Table 1. Relative Binding Affinities (RBAs) of Compounds 2 and 4–6 for Estrogen Receptor α and βa.
Determined by a competitive radiometric binding assay with [3H]estradiol; preparations of purified, full-length human ERα and ERβ (Invitrogen) were used; see the Experimental Section. Values are reported as the mean ± the range or SD of two or more independent experiments; the Kd for estradiol for ERα is 0.2 nM and for ERβ, 0.5 nM. Ki values for the reported compounds can be readily calculated using the formula Ki = (Kd[estradiol]/RBA)100.