BDBM300985 6-((6S,8S)-7- (2,2- difluoroethyl)- 8- (difluoromethyl)- 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 51::US10590130, Example 51::US10961241, Example 51

SMILES FCCCN1CC(C1)Nc1ccc(nc1)[C@H]1N(CC(F)F)[C@@H](Cc2c1ccc1[nH]ncc21)C(F)F

InChI Key InChIKey=FWWHNGKEZAFESY-UHFFFAOYSA-N

Data  8 IC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
   Substructure
Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 8 hits for monomerid = 300985   

TargetEstrogen receptor(Human)
Astrazeneca

US Patent
LigandPNGBDBM300985(6-((6S,8S)-7- (2,2- difluoroethyl)- 8- (difluorome...)
Affinity DataIC50: 2.80nMAssay 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
LigandPNGBDBM300985(6-((6S,8S)-7- (2,2- difluoroethyl)- 8- (difluorome...)
Affinity DataIC50: 0.680nMAssay 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

LigandPNGBDBM300985(6-((6S,8S)-7- (2,2- difluoroethyl)- 8- (difluorome...)
Affinity DataIC50: 9.10E+3nMAssay 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

LigandPNGBDBM300985(6-((6S,8S)-7- (2,2- difluoroethyl)- 8- (difluorome...)
Affinity DataIC50: 2.80nMAssay 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
LigandPNGBDBM300985(6-((6S,8S)-7- (2,2- difluoroethyl)- 8- (difluorome...)
Affinity DataIC50: 9.10E+3nMAssay 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
LigandPNGBDBM300985(6-((6S,8S)-7- (2,2- difluoroethyl)- 8- (difluorome...)
Affinity DataIC50: 2.80nMAssay 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
LigandPNGBDBM300985(6-((6S,8S)-7- (2,2- difluoroethyl)- 8- (difluorome...)
Affinity DataIC50: 2.5nMAssay 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
LigandPNGBDBM300985(6-((6S,8S)-7- (2,2- difluoroethyl)- 8- (difluorome...)
Affinity DataIC50: 0.501nMAssay 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