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afimoxifene (CID 449459) - Compound BioActivity Data
.
BioActivity Outcomes:
Active(155)
 
 
Inactive(713)
 
 
Inconclusive(95)
 
 
Unspecified(106)
 
 
Top Targets:
NR LBD ER(69)
 
 
 
 
 
7TM GPCR Srx(23)
 
 
NR LBD PPAR(22)
 
 
 
7TM GPCR Srsx(18)
 
 
Bcl-2 like(11)
 
 
BioAssay Types:
Screening(557)
 
 
 
 
Confirmatory(284)
 
 
 
 
 
Literature(180)
 
 
 
 
 
Summary(24)
 
 
 
BioActivity Types:
Potency(241)
 
 
 
 
 
IC50(81)
 
 
 
 
EC50(14)
 
 
 
Ki(12)
 
 
 
AC50(1)
 
 
Data download

Chemical Probe    Active    Inactive    Inconclusive    Unspecified   

Total Bioassays: 893    Data Row: 1069   Total Pages: 22   Display: Page     
Sort: [Click the result table header to sort]
#SubstanceActivityBioAssayTargetLinks
OutcomeTypeValue [μM]
1
[SID103169566]
Ki 1.4e-05Antagonistic activity against estrogen receptor beta in presence of 0.1 nM estradiol [AID254433, Type: Literature]Estrogen receptor beta [gi:6166154]
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2
[SID103169566]
EC50 3e-05Effective dose for [3H]- estradiol against proliferation of MCF-7 cells [AID102435, Type: Literature]
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3
[SID103169566]
Ki 4e-05Antagonistic activity against estrogen receptor alpha in presence of 0.1 nM estradiol [AID254436, Type: Literature]Estrogen receptor [gi:544257]
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4
[SID103169566]
EC50 0.00012Effective concentration against MCF-7 breast tumor cells using MCF-7 assay. [AID103375, Type: Literature]
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5
[SID103169566]
Ki 0.00016In vitro displacement of 0.5 nM [3H]17-beta-estradiol from human Estrogen receptor beta [AID70164, Type: Literature]Estrogen receptor beta [gi:6166154]
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6
[SID103169566]
Ki 0.000249Inhibition of estradiol binding to estrogen receptor in Human Breast cancer cytosol (3.3% ethanol) [AID68906, Type: Literature]Estrogen receptor beta [gi:6166154]
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7
[SID103169566]
Ki 0.000249Inhibition of estradiol binding to estrogen receptor in Human Breast cancer cytosol (3.3% ethanol) [AID68906, Type: Literature]Estrogen receptor [gi:544257]
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8
[SID103169566]
Ki 0.00025In vitro displacement of 0.5 nM [3H]17-beta-estradiol from human Estrogen receptor alpha [AID70002, Type: Literature]Estrogen receptor [gi:544257]
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9
[SID103169566]
Ki 0.000346Apparent inhibition constant for estrogen receptor in Human uterine cytosol in 3.3%ethanol [AID68909, Type: Literature]Estrogen receptor [gi:544257]
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10
[SID103169566]
Ki 0.000346Apparent inhibition constant for estrogen receptor in Human uterine cytosol in 3.3%ethanol [AID68909, Type: Literature]Estrogen receptor beta [gi:6166154]
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11
[SID103169566]
Ki 0.00039Displacement of [3H]estradiol from ERalpha after 4 hrs by scintillation counting [AID669588, Type: Literature]
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12
[SID103169566]
IC50 0.0005Antiproliferative activity against human MCF7 cells [AID658133, Type: Literature]
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13
[SID103169566]
IC50 0.0005Antagonism of estrogen action in a mammary tumor cell line was assayed via inhibition of MCF-7 cell proliferation stimulated by 10 e-11 M 17-beta-estradiol (in vitro) [AID103888, Type: Literature]
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14
[SID103169566]
IC50 0.0005Inhibition of estrogen-stimulated MCF-7 cell proliferation [AID102593, Type: Literature]
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15
[SID103169566]
IC50 0.00117Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells [AID103267, Type: Literature]
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16
[SID103169566]
Ki 0.0017Binding affinity towards human estrogen receptor beta in a competitive binding assay using fluorescently labelled estradiol [AID254435, Type: Literature]Estrogen receptor beta [gi:6166154]
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17
[SID103169566]
IC50 0.0019Ability to inhibit release of interleukin-6 from U2OS cell lines transfected with estrogen receptor alpha [AID214256, Type: Literature]
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18
[SID103169566]
IC50 0.002Displacement of [3H]estradiol from ERalpha [AID260520, Type: Literature]Estrogen receptor [gi:544257]
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19
[SID103169566]
IC50 0.0025In vitro inhibition of MCF-7 cell proliferation compared to 0.1 nM [3H]-estradiol. [AID102602, Type: Literature]
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20
[SID103169566]
IC50 0.003Anti-estrogenicity for 50% inhibition of the MVLN cell luciferase activity due to 0.1 nM E2 (estradiol) [AID106081, Type: Literature]
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21
[SID103169566]
Ki 0.0057Binding affinity towards human estrogen receptor alpha in a competitive binding assay using fluorescently labelled estradiol [AID254437, Type: Literature]Estrogen receptor [gi:544257]
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22
[SID103169566]
EC50 0.006In vitro displacement of 3 nM [3H]4-hydroxytamoxifen from estrogen receptor of rat uterine cystol [AID69376, Type: Literature]Estrogen receptor [gi:119600]
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23
[SID103169566]
EC50 0.006In vitro displacement of 3 nM [3H]4-hydroxytamoxifen from estrogen receptor of rat uterine cystol [AID69376, Type: Literature]Estrogen receptor beta [gi:6166156]
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24
[SID103169566]
IC50 0.007Inhibition of estradiol induced estrogen receptor transcriptional activation in MCF-7-2a cells [AID103082, Type: Literature]Estrogen receptor beta [gi:6166154]
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25
[SID103169566]
IC50 0.007Inhibition of estradiol induced estrogen receptor transcriptional activation in MCF-7-2a cells [AID103082, Type: Literature]Estrogen receptor [gi:544257]
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26
[SID144208141]
Ratio Potency (uM) 0.00840245qHTS assay to identify small molecule antagonists of the estrogen receptor alpha (ER-alpha) signaling pathway: Summary [AID743078, Type: summary]estrogen nuclear receptor alpha [Homo sapiens] [gi:348019627]
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27
[SID103169566]
IC50 0.0085Inhibitory concentration against MCF-7 breast tumor cells using MCF-7 assay. [AID103376, Type: Literature]
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28
[SID103169566]
IC50 0.0085Antiproliferative activity against human MCF7 cells after 24 hrs by MTS assay [AID392053, Type: Literature]
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29
[SID103169566]
IC50 0.0103Inhibitory concentration against estrogen receptor alpha using estrogen response element (ERE) assay. [AID70338, Type: Literature]
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30
[SID103169566]
IC50 0.013Displacement of [3H]4-OHT from ERRgamma [AID260519, Type: Literature]Estrogen-related receptor gamma [gi:50402102]
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31
[SID103169566]
EC50 0.015Estrogen-Related Receptor gamma activity in FRET assay [AID246440, Type: Literature]Estrogen-related receptor gamma [gi:50402102]
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32
[SID103169566]
EC50 0.0157Binding affinity for Estrogen receptor alpha [AID69862, Type: Literature]Estrogen receptor [gi:544257]
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33
[SID103169566]
IC50 0.017Inhibitory concentration against estrogen receptor alpha using radioligand binding assay. [AID70339, Type: Literature]
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34
[SID103169566]
IC50 0.02Displacement of fluorescein labeled estradiol from human recombinant ERbeta expressed in baculovirus infected insect cells by fluorescence polarization assay [AID344798, Type: Literature]Estrogen receptor beta [gi:6166154]
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35
[SID103169566]
IC50 0.02Inhibition of interaction between ERRgamma and NR cofactor RIP140 in FRET assay [AID260522, Type: Literature]Estrogen-related receptor gamma [gi:50402102]
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36
[SID103169566]
IC50 0.021Inhibitory concentration against estrogen receptor 2 using radioligand binding assay. [AID70031, Type: Literature]
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37
[SID144208141]
Potency-Replicate_1 0.0217qHTS assay to identify aromatase inhibitors [AID743083, Type: confirmatory]cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_a [Homo sapiens] [gi:119597822]
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38
[SID103169566]
IC50 0.024Antiproliferative activity against MCF-7 cell line [AID103897, Type: Literature]
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39
[SID103169566]
IC50 0.0291Cytotoxicity against human MCF7 cells after 5 days [AID673828, Type: Literature]
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40
[SID103169566]
IC50 0.032Inhibitory concentration against estrogen receptor 2 using estrogen response element (ERE) assay. [AID70030, Type: Literature]
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41
[SID103169566]
IC50 0.04Displacement of fluorescein labeled estradiol from human recombinant ERalpha expressed in baculovirus infected insect cells by fluorescence polarization assay [AID344797, Type: Literature]Estrogen receptor [gi:544257]
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42
[SID103169566]
IC50 0.044Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis [AID498478, Type: Literature]Phospholipase D2 [gi:13124441]
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43
[SID144208141]
ER Potency (uM) 0.0545925qHTS assay to identify small molecule antagonists of the estrogen receptor alpha (ER-alpha) signaling pathway using the BG1 cell line: Summary [AID743091, Type: summary]estrogen nuclear receptor alpha [Homo sapiens] [gi:348019627]
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44
[SID144208141]
Potency-Replicate_1 0.0687qHTS assay to identify small molecule antagonists of the estrogen receptor alpha (ER-alpha) signaling pathway using the BG1 cell line [AID743080, Type: confirmatory]estrogen nuclear receptor alpha [Homo sapiens] [gi:348019627]
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45
[SID103169566]
IC50 0.107Antiproliferative activity against estrogen receptor dependent human MCF7 cells after 72 hrs by MTT assay [AID344791, Type: Literature]
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46
[SID103169566]
IC50 0.21Cytotoxicity against human T47D cells after 5 days [AID673829, Type: Literature]
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47
[SID144208141]
Potency-Replicate_1 0.4336qHTS assay for identifying genotoxic compounds that show differential cytotoxicity against isogenic chicken DT40 cell lines with known DNA damage response pathways - Rev3 mutant cell line [AID743014, Type: confirmatory]
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48
[SID144208141]
Potency-Replicate_1 1.0893qHTS assay for identifying genotoxic compounds that show differential cytotoxicity against isogenic chicken DT40 cell lines with known DNA damage response pathways - Rad54/Ku70 mutant cell line [AID743015, Type: confirmatory]
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49
[SID56422185]
AbsAC40_uM 2.41MLPCN PGC1a Modulators Measured in Cell-Based System Using Plate Reader - 2139-01_Activator_Dose_CherryPick_Activity_Set6 [AID720513, Type: confirmatory]
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50
[SID103169566]
IC50 2.7Antiproliferative activity against human MCF7 cells assessed as incorporation of [methyl-3H]thymidine into cellular DNA in serum free medium in in absence of 6.2 ug/mL RNase 1 [AID711887, Type: Literature]
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