111/bph.12863

Table 3.

Structure activity relationship of 1E7 and its derivatives

Compound number ID Structure Inhibition IC50, CEM T-cells, μM Inhibition IC50, 293T cells, μM Toxicity IC50, μM
Iteration 1
Reference (1H4) Inline graphic 10 5 100
2 1D5 Inline graphic 10 0.1 2
3 1E6 Inline graphic 1 5 >30
4 1G6 Inline graphic 5 4 >30
6 1D9 Inline graphic 15 4 >30
7 1E7 Inline graphic 2 0.9 10
10 2F2 Inline graphic 6 0.2 17
12 2A5 Inline graphic 5 0.1 26
14 3B3 Inline graphic 12 2 >30
15 3A2 Inline graphic ND 10 ND
16 3A7 Inline graphic NA NA ND
17 1B10 Inline graphic >50 ND ND
18 3F8 Inline graphic NA NA ND
19 3G6 Inline graphic NA NA ND
20 3C2 Inline graphic NA NA ND
21 3A3 Inline graphic NA NA ND
22 3G8 Inline graphic NA NA ND
23 3C10 Inline graphic >50 ND ND
24 3G7 Inline graphic NA NA ND
Iteration 2
7a 1E7-01 Inline graphic 8 ND >30
7b 1E7-02 Inline graphic 8 ND >30
7c 1E7-03 Inline graphic 2 ND >300
7d 1E7-04 Inline graphic 3 ND 7
7e 1E7-05 Inline graphic >10 ND >30
7f 1E7-06 Inline graphic >10 ND >30
7g 1E7-07 Inline graphic activation ND >30
7h 1E7-08 Inline graphic >10 ND >30
7i 1E7-09 Inline graphic 8 ND >30
7j 1E7-10 Inline graphic >10 ND >30

The original compound, 1H4, is placed in the beginning of the table as a reference.

NA, not active; ND, not determined.