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Template:Affinities of estrogen receptor ligands for the ERα and ERβ

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Affinities of estrogen receptor ligands for the ERα and ERβ
Ligand Other names Relative binding affinities (RBA, %)a Absolute binding affinities (Ki, nM)a Action
Template:No selflink Template:No selflink Template:No selflink Template:No selflink
Template:No selflink E2; 17β-Estradiol 100 100 Template:Median (0.04–0.24) Template:Median (0.10–2.08) Estrogen
Template:No selflink E1; 17-Ketoestradiol Template:Median (0.7–60) Template:Median (1.36–52) Template:Median (0.3–1.01) Template:Median (0.35–9.24) Estrogen
Template:No selflink E3; 16α-OH-17β-E2 Template:Median (4.03–56) Template:Median (14.0–44.6) Template:Median (0.35–1.4) Template:Median (0.63–0.7) Estrogen
Template:No selflink E4; 15α,16α-Di-OH-17β-E2 4.0 3.0 4.9 19 Estrogen
Template:No selflink 17α-Estradiol Template:Median (7–80.1) Template:Median (2–42) 0.2–0.52 0.43–1.2 Metabolite
Template:No selflink 16β-Hydroxy-17β-estradiol Template:Median (4.94–63) 50 ? ? Metabolite
Template:No selflink 16α-Hydroxy-17α-estradiol Template:Median (29–103) 79–80 ? ? Metabolite
Template:No selflink 16β-Hydroxy-17α-estradiol 1.0 13 ? ? Metabolite
Template:No selflink 2-OH-E2 Template:Median (7–81) 11–35 2.5 1.3 Metabolite
Template:No selflink 2-MeO-E2 0.0027–2.0 1.0 ? ? Metabolite
Template:No selflink 4-OH-E2 Template:Median (8–70) 7–56 1.0 1.9 Metabolite
Template:No selflink 4-MeO-E2 2.0 1.0 ? ? Metabolite
Template:No selflink 2-OH-E1 2.0–4.0 0.2–0.4 ? ? Metabolite
Template:No selflink 2-MeO-E1 <0.001–<1 <1 ? ? Metabolite
Template:No selflink 4-OH-E1 1.0–2.0 1.0 ? ? Metabolite
Template:No selflink 4-MeO-E1 <1 <1 ? ? Metabolite
Template:No selflink 16α-OH-E1; 17-Ketoestriol 2.0–6.5 35 ? ? Metabolite
Template:No selflink 2-OH-E3 2.0 1.0 ? ? Metabolite
Template:No selflink 4-MeO-E3 1.0 1.0 ? ? Metabolite
Template:No selflink E2S; Estradiol 3-sulfate <1 <1 ? ? Metabolite
Template:No selflink Estradiol 3,17β-disulfate 0.0004 ? ? ? Metabolite
Template:No selflink E2-3G 0.0079 ? ? ? Metabolite
Template:No selflink E2-17G 0.0015 ? ? ? Metabolite
Template:No selflink E2-3G-17S 0.0001 ? ? ? Metabolite
Template:No selflink E1S; Estrone 3-sulfate <1 <1 >10 >10 Metabolite
Template:No selflink EB; Estradiol 3-benzoate 10 ? ? ? Estrogen
Template:No selflink E2-17B 11.3 32.6 ? ? Estrogen
Template:No selflink Estrone 3-methyl ether 0.145 ? ? ? Estrogen
Template:No selflink 1-Estradiol 1.31–12.34 9.44–80.07 ? ? Estrogen
Template:No selflink 7-Dehydroestrone Template:Median (4.0–28.9) 13.0–49 0.79 0.36 Estrogen
Template:No selflink 6,8-Didehydroestrone 2.0–15 7.0–20 0.64 0.62 Estrogen
Template:No selflink 7-Dehydro-17β-estradiol 7.9–113 7.9–108 0.09 0.17 Estrogen
Template:No selflink 7-Dehydro-17α-estradiol Template:Median (18–41) 14–32 0.24 0.57 Estrogen
Template:No selflink 6,8-Didehydro-17β-estradiol 35–68 90–100 0.15 0.20 Estrogen
Template:No selflink 6,8-Didehydro-17α-estradiol 20 49 0.50 0.37 Estrogen
Template:No selflink 8,9-Dehydro-17β-estradiol 68 72 0.15 0.25 Estrogen
Template:No selflink 8,9-Dehydroestrone 19 32 0.52 0.57 Estrogen
Template:No selflink EE; 17α-Ethynyl-17β-E2 Template:Median (68.8–480) Template:Median (2.0–144) 0.02–0.05 0.29–0.81 Estrogen
Template:No selflink EE 3-methyl ether ? 2.5 ? ? Estrogen
Template:No selflink RU-2858; 11β-Methoxy-EE 35–43 5–20 0.5 2.6 Estrogen
Template:No selflink 17α-Methyl-17β-estradiol 70 44 ? ? Estrogen
Template:No selflink DES; Stilbestrol Template:Median (89.1–468) Template:Median (61.2–295) 0.04 0.05 Estrogen
Template:No selflink Dihydrodiethylstilbestrol Template:Median (31–302) 60–234 0.06 0.06 Estrogen
Template:No selflink Dehydrostilbestrol Template:Median (20.4–223) 56–404 0.05 0.03 Estrogen
Template:No selflink – 114 ? ? ? Estrogen
Template:No selflink TACE 1.74 ? 15.30 ? Estrogen
Template:No selflink TPE 0.074 ? ? ? Estrogen
Template:No selflink TPBE 2.69 ? ? ? Estrogen
Template:No selflink ICI-46,474 Template:Median (0.1–47) Template:Median (0.28–6) 3.4–9.69 2.5 SERM
Template:No selflink 4-Hydroxytamoxifen; 4-OHT Template:Median (1.7–257) Template:Median (0.98–339) Template:Median (0.1–3.61) 0.04–4.8 SERM
Template:No selflink 4-Chlorotamoxifen; 4-CT ? ? 7.14–20.3 15.4 SERM
Template:No selflink MRL-41 Template:Median (19.2–37.2) 12 0.9 1.2 SERM
Template:No selflink F-6066; Sexovid 151–152 243 ? ? SERM
Template:No selflink U-11,000A 30.9–44 16 0.3 0.8 SERM
Template:No selflink – Template:Median (7.8–69) Template:Median (0.54–16) 0.188–0.52 20.2 SERM
Template:No selflink LY-353,381 ? ? 0.179 ? SERM
Template:No selflink CP-336,156 10.2–166 19.0 0.229 ? SERM
Template:No selflink Centchroman ? ? 0.313 ? SERM
Template:No selflink 6720-CDRI; NNC-460,020 1.55 1.88 ? ? SERM
Template:No selflink Deaminohydroxytoremifene 0.82–2.63 0.59–1.22 ? ? SERM
Template:No selflink – ? ? 0.053 ? SERM
Template:No selflink GW-5638 4.30 11.5 ? ? SERM
Template:No selflink – Template:Median (3.70–97.7) 166 0.2 0.08 Antiestrogen
Template:No selflink ICI-182,780 Template:Median (9.4–325) Template:Median (2.05–40.5) 0.42 1.3 Antiestrogen
Template:No selflink PPT Template:Median (10.0–89.1) 0.12 0.40 92.8 ERα agonist
Template:No selflink 16α-Lactone-17β-estradiol 14.6–57 0.089 0.27 131 ERα agonist
Template:No selflink 16α-Iodo-17β-estradiol 30.2 2.30 ? ? ERα agonist
Template:No selflink MPP 11 0.05 ? ? ERα antagonist
Template:No selflink DPN 0.12–0.25 6.6–18 32.4 1.7 ERβ agonist
Template:No selflink 8β-Vinyl-17β-estradiol 0.35 22.0–83 12.9 0.50 ERβ agonist
Template:No selflink ERB-041; WAY-202,041 0.27 67–72 ? ? ERβ agonist
Template:No selflink WAY-202,196 ? 180 ? ? ERβ agonist
Template:No selflink SERBA-1; LY-500,307 ? ? 2.68 0.19 ERβ agonist
Template:No selflink – ? ? 14.5 1.54 ERβ agonist
Template:No selflink – Template:Median (0.0117–94) Template:Median (0.41–185) 0.14–80.0 0.07–27.0 Xenoestrogen
Template:No selflink – Template:Median (0.0012–16) Template:Median (0.86–87) 2.6–126 0.3–12.8 Xenoestrogen
Template:No selflink – 0.2–0.287 Template:Median (0.10–2.85) ? ? Xenoestrogen
Template:No selflink – Template:Median (0.0018–9.3) Template:Median (0.04–17.1) 2.0 85.3 Xenoestrogen
Template:No selflink – Template:Median (0.022–0.15) Template:Median (0.010–1.2) 174 8.9 Xenoestrogen
Template:No selflink – Template:Median (0.029–0.10) Template:Median (0.002–3.00) ? ? Xenoestrogen
Template:No selflink – Template:Median (<0.001–0.01) Template:Median (0.11–0.33) ? ? Xenoestrogen
Template:No selflink 8-PN 4.4 ? ? ? Xenoestrogen
Template:No selflink – <0.001–0.01 0.002–0.040 ? ? Xenoestrogen
Template:No selflink – <0.01 <0.01 ? ? Xenoestrogen
Template:No selflink – 0.39 ? ? ? Xenoestrogen
Template:No selflink – 2.0 ? ? ? Xenoestrogen
Template:No selflink – <0.001–0.0875 <0.001–0.016 ? ? Xenoestrogen
Template:No selflink – <0.001–0.0032 ? ? ? Xenoestrogen
Template:No selflink – Template:Median (13–52.5) ? ? ? Xenoestrogen
Template:No selflink – Template:Median (0.032–13) ? ? ? Xenoestrogen
Template:No selflink α-Zearalanol 48–111 ? ? ? Xenoestrogen
Template:No selflink β-Zearalanol Template:Median (13–17.8) 14 0.8 0.9 Xenoestrogen
Template:No selflink ZEN Template:Median (2.04–28) Template:Median (2.43–31.5) ? ? Xenoestrogen
Template:No selflink ZAN 0.51 ? ? ? Xenoestrogen
Template:No selflink BPA Template:Median (0.008–1.0) Template:Median (0.002–4.23) 195 35 Xenoestrogen
Template:No selflink EDS <0.001–<0.01 <0.01 ? ? Xenoestrogen
Template:No selflink Chlordecone 0.0069–0.2 ? ? ? Xenoestrogen
Template:No selflink – 0.0073–0.4 ? ? ? Xenoestrogen
Template:No selflink – Template:Median ? ? ? Xenoestrogen
Template:No selflink p,p'-Dimethoxy-DDT Template:Median (<0.001–0.02) 0.01–0.13 ? ? Xenoestrogen
Template:No selflink Hydroxychlor; p,p'-OH-DDT 1.2–1.7 ? ? ? Xenoestrogen
Template:No selflink T; 4-Androstenolone <0.0001–<0.01 <0.002–0.040 >5000 >5000 Androgen
Template:No selflink DHT; 5α-Androstanolone Template:Median (<0.001–0.05) 0.0059–0.17 221–>5000 73–1688 Androgen
Template:No selflink 19-Nortestosterone; 19-NT 0.01 0.23 765 53 Androgen
Template:No selflink DHEA; Prasterone Template:Median (<0.001–0.04) 0.019–0.07 245–1053 163–515 Androgen
Template:No selflink A5; Androstenediol 6 17 3.6 0.9 Androgen
Template:No selflink – 0.5 0.6 23 19 Androgen
Template:No selflink A4; Androstenedione <0.01 <0.01 >10000 >10000 Androgen
Template:No selflink 3α-Adiol 0.07 0.3 260 48 Androgen
Template:No selflink 3β-Adiol 3 7 6 2 Androgen
Template:No selflink 5α-Androstanedione <0.01 <0.01 >10000 >10000 Androgen
Template:No selflink 5β-Androstanedione <0.01 <0.01 >10000 >10000 Androgen
Template:No selflink 17α-Methyltestosterone <0.0001 ? ? ? Androgen
Template:No selflink 17α-Ethynyl-3α-adiol 4.0 <0.07 ? ? Estrogen
Template:No selflink 17α-Ethynyl-3β-adiol 50 5.6 ? ? Estrogen
Template:No selflink P4; 4-Pregnenedione <0.001–0.6 <0.001–0.010 ? ? Progestogen
Template:No selflink NET; 17α-Ethynyl-19-NT Template:Median (0.0015–<0.1) Template:Median (0.01–0.3) 152 1084 Progestogen
Template:No selflink 5(10)-Norethisterone Template:Median (0.3–0.7) <0.1–0.22 14 53 Progestogen
Template:No selflink 7α-Methylnorethynodrel Template:Median (0.45–2.0) 0.2–0.076 ? ? Progestogen
Template:No selflink 7α-Methylnorethisterone 0.069–<0.1 0.027–<0.1 ? ? Progestogen
Template:No selflink – Template:Median (1.06–5.0) 0.6–0.8 ? ? Progestogen
Template:No selflink – Template:Median (0.75–1.9) 0.070–0.1 ? ? Progestogen
Footnotes: a = (1) Binding affinity values are of the format "median (range)" (# (#–#)), "range" (#–#), or "value" (#) depending on the values available. The full sets of values within the ranges can be found in the Wiki code. (2) Binding affinities were determined via displacement studies in a variety of in-vitro systems with labeled estradiol and human ERα and ERβ proteins (except the ERβ values from Kuiper et al. (1997), which are rat ERβ).
Sources: Kuiper et al. (1997, 1998),[1][2][3][4] Bolger et al. (1998),[5] Fritzemeier & Hegele-Hartung (1999),[6] Matthews et al. (2000),[7] Qu et al. (2000),[8] Gutendorf & Westendorf (2001),[9] Han et al. (2002),[10][11] Harris et al. (2002),[12] Tamrazi et al. (2002),[13] de Gooyer et al. (2003),[14] Ohno & Suzuki et al. (2003),[15][16][17] Mueller et al. (2004),[18] Perez et al. (2004, 2005),[19][20][21] Chen et al. (2005),[22] Matsumura et al. (2005),[23] Veeneman (2005),[24] Escande et al. (2006),[25] Sonneveld et al. (2006),[26] Taneja et al. (2006),[27] Zhu et al. (2006),[28][29] Harris (2007),[30] Akahori et al. (2008),[31] Attardi et al. (2008),[32] Bhavnani, Tam, & Lu (2008),[33][34][3][35] NITETooltip National Institute of Technology and Evaluation (2008),[36][37] Visser et al. (2008),[38] Escande et al. (2009),[39] Rider et al. (2009),[40][41] Shanle & Xu (2010),[42] Dang et al. (2010),[11] Toniti et al. (2011),[43] Ahlem et al. (2012),[44] Mizutani et al. (2012),[45] Durmaz et al. (2013),[46] Unkilaa et al. (2013),[47] and Perkins et al. (2018).[48][49] Other sources (not included due to (1) no ER subtype specificity; (2) non-human ERs; and/or (3) only estrogenic potencies without affinity values): [50][51][52][53][54][55][56][57][58][59][60][23][61][62][63][64]
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