Compile Data Set for Download or QSAR
Report error Found 28 Enz. Inhib. hit(s) for PDB: 4Q50
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataKi:  0.0400nMAssay Description:Antagonistic activity against estrogen receptor alpha in presence of 0.1 nM estradiolMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataKi:  0.25nMAssay Description:In vitro displacement of 0.5 nM [3H]17-beta-estradiol from human Estrogen receptor alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 0.309nMAssay Description:Binding affinity to ERalpha receptor (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataKi:  0.390nMAssay Description:Displacement of [3H]estradiol from ERalpha after 4 hrs by scintillation countingMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/7/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 0.5nMAssay Description:Displacement of [3H]-E2 from human ER-alpha incubated for 16 to 20 hrs by liquid scintillation counting analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/6/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataKi:  0.5nMAssay Description:Binding affinity for estrogen receptor alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 0.790nMAssay Description:Antagonist activity at FLAG-tagged ERalpha (unknown origin) expressed in HEK293 cells assessed as reduction in E2-induced ER-alpha-mediated transcrip...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 1.40nMAssay Description:Antagonist activity at estrogen receptor in human T47D cells incubated for 18 hrs by ultra high sensitivity luminescence reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/22/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 2nMpH: 7.4 T: 2°CAssay Description:Binding affinity was measured by a scintillation proximity binding assay using [3H]4-OHT (for ERRgamma) or [3H]estradiol (for ERalpha) as radioligand...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/31/2008
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 2.10nMAssay Description:Binding affinity to GST-tagged human ER alpha ligand-binding domain by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 2.20nMAssay Description:Displacement of fluorescent-labeled E2 from LBD of ERalpha (unknown origin) by TR-FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 2.30nMAssay Description:Antagonist activity at ERalpha (unknown origin) expressed in human U2OS cells assessed as inhibition of E2-induced transactivation by dual luciferase...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor beta(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 2.60nMAssay Description:Inhibition of estradiol-stimulated MCF-7 breast adenocarcinoma cell proliferationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 3nMAssay Description:Antagonist activity at ERalpha in human MCF7 cells assessed as inhibition of estrogen-induced transcription preincubated overnight followed by estrog...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/9/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 3.80nMAssay Description:Antagonist activity at ER-alpha (unknown origin) by ER-alpha coactivator assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 5.60nMAssay Description:Inhibition of ERalpha (unknown origin) by fluorescence polarization-based competition binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/12/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataKi:  5.70nMAssay Description:Binding affinity towards human estrogen receptor alpha in a competitive binding assay using fluorescently labelled estradiolMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor beta(Rat)
University of Georgia

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataEC50:  6nMAssay Description:In vitro displacement of 3 nM [3H]4-hydroxytamoxifen from estrogen receptor of rat uterine cystolMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/3/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 7.5nMAssay Description:Displacement of fluorescent labeled-ligand from ERalpha (unknown origin) by competitive binding assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/7/2023
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataEC50:  9.90nMAssay Description:Antagonist activity against ERalpha in estradiol stimulated HEK293T cells measuring luciferase activity after 24 hrs by luciferase reporter assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/14/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 17nM EC50:  10.3nMpH: 7.4 T: 2°CAssay Description:Radioligand binding assay was performed by using 96-well microtiterplates containing ER, 17beta-estradiol, and the test compound to be tested and SPA...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/16/2008
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataEC50:  16nMAssay Description:Binding affinity for Estrogen receptor alphaMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataKi:  20nMAssay Description:Binding affinity to ERalpha (unknown origin) assessed as inhibition constant incubated for 2 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/16/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Mouse)
National Institute of Health Sciences

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 33nMAssay Description:Antagonist activity at estrogen receptor in mouse GT1-7 cells harboring beta-galactosidase reporter gene assessed as reduction in 17beta-estradiol in...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/2/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 40nMAssay Description:Displacement of fluorescein labeled estradiol from human recombinant ERalpha expressed in baculovirus infected insect cells by fluorescence polarizat...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 4.40E+3nMAssay Description:Antiestrogenic activity at estrogen receptor alpha expressed in yeast cells assessed as inhibition of 17-beta-estradiol-induced beta-galactosidase ac...More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 4.90E+3nMAssay Description:Antagonist activity at ERalpha receptor in human MCF7 cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/11/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetEstrogen receptor(Human)
University of California

Curated by ChEMBL
LigandPNGBDBM20608([3H]4-OHT | cid_449459 | CHEMBL489 | AFIMOXIFENE |...)
Affinity DataIC50: 2.58E+4nMAssay Description:Inhibition of ERalpha (unknown origin) in MCF7 cells measured after 24 to 48 hrs by FRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
6/18/2023
Entry Details
PubMedPDB3D3D Structure (crystal)