| Agonist modea
| Antagonist modeb
|
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 | ERα | ERβ | ERα | ERβ |
---|
Cmpd | EC50 (μM) | Efficacy (%E2) | EC50 (μM) | Efficacy (%E2) | IC50 (μM) | Efficacy (%E2)c
| IC50 (μM) | Eff (%E2) |
---|
WZY-2 | – | -21 ± 13 | – | – | – | 73 ± 8 | 3.02 | 13.9 ± 5.3 |
MJ-22 | 0.47 | 117 ± 8 | 0.61 | 277 ± 15 | – | – | – | – |
MJ-17 | 0.045 | 90 ± 7 | 0.203 | 57 ± 3 | – | – | – | – |
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aLuciferase activity was measured in HEK 293 T cells transfected with 3 × estrogen response element (ERE)-driven luciferase reporter and expression vectors encoding estrogen receptor α (ERα) or ERβ and treated in triplicate with increasing doses (up to 10-5 M) of the compounds. Half maximal effective concentrations (EC50) and standard deviation (mean ± SD), shown as a percentage of 10-8 M 17β-estradiol (E2), were determined
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bHalf maximal inhibitory concentrations (IC50) and standard deviation (mean ± SD) were determined in the percentage of 10-8 M 17β-estradiol (E2) on ERα or ERβ
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cERs have considerable basal activity in HEK 293Â T cells. Omitted EC50 or IC50 values were too high to be determined accurately