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. 2011 Feb 14;286(15):12971–12982. doi: 10.1074/jbc.M110.205112

TABLE 1.

RLAs of different estrogens to ERα and ERβ

The RLA of each ligand was calculated as the ratio of IC50 of 17β-E2 and IC50 of competitor, multiplied by 100. Each value is the mean ± S.D. of measurements obtained from three independent experiments. The ratios of RLA for ERβ/ERα are shown. A ratio greater than 1 indicates higher affinity for ERβ, and a ratio less than 1 indicates higher affinity for ERα. Numbers in brackets ([100] or [1]) are the base values on which the RLA values are calculated. A value of 100 represents a Kd = 0.2 nm for ERα and 0.5 nm for ERβ (18).

Ligand name RLA
RLA β/α
ERα ERβ
17β-E2 [100] [100] [1.0]
E1 4.5 ± 0.7 4.0 ± 1.0 0.89
E3 6.8 ± 0.7 11.6 ± 0.6 1.7
EE2 194 ± 22 151 ± 27 0.78
17α-E2 13.7 ± 1.6 5.3 ± 1.8 0.39
DES 290 ± 56 278 ± 54 0.96
DMS 22.2 ± 4.3 237 ± 28 10.7
Meso-Hex 314 ± 44 697 ± 74 2.2
dl-Hex 4.4 ± 0.3 60.3 ± 5.3 13.7
Equ 2.3 ± 0.2 3.2 ± 0.3 1.4
Eqn 0.35 ± 0.04 2.0 ± 0.3 5.7
Gen 0.06 ± 0.01 7.4 ± 0.5 123