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. Author manuscript; available in PMC: 2020 Dec 26.
Published in final edited form as: J Med Chem. 2019 Dec 10;62(24):11301–11323. doi: 10.1021/acs.jmedchem.9b01580

Table 4.

ER degradation, binding, and activationd,e

graphic file with name nihms-1591873-t0015.jpg
a

ER degradation potency and efficacy normalized to vehicle (100%) and 1 μM 2 (0%).

b

RBA values, determined by radioligand displacement assays expressed as IC50 estradiol/IC50 compound × 100 (RBA, estradiol = 100%).

c

Estrogenic activity (ERE IC50), as determined by ERE dual luciferase in competition with 1 nM E2, normalized to 1 nM E2 alone (100%) and vehicle (0%).

d

Data shown as mean ± SEM from at least three biological and analytical replicates.

e

Data shown as mean ± SEM from three analytical replicates. NA = not applicable; NI = no inhibition.