Table 1.
ER-binding affinities and steroid receptor cross-reactivities of raloxifene and its analogues
| Compound | ERα Ki (nM) | ERβ Ki (nM) | Selectivity [β]/[α] | AR Ki (nM) | PR Ki (nM) | GR Ki (nM) | MR Ki (nM) |
|---|---|---|---|---|---|---|---|
| Raloxifene | 0.24 | 6.30 | 25.9 | 2768 | NA | NA | NA |
| Y108 | 0.14 | 4.74 | 33.1 | 283.3 | 6550 | NA | NA |
| Y110 | 0.57 | 1.07 | 1.9 | NA | NA | NA | NA |
| Y134 | 0.09 | 11.31 | 121.1 | NA | NA | NA | NA |
| 118675 | 1.11 | 2.42 | 2.2 | 57.15 | NA | NA | NA |
| 118676 | 0.95 | 3.67 | 3.9 | 99.93 | NA | NA | NA |
Abbreviations: AR, androgen receptor; ER, oestrogen receptor; GR, glucocorticoid receptor; MR, mineral corticoid receptor; NA, not active, PR, progesterone receptor.