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. 2021 Sep 28;30(11):1955–1980. doi: 10.1007/s00044-021-02787-6

Table 7.

SARs and in vitro profiling of indole and 6-azaindole C-7 carboxamide derivatives

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X R EC50 (nM) CC50 (μM) Caco-2 (nm/s) HLM t1/2 (min) Human plasma protein binding
158 C F 0.52 >300 112 81 99%
169 N F 0.09 >300 124 >100 96%
170 C OCH3 0.76 >300 39 40 N.D.
171 N OCH3 0.28 >150 132 100% rem. 76%