Table 2.

Transcription Potencies of ERβ-ligands of the Salaldox A (1c,d) and Salaldox B (2a–d) series through Estrogen Receptors α and β.^a

Entry	Ligand	hERα activation		hERβ activation		β/α EC50 -selectivity ratio
		EC50 (nM)b	EMAX (%)c	EC50 (nM)b	EMAX (%)c
Salaldox A Series
1	1cd	26	80	11	60	2.4
2	1de	19	95	4.8	85	4.0
Salaldox B Series
3	2ae	17	100	10	100	1.7
4	2b	0.30	90	0.50	80	0.6
5	2c	0.58	100	0.23	100	2.5
6	2d	8.4	100	1.3	100	6.5
7	estradiol	0.09	100	0.72	100	0.12

^aHuman endometrial cancer (HEC-1) cells, transfected with expression vectors for ERα or ERβ and an (ERE)₂-pS2-luc reporter gene and were treated with the indicated compound and resulting luciferase activity was measured as expression of transcription (see Experimental Section).

^bHalf-maximal effective concentration.

^cMaximal effect normalized to the activity with 100 nM estradiol, which was set at 100%.

^dSee Ref. 13.

^eSee Ref. 14.