Table 1.
Relative binding affinities of ligands to full-length ERα or ERβ
|
RBA |
||
---|---|---|---|
Ligand
|
ERα
|
ERβ
|
|
17β-Estradiol | 100 | 100 | |
4-Hydroxytamoxifen | 36 | 43 | |
Raloxifene | 34 | 76 | |
GW-5638
|
5
|
8
|
|
STX | 4.3E-6 | 9.0E-6 |
Relative binding affinities (RBA) are expressed as a percentage of the potency of 17β-estradiol. Under the experimental conditions described in Materials and Methods, 17β-estradiol was found to have an IC50 of 5 nm for ERα and 3 nm for ERβ.