BDBM300978 6-((6S,8R)-7- (2,2- difluoroethyl)- 6,8-dimethyl- 6,7,8,9- tetrahydro-3H- pyrazolo[4,3- f]isoquinolin- 6-yl)-N-(1-(3- fluoropropyl) azetidin-3- yl)pyridin-3- amine::US10131663, Example 44::US10590130, Example 44::US10961241, Example 44

SMILES C[C@@H]1Cc2c(ccc3[nH]ncc23)[C@](C)(N1CC(F)F)c1ccc(NC2CN(CCCF)C2)cn1

InChI Key

Data  7 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 7 hits for monomerid = 300978   

TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300978(6-((6S,8R)-7- (2,2- difluoroethyl)- 6,8-dimethyl- ...)
Affinity DataIC50:  9.60nMAssay 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
LigandPNGBDBM300978(6-((6S,8R)-7- (2,2- difluoroethyl)- 6,8-dimethyl- ...)
Affinity DataIC50:  0.910nMAssay 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
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300978(6-((6S,8R)-7- (2,2- difluoroethyl)- 6,8-dimethyl- ...)
Affinity DataIC50:  9.60nMAssay 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(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300978(6-((6S,8R)-7- (2,2- difluoroethyl)- 6,8-dimethyl- ...)
Affinity DataIC50:  10nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetPotassium voltage-gated channel subfamily H member 2(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300978(6-((6S,8R)-7- (2,2- difluoroethyl)- 6,8-dimethyl- ...)
Affinity DataIC50:  1.30E+4nMAssay Description:Inhibition of human ERG by plate-based planar patch clamp techniqueMore data for this Ligand-Target Pair
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEstrogen receptor(Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300978(6-((6S,8R)-7- (2,2- difluoroethyl)- 6,8-dimethyl- ...)
Affinity DataIC50:  1nMAssay 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
Ligand InfoPC cidPC sid
In DepthDetails ArticlePubMed
TargetEstrogen receptor [307-554](Homo sapiens (Human))
Astrazeneca

US Patent
LigandPNGBDBM300978(6-((6S,8R)-7- (2,2- difluoroethyl)- 6,8-dimethyl- ...)
Affinity DataIC50:  9.60nMAssay 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