|
Displacement of [3H]tamoxifen from antiestrogen binding site (AEBS)
|
Homo sapiens
|
12.0
nM
|
|
|
Binding affinity towards antiestrogen binding site AEBS
|
None
|
1.0
nM
|
|
|
Percent of inhibitory activity against proliferation of BT-20 cells in presence of TPE at 10e-5 M concentration.
|
Homo sapiens
|
56.0
%
|
|
|
Inhibition of Calmodulin activation of cyclic nucleotide phosphodiesterase
|
Homo sapiens
|
44.0
%
|
|
|
Inhibition of [3H]thymidine incorporation into EL4 cell proliferation
|
Mus musculus
|
535.0
nM
|
|
|
Antiestrogenic activity in MCF-7-2a cells as concentration required to reduce estradiol effect by 50%
|
Homo sapiens
|
500.0
nM
|
|
|
Antiproliferative activity against estrogen receptor positive MCF-7 human breast cancer cell line at a dose of 10e-5 M. (p<0.05)
|
None
|
71.9
%
|
|
|
Antiproliferative activity against estrogen receptor positive MCF-7 human breast cancer cell line at a dose of 10e-7 M. (p<0.05)
|
None
|
51.8
%
|
|
|
Antiproliferative activity against estrogen receptor positive MCF-7 human breast cancer cell line at 10e-9 M. (p<0.05)
|
Homo sapiens
|
20.5
%
|
|
|
Binding affinity for estrogen receptor
|
Homo sapiens
|
157.0
nM
|
|
|
Inhibition of estradiol binding to estrogen receptor in Human Breast cancer cytosol (3.3% ethanol)
|
Homo sapiens
|
11.9
nM
|
|
|
Apparent inhibition constant for estrogen receptor in Human uterine cytosol in 3.3%ethanol
|
Homo sapiens
|
34.4
nM
|
|
|
Inhibitory concentration against estrogen receptor alpha using estrogen response element (ERE) assay.
|
None
|
622.0
nM
|
|
|
Displacement of [3H]17-beta-estradiol from human estrogen receptor alpha
|
Homo sapiens
|
42.0
nM
|
|
|
Displacement of radioligand from Estrogen receptor alpha
|
None
|
8.4
nM
|
|
|
Concentration of compound required to induce 50 % of the maximum stimulation of alkaline phosphatase activity in Ishikawa cells
|
Homo sapiens
|
33.0
nM
|
|
|
Inhibition of estrogen receptor positive MCF-7 human breast cancer cell proliferation
|
Homo sapiens
|
150.0
nM
|
|
|
Inhibition of estrogen receptor positive MCF-7 breast cancer cell proliferation
|
Homo sapiens
|
70.0
nM
|
|
|
Percent inhibition of estrogen receptor positive MCF-7 human breast cancer cell proliferation at 10e-7 M
|
Homo sapiens
|
52.0
%
|
|
|
Inhibition of estrogen receptor negative MDA-MB-231 breast cancer cell proliferation
|
Homo sapiens
|
80.0
nM
|
|
|
Effective dose for [3H]- estradiol against proliferation of MCF-7 cells
|
Homo sapiens
|
0.11
nM
|
|
|
Antagonist effect in breast tissue was assayed by inhibition of estrogen stimulated MCF-7 cell proliferation
|
None
|
530.0
nM
|
|
|
In vitro inhibition of MCF-7 cell proliferation compared to 0.1 nM [3H]-estradiol.
|
Homo sapiens
|
219.0
nM
|
|
|
Percent of inhibitory activity against proliferation of MCF-7 cells in presence of 10e-6 M concentration of [3H]estradiol (E2).
|
Homo sapiens
|
49.0
%
|
|
|
Percent of inhibitory activity versus 0.1 nm [3H]estradiol against proliferation of MCF-7 cells.
|
Homo sapiens
|
90.0
%
|
|
|
Inhibition of estradiol induced estrogen receptor transcriptional activation in MCF-7-2a cells
|
Homo sapiens
|
500.0
nM
|
|
|
Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells
|
Homo sapiens
|
481.0
nM
|
|
|
Effective concentration against MCF-7 breast tumor cells using MCF-7 assay.
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibitory concentration against MCF-7 breast tumor cells using MCF-7 assay.
|
Homo sapiens
|
580.0
nM
|
|
|
Cytostatic activity against MCF-7 cell proliferation.
|
Homo sapiens
|
49.0
%
|
|
|
Anti-proliferative activity against estrogen-responsive human breast cancer cell line MCF-7 in the presence of ER at a 10e-4 uM concentration of estradiol
|
Homo sapiens
|
140.0
nM
|
|
|
Inhibition of 17-beta-estradiol (10e-11 M) mediated MCF-7 cell proliferation
|
Homo sapiens
|
904.0
nM
|
|
|
Inhibition of MDA-MB-435 breast cancer cell proliferation
|
Homo sapiens
|
50.0
nM
|
|
|
Anti-estrogenicity for 50% inhibition of the MVLN cell luciferase activity due to 0.1 nM E2 (estradiol)
|
Homo sapiens
|
300.0
nM
|
|
|
Inhibition of estradiol-induced uterine weight gain in ovariectomized BALB/c mice at 20 ug dose twice daily
|
Mus musculus
|
3.0
%
|
|
|
Inhibition of estradiol-induced uterine weight gain in ovariectomized BALB/c mice at 3 ug dose twice daily; nonsignificant
|
Mus musculus
|
7.0
%
|
|
|
Antiestrogenic effect in immature mouse at a dose of 1 ug.
|
Mus musculus
|
0.0
%
|
|
|
Antiestrogenic effect in immature mouse at a dose of 25 ug.
|
Mus musculus
|
11.0
%
|
|
|
In vivo anti-estrogenic effect in immature mice at 5 ug
|
Mus musculus
|
0.0
%
|
|
|
In vitro estrogenic effect in immature mice at 100 ug
|
Mus musculus
|
79.0
%
|
|
|
In vitro estrogenic effect in immature mice at 10 ug
|
Mus musculus
|
100.0
%
|
|
|
In vitro estrogenic effect in immature mice at 1 ug
|
Mus musculus
|
43.0
%
|
|
|
In vivo inhibition of hormone-dependent MXT mammary tumor in mice
|
Mus musculus
|
9.8
%
|
|
|
In vivo inhibition of uterine growth in hormone-dependent MXT mammary tumor bearing mice
|
Mus musculus
|
87.0
%
|
|
|
Concentration giving half of the maximal ATPase activity calculated for the high-affinity binding site of the CHO P-Glycoprotein (P-gp) in two-affinity model
|
Cricetulus griseus
|
100.0
nM
|
|
|
Percent stimulation or inhibition of protein kinase C III activity for phosphatidylserine (PS) in the presence of [Ca2+].
|
Rattus norvegicus
|
49.0
%
|
|
|
Percent stimulation or inhibition of protein kinase C III activity for protamine sulfate in the presence of EGTA.
|
Rattus norvegicus
|
107.0
%
|
|
|
Percent stimulation or inhibition of protein kinase C with [Ca2+] for phosphatidylserine and diolein(PS+DO)
|
Rattus norvegicus
|
21.0
%
|
|
|
Percent inhibition of estradiol stimulated uterine growth in rats
|
Rattus norvegicus
|
37.0
%
|
|
|
Affinity for sigma receptor type 1 of guinea pig using [3H]ifenprodil or (+)-[3H]pentazocine radioligand
|
Cavia porcellus
|
35.0
nM
|
|
|
Affinity for human EMP expressed in ERG2 deficient strain of Saccharomyces cerevisiae using [3H]ifenprodil or (+)-[3H]pentazocine as radioligand
|
Homo sapiens
|
5.0
nM
|
|
|
Inhibition of 17-beta-estradiol mediated luciferase transcription in HeLa cells expressing human estrogen receptor alpha; ERE assay
|
Homo sapiens
|
622.0
nM
|
|
|
Inhibition of estrogen-mediated human breast adenocarcinoma (MCF-7) cell proliferation
|
Homo sapiens
|
580.0
nM
|
|
|
Antagonist activity at ER receptor assessed as inhibition of 17-alpha-ethynylestradiol-induced increase in uterine weight of Sprague-Dawley rat at 3 mg/kg/day, po
|
Rattus norvegicus
|
49.0
%
|
|
|
Growth inhibition of human HL60 cells after 4 hrs by MTT assay
|
Homo sapiens
|
5.9
ug.mL-1
|
|
|
Displacement of fluorescein labeled estradiol from human recombinant ERalpha expressed in baculovirus infected insect cells by fluorescence polarization assay
|
Homo sapiens
|
70.0
nM
|
|
|
Displacement of fluorescein labeled estradiol from human recombinant ERbeta expressed in baculovirus infected insect cells by fluorescence polarization assay
|
Homo sapiens
|
170.0
nM
|
|
|
Antiestrogenic activity in human Ishikawa cells assessed as inhibition of estrogen-induced alkaline phosphatase activity after 72 hrs
|
Homo sapiens
|
170.0
nM
|
|
|
Cytotoxicity against human HT-29 cells by alamar blue assay
|
Homo sapiens
|
1.86
ug.mL-1
|
|
|
Cytotoxicity against human A549 cells by alamar blue assay
|
Homo sapiens
|
1.86
ug.mL-1
|
|
|
Cytotoxicity against human SK-MEL-28 cells by alamar blue assay
|
Homo sapiens
|
1.86
ug.mL-1
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
72.1
%
|
|
|
Antiproliferative activity against human MCF7 cells after 24 hrs by MTS assay
|
Homo sapiens
|
580.0
nM
|
|
|
Antiestrogenic activity in human T47D cells expressing estrogen receptor assessed as estrogen-dependent transcription by luciferase reporter gene assay
|
Homo sapiens
|
100.0
nM
|
|
|
Cytotoxicity against rat L6 cells
|
Rattus norvegicus
|
4.9
ug.mL-1
|
|
|
Antiestrogenic activity in human Ishikawa cells assessed as inhibition of estrogen-induced alkaline phosphatase activity after 4 days by ELISA
|
Homo sapiens
|
420.0
nM
|
|
|
Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes at 20 uM
|
Homo sapiens
|
71.0
%
|
|
|
Estrogenic antagonistic activity in bilaterally ovariectomized Sprague-Dawley rat assessed as inhibition of ethynylesterol-induced uterine weight at 10 mg/kg, po once daily for 3 days measured on day 31 of age
|
Rattus norvegicus
|
27.4
%
|
|
|
Inhibition of human 17beta-HSD7 expressed in HEK293 cells assessed as inhibition of reduction of [14C]estrone into [14C]estradiol at 0.3 uM after 7 hrs
|
Homo sapiens
|
8.9
%
|
|
|
Inhibition of human 17beta-HSD7 expressed in HEK293 cells assessed as inhibition of reduction of [14C]estrone into [14C]estradiol at 3 uM after 7 hrs
|
Homo sapiens
|
3.2
%
|
|
|
Uterotropic activity in rat assessed as inhibition of estrone-stimulated uterine weight at 1 mg/kg, po QD after 3 days
|
Rattus norvegicus
|
0.0
%
|
|
|
Uterotropic activity in rat assessed as stimulation of estrone-induced uterine weight at 1 mg/kg, po QD after 3 days
|
Rattus norvegicus
|
109.0
%
|
|
|
Inhibition of PKC at 0.2 mM after 90 mins by ELISA
|
None
|
25.0
%
|
|
|
Inhibition of PKC at 0.1 mM after 90 mins by ELISA
|
None
|
14.0
%
|
|
|
Antiproliferative activity against human MCF7 cells assessed as viable cells at 100 uM after 24 hrs by MTT assay
|
Homo sapiens
|
93.33
%
|
|
|
Antiproliferative activity against human MDA-MB-231 cells by MTT assay
|
Homo sapiens
|
660.0
nM
|
|
|
Inhibition of LuxR-dependent quorum sensing in Vibrio fischeri assessed as reduction of 3-oxo-C6-HSL-induced bioluminescence intensity at 20 uM
|
Aliivibrio fischeri
|
73.6
%
|
|
|
Inhibition of LuxR-dependent quorum sensing in Vibrio fischeri assessed as reduction of 3-oxo-C6-HSL-induced bioluminescence intensity at 40 uM
|
Aliivibrio fischeri
|
53.0
%
|
|
|
Displacement of [2,4,6,7-3H]estradiol from human ERalpha expressed in HeLa cells after 18 hrs by liquid scintillation counting
|
Homo sapiens
|
31.19
nM
|
|
|
Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
|
Homo sapiens
|
8.31
ug.mL-1
|
|
|
Mechanism based inhibition of human cytochrome P450 3A4 measured by testosterone 6-beta hydroxylation
|
Homo sapiens
|
200.0
nM
|
|
|
Mechanism based inhibition of human cytochrome P450 2B6 measured by 7-EFC O-deethylation
|
Homo sapiens
|
900.0
nM
|
|
|
Antiestrogenic activity in Sprague-Dawley rat assessed as inhibition of uterine weight gain administered as po daily once for 3 days relative to 17alpha-ethynylestradiol
|
Rattus norvegicus
|
49.0
%
|
|
|
DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
681.0
nM
|
|
|
DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
630.0
nM
|
|
|
DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine)
|
None
|
672.0
nM
|
|
|
DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)
|
None
|
967.0
nM
|
|
DRUGMATRIX: Potassium Channel HERG radioligand binding (ligand: [3H] Astemizole)
|
None
|
792.2
nM
|
|
|
DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)
|
None
|
726.0
nM
|
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
460.0
nM
|
|
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)
|
None
|
241.0
nM
|
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
None
|
21.0
nM
|
|
DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)
|
None
|
8.714
nM
|
|
|
DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
|
Rattus norvegicus
|
619.0
nM
|
|
DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil)
|
Rattus norvegicus
|
381.0
nM
|
|
|
DRUGMATRIX: Thromboxane Synthetase enzyme inhibition (substrate: PGH2)
|
Homo sapiens
|
916.0
nM
|
|
|
DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)
|
None
|
364.0
nM
|
|
|
Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay
|
Homo sapiens
|
27.0
nM
|
|
|
Displacement of [3H]estradiol from ERbeta after 4 hrs by scintillation counting
|
None
|
0.51
nM
|
|
|
Cytotoxicity against human MCF7 cells after 5 days
|
Homo sapiens
|
794.0
nM
|
|
|
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability at 100 uM after 24 hrs by MTT assay
|
Homo sapiens
|
93.3
%
|
|
|
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical)(Digoxin: 5 uM, Tamoxifen: 100 uM) in Caco-2 cells
|
None
|
86.0
%
|
|
|
Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting
|
Homo sapiens
|
25.6
%
|
|
|
Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
28.5
%
|
|
|
Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting
|
Homo sapiens
|
11.0
%
|
|
|
Binding affinity to emopamil binding protein (unknown origin)
|
Homo sapiens
|
2.8
nM
|
|
|
Antagonist activity at ERalpha receptor in human MCF7 cells assessed as inhibition of cell growth after 6 days by crystal violet staining method
|
Homo sapiens
|
200.0
nM
|
|
|
Antagonist activity at Gal4 DBD-fused human ERalpha LBD expressed in HEK293T cells assessed as inhibition of estradiol-induced transcriptional activation after 20 hrs by luciferase reporter gene assay
|
Homo sapiens
|
39.0
nM
|
|
|
Antiproliferative activity against human MCF7 cells
|
Homo sapiens
|
10.0
ug.mL-1
|
|
|
Displacement of fluorescent estrogen from recombinant ERalpha (unknown origin) at 0.1 mg/ml by competition binding assay
|
Homo sapiens
|
100.0
%
|
|
|
Displacement of fluorescein-labeled estrogen from human recombinant ERalpha by fluorescence polarization based competitive binding affinity assay
|
Homo sapiens
|
61.0
nM
|
|
|
Displacement of fluorescein-labeled estrogen from human recombinant ERbeta by fluorescence polarization based competitive binding affinity assay
|
Homo sapiens
|
190.0
nM
|
|
|
Binding affinity to human ERalpha
|
Homo sapiens
|
60.9
nM
|
|
|
Binding affinity to human ERbeta
|
Homo sapiens
|
188.0
nM
|
|
|
Cytotoxicity against human MCF7 cells after 48 hrs by sulforhodamine B assay
|
Homo sapiens
|
8.0
ug.mL-1
|
|
|
Inhibition of VEGF production in human MCF7 cells at cytotoxic IC50 level after 24 hrs by ELISA
|
Homo sapiens
|
98.0
%
|
|
|
Inhibition of human OATP1B1-mediated [3H]estrone 3-sulfate at 100 uM after 5 mins relative to control
|
Homo sapiens
|
16.4
%
|
|
|
Inhibition of human OATP1B3-mediated [3H]CCK-8 at 100 uM after 5 mins relative to control
|
Homo sapiens
|
38.1
%
|
|
|
Time dependent inhibition of CYP1A2 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2B6 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C9 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C19 in human liver microsomes at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2D6 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP3A4 (unknown origin) at 100 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Time dependent inhibition of CYP2C8 (unknown origin) at 10 uM by LC/MS system
|
Homo sapiens
|
10.0
%
|
|
|
Binding affinity to ERalpha receptor (unknown origin)
|
Homo sapiens
|
24.55
nM
|
|
|
Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor response
|
Homo sapiens
|
128.82
nM
|
|
|
Antiproliferative activity against human MCF7 cells
|
Homo sapiens
|
57.54
nM
|
|
|
Antiproliferative activity against human GBM1 cells assessed as reduction in cell viability at 10 uM incubated for 72 hrs by WST-1 method
|
Homo sapiens
|
98.4
%
|
|
|
Antiproliferative activity against human GBM2 cells assessed as reduction in cell viability at 10 uM incubated for 72 hrs by WST-1 method
|
Homo sapiens
|
100.8
%
|
|
|
Antiproliferative activity against human GBM3 cells assessed as reduction in cell viability at 10 uM incubated for 72 hrs by WST-1 method
|
Homo sapiens
|
95.7
%
|
|
|
Displacement of [3H]-E2 from human ER-alpha incubated for 16 to 20 hrs by liquid scintillation counting analysis
|
Homo sapiens
|
8.0
nM
|
|
|
Displacement of [3H]-E2 from human ER-beta incubated for 16 to 20 hrs by liquid scintillation counting analysis
|
Homo sapiens
|
180.0
nM
|
|
|
Antiestrogenic activity at ER-alpha in human MCF7 cells assessed as inhibition of E2-induced progesterone receptor mRNA expression at 1 uM by RT-PCR method relative to control
|
Homo sapiens
|
70.0
%
|
|
|
Inhibition of PKC in human SH-SY5Y cells assessed as inhibition of PMA-stimulated MARCKS phosphorylation at 3 uM preincubated for 1 hr followed by PMA-stimulation for 15 mins by Western blot analysis relative to control
|
Homo sapiens
|
27.0
%
|
|
|
Inhibition of PKC in human SH-SY5Y cells assessed as inhibition of PMA-stimulated MARCKS phosphorylation at 10 uM preincubated for 1 hr followed by PMA-stimulation for 15 mins by Western blot analysis relative to control
|
Homo sapiens
|
52.0
%
|
|
|
Displacement of Fluormone ES2 Green from human recombinant full length ERalpha expressed in insect cells measured up to 4 hrs by fluorescence polarization assay
|
Homo sapiens
|
222.0
nM
|
|
|
Displacement of [3H]E2 from GST-fused ERalpha-LBD (unknown origin) expressed in Escherichia coli BL21 incubated for 1 hr by liquid scintillation counting method
|
Homo sapiens
|
226.0
nM
|
|
|
Displacement of [3H]E2 from GST-fused ERbeta-LBD (unknown origin) expressed in Escherichia coli BL21 incubated for 1 hr by liquid scintillation counting method
|
Homo sapiens
|
79.7
nM
|
|
|
Binding affinity to human ERRgamma
|
Homo sapiens
|
62.2
nM
|
|
|
Antagonist activity at full length ERalpha (unknown origin) expressed in human HeLa cells incubated for 24 hrs by ERE-driven luciferase reporter gene assay
|
Homo sapiens
|
341.0
nM
|
|
|
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
|
Ebolavirus
|
730.0
nM
|
|
|
Inhibition of fluorescent estrogen binding to full length untagged human ERalpha expressed in insect cells at 10 uM after 2 hrs by fluorescent polarization assay relative to control
|
Homo sapiens
|
50.0
%
|
|
|
Inhibition of estrogen receptor in human MCF7 cells assessed as inhibition of estradiol-induced PgR mRNA expression at 2 uM by RT-PCR method relative to control
|
Homo sapiens
|
80.0
%
|
|
|
Displacement of fluorescent estrogen ligand from recombinant human ERalpha expressed in insect cells at 10 uM incubated for 2 hrs by polarization
|
Homo sapiens
|
94.79
%
|
|
|
Inhibition of VEGFR2 protein expression in human MCF7 cells at cytotoxic IC50 after 24 hrs by ELISA relative to untreated control
|
Homo sapiens
|
98.0
%
|
|
|
Reduction in uterine wet weight in ethynyl estradiol-stimulated CD-IGS rat at 60 mg/kg, po dosed daily for 3 days by gavage followed 15 mins later by 0.1 mg/kg, po ethynyl estradiol and measured 24 hrs after last dose by immature rat uterine wet weight assay
|
Rattus norvegicus
|
78.0
%
|
|
|
Inhibition of estradiol-induced proliferation in human Ishikawa cells after 72 hrs by Cell-titer-Glo assay
|
Homo sapiens
|
7.87
ug.mL-1
|
|
|
Inhibition of estradiol-induced proliferation in human MCF7 cells after 72 hrs by Cell-titer-Glo assay
|
Homo sapiens
|
3.99
ug.mL-1
|
|
|
Inhibition of estradiol-induced proliferation in human MDA-MB-231 cells after 72 hrs by Cell-titer-Glo assay
|
Homo sapiens
|
7.85
ug.mL-1
|
|
|
Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length estrogen receptor alpha after 2 hrs by fluorescence polarization assay
|
Homo sapiens
|
70.0
nM
|
|
|
Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length estrogen receptor beta after 2 hrs by fluorescence polarization assay
|
Homo sapiens
|
170.0
nM
|
|
|
Antagonist activity at estrogen receptor alpha/beta in human Ishikawa cells after 72 hrs by alkaline phosphatase assay
|
Homo sapiens
|
280.0
nM
|
|
|
Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length untagged estrogen receptor alpha expressed in Spodoptera frugiperda by fluorescence polarization assay
|
Homo sapiens
|
60.9
nM
|
|
|
Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length untagged estrogen receptor beta expressed in insect cells by fluorescence polarization assay
|
Homo sapiens
|
188.0
nM
|
|
|
Displacement of Fluormone ES2 Green from full length human ER-alpha expressed in insect cells at 10 uM after 2 hrs by fluorescence polarization assay relative to control
|
Homo sapiens
|
92.36
%
|
|
|
Displacement of [3H]E2 from human recombinant ERalpha assessed as receptor binding after 45 mins by scintillation counting method
|
Homo sapiens
|
100.0
nM
|
|
|
Inhibition of PKC in rat brain soluble fraction at 3 uM using calf thymus H1 histone, phosphatidylserine and [gamma-32P]ATP by liquid scintillation counting method
|
Rattus norvegicus
|
27.0
%
|
|
|
Inhibition of estrogen receptor (unknown origin)
|
Homo sapiens
|
222.0
nM
|
|
|
Displacement of fluorescent estrogen ligand from recombinant human full length untagged ERalpha expressed in Spodoptera frugiperda insect cells at 20 uM measured after 2 hrs by fluorescence polarization assay relative to control
|
Homo sapiens
|
87.4
%
|
|
|
Inhibition of estrogen receptor-alpha (unknown origin) by ELISA
|
Homo sapiens
|
1.5
nM
|
|
|
Inhibition of beta-estradiol-induced estradiol receptor activation (unknown origin) at 10 uM relative to control
|
Homo sapiens
|
100.0
%
|
|
|
Displacement of fluorescent estrogen ligand from recombinant human full length untagged ERalpha expressed in baculovirus infected insect cells incubated in dark for 2 hrs by Beacon single-tube fluorescent polarization assay
|
Homo sapiens
|
70.0
nM
|
|
|
Displacement of fluorescent estrogen ligand from recombinant human full length untagged ERbeta expressed in baculovirus infected insect cells incubated in dark for 2 hrs by Beacon single-tube fluorescent polarization assay
|
Homo sapiens
|
170.0
nM
|
|
|
Antagonist activity at ERalpha (unknown origin)
|
Homo sapiens
|
60.9
nM
|
|
|
Antagonist activity at ERbeta (unknown origin)
|
Homo sapiens
|
188.0
nM
|
|
|
Antiviral activity against pseudotyped Ebola virus - Mayinga, Zaire infected in human A549 cells assessed as reduction in viral infection incubated for 48 hrs by luciferase reporter gene assay
|
Zaire ebolavirus
|
100.0
nM
|
|
|
Antiproliferative activity against human MCF-7 cells assessed as inhibition of colony formation measured after 3 weeks by crystal violet staining based soft agar colony formation assay
|
Homo sapiens
|
1.31
ug.mL-1
|
|
|
Cytotoxicity against human MCF7 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay
|
Homo sapiens
|
20.0
nM
|
|
|
Antagonist activity at estrogen receptor in human T47D cells incubated for 18 hrs by ultra high sensitivity luminescence reporter gene assay
|
Homo sapiens
|
58.0
nM
|
|
|
Antiproliferative activity against human MCF-7 cells incubated for 72 hrs by Cell-titer Glo assay
|
Homo sapiens
|
200.0
nM
|
|
|
Displacement of fluorescent labeled-ligand from ERalpha (unknown origin) by competitive binding assay
|
Homo sapiens
|
69.0
nM
|
|
