BDBM300930 N-(4-((6S,8R)-7-((1-fluorocyclopropyl)methyl)-8-methyl-6,7,8,9-tetrahydro-3H-pyrazolo[4,3-f]isoquinolin-6-yl)-3-methoxyphenyl)-1-(3-fluoropropyl)azetidin-3-amine::US10131663, Example 6::US10590130, Example 6::US10961241, Example 6

SMILES COc1cc(NC2CN(CCCF)C2)ccc1[C@H]1N(CC2(F)CC2)[C@H](C)Cc2c1ccc1[nH]ncc21

InChI Key InChIKey=YZMMWVWLDOCLCK-UHFFFAOYSA-N

Data  11 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 11 hits for monomerid = 300930   

TargetEstrogen receptor(Human)
Astrazeneca

US Patent
LigandPNGBDBM300930(N-(4-((6S,8R)-7-((1-fluorocyclopropyl)methyl)-8-me...)
Affinity DataIC50: 8.80nMAssay 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
LigandPNGBDBM300930(N-(4-((6S,8R)-7-((1-fluorocyclopropyl)methyl)-8-me...)
Affinity DataIC50: 0.350nMAssay 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

LigandPNGBDBM300930(N-(4-((6S,8R)-7-((1-fluorocyclopropyl)methyl)-8-me...)
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

LigandPNGBDBM300930(N-(4-((6S,8R)-7-((1-fluorocyclopropyl)methyl)-8-me...)
Affinity DataIC50: 8.80nMAssay 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
LigandPNGBDBM300930(N-(4-((6S,8R)-7-((1-fluorocyclopropyl)methyl)-8-me...)
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
LigandPNGBDBM300930(N-(4-((6S,8R)-7-((1-fluorocyclopropyl)methyl)-8-me...)
Affinity DataIC50: 8.80nMAssay 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

LigandPNGBDBM300930(N-(4-((6S,8R)-7-((1-fluorocyclopropyl)methyl)-8-me...)
Affinity DataIC50: 9.10E+3nMAssay Description:Inhibition of human ERG by plate-based planar patch clamp techniqueMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetCytochrome P450 3A4(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM300930(N-(4-((6S,8R)-7-((1-fluorocyclopropyl)methyl)-8-me...)
Affinity DataIC50: 1.10E+4nMAssay Description:Inhibition of CYP3A4 in human liver microsomesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetCytochrome P450 2D6(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM300930(N-(4-((6S,8R)-7-((1-fluorocyclopropyl)methyl)-8-me...)
Affinity DataIC50: 1.20E+3nMAssay Description:Inhibition of CYP2D6 in human liver microsomesMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/22/2022
Entry Details Article
PubMed
TargetEstrogen receptor(Human)
Astrazeneca

US Patent
LigandPNGBDBM300930(N-(4-((6S,8R)-7-((1-fluorocyclopropyl)methyl)-8-me...)
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
LigandPNGBDBM300930(N-(4-((6S,8R)-7-((1-fluorocyclopropyl)methyl)-8-me...)
Affinity DataIC50: 7.90nMAssay 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