BDBM300994 2,2-difluoro-3- ((6S,8R)-6-(4- ((1-(3- fluoropropyl) azetidin-3- yl)amino)-2- methoxyphenyl)- 8-methyl- 3,6,8,9- tetrahydro-7H- pyrazolo[4,3- f]isoquinolin- 7-yl)propan-1- ol::US10131663, Example 60::US10961241, Example 60
SMILES COc1cc(NC2CN(CCCF)C2)ccc1[C@H]1N(CC(F)(F)CO)[C@H](C)Cc2c1ccc1[nH]ncc21
InChI Key
Data 6 IC50
Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB
Found 6 hits for monomerid = 300994
Affinity DataIC50: 4.70nMAssay 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
Affinity DataIC50: 0.190nMAssay 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
Affinity DataIC50: 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
Affinity DataIC50: 4.70nMAssay Description:The assay was performed as follows with all reagent additions carried out using the Beckman Coulter BioRAPTR FRD microfluidic workstation:1. Acoustic...More data for this Ligand-Target Pair
Affinity DataIC50: 0.200nMAssay 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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca
US Patent
Astrazeneca
US Patent
Affinity DataIC50: 1.10E+4nMAssay 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...More data for this Ligand-Target Pair