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. 2020 Jul 29;11(9):1751–1758. doi: 10.1021/acsmedchemlett.0c00264

Table 3. SAR of Indole N-1 and C-3 Positions.

graphic file with name ml0c00264_0011.jpg

compd R1 R2 TLR7 IC50 (nM)a TLR9 IC50 (nM)a
5n H Me 250 ± 160 430 ± 260
7a Me Me 5260 ± 1540 740 ± 170
7b H Cl 1880 ± 710 430 ± 170
7c H CN >10 000 260 ± 200
7d H CH2CH3 130 ± 100 490 ± 370
7e H CH2CF3 70 ± 40 750 ± 270
7f H isopropyl 10 ± 7 700 ± 390
7g H isobutyl 1290 ± 770 830 ± 770
a

IC50 values are a mean of two or more individual determinations.