MCF7 |
Antiproliferative assay |
0.625 nM |
24 hrs |
Antiproliferative activity against human MCF7 cells at 0.625 nM after 24 hrs by MTS assay |
18272256 |
MCF7 |
Antiproliferative assay |
0.625 to 10 nM |
24 hrs |
Antiproliferative activity against human MCF7 cells at >0.625 to 10 nM after 24 hrs by MTS assay |
18272256 |
MCF7:WS8 |
Antiestrogenic assay |
1 uM |
7 days |
Antiestrogenic activity in human ERalpha expressing MCF7:WS8 cells assessed as inhibition of estradiol-induced proliferation at 1 uM after 7 days |
20334368 |
MCF7 |
Function assay |
1 μM |
6 days |
Drug uptake in human MCF7 cells at 10'-6 M after 6 days by HPLC-MS/MS analysis |
23864928 |
MCF7 |
Function assay |
10 uM |
6 hrs |
Upregulation of ERalpha protein levels in human MCF7 cells at 10 uM after 6 hrs by Western blot method |
24332630 |
MCF7:WS8 |
Function assay |
1 μM |
48 hrs |
Agonist activity at ER in human MCF7:WS8 cells assessed as pS2 gene expression at 10'-6 M after 48 hrs by RT-PCR analysis |
24805199 |
MCF7:WS8 |
Function assay |
1 μM |
48 hrs |
Agonist activity at ER in human MCF7:WS8 cells assessed as GREB1 gene expression at 10'-6 M after 48 hrs by RT-PCR analysis |
24805199 |
GH3 |
Function assay |
1 μM |
48 hrs |
Antagonist activity at ER in rat GH3 cells assessed as inhibition of estradiol-induced prolactin gene expression at 10'-6 M after 48 hrs by RT-PCR analysis |
24805199 |
GH3 |
Function assay |
0.1 nM to 1 μM |
48 hrs |
Antagonist activity at ER in rat GH3 cells assessed as inhibition of estradiol-induced prolactin gene expression at 10'-10 to 10'-6 M after 48 hrs by RT-PCR analysis |
24805199 |
MCF7 |
Anticancer assay |
250 to 500 nM |
5 days |
Anticancer against human ER-positive MCF7 cells assessed as inhibition of estradiol-induced cell proliferation at 250 to 500 nM after 5 days |
24946145 |
MCF7 |
Function assay |
5 uM |
24 hrs |
Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of MYC mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis |
30078609 |
MCF7 |
Function assay |
5 uM |
24 hrs |
Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of TFF1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis |
30078609 |
MCF7 |
Function assay |
5 uM |
24 hrs |
Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of GREB1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis |
30078609 |
MCF7 |
Function assay |
5 uM |
24 hrs |
Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of MYBL2 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis |
30078609 |
MCF7 |
Function assay |
5 uM |
24 hrs |
Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of CCND1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis |
30078609 |
MCF7 |
Function assay |
5 uM |
24 hrs |
Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of CDC6 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis |
30078609 |
MCF7 |
Function assay |
5 uM |
24 hrs |
Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of E2F1 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis |
30078609 |
MCF7 |
Function assay |
5 uM |
24 hrs |
Antagonist activity at ERalpha in human MCF7 cells assessed as suppression of MKI67 mRNA expression at 5 uM after 24 hrs by QIAzol reagent based RT-qPCR analysis |
30078609 |
BT-20 |
Function assay |
10 μM |
|
Inhibitory activity against proliferation of BT-20 cells in presence of TPE at 10e-5 M concentration, IC30 = 4.8 μM. |
2769681 |
HEK293 |
Function assay |
|
1 hr |
Antagonist activity at recombinant human ERalpha expressed in HEK293 cells assessed as inhibition of estradiol-induced YFP-fused SRC1 coactivator recruitment measured after 1 hr in presence of Coelenterazine H by BRET assay, IC50 = 0.07 μM. |
30078609 |
HEK293 |
Function assay |
|
30 mins |
Inhibition of GFP-tagged human PLD2 expressed in human HEK293 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis, IC50 = 0.044 μM. |
19136975 |
GT1-7 |
Function assay |
|
20 to 24 hrs |
Antagonist activity at estrogen receptor in mouse GT1-7 cells harboring beta-galactosidase reporter gene assessed as reduction in 17beta-estradiol induced response measured after 20 to 24 hrs by luciferase reporter gene assay, IC50 = 0.0332 μM. |
28400239 |
MCF7 |
Cytotoxicity assay |
|
5 days |
Cytotoxicity against human MCF7 cells after 5 days, IC50 = 0.0291 μM. |
23864928 |
Ishikawa cells |
Function assay |
|
72 hrs |
Antagonist activity at estrogen receptor alpha/beta in human Ishikawa cells after 72 hrs by alkaline phosphatase assay, IC50 = 0.01 μM. |
28426931 |
MCF7 |
Antiproliferative assay |
|
24 hrs |
Antiproliferative activity against human MCF7 cells after 24 hrs by MTS assay, IC50 = 0.0085 μM. |
18272256 |
Rosetta 2 DE3 |
Function assay |
|
1 hr |
Displacement of [3H]-estradiol from recombinant human N-terminal His-tagged ERalpha LBD harboring C381S/C417S/C530S mutant expressed in Rosetta 2 DE3 competent cells after 1 hr by SPA binding assay, IC50 = 0.004 μM. |
28296398 |
MCF7 |
Function assay |
|
24 hrs |
Antagonist activity at ERalpha in human MCF7 cells assessed as inhibition of estrogen-induced transcription preincubated overnight followed by estrogen addition measured after 24 hrs by dual luciferase reporter gene assay, IC50 = 0.003 μM. |
28296398 |
MCF7 |
Function assay |
|
4 hrs |
Induction of ERalpha degradation in human MCF7 cells in phenol red free RPMI medium containing 5% charcoal dextran-treated FBS incubated for 4 hrs by SP1 and anti-ER rabbit monocolnal antibody based in-cell Western assay, Activity = 0.0001 μM. |
30086626 |
MCF7 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against estrogen receptor dependent human MCF7 cells after 72 hrs by MTT assay, IC50 = 0.107 μM. |
18835176 |
MCF7 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MCF7 cells after 72 hrs by trypan blue assay, GI50 = 0.107 μM. |
23735829 |
MCF7 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against ER-dependent human MCF7 cells after 72 hrs by MTT assay, IC50 = 0.11 μM. |
28426931 |
T47D |
Cytotoxicity assay |
|
5 days |
Cytotoxicity against human T47D cells after 5 days, IC50 = 0.21 μM. |
23864928 |
CV1 |
Function assay |
|
45 hrs |
Inverse agonist activity at GAL4-DNA binding domain-fused mouse ERRgamma ligand binding domain expressed in African green monkey CV1 cells assessed as decrease in receptor transcriptional activity after 45 hrs by luciferase reporter gene assay, IC50 = 0.6 μM. |
28189393 |
CV1 |
Function assay |
|
45 hrs |
Inverse agonist activity at GAL4-DNA binding domain-fused human ERRbeta ligand binding domain expressed in African green monkey CV1 cells assessed as decrease in receptor transcriptional activity after 45 hrs by luciferase reporter gene assay, IC50 = 0.65 μM. |
28189393 |
MCF7 |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50 = 1.41254 μM. |
21513275 |
MCF7 |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50 = 1.90546 μM. |
21513275 |
HeLa |
Function assay |
|
4.5 hrs |
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay, IC50 = 1.96 μM. |
29624387 |
MDA-MB-231 |
Cytotoxicity assay |
|
4 days |
Cytotoxicity against ER negative human MDA-MB-231 cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay, IC50 = 2.5 μM. |
30078609 |
MCF7 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 2.79 μM. |
26896706 |
MCF12A |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50 = 3.23594 μM. |
21513275 |
MCF7 |
Cytotoxicity assay |
|
4 days |
Cytotoxicity against ER positive human MCF7 cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay, IC50 = 3.3 μM. |
30078609 |
MCF12A |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50 = 3.31131 μM. |
21513275 |
MCF7 |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against human MCF7 cells expressing estrogen receptor incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50 = 3.46737 μM. |
21513275 |
MDA-MB-231 |
Cytotoxicity assay |
|
4 days |
Cytotoxicity against ER negative human MDA-MB-231 cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay, IC50 = 3.5 μM. |
30078609 |
MCF12A |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against estrogen receptor-deficient human MCF12A cells incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50 = 3.89045 μM. |
21513275 |
MCF7 |
Cytotoxicity assay |
|
4 days |
Cytotoxicity against ER positive human MCF7 cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay, IC50 = 3.9 μM. |
30078609 |
MCF10A |
Cytotoxicity assay |
|
4 days |
Cytotoxicity against ER negative human MCF10A cells treated every 2 days for 4 days measured post last dose by CellTiter-Glo luminescence assay, IC50 = 4 μM. |
30078609 |
MCF10A |
Cytotoxicity assay |
|
4 days |
Cytotoxicity against ER negative human MCF10A cells treated every 2 days for 4 days measured after 7 days by CellTiter-Glo luminescence assay, IC50 = 4 μM. |
30078609 |
NCI-ADR-RES |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.003 nM of estradiol and 0.01 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of 5% fetal bovine serum, GI50 = 4.46684 μM. |
21513275 |
Calu-1 |
Function assay |
|
30 mins |
Inhibition of PLD1 in human Calu-1 cells assessed as decrease in phosphatidylbutanol-[d9] production after 30 mins by mass spectrometric analysis, IC50 = 4.8 μM. |
19136975 |
MDA-MB-231 |
Anticancer assay |
|
48 hrs |
Anticancer against human ER-positive MDA-MB-231 cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 5.4 μM. |
24946145 |
NCI-ADR-RES |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 0.06 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50 = 6.16595 μM. |
21513275 |
AU565 |
Anticancer assay |
|
48 hrs |
Anticancer against human ER-negative AU565 cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 6.2 μM. |
24946145 |
MCF7L |
Anticancer assay |
|
48 hrs |
Anticancer against human ER-positive MCF7L cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 6.3 μM. |
24946145 |
SKOV3-MDR1-M6/6 |
Anticancer assay |
|
48 hrs |
Anticancer against human SKOV3-MDR1-M6/6 cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 6.49 μM. |
24946145 |
MCF7 |
Antiproliferative assay |
|
24 hrs |
Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 7.2 μM. |
24189055 |
SKOV3 |
Anticancer assay |
|
48 hrs |
Anticancer against human SKOV3 cells overexpressing P-gp assessed as cell viability after 48 hrs by SRB assay, IC50 = 7.46 μM. |
24946145 |
PC3 |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against androgen receptor-deficient human PC3 cells incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50 = 7.58578 μM. |
21513275 |
NCI-ADR-RES |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against estrogen receptor-deficient human NCI-ADR-RES cells incubated with 100 nM of estradiol and 0.07 nM of testosterone after 48 hrs by sulforhodamine B assay in presence of fetal bovine serum and NuSerum, GI50 = 7.76247 μM. |
21513275 |
LNCAP |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against human LNCAP cells expressing androgen receptor incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50 = 8.31764 μM. |
21513275 |
MCF7 |
Antiproliferative assay |
|
5 days |
Antiproliferative activity against human MCF7 cells after 5 days by WST-8 assay, IC50 = 8.9 μM. |
25614118 |
MCF7 |
Anticancer assay |
|
48 hrs |
Anticancer against human ER-positive MCF7 cells assessed as cell viability after 48 hrs by SRB assay, IC50 = 9.2 μM. |
24946145 |
MDA-MB-231 |
Antiproliferative assay |
|
24 hrs |
Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 10.4 μM. |
24189055 |
MDA-MB-453 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MDA-MB-453 cells after 72 hrs by MTT assay, IC50 = 10.4 μM. |
28506582 |
DU145 |
Antiproliferative assay |
|
48 hrs |
Antiproliferative activity against androgen receptor-deficient human DU145 cells incubated with 0.6 nM of estradiol and 0.7 nM of testosterone after 48 hrs by sulforhodamine B assay, GI50 = 10.7152 μM. |
21513275 |
MCF7 |
Cytotoxicity assay |
|
48 hrs |
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 13.6 μM. |
25618595 |
Vero |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against african green monkey Vero cells assessed as inhibition of cell viability after 72 hrs by MTT assay, IC50 = 15.1 μM. |
25993269 |
DU145 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human DU145 cells assessed as inhibition of cell viability after 72 hrs by MTT assay, IC50 = 15.3 μM. |
25993269 |
MCF7 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 15.6 μM. |
28506582 |
MCF7 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay, IC50 = 15.6 μM. |
25993269 |
MDA-MB-231 |
Antiproliferative assay |
|
72 hrs |
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay, IC50 = 20.1 μM. |
28506582 |
MDA-MB-231 |
Cytotoxicity assay |
|
3 days |
Cytostatic activity against human MDA-MB-231 cells after 3 days by microtiter assay |
20598555 |
insect cells |
Function assay |
|
|
Displacement of fluorescein labeled estradiol from human recombinant ERalpha expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.04 μM. |
18835176 |
insect cells |
Function assay |
|
|
Displacement of fluorescein labeled estradiol from human recombinant ERbeta expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.02 μM. |
18835176 |
MCF7 |
Function assay |
|
|
Inhibitory concentration against MCF-7 breast tumor cells using MCF-7 assay, IC50 = 0.0085 μM. |
12825935 |
MCF-7-2a |
Function assay |
|
|
Inhibition of estradiol induced estrogen receptor transcriptional activation in MCF-7-2a cells, IC50 = 0.007 μM. |
12672249 |
insect cells |
Function assay |
|
|
Inhibition of fluormone ES2 green binding to recombinant full length human ERalpha expressed in insect cells by fluorescence polarization assay, IC50 = 0.00629 μM. |
28735214 |
MCF7 |
Function assay |
|
|
Inhibition of estrogen-induced proliferation in human MCF-7 breast cancer cells, IC50 = 0.00117 μM. |
9154963 |
MCF |
Function assay |
|
|
Antagonist activity at progesterone receptor in human MCF cells assessed as estradiol-induced receptor response, IC50 = 0.0007943 μM. |
26407012 |
Ishikawa endometrial cells |
Function assay |
|
|
Agonist activity as alkaline phosphatase induction in Ishikawa endometrial cells compared to E2, EC50 = 0.0008 μM. |
15380208 |
MCF7 |
Antiproliferative assay |
|
|
Antiproliferative activity against human MCF7 cells, IC50 = 0.000537 μM. |
26407012 |
MCF7 |
Function assay |
|
|
Effective concentration against MCF-7 breast tumor cells using MCF-7 assay, EC50 = 0.00012 μM. |
12825935 |
MCF7 |
Antiproliferative assay |
|
|
Antiproliferative activity against human MCF7 cells, IC50 = 0.0005 μM. |
22405286 |
MCF7 |
Function assay |
|
|
Effective dose for [3H]- estradiol against proliferation of MCF-7 cells, EC50 = 0.00003 μM. |
2769681 |
MCF7 cells |
Proliferation assay |
|
|
Inhibition of estrogen-stimulated MCF-7 cell proliferation, IC50=0.5 nM |
9548817 |
Ishikawa endometrial cells |
Function assay |
|
|
Antagonist activity as inhibition of 1 nM 17-beta-estradiol stimulated alkaline phosphatase induction in Ishikawa endometrial cells, IC50 = 0.51 μM. |
15380208 |
HEK293 |
Function assay |
|
|
Agonist activity at human estrogen related receptor gamma expressed in HEK293 cells by luciferase reporter gene assay, IC50 = 1.35 μM. |
25305688 |
MCF7 |
Antiproliferative assay |
|
|
Antiproliferative 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, IC50 = 2.7 μM. |
22611478 |
MCF7 |
Function assay |
|
|
Inhibitory activity against proliferation of MCF-7 cells in presence of 10e-6 M concentration of [3H]- estradiol (E2), IC30 = 4 μM. |
2769681 |
yeast cells |
Antiestrogenic assay |
|
|
Antiestrogenic activity at estrogen receptor alpha expressed in yeast cells assessed as inhibition of 17-beta-estradiol-induced beta-galactosidase activity by two hybrid assay, IC50 = 4.4 μM. |
16441086 |
MCF7 |
Function assay |
|
|
Antagonist activity at ERalpha receptor in human MCF7 cells, IC50 = 4.89779 μM. |
26407012 |
MCF-7 |
Cytotoxicity assay |
|
|
Cytotoxicity against MCF-7 cells in the absence of 1 uM E2 (estradiol), Cytotoxicity = 6 μM. |
9089332 |
MCF-7 |
Cytotoxicity assay |
|
|
Cytostaticity against MCF-7 cells in the presence of 1 uMolar E2 (estradiol), IC50 = 8 μM. |
9089332 |
MCF-7 |
Cytotoxicity assay |
|
|
Cytotoxicity against MCF-7 cells in presence of 1 uM E2 (estradiol), Cytotoxicity = 9.4 μM. |
9089332 |
MCF7:WS8 |
Function assay |
|
|
Activation of human ER in human MCF7:WS8 cells expressing estrogen responsive element by luciferase reporter gene assay |
20334368 |
MCF7 |
Antiestrogenic assay |
|
|
Antiestrogenic activity in human MCF7 cells assessed as inhibition of estradiol-stimulated prolactin gene expression |
20334368 |
MCF7 |
Antiestrogenic assay |
|
|
Antiestrogenic activity in human MCF7 cells assessed as inhibition of estradiol-stimulated proliferation |
20334368 |
T47D:C:4:2 |
Function assay |
|
|
Estrogenic activity at wild type ER alpha expressed in T47D:C:4:2 cells coexpressing estrogen response element by duel luciferase reporter gene assay |
20334368 |
T47D:C:4:2 |
Function assay |
|
|
Estrogenic activity at wild type ER alpha D351G mutant expressed in T47D:C:4:2 cells coexpressing estrogen response element by duel luciferase reporter gene assay |
20334368 |