Table 2.
Compound # | Structure | ERα, ERβ relative binding affinity (RBA) |
---|---|---|
10 | (See Scheme 2) | 0.188, 0.084 |
11 | (See Scheme 2) | 2.17, 0.24 |
13 | (See Scheme 2) | 0.314, 0.046 |
15 | (See Scheme 2) | 0.226, 0.048 |
19 | 0.5±0.1, 0.1±0.1 |
|
20 | (See Scheme 3) | 1.3±0.2a, <0.007a |
RBA values for the dendrimer conjugate are based on the concentration of ligand, not the dendrimer conjugate. Based on the dendrimer, RBA values would be 25-fold higher.