|
Percent of inhibitory activity against proliferation of BT-20 cells in presence of TPE at 10e-5 M concentration.
|
Homo sapiens
|
14.0
%
|
|
|
Affinity for estrogen receptor
|
Homo sapiens
|
0.996
nM
|
|
|
Affinity estrogen receptor of MCF-7 human mammary cancer cells
|
Homo sapiens
|
3.8
nM
|
|
|
Affinity for estrogen receptor of human MCF-7 cells
|
Homo sapiens
|
0.18
nM
|
|
|
Binding affinity for estrogen receptor, by competition with [3H]estradiol
|
None
|
1.6
nM
|
|
|
Displacement of [3H]-estradiol from estrogen receptor (ER)
|
Homo sapiens
|
3.0
nM
|
|
|
Displacement of [3H]estradiol from Estrogen receptor in MCF-7 cells
|
Homo sapiens
|
3.0
nM
|
|
|
Binding affinity for human estrogen receptor
|
Homo sapiens
|
0.38
nM
|
|
|
Apparent inhibition constant for estrogen receptor in Human Breast cancer cytosol in 2.5%DMF
|
Homo sapiens
|
0.113
nM
|
|
|
Inhibition of estradiol binding to estrogen receptor in Human Breast cancer cytosol (3.3% ethanol)
|
Homo sapiens
|
0.138
nM
|
|
|
Apparent inhibition constant for estrogen receptor in Human uterine cytosol in 2.5%DMF
|
Homo sapiens
|
0.181
nM
|
|
|
Apparent inhibition constant for estrogen receptor in Human uterine cytosol in 3.3%ethanol
|
Homo sapiens
|
0.12
nM
|
|
|
Displacement of [3H]estradiol from estrogen receptor in immature rabbit
|
Oryctolagus cuniculus
|
0.5
ug.mL-1
|
|
|
Displacement of [3H]17-beta-estradiol from Estrogen receptor of rabbit uterine tissue
|
Oryctolagus cuniculus
|
0.5
nM
|
|
|
Inhibitory activity against Estrogen receptor by displacement of [3H]17-beta-estradiol in ER-rich cytosol from rabbit uterine tissue
|
Oryctolagus cuniculus
|
0.7
nM
|
|
|
Binding affinity for estrogen receptor of rabbit uterine skeletal muscle tissue
|
Oryctolagus cuniculus
|
0.7
nM
|
|
|
Displacement of [3H]-estradiol from estrogen receptor in mature rat
|
Rattus norvegicus
|
0.5
ug.mL-1
|
|
|
In vitro displacement of [3H]estradiol from estrogen receptor of rat uterine cystol
|
Rattus norvegicus
|
5.7
nM
|
|
|
Displacement of [3H]- Estradiol from Estrogen receptor of rat uterine cytosol
|
Rattus norvegicus
|
1.8
nM
|
|
|
Inhibition of estradiol binding to estrogen receptor
|
Rattus norvegicus
|
0.354
nM
|
|
|
Relative binding affinity for sheep uterine estrogen receptor by displacement of [3H]estradiol
|
Ovis aries
|
100.0
|
|
|
Displacement of [3H]estradiol from estrogen receptor-ligand binding domain
|
None
|
1.0
nM
|
|
|
Binding affinity for human estrogen receptor alpha
|
Homo sapiens
|
0.2
nM
|
|
|
Binding affinity for human estrogen receptor alpha by displacement of [3H]estradiol
|
Homo sapiens
|
100.0
nM
|
|
|
Agonist effect on transcriptional activation of T47D cells expressing human estrogen receptor beta
|
Homo sapiens
|
0.8
nM
|
|
|
Transcriptional potency (EC50) at Human estrogen receptor Beta
|
None
|
0.039
nM
|
|
|
Inhibitory concentration against estrogen receptor 2 using radioligand binding assay.
|
None
|
24.0
nM
|
|
|
Binding affinity for human estrogen receptor beta
|
Homo sapiens
|
0.5
nM
|
|
|
Relative binding affinity for human estrogen receptor beta by displacement of [3H]estradiol
|
Homo sapiens
|
100.0
|
|
|
Relative binding affinity for human estrogen receptor beta compared to [3H]-estradiol
|
Homo sapiens
|
100.0
nM
|
|
|
Ability to activate estrogen receptor 1-mediated transcription.
|
None
|
0.48
nM
|
|
|
Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor alpha.
|
None
|
0.02
nM
|
|
|
Agonist effect on transcriptional activation in MCF-7 cells expressing estrogen receptor alpha
|
Homo sapiens
|
0.007
nM
|
|
|
Agonist effect on transcriptional activation in T47D cells expressing estrogen receptor alpha
|
Homo sapiens
|
0.07
nM
|
|
|
Inhibition of [3H]17-beta-estradiol binding to human recombinant Estrogen receptor alpha.
|
None
|
24.0
nM
|
|
|
Binding affinity against human estrogen receptor alpha in competitive binding assay
|
None
|
1.3
nM
|
|
|
Binding affinity towards estrogen receptor alpha by [3H]17-beta-estradiol displacement.
|
None
|
11.0
nM
|
|
|
Binding affinity for human estrogen receptor alpha
|
Homo sapiens
|
1.3
nM
|
|
|
Binding affinity for human estrogen receptor alpha
|
Homo sapiens
|
1.3
nM
|
|
|
Binding affinity towards human estrogen receptor alpha(ERalpha)
|
None
|
3.2
nM
|
|
|
Binding affinity towards human recombinant Estrogen receptor alpha was determined
|
None
|
1.3
nM
|
|
|
Displacement of [3H]17-beta-estradiol from human Estrogen receptor alpha
|
Homo sapiens
|
3.0
nM
|
|
|
In vitro binding affinity for estrogen receptor alpha
|
Homo sapiens
|
2.0
nM
|
|
|
Inhibition of [3H]E2 binding to estrogen receptor alpha in MCF-7 cell lysate
|
Homo sapiens
|
1.5
nM
|
|
|
Inhibitory concentration against estrogen receptor alpha using radioligand binding assay.
|
None
|
28.0
nM
|
|
|
Displacement of [3H]17-beta-estradiol from human estrogen receptor alpha
|
Homo sapiens
|
5.9
nM
|
|
|
Ability to displace [3H]17-beta-estradiol from Estrogen receptor alpha by scintillation proximity assay.
|
None
|
2.2
nM
|
|
|
Displacement of radioligand from Estrogen receptor alpha
|
None
|
3.4
nM
|
|
|
Ability to activate estrogen receptor 2-mediated transcription.
|
None
|
0.67
nM
|
|
|
Activation of estrogen response element in HeLa cells stably transfected with human Estrogen receptor beta.
|
None
|
0.07
nM
|
|
|
Agonist activity in transcriptional activation assay in SH-SY5Y neuroblastoma cells expressing Estrogen receptor beta
|
Homo sapiens
|
0.1
nM
|
|
|
Inhibition of [3H]17-beta-estradiol binding to human recombinant Estrogen receptor beta.
|
None
|
24.0
nM
|
|
|
Binding affinity against human estrogen receptor beta (ER beta) in competitive binding assay
|
None
|
1.1
nM
|
|
|
Binding affinity towards estrogen receptor beta by [3H]17-beta-estradiol displacement.
|
None
|
19.0
nM
|
|
|
Binding affinity for human estrogen receptor beta
|
Homo sapiens
|
1.1
nM
|
|
|
Binding affinity for human estrogen receptor beta
|
Homo sapiens
|
1.1
nM
|
|
|
Binding affinity towards human estrogen receptor beta (ERbeta)
|
None
|
3.6
nM
|
|
|
Binding affinity towards human recombinant Estrogen receptor beta was determined
|
None
|
1.1
nM
|
|
|
Displacement of [3H]17-beta-estradiol from human Estrogen receptor beta
|
Homo sapiens
|
4.0
nM
|
|
|
In vitro binding affinity for estrogen receptor beta
|
Homo sapiens
|
2.0
nM
|
|
|
Ability to displace [3H]17-beta-estradiol from Estrogen receptor beta by scintillation proximity assay.
|
None
|
3.5
nM
|
|
|
Binding to Estrogen receptor- alpha (ER alpha) receptor
|
None
|
2.0
nM
|
|
|
Binding to Estrogen receptor- beta (ER beta) receptor
|
None
|
2.0
nM
|
|
|
Displacement of [3H]estradiol from estrogen receptor in squirrel monkey
|
monkey
|
0.7
ug.mL-1
|
|
|
Concentration of compound required to induce 50 % of the maximum stimulation of alkaline phosphatase activity in Ishikawa cells
|
Homo sapiens
|
0.01
nM
|
|
|
Effect on estradiol-stimulated MCF-7 cell proliferation
|
Homo sapiens
|
0.32
nM
|
|
|
Effective dose for [3H]- estradiol against proliferation of MCF-7 cells
|
Homo sapiens
|
0.02
nM
|
|
|
Percent agonistic activity for estrogen-induced pS2 expression in MCF-7 cells
|
Homo sapiens
|
0.01
nM
|
|
|
In vitro inhibition of estrogen-stimulated MCF-7 cell proliferation
|
Homo sapiens
|
0.01
nM
|
|
|
Percent of inhibitory activity against proliferation of MCF-7 cells in presence of 10e-6 M concentration of [3H]estradiol (E2).
|
Homo sapiens
|
25.0
%
|
|
|
Percent of inhibitory activity versus 0.1 nm [3H]estradiol against proliferation of MCF-7 cells.
|
Homo sapiens
|
0.0
%
|
|
|
Agonist activity in transcriptional activation assay in MCF-7-2a cells compared to estradiol E2
|
Homo sapiens
|
0.49
nM
|
|
|
Concentration required to activate luciferase expression in MCF-7-2a cells
|
Homo sapiens
|
0.08
nM
|
|
|
Effective concentration against MCF-7 breast tumor cells using MCF-7 assay.
|
Homo sapiens
|
0.01
nM
|
|
|
Induction of pS2 Gene expression in human MCF-7 cells
|
Homo sapiens
|
0.0301
nM
|
|
|
Induction of pS2 mRNA expression in human MCF-7 mammary carcinoma cells
|
Homo sapiens
|
0.0996
nM
|
|
|
Induction of pS2 mRNA expression in human MCF-7 mammary carcinoma cells
|
Homo sapiens
|
0.292
nM
|
|
|
Growth response in cultures of MCF-7 (human breast cancer cell line) cells
|
Homo sapiens
|
0.00152
nM
|
|
|
Stimulation of MCF-7 cell proliferation
|
Homo sapiens
|
0.7
nM
|
|
|
Inhibition of MCF-7 cell proliferation at 5 uM
|
Homo sapiens
|
57.0
%
|
|
|
Cytostatic activity against MCF-7 cell proliferation.
|
Homo sapiens
|
25.0
%
|
|
|
The percent stimulation or inhibition of protein kinase C III activity was determined for phosphatidylserine (PS) and diolein(PS+DO) in the presence of [Ca2+]
|
Rattus norvegicus
|
89.0
%
|
|
|
Percent stimulation or inhibition of protein kinase C III activity for phosphatidylserine (PS) in the presence of [Ca2+].
|
Rattus norvegicus
|
77.0
%
|
|
|
Percent stimulation or inhibition of protein kinase C III activity for protamine sulfate in the presence of EGTA.
|
Rattus norvegicus
|
99.0
%
|
|
|
Displacement of [3H]estradiol from estrogen receptor in immature rat
|
Rattus norvegicus
|
0.25
ug.mL-1
|
|
|
Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on voltage dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 10 uM
|
Cavia porcellus
|
17.8
%
|
|
|
Inhibition of binding of Batrachotoxinin [3H]BTX-B to high-affinity sites on voltage-dependent sodium channels in a vesicular preparation from guinea pig cerebral cortex at 100 uM
|
Cavia porcellus
|
53.3
%
|
|
|
Relative binding affinity for human estrogen receptor alpha by displacement of [3H]-estradiol
|
Homo sapiens
|
100.0
|
|
|
Transcriptional potency (EC50) at Human estrogen receptor alpha
|
None
|
0.018
nM
|
|
|
Dissociation constant for [3H]estradiol at human estrogen receptor at 273 K
|
Homo sapiens
|
0.72
nM
|
|
|
Dissociation constant for [3H]estradiol at human estrogen receptor at 278 K
|
Homo sapiens
|
0.62
nM
|
|
|
Dissociation constant for [3H]estradiol at human estrogen receptor at 283 K
|
Homo sapiens
|
0.53
nM
|
|
|
Dissociation constant for [3H]estradiol at human estrogen receptor at 288 K
|
Homo sapiens
|
0.43
nM
|
|
|
Dissociation constant for [3H]estradiol at human estrogen receptor at 293K
|
Homo sapiens
|
0.45
nM
|
|
|
Dissociation constant for [3H]estradiol at human estrogen receptor at 298 K
|
Homo sapiens
|
0.53
nM
|
|
|
Dissociation constant for [3H]estradiol at human estrogen receptor at 303 K
|
Homo sapiens
|
0.59
nM
|
|
|
Dissociation constant for [3H]estradiol at human estrogen receptor at 308 K
|
Homo sapiens
|
0.79
nM
|
|
|
Dissociation constant for [3H]-estradiol at human estrogen receptor at 310K
|
Homo sapiens
|
0.87
nM
|
|
|
Binding affinity for Estrogen receptor
|
None
|
0.5
nM
|
|
|
Binding affinity for Estrogen receptor alpha
|
None
|
0.003
nM
|
|
|
Binding affinity for human estrogen receptor beta
|
Homo sapiens
|
3.162
nM
|
|
|
Binding affinity for human estrogen receptor alpha
|
Homo sapiens
|
1.995
nM
|
|
|
Binding potency for human ER beta
|
Homo sapiens
|
1.1
nM
|
|
|
Binding potency for human ER beta
|
Homo sapiens
|
1.1
nM
|
|
|
Binding potency for human ER alpha
|
Homo sapiens
|
1.3
nM
|
|
|
Binding potency for human ER alpha
|
Homo sapiens
|
1.3
nM
|
|
|
Inhibition of human estrogen receptor beta
|
Homo sapiens
|
3.6
nM
|
|
|
Inhibition of human estrogen receptor alpha
|
Homo sapiens
|
3.2
nM
|
|
|
Binding affinity for human estrogen receptor beta
|
Homo sapiens
|
1.1
nM
|
|
|
Binding affinity for human estrogen receptor alpha
|
Homo sapiens
|
1.3
nM
|
|
|
Inhibition of estrogen receptor beta
|
Homo sapiens
|
1.1
nM
|
|
|
Inhibition of estrogen receptor alpha
|
Homo sapiens
|
1.3
nM
|
|
|
Binding affinity for human Estrogen receptor beta
|
Homo sapiens
|
3.6
nM
|
|
|
Binding affinity for human Estrogen receptor alpha
|
Homo sapiens
|
3.2
nM
|
|
|
Inhibition of binding to recombinant human estrogen receptor beta
|
Homo sapiens
|
1.1
nM
|
|
|
Inhibition of bindign to recombinant human estrogen receptor alpha
|
Homo sapiens
|
1.3
nM
|
|
|
Inhibition of [3H]estradiol binding to human estrogen receptor beta expressed in HeLa cells
|
Homo sapiens
|
24.0
nM
|
|
|
Inhibition of [3H]estradiol binding to human estrogen receptor alpha expressed in HeLa cells
|
Homo sapiens
|
28.0
nM
|
|
|
Inhibition of [3H]17-beta-estradiol binding to human estrogen receptor beta expressed in Escherichia coli
|
Homo sapiens
|
3.6
nM
|
|
|
Inhibition of [3H]17-beta-estradiol binding to human estrogen receptor alpha expressed in Escherichia coli
|
Homo sapiens
|
3.2
nM
|
|
|
Inhibition of [3H]17-beta-estradiol binding to rat ER beta expressed in Escherichia coli
|
Rattus norvegicus
|
1.7
nM
|
|
|
Inhibition of [3H]17-beta-estradiol binding to rat ER alpha expressed in Escherichia coli
|
Rattus norvegicus
|
1.9
nM
|
|
|
Inhibitory concentration against human ER beta expressed in Escherichia coli was determined using [3H]17-beta-estradiol as radio ligand
|
Homo sapiens
|
3.6
nM
|
|
|
Inhibition of [3H]17-beta-estradiol binding to mouse ER beta expressed in Escherichia coli
|
Mus musculus
|
2.3
nM
|
|
|
Inhibitory concentration against human ER alpha expressed in Escherichia coli was determined using [3H]17-beta-estradiol as radio ligand
|
Homo sapiens
|
3.2
nM
|
|
|
Inhibition of [3H]17-beta-estradiol binding to mouse ER alpha expressed in Escherichia coli
|
Mus musculus
|
2.2
nM
|
|
|
Inhibition of human estrogen receptor 2 using tritiated estradiol incubated for 3 hr
|
Homo sapiens
|
1.1
nM
|
|
|
In vitro agonist activity for estrogen receptor beta expressed in COS-1 cells
|
None
|
9.7
nM
|
|
|
In vitro agonist activity for estrogen receptor alpha expressed in COS-1 cells
|
Homo sapiens
|
2.4
nM
|
|
|
Estrogenic effect in rat uterine weight assay
|
Rattus norvegicus
|
100.0
%
|
|
|
Transcriptional activation of estrogen receptor beta in U2OS cell using estrogen-regulated luciferase reporter gene plasmid upon incubation for 20-30 mins at RT
|
Homo sapiens
|
0.098
nM
|
|
|
Transcriptional activation of estrogen receptor alpha in U2OS cell using estrogen-regulated luciferase reporter gene plasmid upon incubation for 20-30 mins at RT
|
Homo sapiens
|
0.019
nM
|
|
|
Binding affinity for human Estrogen receptor beta
|
Homo sapiens
|
3.6
nM
|
|
|
Binding affinity for human Estrogen receptor alpha
|
Homo sapiens
|
3.2
nM
|
|
|
Inhibitory concentration against recombinant rat androgen receptor expressed in Escherichia coli using [3H]methyltrienolone (R 1881)
|
Rattus norvegicus
|
407.38
nM
|
|
|
Effective concentration against human ER positive MCF-7 breast cancer cell line evaluated by luciferase assay
|
Homo sapiens
|
0.08
nM
|
|
|
Displacement of [3H]17beta-estradiol from recombinant human ERalpha expressed in 293T cells
|
Homo sapiens
|
0.75
nM
|
|
|
Displacement of [3H]17beta-estradiol from recombinant human ERbeta expressed in 293T cells
|
Homo sapiens
|
1.18
nM
|
|
|
Effect on ERalpha in MCF7 cell line transfected with ER responsive luciferase reporter
|
Homo sapiens
|
0.01
nM
|
|
|
Effect on ERbeta in rat ovary granulosa cell line transfected with ER responsive luciferase reporter
|
Rattus norvegicus
|
0.14
nM
|
|
|
Binding affinity to human ERalpha
|
Homo sapiens
|
1.4
nM
|
|
|
Binding affinity to human ERbeta
|
Homo sapiens
|
1.2
nM
|
|
|
Effect on transactivation of ALP gene expression in HEK293 cells transfected with hERalpha
|
Homo sapiens
|
0.75
nM
|
|
|
Effect on transactivation of ALP gene expression in HEK293 cells transfected with hERbeta
|
Homo sapiens
|
2.1
nM
|
|
|
Inhibitory activity against AR
|
Homo sapiens
|
19.1
nM
|
|
|
Binding affinity to ERalpha
|
Homo sapiens
|
1.35
nM
|
|
|
Binding affinity to ERbeta
|
Homo sapiens
|
1.2
nM
|
|
|
Displacement of [3H]estrone from ER beta
|
Homo sapiens
|
11.0
nM
|
|
|
Displacement of [3H]estrone from ER alpha
|
Homo sapiens
|
10.0
nM
|
|
|
Inhibition of ER beta-mediated transactivation of ERE in HeLa cell luciferase assay
|
Homo sapiens
|
0.84
nM
|
|
|
Inhibition of ER beta-mediated transactivation of ERE in HeLa cell luciferase assay at 10 uM
|
Homo sapiens
|
0.59
nM
|
|
|
Binding affinity to ERalpha by scintillation proximity assay
|
Homo sapiens
|
1.3
nM
|
|
|
Binding affinity to ERbeta by scintillation proximity assay
|
Homo sapiens
|
1.2
nM
|
|
|
Displacement of [3H]estradiol from human ERalpha
|
Homo sapiens
|
0.2
nM
|
|
|
Displacement of [3H]estradiol from human ERbeta
|
Homo sapiens
|
0.5
nM
|
|
|
Binding affinity to human ERalpha
|
Homo sapiens
|
1.3
nM
|
|
|
Binding affinity to human ERbeta
|
Homo sapiens
|
1.2
nM
|
|
|
Binding affinity to human recombinant ERalpha by scintillation proximity assay
|
Homo sapiens
|
1.3
nM
|
|
|
Binding affinity to human recombinant ERbeta by scintillation proximity assay
|
Homo sapiens
|
1.1
nM
|
|
|
Binding affinity to ERalpha L384M/M421G mutant
|
Homo sapiens
|
46.0
nM
|
|
|
Binding affinity to human ER alpha
|
Homo sapiens
|
1.6
nM
|
|
|
Binding affinity to human ER beta
|
Homo sapiens
|
1.4
nM
|
|
|
Displacement of [3H]E2 from human recombinant ERalpha LBD by SPA
|
Homo sapiens
|
1.2
nM
|
|
|
Displacement of [3H]E2 from human recombinant ERbeta LBD by SPA
|
Homo sapiens
|
1.4
nM
|
|
|
Displacement of [3H]DHT from human SHBG
|
Homo sapiens
|
50.0
nM
|
|
|
Inhibition of human LBD of of ERalpha
|
Homo sapiens
|
3.6
nM
|
|
|
Inhibition of human LBD of ERbeta
|
Homo sapiens
|
3.2
nM
|
|
|
Inhibition of human ERbeta by radioligand binding assay
|
Homo sapiens
|
3.6
nM
|
|
|
Inhibition of human ERalpha by radioligand binding assay
|
Homo sapiens
|
3.2
nM
|
|
|
Binding affinity to human ERalpha
|
Homo sapiens
|
4.7
nM
|
|
|
Binding affinity to human ERbeta
|
Homo sapiens
|
16.7
nM
|
|
|
Displacement of [3H]estradiol from full length human recombinant ERalpha after 3 hrs by scintillation proximity assay
|
Homo sapiens
|
1.0
nM
|
|
|
Displacement of [3H]estradiol from full length human recombinant ERbeta after 3 hrs by scintillation proximity assay
|
Homo sapiens
|
1.0
nM
|
|
|
Binding affinity to ERalpha
|
None
|
12.0
nM
|
|
|
Binding affinity to human recombinant ERalpha by scintillation proximity assay
|
Homo sapiens
|
1.4
nM
|
|
|
Binding affinity to human recombinant ERbeta by scintillation proximity assay
|
Homo sapiens
|
1.2
nM
|
|
|
Agonist activity at human recombinant ERalpha expressed in HEK293 cells by transactivation assay
|
Homo sapiens
|
0.75
nM
|
|
|
Agonist activity at human recombinant ERbeta expressed in HEK293 cells by transactivation assay
|
Homo sapiens
|
2.1
nM
|
|
|
Binding affinity to androgen receptor
|
None
|
19.1
nM
|
|
|
Inhibition of human ERalpha
|
Homo sapiens
|
3.6
nM
|
|
|
Inhibition of human ERbeta
|
Homo sapiens
|
3.2
nM
|
|
|
Binding affinity at human recombinant ERalpha
|
Homo sapiens
|
1.4
nM
|
|
|
Binding affinity at human recombinant ERbeta
|
Homo sapiens
|
1.2
nM
|
|
|
Agonist activity at ERalpha expressed in HEK293 cells by transactivation assay
|
Homo sapiens
|
0.75
nM
|
|
|
Agonist activity at ERbeta expressed in HEK293 cells by transactivation assay
|
Homo sapiens
|
2.1
nM
|
|
|
Binding affinity at AR
|
None
|
26.0
nM
|
|
|
Displacement of [3H]5alpha dihydrotestosterone from human sex hormone binding globulin
|
Homo sapiens
|
1.479
nM
|
|
|
Estrogenic activity at human estrogen receptor expressing Saccharomyces cerevisiae carrying estrogen responsive sequence containing plasmid assessed as metabolism of chlorophenol res beta-D-galactopyranoside
|
Homo sapiens
|
0.37
nM
|
|
|
Estrogenic activity at estrogen receptor in human Ishikawa Var-1 cells assessed as stimulation of alkaline phosphatase activity measured by metabolism of p-nitrophenol phosphatase after 72 hrs
|
Homo sapiens
|
0.047
nM
|
|
|
Binding affinity to human recombinant ERalpha receptor by liquid scintillation counter
|
Homo sapiens
|
4.0
nM
|
|
|
Binding affinity to human recombinant ERbeta receptor by liquid scintillation counter
|
Homo sapiens
|
4.0
nM
|
|
|
Estrogenic activity in human MCF7 cells assessed as cell proliferation after 6 days by WST8 assay
|
Homo sapiens
|
0.0037
nM
|
|
|
Binding affinity to full-length human estrogen receptor alpha
|
Homo sapiens
|
0.2
nM
|
|
|
Binding affinity to full-length human estrogen receptor beta
|
Homo sapiens
|
0.5
nM
|
|
|
Agonist activity at full-length human estrogen receptor beta expressed in human HEC1 cells assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.13
nM
|
|
|
Agonist activity at full-length human estrogen receptor alpha expressed in human HEC1 cells assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.7
nM
|
|
|
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy
|
Homo sapiens
|
83.5
%
|
|
|
Displacement of [3H]estradiol from full length biotinylated human ERalpha by scintillation proximity assay
|
Homo sapiens
|
2.0
nM
|
|
|
Displacement of [3H]estradiol from full length biotinylated human ERbeta by scintillation proximity assay
|
Homo sapiens
|
2.0
nM
|
|
|
Binding affinity to full-length human estrogen receptor alpha
|
Homo sapiens
|
0.2
nM
|
|
|
Binding affinity to full-length human estrogen receptor beta
|
Homo sapiens
|
0.5
nM
|
|
|
Agonist activity at ERalpha expressed in human HEC1 cells assessed as transcriptional potency after 24 hrs by luciferase-beta galactosidase reporter gene assay
|
None
|
0.1
nM
|
|
|
Agonist activity at ERbeta expressed in human HEC1 cells assessed as transcriptional potency after 24 hrs by luciferase-beta galactosidase reporter gene assay
|
None
|
0.5
nM
|
|
|
Binding affinity to human full length ERalpha receptor
|
Homo sapiens
|
0.2
nM
|
|
|
Binding affinity to human full length ERbeta receptor
|
Homo sapiens
|
0.5
nM
|
|
|
Displacement of estradiol-Alexa 633 from GFP-tagged ERalpha expressed in COS7 cells at 10 uM
|
None
|
78.2
%
|
|
|
Displacement of estradiol-Alexa 633 from GFP-tagged ERbeta expressed in COS7 cells at 10 uM
|
None
|
75.9
%
|
|
|
Displacement of [3H]17beta-estradiol from human ERalpha expressed in SF9 cells
|
Homo sapiens
|
12.5
nM
|
|
|
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
|
1.1
%
|
|
|
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
|
0.0
%
|
|
|
Agonist activity at estrogen receptor alpha ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay
|
None
|
3.2
nM
|
|
|
Agonist activity at estrogen receptor beta ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay
|
None
|
11.0
nM
|
|
|
Displacement of fluorescent estrogen ES2 from human recombinant ERalpha by fluorescence polarization assay
|
Homo sapiens
|
3.2
nM
|
|
|
Displacement of fluorescent estrogen ES2 from human recombinant ERbeta by fluorescence polarization assay
|
Homo sapiens
|
2.9
nM
|
|
|
Estrogenic activity in human ERalpha expressing MCF7:WS8 cells assessed as stimulation of cell proliferation after 7 days
|
Homo sapiens
|
0.001
nM
|
|
|
Binding affinity to ERalpha by fluorescence polarization-based competitive binding assay
|
None
|
10.12
nM
|
|
|
Binding affinity to ERbeta by fluorescence polarization-based competitive binding assay
|
None
|
11.35
nM
|
|
|
Transactivation of human ERalpha expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.06457
nM
|
|
|
Transactivation of human ERbeta expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.06166
nM
|
|
|
Agonist activity at ERbeta expressed in yeast assessed as alpha-galactosidase activity
|
None
|
1.08
nM
|
|
|
Agonist activity at ERalpha expressed in yeast assessed as alpha-galactosidase activity
|
None
|
1.05
nM
|
|
|
Agonist activity at ERalpha expressed in CHO-K1 cells by luciferase reporter gene transactivation assay
|
None
|
50.0
nM
|
|
|
Agonist activity at ERbeta expressed in CHO-K1 cells by luciferase reporter gene transactivation assay
|
None
|
30.0
nM
|
|
|
Displacement of [2,4,6,7-3H]estradiol from human ERalpha expressed in HeLa cells after 18 hrs by liquid scintillation counting
|
Homo sapiens
|
0.16
nM
|
|
|
Agonist activity at human ERalpha E353A mutant expressed in HEK293T cells co-expressing ERE assessed as transactivation activity by luciferase reporter gene assay
|
Homo sapiens
|
2.5
nM
|
|
|
Agonist activity at human ERbeta E305A mutant expressed in HEK293T cells co-expressing ERE assessed as transactivation activity by luciferase reporter gene assay
|
Homo sapiens
|
10.4
nM
|
|
|
Displacement of E2-Alexa633 from GFP-tagged GPR30 expressed in COS7 cells by FACS
|
None
|
5.7
nM
|
|
|
Displacement of E2-Alexa633 from GFP-tagged ERalpha expressed in COS7 cells by FACS
|
None
|
0.3
nM
|
|
|
Displacement of E2-Alexa633 from GFP-tagged ERbeta expressed in COS7 cells by FACS
|
None
|
0.38
nM
|
|
|
Agonist activity at GFP-tagged GPR30 expressed in COS7 cells assessed as half life for increase in intracellular calcium level by spectrofluorimetry
|
None
|
0.3
nM
|
|
|
Inhibition of chemoattractant-induced cell migration of human SK-BR-3 cells after 48 hrs by transwell migration assay
|
Homo sapiens
|
0.1
nM
|
|
|
Inhibition of chemoattractant-induced cell migration of human MCF7 cells after 48 hrs by transwell migration assay
|
Homo sapiens
|
0.4
nM
|
|
|
Agonist activity at ERalpha-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase of transactivation activity after 18 hrs by luciferase reporter gene assay
|
Homo sapiens
|
2.773
nM
|
|
|
Agonist activity at ERbeta-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase of transactivation activity after 18 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.4581
nM
|
|
|
Antagonist activity at ERalpha-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay
|
Homo sapiens
|
21.04
nM
|
|
|
Antagonist activity at ERbeta-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay
|
Homo sapiens
|
10.74
nM
|
|
|
Inhibition of human aldehyde oxidase
|
Homo sapiens
|
80.0
nM
|
|
|
Inhibition of human estrogen receptor beta
|
Homo sapiens
|
46.0
nM
|
|
|
Agonist activity at 6his-tagged ERRalpha LBD assessed as recruitment of GST-labeled coactivator Scr2 by TR-FRET assay
|
None
|
5.9
nM
|
|
|
Agonist activity at ZFP-fused ERRbeta LBD expressed in HEK293 cells by TR-FRET assay
|
None
|
4.6
nM
|
|
|
Agonist activity at human ERalpha LBD in human MCF7 cells assessed as induction of cell proliferation after up to 6 days by celltiter-glo assay
|
Homo sapiens
|
10.0
nM
|
|
|
Agonist activity at human ERbeta LBD by cell based luciferase reporter gene assay
|
Homo sapiens
|
1.4
nM
|
|
|
Displacement of [3H]17-beta-estradiol from rabbit ER by liquid scintillation counting
|
Oryctolagus cuniculus
|
2.3
nM
|
|
|
Agonist activity at human N-terminal His6-tagged ERalpha receptor LBD expressed in Escherichia coli BL21 (DE3) assessed as induction of SRC1 peptide recruitment after 1 hr by fluorescence polarization assay
|
Homo sapiens
|
130.0
nM
|
|
|
Agonist activity at human N-terminal His6-tagged ERbeta receptor LBD expressed in Escherichia coli BL21 (DE3) assessed as induction of SRC1 peptide recruitment after 1 hr by fluorescence polarization assay
|
Homo sapiens
|
280.0
nM
|
|
|
Agonist activity at human full-length ERalpha receptor expressed in human HEC1 cells co-expressing (ERE)2-pS2-luc gene assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.09
nM
|
|
|
Agonist activity at human full-length ERbeta receptor expressed in human HEC1 cells co-expressing (ERE)2-pS2-luc gene assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.72
nM
|
|
|
Binding affinity to human full-length ERalpha receptor
|
Homo sapiens
|
0.2
nM
|
|
|
Binding affinity to human full-length ERbeta receptor
|
Homo sapiens
|
0.5
nM
|
|
|
Inhibition of fluorescence-labeled 17beta-estradiol binding to ERalpha receptor at 0.1 microM after 2 hrs by fluorometric analysis
|
None
|
100.0
%
|
|
|
Inhibition of fluorescence-labeled 17beta-estradiol binding to ERalpha receptor after 2 hrs by fluorometric analysis
|
None
|
18.0
nM
|
|
|
Binding affinity to estrogen receptor-alpha after 2 hrs by TR-FRET assay
|
None
|
0.57
nM
|
|
|
Agonist activity at ERbeta expressed in UAS cells co-expressing beta-lactamase after 18 hrs by beta-lactamase reporter gene assay
|
None
|
0.25
nM
|
|
|
Agonist activity at ERalpha expressed in HEK cells co-expressing beta-lactamase after 18 hrs by beta-lactamase reporter gene assay
|
None
|
0.046
nM
|
|
|
DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
|
Escherichia coli
|
353.0
nM
|
|
DRUGMATRIX: Androgen (Testosterone) AR radioligand binding (ligand: [3H] Mibolerone)
|
Escherichia coli
|
235.0
nM
|
|
|
DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol)
|
None
|
1.607
nM
|
|
DRUGMATRIX: Estrogen ERalpha radioligand binding (ligand: [3H] Estradiol)
|
None
|
0.459
nM
|
|
|
Displacement of [3H]E2 from estrogen receptor in JW rabbit uterus after 2 hrs by liquid scintillation counting
|
Oryctolagus cuniculus
|
2.3
nM
|
|
|
Agonist activity at estrogen receptor in human Ishikawa cells assessed as increase of alkaline phosphatase level after 3 days using P-nitrophenyl phosphate as substrate
|
Homo sapiens
|
0.9
nM
|
|
|
Agonist activity at human N-His6-tagged terbium-labelled NRID-SRC3 of ERbeta ligand binding domain expressed in Escherichia coli BL21 cells after 1 hr by TR-FRET assay
|
Homo sapiens
|
0.9
nM
|
|
|
Agonist activity at human N-His6-tagged terbium-labelled NRID-SRC3 of ERalpha ligand binding domain expressed in Escherichia coli BL21 cells after 1 hr by TR-FRET assay
|
Homo sapiens
|
0.56
nM
|
|
|
Agonist activity at human N-His6-tagged terbium-labelled ERbeta ligand binding domain expressed in Escherichia coli BL21 cells assessed as recruitment of fluorescein-labelled SRC3 after 1 hr by TR-FRET assay
|
Homo sapiens
|
1.5
nM
|
|
|
Agonist activity at human N-His6-tagged terbium-labelled ERalpha ligand binding domain expressed in Escherichia coli BL21 cells assessed as recruitment of fluorescein-labelled SRC3 after 1 hr by TR-FRET assay
|
Homo sapiens
|
3.0
nM
|
|
|
Agonist activity at human ERbeta expressed in HEC-1 cells coexpressing beta-gal assessed as luciferase activity after 24 hrs by reporter gene assay
|
Homo sapiens
|
0.2
nM
|
|
|
Agonist activity at human ERalpha expressed in HEC-1 cells coexpressing beta-gal assessed as luciferase activity after 24 hrs by reporter gene assay
|
Homo sapiens
|
0.123
nM
|
|
|
Agonist activity at human ERbeta expressed in U2OS cells coexpressing pCMX-hSRC3 assessed as luciferase activity after 24 hrs by reporter gene assay
|
Homo sapiens
|
0.4
nM
|
|
|
Agonist activity at human ERalpha expressed in U2OS cells coexpressing pCMX-hSRC3 assessed as luciferase activity after 24 hrs by reporter gene assay
|
Homo sapiens
|
0.15
nM
|
|
|
Estrogenic activity at estrogen receptor in human MCF7:D5L cells co-expressing ERE assessed as induction of luciferase gene expression after 16 hrs by microplate reader
|
Homo sapiens
|
0.0196
nM
|
|
|
Antiproliferative activity against estrogen-deficient human MCF7 cells after 72 hrs by MTT assay
|
Homo sapiens
|
0.0064
nM
|
|
|
Estrogenic activity at estrogen receptor in human Ishikawa cells assessed as induction of alkaline phosphatase expression after 72 hrs by microplate reader
|
Homo sapiens
|
0.0246
nM
|
|
|
Agonist activity at human ERalpha expressed in HepG2 cells after 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
2.2
nM
|
|
|
Agonist activity at human ERbeta expressed in HepG2 cells after 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
11.0
nM
|
|
|
Agonist activity at ERalpha receptor LBD expressed in yeast AH109 cells assessed as interaction with SRC1 after 24 hrs by alpha-galactosidase assay
|
Homo sapiens
|
1.05
nM
|
|
|
Agonist activity at ERbeta receptor LBD expressed in yeast AH109 cells assessed as interaction with SRC1 after 24 hrs by alpha-galactosidase assay
|
Homo sapiens
|
1.08
nM
|
|
|
Transcriptional activation of ERalpha receptor expressed in CHO-K1 cells after 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.05
nM
|
|
|
Transcriptional activation of ERbeta receptor expressed in CHO-K1 cells after 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.036
nM
|
|
|
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
|
102.8
%
|
|
|
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
|
39.3
%
|
|
|
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
|
47.4
%
|
|
|
Activation of human ERalpha expressed in human U2-OS cells by luciferase reporter gene assay relative to untreated control
|
Homo sapiens
|
0.004
nM
|
|
|
Activation of ERalpha in human MCF7/2a cells by luciferase reporter gene assay relative to untreated control
|
Homo sapiens
|
0.1
nM
|
|
|
Activation of human ERbeta expressed in human U2-OS cells by luciferase reporter gene assay relative to untreated control
|
Homo sapiens
|
0.01
nM
|
|
|
Displacement of [3H]E2 from human recombinant ERbeta receptor after overnight incubation by liquid scintillation counting analysis
|
Homo sapiens
|
8.7
nM
|
|
|
Displacement of [3H]E2 from human recombinant ERalpha receptor after overnight incubation by liquid scintillation counting analysis
|
Homo sapiens
|
6.0
nM
|
|
|
Binding affinity to human full length estrogen receptor beta by Scatchard plot analysis
|
Homo sapiens
|
0.5
nM
|
|
|
Binding affinity to human full length estrogen receptor alpha by Scatchard plot analysis
|
Homo sapiens
|
0.2
nM
|
|
|
Agonist activity at human estrogen receptor-beta by yeast two-hybrid assay in presence of SRC1
|
Homo sapiens
|
1.05
nM
|
|
|
Agonist activity at human estrogen receptor-alpha by yeast two-hybrid assay in presence of SRC1
|
Homo sapiens
|
1.08
nM
|
|
|
Inhibition of estrogen binding to GPR30 (unknown origin)
|
Homo sapiens
|
5.7
nM
|
|
|
Agonist activity at GPR30 (unknown origin) by calcium mobilization assay
|
Homo sapiens
|
0.3
nM
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
125.9
%
|
|
|
Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM
|
Cricetulus griseus
|
131.94
%
|
|
|
Antagonist activity at ERbeta (unknown origin) by cell-based assay
|
Homo sapiens
|
0.046
nM
|
|
|
Agonist activity at ERalpha (unknown origin) by cell-based assay
|
Homo sapiens
|
1.3
nM
|
|
|
Displacement of fluorescein-labeled ES2 from human recombinant ERalpha receptor after 2 hrs by fluorescence polarization assay
|
Homo sapiens
|
3.0
nM
|
|
|
Agonist activity at ER-beta (unknown origin) transfected in HEK293T cells after 24 hrs by Steady-Glo luciferase reporter gene assay
|
Homo sapiens
|
0.03981
nM
|
|
|
Agonist activity at ER-alpha (unknown origin) transfected in HEK293T cells after 24 hrs by Steady-Glo luciferase reporter gene assay
|
Homo sapiens
|
0.1
nM
|
|
|
Displacement of fluorescein-labeled estrogen from human recombinant ERalpha by fluorescence polarization based competitive binding affinity assay
|
Homo sapiens
|
5.7
nM
|
|
|
Displacement of fluorescein-labeled estrogen from human recombinant ERbeta by fluorescence polarization based competitive binding affinity assay
|
Homo sapiens
|
5.6
nM
|
|
|
Agonist activity at human ERalpha expressed in HEK293 cells by luciferase reporter gene assay
|
Homo sapiens
|
0.024
nM
|
|
|
Agonist activity at human ERbeta expressed in HEK293 cells by luciferase reporter gene assay
|
Homo sapiens
|
0.085
nM
|
|
|
Agonist activity at human ERalpha expressed in human HEC1 cells assessed as transcriptional activation after 24 hrs by ERE-luciferase reporter gene transfection assay
|
Homo sapiens
|
0.16
nM
|
|
|
Agonist activity at human ERbeta expressed in human HEC1 cells assessed as transcriptional activation after 24 hrs by ERE-luciferase reporter gene transfection assay
|
Homo sapiens
|
0.38
nM
|
|
|
Agonist activity at human ERalpha in human MCF7 cells assessed as progesterone receptor endogenous genes activation after 24 hrs by qPCR
|
Homo sapiens
|
0.0084
nM
|
|
|
Agonist activity at human ERbeta in human MCF7 cells assessed as otubain 2 endogenous genes activation after 24 hrs by qPCR
|
Homo sapiens
|
0.3
nM
|
|
|
Competitive inhibition of human liver cytosolic aldehyde oxidase using DACA as substrate assessed as free enzyme by Lineweaver-Burk plot analysis
|
Homo sapiens
|
870.0
nM
|
|
|
Inhibition of estrogen receptor alpha (unknown origin)-SRC1 coactivator interaction incubated for 1 hr by receptor cofactor assay system based method
|
Homo sapiens
|
0.9
nM
|
|
|
Binding Assay: The method employed was adapted from the scientific literature and described in detail by Osbourn et al. (1993, Biochemistry, 32, 6229-6236). Recombinant human ERalpha and ERR proteins were purified from transfected Sf9-cells. The in vitro assays involved the use of either ERalpha or ERbeta proteins and [3H]E2, at a fixed concentration of 0.5 nM, as the labeled ligand. Recombinant human ERalpha or ERbeta proteins were dissolved in binding buffer (10 mM Tris-HCL, pH 7.5, 10% glycerol, 1 mM DTT, 1 mg/ml BSA) and duplicate aliquots were then incubated with [3H]E2 at a final concentration of 0.5 nM, together with a vehicle control (0.4% DMSO), or the same amount of vehicle containing increasing concentrations of unlabeled steroid ligands as competitors. After incubation for 2 h at 25 C., the unbound ligands were removed and the amounts of [3H]E2 bound to either ERalpha or ERbeta proteins were measured.
|
Homo sapiens
|
0.21
nM
|
|
|
Inhibition Assay: The method employed was adapted from the scientific literature and described in detail by Osboum et al. (1993, Biochemistry, 32, 6229-6236). Recombinant human ERalpha and ERbeta proteins were purified from transfected Sf9-cells. The in vitro assays involved the use of either ERalpha or ERbeta proteins and [3H]E2, at a fixed concentration of 0.5 nM, as the labeled ligand. Recombinant human ERalpha or ERbeta proteins were dissolved in binding buffer (10 mM Tris-HCL, pH 7.5, 10% glycerol, 1 mM DTT, 1 mg/ml BSA) and duplicate aliquots were then incubated with [3H]E2 at a final concentration of 0.5 nM, together with a vehicle control (0.4% DMSO), or the same amount of vehicle containing increasing concentrations of unlabeled steroid ligands as competitors. After incubation for 2 h at 25 C., the unbound ligands were removed and the amounts of [3H]E2 bound to either ERalpha or ERbeta proteins were measured.
|
Homo sapiens
|
0.21
nM
|
|
|
Inhibition Assay: The method employed was adapted from the scientific literature and described in detail by Osboum et al. (1993, Biochemistry, 32, 6229-6236). Recombinant human ERalpha and ERbeta proteins were purified from transfected Sf9-cells. The in vitro assays involved the use of either ERalpha or ERbeta proteins and [3H]E2, at a fixed concentration of 0.5 nM, as the labeled ligand. Recombinant human ERalpha or ERbeta proteins were dissolved in binding buffer (10 mM Tris-HCL, pH 7.5, 10% glycerol, 1 mM DTT, 1 mg/ml BSA) and duplicate aliquots were then incubated with [3H]E2 at a final concentration of 0.5 nM, together with a vehicle control (0.4% DMSO), or the same amount of vehicle containing increasing concentrations of unlabeled steroid ligands as competitors. After incubation for 2 h at 25 C., the unbound ligands were removed and the amounts of [3H]E2 bound to either ERalpha or ERbeta proteins were measured.
|
Homo sapiens
|
0.015
nM
|
|
|
Binding Assay: The method employed was adapted from the scientific literature and described in detail by Osbourn et al. (1993, Biochemistry, 32, 6229-6236). Recombinant human ERalpha and ERR proteins were purified from transfected Sf9-cells. The in vitro assays involved the use of either ERalpha or ERbeta proteins and [3H]E2, at a fixed concentration of 0.5 nM, as the labeled ligand. Recombinant human ERalpha or ERbeta proteins were dissolved in binding buffer (10 mM Tris-HCL, pH 7.5, 10% glycerol, 1 mM DTT, 1 mg/ml BSA) and duplicate aliquots were then incubated with [3H]E2 at a final concentration of 0.5 nM, together with a vehicle control (0.4% DMSO), or the same amount of vehicle containing increasing concentrations of unlabeled steroid ligands as competitors. After incubation for 2 h at 25 C., the unbound ligands were removed and the amounts of [3H]E2 bound to either ERalpha or ERbeta proteins were measured.
|
Homo sapiens
|
0.015
nM
|
|
|
Antiproliferative activity against tamoxifen resistant human MCF7:5C cells assessed as inhibition of cell growth after 9 days by MTS assay
|
Homo sapiens
|
60.0
%
|
|
|
Competitive binding affinity to G-protein coupled estrogen receptor (unknown origin) expressed in COS7 cells by E2 Alexa 633 staining based fluorescence analysis
|
Homo sapiens
|
2.7
nM
|
|
|
Inhibition of ER-alpha (unknown origin) by Lanthascreen-FRET assay
|
Homo sapiens
|
1.7
nM
|
|
|
Inhibition of ER-beta (unknown origin) by Lanthascreen-FRET assay
|
Homo sapiens
|
3.0
nM
|
|
|
Displacement of fluorescent ES2 from recombinant human ERalpha after 2 hrs in absence of light by fluorometric analysis
|
Homo sapiens
|
5.7
nM
|
|
|
Displacement of fluorescent ES2 from recombinant human ERbeta after 2 hrs in absence of light by fluorometric analysis
|
Homo sapiens
|
5.6
nM
|
|
|
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
|
4.4
nM
|
|
|
Displacement of fluormone-labeled ES2 from recombinant full length human ERalpha ligand binding domain expressed in insect cells after 2 hrs by TR-FRET assay
|
Homo sapiens
|
0.41
nM
|
|
|
Luciferase Assay: Estrogen receptor-negative CV-1 kidney cells are maintained in Dulbecco's modified Eagle's medium with 4.5 g/L glucose supplemented with 10% fetal bovine serum and 100 units/ml penicillin-streptomycin at 37° C. in a humidified 5% CO2 atmosphere. The cells are then plated in 6-well dishes at a density of 2×10^5 cells per well in phenol-red free Dulbecco's modified Eagle's medium containing 10% charcoal-dextran-stripped fetal bovine serum. CV-1 cells are transfected using LipofectAMINE reagent according to the manufacturer's protocol. Transfections containing 1.5 μg of reporter plasmid (containing ERE-tk-luciferase containing a single ERE cloned upstream of the thymidine kinase promoter and luciferase gene) and 0.5 μg of either ERα or ERβ expression vector (containing CMV-ERα or CMV-ERβ full length coding sequence respectively). The next day, cells receive no treatment (controls) or are treated with estradiol alone (1 nM) or estradiol plus a compound of the invention (at varying concentrations). After 16-24 hours, cells are harvested and assayed for luciferase activity. At the outset, cell monolayers are washed twice with ice-cold phosphate-buffered saline and incubated for 15 minutes in 250 μl of 1× cell culture lysis reagent (Promega, Madison, Wis.). Cell extracts are transferred to a fresh tube and assayed using the luciferase assay system (Promega). For each assay, 10 μl of extract is diluted with 90 μl of 1× cell culture lysis reagent. Luminescence is read using an AutoLumat LB953 luminometer.
|
Homo sapiens
|
1.9
nM
|
|
|
Luciferase Assay: Estrogen receptor-negative CV-1 kidney cells are maintained in Dulbecco's modified Eagle's medium with 4.5 g/L glucose supplemented with 10% fetal bovine serum and 100 units/ml penicillin-streptomycin at 37° C. in a humidified 5% CO2 atmosphere. The cells are then plated in 6-well dishes at a density of 2×10^5 cells per well in phenol-red free Dulbecco's modified Eagle's medium containing 10% charcoal-dextran-stripped fetal bovine serum. CV-1 cells are transfected using LipofectAMINE reagent according to the manufacturer's protocol. Transfections containing 1.5 μg of reporter plasmid (containing ERE-tk-luciferase containing a single ERE cloned upstream of the thymidine kinase promoter and luciferase gene) and 0.5 μg of either ERα or ERβ expression vector (containing CMV-ERα or CMV-ERβ full length coding sequence respectively). The next day, cells receive no treatment (controls) or are treated with estradiol alone (1 nM) or estradiol plus a compound of the invention (at varying concentrations). After 16-24 hours, cells are harvested and assayed for luciferase activity. At the outset, cell monolayers are washed twice with ice-cold phosphate-buffered saline and incubated for 15 minutes in 250 μl of 1× cell culture lysis reagent (Promega, Madison, Wis.). Cell extracts are transferred to a fresh tube and assayed using the luciferase assay system (Promega). For each assay, 10 μl of extract is diluted with 90 μl of 1× cell culture lysis reagent. Luminescence is read using an AutoLumat LB953 luminometer.
|
Homo sapiens
|
1.7
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
|
0.82
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
|
1.59
nM
|
|
|
Binding affinity to ER (unknown origin) expressed in UAS-bla GripTite 293 cells by Select screen competitive binding assay
|
Homo sapiens
|
2.3
nM
|
|
|
Inhibition of fluormone ES2 binding to recombinant full length human ERbeta expressed in insect cells by fluorescence polarization assay
|
Homo sapiens
|
6.65
nM
|
|
|
Inhibition of recombinant human CYP1B1 expressed in supersomes coexpressing P450 reductase at 0.3 uM using 7-ethyl-O-resorufin as substrate after 45 mins in presence of NADPH by fluorescence assay relative to control
|
Homo sapiens
|
12.4
%
|
|
|
Displacement of Fluor.ES2 Green from human ERalpha by TR-FRET competitive binding assay
|
Homo sapiens
|
0.452
nM
|
|
|
Inhibition of fluoromone binding to recombinant human full length untagged ERalpha expressed in insect cells after 2 hrs by fluorescence polarization assay
|
Homo sapiens
|
4.804
nM
|
|
|
Inhibition of fluoromone binding to recombinant human full length untagged ERbeta expressed in insect cells after 2 hrs by fluorescence polarization assay
|
Homo sapiens
|
1.28
nM
|
|
|
Estrogenic activity at estrogen receptor alpha in human Ishikawa cells assessed as induction of alkaline phosphatase activity using p-Nitrophenol phosphate as substrate pretreated for 96 hrs followed by substrate addition measured every 15 secs by scanning spectrophotometric analysis
|
Homo sapiens
|
0.2
nM
|
|
|
Displacement of Fluormone ES2 Green from full-length estrogen receptor alpha (unknown origin) after 2 hrs by fluorescence polarization assay
|
Homo sapiens
|
5.7
nM
|
|
|
Displacement of Fluormone ES2 Green from full-length estrogen receptor beta (unknown origin) after 2 hrs by fluorescence polarization assay
|
Homo sapiens
|
5.6
nM
|
|
|
Agonist activity at recombinant human GAL4-fused ERalpha expressed in HEk293 cells by luciferase reporter gene assay
|
Homo sapiens
|
0.11
nM
|
|
|
Estrogenic activity at ERalpha in human Ishikawa cells assessed as induction of alkaline phosphatase activity using p-nitrophenol as substrate treated for 96 hrs followed by substrate addition by spectrophotometric method
|
Homo sapiens
|
0.03
nM
|
|
|
Estrogenic activity at ERbeta (unknown origin) expressed in human MDA-MB-231/beta41 cells after 18 hrs by renilla luciferase reporter gene assay
|
Homo sapiens
|
0.03
nM
|
|
|
Inhibition of fluorescein-tagged estrogen binding to GST-tagged ERbeta (unknown origin) ligand binding domain after 1 hr by LanthaScreen TR-FRET assay
|
Homo sapiens
|
0.25
nM
|
|
|
Inhibition of fluorescein-tagged estrogen binding to GST-tagged ERalpha (unknown origin) ligand binding domain after 1 hr by LanthaScreen TR-FRET assay
|
Homo sapiens
|
0.26
nM
|
|
|
Agonist activity at full length ERalpha (unknown origin) after 24 hrs by ERE-driven luciferase reporter gene assay
|
Homo sapiens
|
0.31
nM
|
|
|
Agonist activity at full length ERbeta (unknown origin) after 24 hrs by cell based ERE-driven luciferase reporter gene assay
|
Homo sapiens
|
0.022
nM
|
|
|
Agonist activity at GAL4 DNA-binding domain fused ERalpha (unknown origin) ligand binding domain expressed in UAS-bla GripTite 293 cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay
|
Homo sapiens
|
0.107
nM
|
|
|
Agonist activity at GAL4 DNA-binding domain fused ERbeta (unknown origin) ligand binding domain expressed in UAS-bla GripTite 293 cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay
|
Homo sapiens
|
0.579
nM
|
|
|
Antibacterial activity against Staphylococcus aureus MRSA ATCC 43300 (CO-ADD:GP_020); MIC in CAMBH media, using NBS plates, by OD(600)
|
Staphylococcus aureus subsp. aureus
|
2.2
%
|
|
|
Antibacterial activity against Escherichia coli ATCC 25922 (CO-ADD:GN_001); MIC in CAMBH media using NBS plates, by OD(600)
|
Escherichia coli
|
-0.2
%
|
|
|
Antibacterial activity against Klebsiella pneumoniae MDR ATCC 70063 (CO-ADD:GN_003); MIC in CAMBH media using NBS plates, by OD(600)
|
Klebsiella pneumoniae
|
5.27
%
|
|
|
Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 (CO-ADD:GN_042); MIC in CAMBH media using NBS plates, by OD(600)
|
Pseudomonas aeruginosa
|
2.47
%
|
|
|
Antibacterial activity against Acinetobacter baumannii ATCC 19606 (CO-ADD:GN_034); MIC in CAMBH media using NBS plates, by OD600
|
Acinetobacter baumannii
|
15.11
%
|
|
|
Antifungal activity against Candida albicans ATCC 90028 (CO-ADD:FG_001); MIC in YNB media using NBS plates, by OD630
|
Candida albicans
|
5.91
%
|
|
|
Antifungal activity against Cryptococcus neoformans H99 ATCC 208821 (CO-ADD:FG_002); MIC in YNB media using NBS plates, by Resazurin OD(600-570)
|
Cryptococcus neoformans
|
-4.05
%
|
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells at 10 uM after 48 hours by high content imaging
|
Homo sapiens
|
2.32
%
|
|
|
Binding affinity to purified human ERalpha LBD assessed as dissociation constant incubated for 2 hrs by fluorescence tracer based competitive fluorometric binding assay
|
Homo sapiens
|
3.49
nM
|
|
|
Binding affinity to ERbeta (unknown origin) assessed as dissociation constant incubated for 2 hrs by fluorescence tracer based competitive fluorometric binding assay
|
Homo sapiens
|
4.12
nM
|
|
|
Binding affinity to human GST-tagged estrogen receptor beta ligand binding domain after 1 hr by TR-FRET assay
|
Homo sapiens
|
0.25
nM
|
|
|
Agonist activity at GAL4 DNA binding domain fused full-length chimeric estrogen receptor beta (unknown origin) by FRET-based assay
|
Homo sapiens
|
0.151
nM
|
|
|
Agonist activity at GAL4 DNA binding domain fused full-length chimeric estrogen receptor alpha (unknown origin) by FRET-based assay
|
Homo sapiens
|
0.107
nM
|
|
|
Agonist activity at human GST-tagged estrogen receptor beta ligand binding domain assessed as coactivator peptide PGC1a recruitment by TR-FRET assay
|
Homo sapiens
|
2.79
nM
|
|
|
Agonist activity at human GST-tagged estrogen receptor alpha ligand binding domain assessed as coactivator peptide PGC1a recruitment by TR-FRET assay
|
Homo sapiens
|
2.58
nM
|
|
|
Agonist activity at estrogen receptor beta (unknown origin) after 22 hrs by cell-based luciferase reporter gene assay
|
Homo sapiens
|
0.022
nM
|
|
|
Agonist activity at estrogen receptor alpha (unknown origin) after 22 hrs by cell-based luciferase reporter gene assay
|
Homo sapiens
|
0.31
nM
|
|
|
Agonist activity at ER (unknown origin) by Alpha Screen assay
|
Homo sapiens
|
1.0
nM
|
|
|
Agonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ER-alpha-mediated transcriptional activity by luciferase reporter gene assay
|
Homo sapiens
|
0.13
nM
|
|
|
Selective estrogen receptor down-regulator activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as induction of ERalpha degradation by luciferase reporter gene assay
|
Homo sapiens
|
0.09
nM
|
|
|
Activation of human ERbeta assessed as induction of transcriptional activation incubated for 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.02
nM
|
|
|
Activation of human ERbeta assessed as induction of transcriptional activation by luciferase reporter gene assay
|
Homo sapiens
|
0.03
nM
|
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
24.22
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
8.25
%
|
|
SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response from peptide substrate
|
Severe acute respiratory syndrome coronavirus 2
|
15.0
%
|
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.94
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.18
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.07
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.94
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
-0.07
%
|
|
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
|
Chlorocebus sabaeus
|
0.18
%
|
|
|
Displacement of [3H]17-beta estradiol from GST-fused human recombinant ERalpha ligand binding domain expressed in Escherichia coli BL21alpha cells incubated for 1 hr by liquid scintillation counting method
|
Homo sapiens
|
0.72
nM
|
|
|
Displacement of [3H]17-beta estradiol from GST-fused human recombinant ERbeta ligand binding domain expressed in Escherichia coli BL21alpha cells incubated for 1 hr by liquid scintillation counting method
|
Homo sapiens
|
0.67
nM
|
|
|
Agonist activity at ERalpha (unknown origin) expressed in human HeLa cells assessed as transcriptional activation measured after 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.21
nM
|
|
|
Agonist activity at ERbeta (unknown origin) expressed in human HeLa cells assessed as transcriptional activation measured after 24 hrs by luciferase reporter gene assay
|
Homo sapiens
|
0.37
nM
|
|
|
Agonist activity at human ER
|
Homo sapiens
|
1.0
nM
|
|
|
Displacement of fluorescent-labelled E2 from recombinant human GST-tagged ERalpha by LanthaScreen TR-FRET assay
|
Homo sapiens
|
0.33
nM
|
|
|
Displacement of fluorescent-labelled E2 from recombinant human GST-tagged ERbeta by LanthaScreen TR-FRET assay
|
Homo sapiens
|
1.02
nM
|
|
|
Agonist activity at human ERbeta receptor expressed in HEK293T cells transfected with pGL4.27-(ERE)3-Luc assessed as transcriptional activation measured after 16 hrs by Dual-Glo luciferase assay
|
Homo sapiens
|
0.04
nM
|
|
|
Agonist activity at human ERalpha receptor expressed in HEK293T cells transfected with pGL4.27-(ERE)3-Luc assessed as transcriptional activation measured after 16 hrs by Dual-Glo luciferase assay
|
Homo sapiens
|
0.35
nM
|
|
|
Displacement of fluormone from GST-tagged ERbeta receptor LBD (unknown origin) measured after 60 mins by TR-FRET competitive binding assay
|
Homo sapiens
|
0.21
nM
|
|
|
Agonist activity at full length human ERalpha receptor assessed as transcriptional activity incubated for 22 to 24 hrs by cell based luciferase reporter gene assay
|
Homo sapiens
|
0.31
nM
|
|
|
Agonist activity at full length human ERbeta receptor assessed as transcriptional activity incubated for 22 to 24 hrs by cell based luciferase reporter gene assay
|
Homo sapiens
|
0.022
nM
|
|
|
Binding affinity of ERalpha LBD (unknown origin) incubated for 2 hrs by LanthaScreen TR-FRET assay
|
Homo sapiens
|
0.58
nM
|
|
|
Binding affinity to human ERalpha by competitive fluorometric receptor binding assay
|
Homo sapiens
|
1.1
nM
|
|
|
Displacement of fluorescent-labeled E2 from LBD of ERalpha (unknown origin) by TR-FRET assay
|
Homo sapiens
|
0.33
nM
|
|
|
Displacement of fluorescent-labeled E2 from LBD of ERbeta (unknown origin) by TR-FRET assay
|
Homo sapiens
|
1.02
nM
|
|
|
Antagonist activity at ERalpha (unknown origin) assessed as inhibition of fluorescein-labelled coactivator PGC1 peptide recruitment at 4 nM incubated for 10 mins by LanthaScreen TR-FRET assay relative to control
|
Homo sapiens
|
80.0
%
|
|
|
Antagonist activity at ERalpha (unknown origin) assessed as inhibition of fluorescein-labelled coactivator PGC1 peptide recruitment at 4 nM incubated for 30 mins by LanthaScreen TR-FRET assay relative to control
|
Homo sapiens
|
80.0
%
|
|
|
Antagonist activity at ERbeta (unknown origin) assessed as inhibition of fluorescein-labelled coactivator PGC1 peptide recruitment at 34 nM incubated for 30 mins by LanthaScreen TR-FRET assay relative to control
|
Homo sapiens
|
80.0
%
|
|
