TABLE 1

In Vitro Selectivity of BI 689648, LCI699, and FADs

In vitro IC50 values and selectivity of AS inhibitors determined using the cynomolgus monkey adrenal homogenate (CAH) assay. Data represent average results from n = 1–3 preparations.

AssayCompound
CAH IC50 (nM)S-FADLCI699FAD286BI 689648
Cortisol synthase (CYP11B1)a87794310
Aldosterone synthase (CYP11B2)b230102.52.1
Selectivityc0.047.738149

  • ↵a S-FAD (n = 2); LCI699 (n = 1); FAD286 (n = 2); BI 689648 (n = 1).

  • ↵b S-FAD (n = 3); LCI699 (n = 1); FAD286 (n = 3); BI 689648 (n = 1).

  • ↵c Calculated as: CAH IC50 CYP11B1 divided by CAH IC50 CYP11B2.