Table 3.
Ligand | Potency from cellular activities |
Potency from cell-free activities |
||||
---|---|---|---|---|---|---|
Gene stimulation, EC50 (nM) |
β/α potency selectivity [relative to E2] | β/α selectivity RBA × RCA [relative to E2] | β/α RCA selectivity | β/α RBA selectivity | ||
ERβ only, OTUB2 | ERα only, PgR | |||||
E2 | 1.67 | 0.02 | 0.012 [1.0] | [1.0] | [1.00] | [1.00] |
Genistein | 4 | 24 | 6 [500] | 1750 | 5.4 | 324 |
S-equol | 1.4 | 14 | 10 [830] | 2600 | 108 | 24 |
Daidzein | 50 | 200 | 4 [340] | 1024 | 62 | 17 |
Liquiritigenin | 60 | 300 | 5 [420] | 400 | 19 | 21 |
OTUB2, otubain 2; PgR, progesterone receptor.