BDBM140009 US8901310, Example 1

SMILES Cc1ncccc1NC(=O)c1ccc2c(CC[C@@H]3C[C@](O)(CC[C@@]23Cc2ccccc2)C(F)(F)F)c1

InChI Key InChIKey=QJJBNCHSWFGXML-UHFFFAOYSA-N

Data  5 IC50  1 EC50

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 6 hits for monomerid = 140009   

TargetGlucocorticoid receptor(Human)
Pfizer

US Patent
LigandPNGBDBM140009(US8901310, Example 1 )
Affinity DataIC50: 1.31nMAssay Description:The glucocorticoid receptor fluorescence polarization ligand binding (GRFP) assay is used to evaluate direct binding of testing compounds to full-len...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/4/2015
Entry Details
Go to US Patent

TargetGlucocorticoid receptor(Human)
Pfizer

US Patent
LigandPNGBDBM140009(US8901310, Example 1 )
Affinity DataIC50: 0.690nMAssay Description:Transrepression activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of PMA-stimulated gene e...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

US Patent
LigandPNGBDBM140009(US8901310, Example 1 )
Affinity DataIC50: 35nMAssay Description:Transrepression of GR in human whole blood assessed as inhibition of LPS-induced TNF-alpha release preincubated for 45 mins followed by LPS addition ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

US Patent
LigandPNGBDBM140009(US8901310, Example 1 )
Affinity DataIC50: 7.20nMAssay Description:Displacement of fluormone RED from human full length glucocorticoid receptor after 4 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

US Patent
LigandPNGBDBM140009(US8901310, Example 1 )
Affinity DataEC50:  4.80nMAssay Description:Transactivation activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells incubated for 24 hrs by beta-galactosidase repo...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Pfizer

US Patent
LigandPNGBDBM140009(US8901310, Example 1 )
Affinity DataIC50: 8.90nMAssay Description:Antagonist activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of dexamethasone induced tran...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/16/2020
Entry Details Article
PubMed