Binding affinities of estrogenic ligands to estrogen receptors
| Ligand | ERαa | ERαa | GPERb |
|---|---|---|---|
| nM | nM | nM | |
| 17β-E2 | 0.05–0.4 | 0.09–0.4 | 3–6 |
| 17α-E2 | 0.2–0.7 | 1–5 | >10 μM |
| E1 | 0.3 | 0.4 | >10 μM |
| E3 | 1.4 | 0.7 | >1 μM |
| DES | 0.02–0.04 | 0.04–0.05 | >1 μM |
| 4-OHT | 0.02–0.1 | 0.04 | 0.1–1 μM |
| ICI 182,780 | 0.2 | 0.08 | 10–100 |
| Bisphenol A | 5–200 | 9–35 | 630 |
| Genistein | 1–13 | 0.1–0.7 | 130 |
↵a Binding affinities for recombinant ERα and ERβ are compiled from multiple sources (Kuiper et al., 1997, 1998; Bologa et al., 2006; Lin et al., 2013), assessed by both direct and competition binding assays, and are consistent with values from Blair et al. (2000) for endogenous ER isolated from rat uterus. Where reported values differ in the various sources, the range is provided. Values for ICI 182,780 include those for the analog ICI 164,384.
↵b GPER values are taken from the sources listed in Table 2.