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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)) | BDBM300953 (N-(4-((6S,8R)-7-(2,2-difluoropropyl)-8-methyl-6,7,...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet  | PC cid PC sid UniChem | Article PubMed | n/a | n/a | 0.0398 | 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)) | BDBM300953 (N-(4-((6S,8R)-7-(2,2-difluoropropyl)-8-methyl-6,7,...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | US Patent | n/a | n/a | 0.0630 | 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)) | BDBM300953 (N-(4-((6S,8R)-7-(2,2-difluoropropyl)-8-methyl-6,7,...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | 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)) | BDBM300953 (N-(4-((6S,8R)-7-(2,2-difluoropropyl)-8-methyl-6,7,...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | US Patent | n/a | n/a | 2.60 | 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 | |||||||||||||
| Potassium voltage-gated channel subfamily H member 2 (Homo sapiens (Human)) | BDBM300953 (N-(4-((6S,8R)-7-(2,2-difluoropropyl)-8-methyl-6,7,...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | US Patent | n/a | n/a | 2.60 | n/a | n/a | n/a | n/a | n/a | n/a |
AstraZeneca AB US Patent | Assay Description hERG (human ether go go-related gene) potassium channels are essential for normal electrical activity in the heart. Arrhythmia can be induced by a bl... | US Patent US10590130 (2020) BindingDB Entry DOI: 10.7270/Q28S4SX5 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Estrogen receptor [307-554] (Homo sapiens (Human)) | BDBM300953 (N-(4-((6S,8R)-7-(2,2-difluoropropyl)-8-methyl-6,7,...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | PC cid PC sid UniChem | US Patent | n/a | n/a | 2.60 | n/a | n/a | n/a | n/a | n/a | n/a |
AstraZeneca AB US Patent | Assay Description The assay was performed as follows with all reagent additions carried out using the Beckman Coulter BioRAPTR FRD microfluidic workstation:1. Acoustic... | US Patent US10961241 (2021) BindingDB Entry DOI: 10.7270/Q2BR8W8P | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Potassium voltage-gated channel subfamily H member 2 (Homo sapiens (Human)) | BDBM300953 (N-(4-((6S,8R)-7-(2,2-difluoropropyl)-8-methyl-6,7,...) | PDB MMDB Reactome pathway KEGG UniProtKB/SwissProt B.MOAD DrugBank antibodypedia GoogleScholar AffyNet | PC cid PC sid UniChem | US Patent | n/a | n/a | 5.40E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
AstraZeneca AB US Patent | Assay Description hERG (human ether go go-related gene) potassium channels are essential for normal electrical activity in the heart. Arrhythmia can be induced by a bl... | US Patent US10131663 (2018) BindingDB Entry DOI: 10.7270/Q2P55QJ9 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Estrogen receptor [307-554] (Homo sapiens (Human)) | BDBM300953 (N-(4-((6S,8R)-7-(2,2-difluoropropyl)-8-methyl-6,7,...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | PC cid PC sid UniChem | US Patent | n/a | n/a | 5.40E+3 | n/a | n/a | n/a | n/a | n/a | n/a |
AstraZeneca AB US Patent | Assay Description ER: The ability of compounds to bind to isolated Estrogen Receptor Alpha Ligand binding domain (ER alpha-LBD (GST)) was assessed in competition assay... | US Patent US10590130 (2020) BindingDB Entry DOI: 10.7270/Q28S4SX5 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
