BDBM50276802 4-OHT::Afimoxifene::TamoGel

SMILES CCC(=C(c1ccc(O)cc1)c1ccc(OCCN(C)C)cc1)c1ccccc1

InChI Key InChIKey=TXUZVZSFRXZGTL-QPLCGJKRSA-N

Data  4 KI  13 IC50  1 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 18 hits for monomerid = 50276802   

TargetEstrogen receptor beta(Homo sapiens (Human))
Le Centre Hospitalier Universitaire De Qu£Bec

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataKi:  0.249nMAssay Description:Inhibition of estradiol binding to estrogen receptor in Human Breast cancer cytosol (3.3% ethanol)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor beta(Homo sapiens (Human))
Le Centre Hospitalier Universitaire De Qu£Bec

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataKi:  0.346nMAssay Description:Apparent inhibition constant for estrogen receptor in Human uterine cytosol in 3.3%ethanolMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Glaxosmithkline Research & Development

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataKi:  2.5nMAssay Description:Binding affinity for human estrogen receptor alphaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor beta(Homo sapiens (Human))
Glaxosmithkline Research & Development

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataKi:  3.20nMAssay Description:Binding affinity for human estrogen receptor betaMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor beta(Homo sapiens (Human))
Le Centre Hospitalier Universitaire De Qu£Bec

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataIC50:  10nMAssay Description:Antagonist activity at estrogen receptor alpha/beta in human Ishikawa cells after 72 hrs by alkaline phosphatase assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor beta(Homo sapiens (Human))
Glaxosmithkline Research & Development

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataIC50:  26nMAssay Description:Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length estrogen receptor beta after 2 hrs by fluorescence pola...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Glaxosmithkline Research & Development

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataIC50:  26nMAssay Description:Displacement of fluorescein-labeled estradiol (fluoromone) from human recombinant full-length estrogen receptor alpha after 2 hrs by fluorescence pol...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor beta(Homo sapiens (Human))
Le Centre Hospitalier Universitaire De Qu£Bec

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataIC50:  0.5nMAssay Description:Antagonism of estrogen action in a mammary tumor cell line was assayed via inhibition of MCF-7 cell proliferation stimulated by 10 e-11 M 17-beta-est...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor beta(Homo sapiens (Human))
Le Centre Hospitalier Universitaire De Qu£Bec

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataIC50:  3nMAssay Description:Anti-estrogenicity for 50% inhibition of the MVLN cell luciferase activity due to 0.1 nM E2 (estradiol)More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor beta(Homo sapiens (Human))
Le Centre Hospitalier Universitaire De Qu£Bec

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataIC50:  7nMAssay Description:Inhibition of estradiol induced estrogen receptor transcriptional activation in MCF-7-2a cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor beta(Homo sapiens (Human))
Le Centre Hospitalier Universitaire De Qu£Bec

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataIC50:  510nMAssay Description:Antagonist activity as inhibition of 1 nM 17-beta-estradiol stimulated alkaline phosphatase induction in Ishikawa endometrial cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor beta(Homo sapiens (Human))
Le Centre Hospitalier Universitaire De Qu£Bec

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataEC50:  0.800nMAssay Description:Agonist activity as alkaline phosphatase induction in Ishikawa endometrial cells compared to E2More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor beta(Homo sapiens (Human))
Le Centre Hospitalier Universitaire De Qu£Bec

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataIC50:  2.60nMAssay Description:Antagonist effect against 10 pM 17-beta-estradiol induced MCF-7 cell proliferationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Glaxosmithkline Research & Development

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataIC50:  70nMAssay Description:Antagonist activity at recombinant human ERalpha expressed in HEK293 cells assessed as inhibition of estradiol-induced YFP-fused SRC1 coactivator rec...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetSteroid hormone receptor ERR2(Homo sapiens (Human))
Janssen Research And Development

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataIC50:  886nMAssay Description:Antagonist activity at recombinant GST-tagged human ERRbeta LBD assessed as inhibition of fluorescein-labeled coactivator peptide recruitment preincu...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor beta(Homo sapiens (Human))
Le Centre Hospitalier Universitaire De Qu£Bec

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataIC50:  1.60nMAssay Description:pIC50 for 1 nM estradiol-induced Ishikawa cell proliferationMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen-related receptor gamma(Homo sapiens (Human))
Janssen Research And Development

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataIC50:  11nMAssay Description:Antagonist activity at ERRgamma (unknown origin) assessed as inhibition of co-activator peptide recruitment by TR-FRET assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Glaxosmithkline Research & Development

Curated by ChEMBL
LigandPNGBDBM50276802(4-OHT | Afimoxifene | TamoGel)
Affinity DataIC50:  6.30nMAssay Description:Inhibition of fluormone ES2 green binding to recombinant full length human ERalpha expressed in insect cells by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed