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| Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Estrogen receptor (Homo sapiens (Human)) | BDBM300969 (BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet  | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 0.120 | n/a | n/a | n/a | n/a | n/a | n/a |
AstraZeneca AB US Patent | Assay 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... | US Patent US10131663 (2018) BindingDB Entry DOI: 10.7270/Q2P55QJ9 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Estrogen receptor (Homo sapiens (Human)) | BDBM300969 (BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | Article PubMed | n/a | n/a | 0.126 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha expression in presence of cycloheximide by Western blot analysis | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c01163 BindingDB Entry DOI: 10.7270/Q2KK9GDB | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Estrogen receptor (Homo sapiens (Human)) | BDBM300969 (BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | Article PubMed | n/a | n/a | 0.158 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay 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... | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c01163 BindingDB Entry DOI: 10.7270/Q2KK9GDB | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Estrogen receptor (Homo sapiens (Human)) | BDBM300969 (BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | Article PubMed | n/a | n/a | 0.158 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha expression by Western blot analysis | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c01163 BindingDB Entry DOI: 10.7270/Q2KK9GDB | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Estrogen receptor (Homo sapiens (Human)) | BDBM300969 (BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | Article PubMed | n/a | n/a | 0.158 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Induction of ERalpha degradation in human MCF7 cells incubated for 18 to 22 hrs by immuno-fluorescence assay | Citation and Details Article DOI: 10.1021/acsmedchemlett.0c00505 BindingDB Entry DOI: 10.7270/Q2PR80PD | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Estrogen receptor (Homo sapiens (Human)) | BDBM300969 (BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 0.170 | n/a | n/a | n/a | n/a | n/a | n/a |
AstraZeneca AB US Patent | Assay 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... | US Patent US10131663 (2018) BindingDB Entry DOI: 10.7270/Q2P55QJ9 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Estrogen receptor (Homo sapiens (Human)) | BDBM300969 (BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 1.5 | n/a | n/a | n/a | n/a | n/a | n/a |
AstraZeneca AB US Patent | Assay 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... | US Patent US10131663 (2018) BindingDB Entry DOI: 10.7270/Q2P55QJ9 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Estrogen receptor (Homo sapiens (Human)) | BDBM300969 (BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | US Patent | n/a | n/a | 1.80 | n/a | n/a | n/a | n/a | n/a | n/a |
AstraZeneca AB US Patent | Assay 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... | US Patent US10131663 (2018) BindingDB Entry DOI: 10.7270/Q2P55QJ9 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Estrogen receptor (Homo sapiens (Human)) | BDBM300969 (BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | Article PubMed | n/a | n/a | 2.5 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Displacement of fluorescent labelled fluormone ES2 from human recombinant GST tagged ER alpha LBD ( 282 to 595 residues) expressed in baculovirus inf... | Citation and Details Article DOI: 10.1021/acsmedchemlett.0c00505 BindingDB Entry DOI: 10.7270/Q2PR80PD | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Estrogen receptor (Homo sapiens (Human)) | BDBM300969 (BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | Article PubMed | n/a | n/a | 2.5 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Displacement of fluormone ES2 green reagent from human GST-tagged ERalpha LBD (282 to 595 residues) expressed in baculovirus infected insect cells in... | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c01163 BindingDB Entry DOI: 10.7270/Q2KK9GDB | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Estrogen receptor (Homo sapiens (Human)) | BDBM300969 (BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | Article PubMed | n/a | n/a | 6.30 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Induction of ERalpha degradation in human MCF7 cells assessed as decrease in ERalpha expression in presence of tamoxifen by Western blot analysis | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c01163 BindingDB Entry DOI: 10.7270/Q2KK9GDB | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Estrogen receptor (Homo sapiens (Human)) | BDBM300969 (BDBM300970 | N-(1-(3- fluoropropyl) azetidin-3-yl)...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase MCE PC cid PC sid UniChem | Article PubMed | n/a | n/a | <316 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Agonist activity at ERalpha in human MCF7 cells assessed as increase in progesterone receptor expression level by western blot analysis | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c01163 BindingDB Entry DOI: 10.7270/Q2KK9GDB | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
