BDBM301005 5-fluoro-N-(1- (3- fluoropropyl) azetidin-3-yl)-6- ((6S,8R)-8- methyl-7- (2,2,3- trifluoropropyl)- 6,7,8,9- tetrahydro-3H- pyrazolo[4,3- f]isoquinolin- 6-yl)pyridin-3- amine::US10131663, Example 71::US10590130, Example 71::US10961241, Example 71

SMILES C[C@@H]1Cc2c(ccc3[nH]ncc23)[C@H](N1CC(F)(F)CF)c1ncc(NC2CN(CCCF)C2)cc1F

InChI Key InChIKey=GGSBMAVBGZRJPI-UHFFFAOYSA-N

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 = 301005   

TargetEstrogen receptor(Human)
Astrazeneca

US Patent
LigandPNGBDBM301005(5-fluoro-N-(1- (3- fluoropropyl) azetidin-3-yl)-6-...)
Affinity DataIC50: 2nMAssay 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
LigandPNGBDBM301005(5-fluoro-N-(1- (3- fluoropropyl) azetidin-3-yl)-6-...)
Affinity DataIC50: 0.170nMAssay 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

LigandPNGBDBM301005(5-fluoro-N-(1- (3- fluoropropyl) azetidin-3-yl)-6-...)
Affinity DataIC50: 2nMAssay 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
LigandPNGBDBM301005(5-fluoro-N-(1- (3- fluoropropyl) azetidin-3-yl)-6-...)
Affinity DataIC50: 2nMAssay 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
LigandPNGBDBM301005(5-fluoro-N-(1- (3- fluoropropyl) azetidin-3-yl)-6-...)
Affinity DataIC50: 2nMAssay 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
LigandPNGBDBM301005(5-fluoro-N-(1- (3- fluoropropyl) azetidin-3-yl)-6-...)
Affinity DataIC50: 0.126nMAssay 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