BDBM301006 (S)-6-(8,8- dimethyl-7- (2,2,2- trifluoroethyl)- 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 72::US10590130, Example 72::US10961241, Example 72

SMILES CC1(C)Cc2c(ccc3[nH]ncc23)[C@H](N1CC(F)(F)F)c1ccc(NC2CN(CCCF)C2)cn1

InChI Key InChIKey=QIMVRHMVKAJIDE-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 = 301006   

TargetEstrogen receptor(Human)
Astrazeneca

US Patent
LigandPNGBDBM301006((S)-6-(8,8- dimethyl-7- (2,2,2- trifluoroethyl)- 6...)
Affinity DataIC50: 2.90nMAssay 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
LigandPNGBDBM301006((S)-6-(8,8- dimethyl-7- (2,2,2- trifluoroethyl)- 6...)
Affinity DataIC50: 0.510nMAssay 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

LigandPNGBDBM301006((S)-6-(8,8- dimethyl-7- (2,2,2- trifluoroethyl)- 6...)
Affinity DataIC50: 2.90nMAssay 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
LigandPNGBDBM301006((S)-6-(8,8- dimethyl-7- (2,2,2- trifluoroethyl)- 6...)
Affinity DataIC50: 2.90nMAssay 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
LigandPNGBDBM301006((S)-6-(8,8- dimethyl-7- (2,2,2- trifluoroethyl)- 6...)
Affinity DataIC50: 0.501nMAssay 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
LigandPNGBDBM301006((S)-6-(8,8- dimethyl-7- (2,2,2- trifluoroethyl)- 6...)
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