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

Table 2. ERα Activity of Compounds 2a–g.

graphic file with name ml2c00180_0008.jpg

    EC50 (nM)
compd R ERα bindinga ERα agonismb
2a Ph 11 48
2b Me 1700 6600
2c i-Pr 6200 >10 000
2d i-Bu 31 240
2e t-Bu 890 2000
2f c-C6H11 95 350
2g 2-Cl-Ph 43 170
a

ERα LiSA assay.

b

(ERE)7-TK-Luc reporter assay in HepG2 cells; all data in triplicate ±15%.