. 2014 Mar 26;57(8):3532–3545. doi: 10.1021/jm500268j

Table 2. Effects of Imines on the Transcriptional Activities of Estrogen Receptor α and β.

	agonist mode^a				antagonist mode^a
	ERα		ERβ		ERα		ERβ
	EC₅₀ (nM)	eff (% E2)	EC₅₀ (nM)	eff (% E2)	IC₅₀ (nM)	eff (% E2)	IC₅₀ (nM)	eff (% E2)
2a	3	110 ± 5		34 ± 12		126 ± 4	13	17 ± 3
2c	7	103 ± 6		8 ± 3		149 ± 6	6	27 ± 9
2d	5	109 ± 3		13 ± 9		93 ± 5	41	14 ± 0
2e	nd	nd		7 ± 9		nd	45	10 ± 2
2f	1	104 ± 3		37 ± 9		83 ± 9	19	30 ± 3
2g	10	102 ± 3		10 ± 3		109 ± 5	16	11 ± 2
2h	2	114 ± 4		9 ± 3		138 ± 8	9	6 ± 2
2i	23	89 ± 3		3 ± 2		104 ± 6	24	11 ± 5
2j	2	114 ± 4		10 ± 3		113 ± 4	7	8 ± 2
2k	1	105 ± 2		11 ± 1		128 ± 10	6	4 ± 3
2n	14	95 ± 2	332	16 ± 8		111 ± 4	300	33 ± 9
4b	7	102 ± 2	628	25 ± 8		134 ± 34	6	23 ± 12
4c		111 ± 4	2	31 ± 3		100 ± 5	16	29 ± 4
4d	14	95 ± 2		9 ± 2		101 ± 2	51	11 ± 3
4e	16	103 ± 3	10 860	20 ± 9		122 ± 34	241	21 ± 9
4f	0.1	113 ± 4		54 ± 1		136 ± 13	6	33 ± 6
4g	15	117 ± 6		15 ± 2		118 ± 23	67	15 ± 0
4h	4	114 ± 3	385	19 ± 5		123 ± 18	180	15 ± 1
4i	57	100 ± 4		11 ± 6		95 ± 9	28	16 ± 2
4j	10	108 ± 3		23 ± 8		124 ± 6	139	14 ± 2
4k	9	113 ± 4	12 460	24 ± 2		111 ± 5	100	13 ± 6
4l	17	102 ± 3	276	38 ± 13		102 ± 6		20 ± 24
4n	7	97 ± 3		51 ± 10		108 ± 4	417	25 ± 10

In the agonist mode, ERE-luciferase assays were performed with 12-point dose curves of the indicated ligands, whereas in the antagonist mode, this was done in the presence of 10 nM E2.