BDBM300963 2-fluoro-N-(1-(3-fluoropropyl)azetidin-3-yl)-6-((6S,8R)-8-methyl-7-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinolin-6-yl)pyridin-3-amine::US10131663, Example 29::US10590130, Example 29::US10961241, Example 29

SMILES C[C@@H]1Cc2c(ccc3[nH]ncc23)[C@H](N1CC(F)(F)F)c1ccc(NC2CN(CCCF)C2)c(F)n1

InChI Key InChIKey=CRBIBFLRQNHOTI-UHFFFAOYSA-N

Data  8 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 8 hits for monomerid = 300963   

TargetEstrogen receptor(Human)
Astrazeneca

US Patent
LigandPNGBDBM300963(2-fluoro-N-(1-(3-fluoropropyl)azetidin-3-yl)-6-((6...)
Affinity DataIC50: 1.60nMAssay 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
In Depth
Date in BDB:
3/29/2019
Entry Details
Go to US Patent

TargetEstrogen receptor(Human)
Astrazeneca

US Patent
LigandPNGBDBM300963(2-fluoro-N-(1-(3-fluoropropyl)azetidin-3-yl)-6-((6...)
Affinity DataIC50: 0.200nMAssay 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

LigandPNGBDBM300963(2-fluoro-N-(1-(3-fluoropropyl)azetidin-3-yl)-6-((6...)
Affinity DataIC50: 2.70E+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

LigandPNGBDBM300963(2-fluoro-N-(1-(3-fluoropropyl)azetidin-3-yl)-6-((6...)
Affinity DataIC50: 1.60nMAssay 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
In Depth
Date in BDB:
12/7/2020
Entry Details
Go to US Patent

TargetEstrogen receptor [307-554](Human)
Astrazeneca

US Patent
LigandPNGBDBM300963(2-fluoro-N-(1-(3-fluoropropyl)azetidin-3-yl)-6-((6...)
Affinity DataIC50: 2.70E+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
LigandPNGBDBM300963(2-fluoro-N-(1-(3-fluoropropyl)azetidin-3-yl)-6-((6...)
Affinity DataIC50: 1.60nMAssay 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
In Depth
Date in BDB:
10/4/2021
Entry Details
Go to US Patent

TargetEstrogen receptor(Human)
Astrazeneca

US Patent
LigandPNGBDBM300963(2-fluoro-N-(1-(3-fluoropropyl)azetidin-3-yl)-6-((6...)
Affinity DataIC50: 1.60nMAssay Description:Displacement of fluorescent labelled fluormone ES2 from human recombinant GST tagged ER alpha LBD ( 282 to 595 residues) expressed in baculovirus inf...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

US Patent
LigandPNGBDBM300963(2-fluoro-N-(1-(3-fluoropropyl)azetidin-3-yl)-6-((6...)
Affinity DataIC50: 0.200nMAssay Description:Induction of ERalpha degradation in human MCF7 cells incubated for 18 to 22 hrs by immuno-fluorescence assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/28/2022
Entry Details Article
PubMed