. Author manuscript; available in PMC: 2011 May 19.

Published in final edited form as: Bioconjug Chem. 2010 May 19;21(5):903–910. doi: 10.1021/bc900461h

Table 1.

Estrogen receptor modulation properties of conjugates

Compound	ER alpha IC₅₀ (nM)^a	ER beta IC₅₀ (nM)^a	ERE IC₅₀ (nM)^b
Estradiol	2.5 ± 0.2	3.7 ± 1.0	16 ± 10 ^d
OHT	8.5 ± 3.9	13 ± 7	40 ± 10 ^c
OHT-6C (R=H)	15 ± 5	9 ± 5	85 ± 50 ^c
OHT-6C-FL	25 ± 10	35 ± 20	900 ± 600 ^c
OHT-6C-BODIPY	30 ± 10	40 ± 20	250 ± 110^c
OHT-6C-AF546	180 ± 30	240 ± 70	600 ± 350 ^c
EE-Bn-NH₂	7 ± 4	6 ± 4	150 ± 20^d
EE-Bn-AF546	10 ± 2	35 ± 20	140 ± 90 ^d

ER binding determined using competition experiments with purified ER and ³H-labeled estradiol as described in the experimental procedures

ERE activity determined using MCF7 cells transfected with luciferase reporter plasmid under control of consensus ERE as described in the experimental procedures.

IC₅₀ values determined in the presence of 10 nM estradiol

IC₅₀ values determined in the presence of 5 nM raloxifene