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Found 12 Enz. Inhib. hit(s) with Target = 'Estrogen receptor' and Ligand = 'BDBM300969'
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300969(BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...)
Affinity DataIC50:  0.120nMAssay Description:The ability of compounds to down-regulate Estrogen Receptor (ER) numbers was assessed in a cell based immuno-fluorescence assay using the MCF-7 human...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300969(BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...)
Affinity DataIC50:  0.126nMAssay Description:Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha expression in presence of cycloheximide by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300969(BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...)
Affinity DataIC50:  0.158nMAssay Description:Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ER-alpha level incubated for 18 to 24 hrs by Alexa fluor 488/Hoechst sta...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300969(BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...)
Affinity DataIC50:  0.158nMAssay Description:Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha expression by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300969(BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...)
Affinity DataIC50:  0.158nMAssay Description:Induction of ERalpha degradation in human MCF7 cells incubated for 18 to 22 hrs by immuno-fluorescence assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300969(BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...)
Affinity DataIC50:  0.170nMAssay Description:The ability of compounds to down-regulate Estrogen Receptor (ER) numbers was assessed in a cell based immuno-fluorescence assay using the MCF-7 human...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300969(BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...)
Affinity DataIC50:  1.5nMAssay Description:The assay principle is that ER alpha-LBD (GST) is added to a fluorescent ligand to form a receptor/fluorophore complex. A terbium-labelled anti-GST a...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300969(BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...)
Affinity DataIC50:  1.80nMAssay Description:The assay principle is that ER alpha-LBD (GST) is added to a fluorescent ligand to form a receptor/fluorophore complex. A terbium-labelled anti-GST a...More data for this Ligand-Target Pair
In DepthDetails US Patent
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300969(BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...)
Affinity DataIC50:  2.5nMAssay Description:Displacement of fluorescent labelled fluormone ES2 from human recombinant GST tagged ER alpha LBD ( 282 to 595 residues) expressed in baculovirus inf...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300969(BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...)
Affinity DataIC50:  2.5nMAssay Description:Displacement of fluormone ES2 green reagent from human GST-tagged ERalpha LBD (282 to 595 residues) expressed in baculovirus infected insect cells in...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300969(BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...)
Affinity DataIC50:  6.30nMAssay Description:Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha expression in presence of tamoxifen by Western blot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300969(BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...)
Affinity DataIC50: <316nMAssay Description:Agonist activity at ERalpha in human MCF7 cells assessed as increase in progesterone receptor expression level by western blot analysisMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed