. 2015 Jan 5;58(3):1184–1194. doi: 10.1021/jm501829f

Table 3. Activation of Endogenous Genes in Human Breast Cancer (MCF-7) Cells Containing Only ERα or Both ERα and ERβ: Transcriptional Activities of Estradiol and Compounds 2a and 2c^a.

	hERα		hERα+β
ligand	EC₅₀ (nM)	RTP (%)	EC₅₀ (nM)	RTP (%)	EC₅₀((α + β)/α) ratio	RTP((α + β)/α) ratio
estradiol	0.0084 ± 0.0060	100	0.30 ± 0.20	100	0.028	1
2a	83.8 ± 17.0	0.0095	12.7 ± 5.0	2.35	6.58	247
2c	2090 ± 1781	0.0004	35.0 ± 20.0	0.857	59.7	2140

EC₅₀ values give absolute potencies. The ERβ/ERα relative transcriptional potencies (RTP) and ratios (RTP (β/α)) are calculated, as explained in the text. Cells were exposed to the compounds for 24 h prior to measurements. See refs (24−26).

Table 3. Activation of Endogenous Genes in Human Breast Cancer (MCF-7) Cells Containing Only ERα or Both ERα and ERβ: Transcriptional Activities of Estradiol and Compounds 2a and 2ca.

Table 3. Activation of Endogenous Genes in Human Breast Cancer (MCF-7) Cells Containing Only ERα or Both ERα and ERβ: Transcriptional Activities of Estradiol and Compounds 2a and 2c^a.