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. 2020 Sep 16;11(11):2195–2203. doi: 10.1021/acsmedchemlett.0c00335

Table 2. In Vitro Potency of Carbazoles 6.

graphic file with name ml0c00335_0009.jpg

  in vitro activity
compd R3 chirality BTK IC50 (nM)a JAK2/BTK selectivity Ramos IC50 (nM)a hWB IC50 (nM)a
6a Cl homochiral 180 (n = 1) 11× >300 ND
6b Cl homochiral 0.55 ± 0.16 2600× 10 ± 2 162 (n = 1)
6c Cl homochiral 17 (n = 1) 60× 87 (n = 1) ND
6d Cl homochiral 0.26 ± 0.12 3800× 6.9 ± 3.4 25 ± 19
6e F homochiral 6.3 (n = 1) 330× 600 (n = 1) ND
6f F homochiral 0.22 ± 0.07 6000× 6.6 ± 0.9 64 (n = 2)
6g F homochiral 7.2 (n = 1) 140× 170 (n = 2) ND
6h F homochiral 0.19 ± 0.02 7200× 7.6 ± 2.4 37 (n = 2)
a

IC50 values are shown as mean values of at least three determinations unless specified otherwise; ND = Not determined.