BDBM18627 (10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyl-14-(prop-1-yn-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-dien-5-one::Mifeprex::Mifepristone::RU-486::RU486 (tetramethyl-rhodamine conjugated)

SMILES [H][C@@]12CC[C@@](O)(C#CC)[C@@]1(C)C[C@@H](C1=C3CCC(=O)C=C3CC[C@@]21[H])c1ccc(cc1)N(C)C

InChI Key InChIKey=VKHAHZOOUSRJNA-GCNJZUOMSA-N

Data  44 KI  134 IC50  2 Kd  13 EC50

PDB links: 7 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 83 hits for monomerid = 18627   

TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  0.0900nMAssay Description:Displacement of fluormone GS Red from human glucocorticoid receptor after 4 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  0.100nMAssay Description:Inhibition of human glucocorticoid receptorMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  0.240nMAssay Description:Displacement of 10 nM [3H]dexamethasone from human Glucocorticoid receptorMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  0.240nMAssay Description:Displacement of [3H]DEX from human glucocorticoid receptorMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  0.299nMAssay Description:Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells by scintillation counting based radioligand competiti...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  0.400nMAssay Description:Displacement of [3H]dexamethasone from human glucocorticoid receptor expressed in recombinant baculovirusMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  0.400nMAssay Description:Displacement of [3H]dexamethasone from human recombinant GRMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  0.440nMAssay Description:Inhibition of glucocorticoid receptor dependent alkaline phosphatase activityMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  0.680nMAssay Description:Binding affinity was determined for human glucocorticoid receptor(hGR).More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  0.820nMAssay Description:Binding affinity to glucocorticoid receptor in SW1353 cells by whole-cell binding assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  0.840nMAssay Description:Displacement of [3H]dexamethasone from human glucocorticoid receptor after 16 hrs by scintillation countingMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  1nMAssay Description:Antagonist activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of corticoid-induced transcription by glucocortic...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  1.10nMAssay Description:Displacement of radiolabeled Dexamethasone from human GRMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  1.20nMAssay Description:Antagonist activity at human glucocorticoid receptor in SW1353 cells assessed as inhibition of dexamethasone-induced luciferase expression by MMTV5 r...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  1.20nMAssay Description:Antagonist activity at GR in SW1353/MMTV5 cells assessed as inhibition of dexamethasone-induced luciferase expressionMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  3nMAssay Description:Antagonist activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of dexamethasone-induced tyrosine amino transferase activi...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  5nMAssay Description:Inhibition of human GR expressed in hGRAF cellsMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  6nMAssay Description:Displacement of [3H]-dexamethasone from cytosolic fraction of human recombinant glucocorticoid receptor by scintillation counting analysisMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  120nMAssay Description:Inhibition of glucocorticoid receptor mediated tyrosine amino transferase activityMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataKi:  169nMAssay Description:Inhibition of human GR transcriptional activation by HepTAT cellsMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataEC50:  0.600nMpH: 7.5Assay Description:GR-Mediated Antagonist Activity Assay- GR-mediated antagonist activity is measured in the presence of a concentration of dexamethasone empirically de...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  1.10nM EC50:  4.80nMpH: 8.0 T: 2°CAssay Description:For compounds able to displace the 3(H)-dexamethasone from the receptor an IC50 value (the concentration required to inhibit 50% of the binding of 3(...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(RAT)
Abbott Laboratories

LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  1.40nMpH: 8.0 T: 2°CAssay Description:For compounds able to displace the radiolabeled ligand (competitor) from the receptor an IC50 value (the concentration required to inhibit 50% of the...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of Dexamethasone binding to Glucocorticoid receptorMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  1nMAssay Description:Displacement of [3H]dexamethasone from human Glucocorticoid receptor (GR)More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50: <1.00E+3nMAssay Description:Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cellsChecked by AuthorMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  4.70nMAssay Description:Activity at GR assessed as ability to antagonize dexamethasone-induced MMTV luciferase reporter gene transactivation in human A549 cellsChecked by AuthorMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  5.80nMAssay Description:Inhibition of fluorescent-labeled Dexamethasone binding to GRChecked by AuthorMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  0.298nMAssay Description:Antagonist activity against glucocorticoid receptor (unknown origin) expressed in HEK293 cells by GRE-dependent luciferase reporter gene assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(RAT)
Abbott Laboratories

LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  1.90nMAssay Description:Antagonist activity against glucocorticoid receptor in rat H4-IIE cells assessed as inhibition of dexamethasone-induced receptor transactivation pre-...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  6.90nMAssay Description:Binding affinity to glucocorticoid receptorMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  11nMAssay Description:Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexametha...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  6.31nMAssay Description:Antagonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as inhibition of dexamethasone-induce...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  0.950nMAssay Description:Antagonist activity at human glucocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc by luciferase reporter ...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataEC50:  872nMAssay Description:Agonist activity at human glucocorticoid receptor expressed in african green monkey CV1 cells co-transfected with MMTV-Luc after 24 hrs by luciferase...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  0.800nMAssay Description:Inhibition of antagonist activity towards glucocorticoid receptorMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(RAT)
Abbott Laboratories

LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  410nMAssay Description:Inhibition of prednisilone-induced tyrosine aminotransferase (TAT) activity in rat hepatocytesMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  1.10nMAssay Description:Inhibition of [3H]dexamethasone binding to human glucocorticoid receptorMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  4.80nMAssay Description:Inhibition of dexamethasone-induced glucocorticoid receptor mediated alkaline phosphatase activityMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(RAT)
Abbott Laboratories

LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  270nMAssay Description:Inhibition of dexamethasone-induced glucocorticoid receptor mediated tyrosine aminotransferase in rat hepatocytesMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  4.80nMAssay Description:Inhibition of glucocorticoid receptor Dexamethasone response in reporter gene assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(RAT)
Abbott Laboratories

LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  270nMAssay Description:Inhibition of dexamethasone-induced GR-mediated tyrosine amino transferase activity in rat hepatocytesMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(MOUSE)
Schering

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  2.20nMAssay Description:In vitro antagonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptorMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  0.600nMAssay Description:Antagonist activity at glucocorticoid receptor ligand binding domain by two hybrid assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  0.600nMAssay Description:Antagonist activity at human GR ligand binding domain expressed in african green monkey COS7 cells in presence of Dexamethasone by Gal4 hybrid assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  0.800nMAssay Description:Inhibitory activity against human glucocorticoid receptor (hGR)More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  0.00800nMAssay Description:Inhibition of CHO-K1 cells expressing glucocorticoid receptorMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  1.10nMAssay Description:Binding affinity to human GRMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  5nMAssay Description:Activity at GR expressed in CHO cells assessed as decrease in dexamethasone-stimulated alkaline phosphatase production by GRAF assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Homo sapiens (Human))
Corcept Therapeutics

Curated by ChEMBL
LigandPNGBDBM18627((10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]...)
Affinity DataIC50:  1.60nMAssay Description:Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced transcription after 16 hrs by glucocor...More data for this Ligand-Target Pair