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. 2022 Jun 10;13(7):1151–1158. doi: 10.1021/acsmedchemlett.2c00180

Table 4. ERα Activity of Compounds 6a and 6b.

graphic file with name ml2c00180_0010.jpg

    EC50 (nM)
compd R ERα bindinga ERα agonismb
6a OMe 229 1100
6bc OH 40 48
a

ERα LiSA assay.

b

(ERE)7-TK-Luc reporter assay in HepG2 cells.

c

The bioactive tautomer is assumed to be the enol form (6b) based on the X-ray co-crystal structure. All data in triplicate ±15%.