Table 4.

Potency and Intrinsic Activity of Thiophene and Furan Core Ligands^a

				HepG2				Ishikawa
				ERα		ERβ		ERα
cmpd	core		R	EC50 (µM)	Eff (% E2)	EC50 (µM)	Eff (% E2)	Eff (% E2)
THIOPHENES
2a	2,5-	4-OH	H	2.35	125 ± 4	1.54	198 ± 4	111 ± 32
2b		4-OH	2-Me	-	78 ± 4	6.60	87 ± 15	148 ± 23
2e		4-OH	2-F	-	181 ± 14	-	336 ± 63	315 ± 125
2f		4-OH	2-Cl	2.18	111 ± 5	1.94	169 ± 18	169 ± 14
2l		4-OH	2-Me, 2'-F	0.47	117 ± 8	0.61	277 ± 15	8 ± 5
2m		4-OH	2,Me, 2'-Cl	1.91	78 ± 3	1.92	111 ± 7	102 ± 7
4a	3,4-		H	2.25	69 ± 4	1.27	73 ± 2	46 ± 4
4b			2-Me	3.15	97 ± 11	1.87	67 ± 4	120 ± 14
4c			3-Me	-	73 ± 5	-	70 ± 4	4 ± 0
4e			2-F	0.12	79 ± 3	0.780	29 ± 4	63 ± 5
4f			2-Cl	0.045	90 ± 7	0.203	57 ± 3	90 ± 3
6a	2,4-		2-F	1.06	123 ± 6	1.34	177 ± 17	201 ± 13
6b			2-Cl	0.563	87 ± 5	0.660	117 ± 2	81 ± 5
8a	2,3-		2-F	65.9	69 ± 3	-	33 ± 10	67 ± 6
8b			2-Cl	1.16	82 ± 8	5.70	116 ± 14	114 ± 6
10a	2,5-	3-Me	H	1.52	116 ± 5	1.23	200 ± 10	225 ± 27
10b		3-Me	2-Me	0.439	70 ± 5	2.46	106 ± 23	56 ± 4
10c		3-Me	2-F	0.447	149 ± 1	10.8	284 ± 44	260 ± 53
10d		3-Me	2-Cl	0.101	82 ± 1	0.295	113 ± 4	72 ± 8
12a	2,5-	3-Ph	2-F	0.615	70 ± 1	-	39 ± 11	91 ± 15
12b		3-Ph	2-Cl	0.066	72 ± 2	-	1 ± 1	92 ± 4
14a	2,3,5-		H	0.485	82 ± 6	2.23	−22 ± 1	145 ± 9
14b			2-F	0.387	84 ± 5	-	−1 ± 4	63 ± 2
14c			2-Cl	0.009	52 ± 5	-	−13 ± 2	35 ± 1
FURANS
16a	2,5-		H	-	62 ± 3	-	94 ± 26	91 ± 21
16b			Me	3.79	36 ± 4	-	8 ± 6	58 ± 8
16c			F	-	154 ± 7	-	159 ± 13	61 ± 48
16d			Cl	3.89	82 ± 7	-	106 ± 3	118 ± 11
18a	3,4-		H	10.6	81 ± 2	-	37 ± 5	82 ± 25
18b			Me	0.944	97 ± 5	5.11	56 ± 3	104 ± 6
18c			F	3.64	73 ± 2	-	85 ± 16	85 ± 11
18d			Cl	0.266	86 ± 6	17.5	54 ± 4	116 ± 9

^aSee footnote a in Table 1.

Values indicating pronounced superagonism (i.e., Eff values ≥120) are indicated in boldface type.