BDBM19202 (1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4H,4aH,5H,6H,7H,8H-cyclohexa[f]indazol-5-yl]-1-(thiophen-3-yl)ethan-1-ol::CHEMBL310570::N-Arylpyrazolo[3,2-c]-Based Ligand, 25

SMILES [H][C@@]1(CCCC2=Cc3c(C[C@]12C)cnn3-c1ccc(F)cc1)[C@](C)(O)c1ccsc1

InChI Key InChIKey=ZYRBSUDYHJGRMJ-KMDXXIMOSA-N

Data  1 KI  3 IC50  7 EC50

  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 10 hits for monomerid = 19202   

TargetGlucocorticoid receptor(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM19202((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataKi:  0.800nMAssay Description:Displacement of GS-red from human glucocorticoid receptor by fluorescent polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM19202((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of human glucocorticoid receptor alpha by displacement of [3H]-dexamethasoneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM19202((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataEC50:  36nMAssay Description:Inhibition of GR-mediated tyrosine amino transferase activity in human HepG2 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM19202((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataEC50:  0.960nMAssay Description:GR-mediated transrepression of IL-6 in human A549 lung carcinoma cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM19202((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataEC50:  1nMAssay 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 DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(MOUSE)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19202((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataEC50:  8.30nMAssay Description:Inhibition of mouse glutamine synthetase by GR-mediated transactivation in C2C12 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM19202((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataEC50:  36nMAssay 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 DepthDetails ArticlePubMed
TargetAndrogen receptor(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM19202((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataIC50: >4.00E+3nMAssay Description:Binding affinity to androgen receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(Homo sapiens (Human))
Bristol-Myers Squibb

Curated by ChEMBL
LigandPNGBDBM19202((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataIC50:  0.800nM EC50:  1nMpH: 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 DepthDetails ArticlePubMed
TargetGlucocorticoid receptor(MOUSE)
Merck Research Laboratories

Curated by ChEMBL
LigandPNGBDBM19202((1S)-1-[(4aR,5S)-1-(4-fluorophenyl)-4a-methyl-1H,4...)
Affinity DataEC50:  5.20nMAssay Description:GR-mediated transrepression of IL-6 in peritoneal exudate cells harvested from C57BI/6 miceMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMed