Compile Data Set for Download or QSAR
Report error Found 6 Enz. Inhib. hit(s) with Target = 'Glucocorticoid receptor' and Ligand = 'BDBM19201'
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM19201((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataEC50:  57nMAssay Description:Transactivation of GAL-4 tagged glucocorticoid receptor ligand binding domain expressed in human HeLa cells assessed as NP1 activation by luciferase ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM19201((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataEC50:  2.20nMAssay Description:Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of PMA-induced AP1 activity after 6 hrs by l...More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2012
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Rat)
University of Tennessee

Curated by ChEMBL
LigandPNGBDBM19201((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataEC50:  16nMAssay Description:Agonist activity at glucocorticoid receptor in rat INS-1 832/13 cells transfected with 3XGRE-promoter luciferase plasmid construct assessed as induct...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/24/2022
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM19201((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataIC50: 2.5nM EC50:  2.20nMpH: 7.5 T: 2°CAssay Description:The IC50s were determined by incubating the receptors with radiolabeled dexamethasone in the presence of full log scale concentrations (10-11 M to 10...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/24/2007
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Rat)
University of Tennessee

Curated by ChEMBL
LigandPNGBDBM19201((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataIC50: 5nMAssay Description:Agonist activity at glucocorticoid receptor in rat INS-1 832/13 cells transfected with CCL2-promoter luciferase plasmid construct assessed as reducti...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/24/2022
Entry Details Article
PubMed
TargetGlucocorticoid receptor(Human)
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM19201((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataKi:  2.5nMAssay Description:Displacement of GS-red from human glucocorticoid receptor by fluorescent polarization assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
12/27/2012
Entry Details Article
PubMed