BDBM300991 6-((6S,8R)-7- ((1- fluorocyclo- propyl)methyl)-8- methyl- 6,7,8,9- tetrahydro-3H- pyrazolo[4 3- f]isoquinolin- 6-yl)-N-(1-(3- fluoropropyl) azetidin-3-yl)- N- methylpyridin- 3-amine::US10131663, Example 57::US10590130, Example 57::US10961241, Example 57

SMILES C[C@@H]1Cc2c(ccc3[nH]ncc23)[C@H](N1CC1(F)CC1)c1ccc(cn1)N(C)C1CN(CCCF)C1

InChI Key

Data  6 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 6 hits for monomerid = 300991   

TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300991(6-((6S,8R)-7- ((1- fluorocyclo- propyl)methyl)-8- ...)
Affinity DataIC50:  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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300991(6-((6S,8R)-7- ((1- fluorocyclo- propyl)methyl)-8- ...)
Affinity DataIC50:  0.360nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetEstrogen receptor [307-554](Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300991(6-((6S,8R)-7- ((1- fluorocyclo- propyl)methyl)-8- ...)
Affinity DataIC50:  5nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300991(6-((6S,8R)-7- ((1- fluorocyclo- propyl)methyl)-8- ...)
Affinity DataIC50:  5nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetEstrogen receptor [307-554](Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300991(6-((6S,8R)-7- ((1- fluorocyclo- propyl)methyl)-8- ...)
Affinity DataIC50:  1.60E+4nMAssay 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...More data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails US Patent
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300991(6-((6S,8R)-7- ((1- fluorocyclo- propyl)methyl)-8- ...)
Affinity DataIC50:  1.60E+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
Ligand InfoPC cidPC sid
In DepthDetails US Patent