BDBM300997 6-((6S,8R)-7- (2-fluoro-2- methylpropyl)- 8-methyl- 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 63::US10590130, Example 70::US10961241, Example 63

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

InChI Key InChIKey=RMHSPVDIAHEXNT-UHFFFAOYSA-N

Data  10 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 10 hits for monomerid = 300997   

TargetEstrogen receptor(Human)
Astrazeneca

US Patent
LigandPNGBDBM300997(6-((6S,8R)-7- (2-fluoro-2- methylpropyl)- 8-methyl...)
Affinity DataIC50: 73nMAssay 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
In Depth
Date in BDB:
3/29/2019
Entry Details
Go to US Patent

TargetEstrogen receptor(Human)
Astrazeneca

US Patent
LigandPNGBDBM300997(6-((6S,8R)-7- (2-fluoro-2- methylpropyl)- 8-methyl...)
Affinity DataIC50: 0.310nMAssay 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
In Depth
Date in BDB:
3/29/2019
Entry Details
Go to US Patent

LigandPNGBDBM300997(6-((6S,8R)-7- (2-fluoro-2- methylpropyl)- 8-methyl...)
Affinity DataIC50: 1.30E+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
In Depth
Date in BDB:
3/29/2019
Entry Details
Go to US Patent

LigandPNGBDBM300997(6-((6S,8R)-7- (2-fluoro-2- methylpropyl)- 8-methyl...)
Affinity DataIC50: 73nMAssay 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
In Depth
Date in BDB:
12/7/2020
Entry Details
Go to US Patent

LigandPNGBDBM300997(6-((6S,8R)-7- (2-fluoro-2- methylpropyl)- 8-methyl...)
Affinity DataIC50: 4.30nMAssay 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
In Depth
Date in BDB:
12/7/2020
Entry Details
Go to US Patent

TargetEstrogen receptor [307-554](Human)
Astrazeneca

US Patent
LigandPNGBDBM300997(6-((6S,8R)-7- (2-fluoro-2- methylpropyl)- 8-methyl...)
Affinity DataIC50: 1.30E+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
In Depth
Date in BDB:
12/7/2020
Entry Details
Go to US Patent

TargetEstrogen receptor [307-554](Human)
Astrazeneca

US Patent
LigandPNGBDBM300997(6-((6S,8R)-7- (2-fluoro-2- methylpropyl)- 8-methyl...)
Affinity DataIC50: 2.40E+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
In Depth
Date in BDB:
12/7/2020
Entry Details
Go to US Patent

TargetEstrogen receptor [307-554](Human)
Astrazeneca

US Patent
LigandPNGBDBM300997(6-((6S,8R)-7- (2-fluoro-2- methylpropyl)- 8-methyl...)
Affinity DataIC50: 73nMAssay 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
In Depth
Date in BDB:
10/4/2021
Entry Details
Go to US Patent

TargetEstrogen receptor(Human)
Astrazeneca

US Patent
LigandPNGBDBM300997(6-((6S,8R)-7- (2-fluoro-2- methylpropyl)- 8-methyl...)
Affinity DataIC50: 0.316nMAssay 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
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

US Patent
LigandPNGBDBM300997(6-((6S,8R)-7- (2-fluoro-2- methylpropyl)- 8-methyl...)
Affinity DataIC50: 3.20nMAssay 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
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed