BDBM18207 (1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,13,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one::US10869929, Compound Dexamethasone::US11554172, Compound Dexamethasone::dexamethasone::dexamethasone (tetramethyl-rhodamine conjugated )

SMILES C[C@@H]1C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)CO

InChI Key InChIKey=UREBDLICKHMUKA-UHFFFAOYSA-N

Data  25 KI  107 IC50  4 Kd  42 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 176 hits for monomerid = 18207   

TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 12.6nMAssay Description:Displacement of fluorescent-labelled Dexamethasone from glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 1nMAssay Description:Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 3.98nMAssay Description:Agonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activityMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPhospholipase A2(Human)
Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz, 50300, Kuala Lumpur, Malaysia

LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 610nMpH: 8.0 T: 2°CAssay Description:Substrate 1,2-bis(heptanoylthio)-glycerophosphocholine and human recombinant PLA2-V were resuspended in assay buffer, and DTNB was dissolved in an aq...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetPhospholipase A2 group V(Human)
Universiti Kebangsaan Malaysia, Jalan Raja Muda Abdul Aziz

LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 620nMpH: 7.5 T: 2°CAssay Description:Briefly, sn-2ester bond of the substrate 1,2-bis(heptanoylthio)-glycerophosphocholine was hydrolyzed by PLA2-V followed by the exposure of free thiol...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 7.90nMAssay Description:Inhibition of fluorescent-labeled Dexamethasone binding to GRMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 1.20nMAssay Description:Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 1.00E+4nMAssay Description:Activity at GR assessed as ability to antagonize dexamethasone-induced MMTV luciferase reporter gene transactivation in human A549 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataEC50:  5nMAssay Description:Agonist activity at GR assessed as MMTV-mediated transactivation of renilla luciferase gene in human A549 cells relative to DexamethasoneMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataEC50:  17nMAssay Description:Transactivation of glucocorticoid receptor in human HeLa cells harboring MMTV promoter by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 3nMAssay Description:Displacement of TAMRA-labeled dexamethasone from glucocorticoid receptor (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetProgesterone receptor(Human)
Boehringer Ingelheim Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 2.00E+3nMAssay Description:Displacement of TAMRA-labeled mifepristone from progesterone receptor (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMineralocorticoid receptor(Human)
Boehringer Ingelheim Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 33nMAssay Description:Displacement of TAMRA-labeled dexamethasone from mineralocorticoid receptor (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 0.5nMAssay Description:Agonist activity at glucocorticoid receptor in human foreskin fibroblasts assessed as inhibition of IL-1-induced IL-6 production by trans-repression ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataEC50:  1.30nMAssay Description:Agonist activity at human GCR expressed in HEK293 cells by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 1nMAssay Description:Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 productionMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataEC50:  2.5nMAssay Description:Agonist activity at glucocorticoid receptor in human A549 cells assessed as AP-1 transrepression by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataEC50:  1.10nMAssay Description:Agonist activity at glucocorticoid receptor in human A549 cells assessed as E-selectin transrepression by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataEC50:  4.5nMAssay Description:Agonist activity at glucocorticoid receptor in human HeLa cells assessed as NP-1 transactivation by luciferase reporter gene assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataEC50:  6.90nMAssay Description:Agonist activity at glucocorticoid receptor in human whole blood assessed as inhibition of LPS-induced TNF production incubated for 20 hrs prior to L...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 3.5nMAssay Description:Binding affinity to human GRMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 1.80nMAssay Description:Transrepression activity at glucocorticoid receptor in human SW1353 cells assessed as repression of IL-1-induced MMP-13 production after 24 hrs by EL...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 21nMAssay Description:Transrepression activity at glucocorticoid receptor in human whole blood assessed as repression of IL-1-induced TNF-alpha production after 4 hrs by E...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetNuclear receptor subfamily 1 group I member 2(Rat)
National Institutes of Health Chemical Genomics Center

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataEC50:  2.60E+3nMAssay Description:Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysisMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBile salt export pump(Rat)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 2.32E+5nMAssay Description:Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate up...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetBile salt export pump(Human)
Astrazeneca

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 1.37E+5nMAssay Description:Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptakeMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 2J2(Human)
Tongji University

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of human recombinant CYP2J2 assessed as reduction in astemizole O-demethylation by LC-MS/MS methodMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 3.80nMAssay Description:Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM9 cellsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Rat)
Kaken Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 22nMAssay Description:Displacement of [3H]dexamethasone from Sprague-Dawley rat GR by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Rat)
Kaken Pharmaceutical

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 22nMAssay Description:Displacement of [3H]Dex from glucocorticoid receptor in Sprague-Dawley rat liver after 2 hrs by liquid scintillation countingMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMineralocorticoid receptor(Human)
Boehringer Ingelheim Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 33nMAssay Description:Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant mineralocorticoid receptor expressed in baculovirus infected insect...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 3nMAssay Description:Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant glucocorticoid receptor expressed in baculovirus infected insect ce...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetProgesterone receptor(Human)
Boehringer Ingelheim Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 2.00E+3nMAssay Description:Displacement of tetramethylrhodamine-labeled RU-486 from human recombinant progesterone receptor expressed in baculovirus infected insect cells by fl...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 0.510nMAssay Description:Agonist activity at glucocorticoid receptor in HFF assessed as inhibition of IL1-induced IL-6 production after 18 to 24 hrsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataEC50:  1.80nMAssay Description:Transactivation activity of glucocorticoid receptor in HFF assessed as induction of aromatase activity by measuring beta-estradiol activity after 18 ...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataEC50:  17nMAssay Description:Agonist activity at glucocorticoid receptor in human HeLa cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase trans...More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 7.50E+5nMAssay Description:Tested for its inhibitory activity against Phospholipase A2 (PLA2)More data for this Ligand-Target Pair
In DepthDetails Article

LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 1.20E+5nMAssay Description:Tested for its inhibitory activity against 5-lipoxygenaseMore data for this Ligand-Target Pair
In DepthDetails Article

LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 2.50E+4nMAssay Description:Inhibition of rat basophilic leukemia cell 5-lipoxygenaseMore data for this Ligand-Target Pair
In DepthDetails Article

TargetPhospholipase A2(Rat)
TBA

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 7.50E+5nMAssay Description:Inhibitory activity against polymorphonuclear cell phospholipase-A2 in ratMore data for this Ligand-Target Pair
In DepthDetails Article

TargetATP-dependent translocase ABCB1(Human)
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetATP-dependent translocase ABCB1(Mouse)
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetATP-dependent translocase ABCB1(Mouse)
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetATP-dependent translocase ABCB1(Human)
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of P-glycoprotein using calcein-AM assay transfected in porcine PBCECMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetCytochrome P450 3A4(Human)
F. Hoffmann-La Roche

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 5.00E+4nMAssay Description:Inhibition of human cytochrome P450 3A4More data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataEC50:  1nMAssay Description:Effective agonist concentration for transcriptional repression of IL-6 production in IL-1 stimulated human foreskin fibroblastsMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 3.40nMAssay Description:Inhibition of human GRMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetProgesterone receptor(Human)
Boehringer Ingelheim Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 2.00E+3nMAssay Description:Inhibition of human PRMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetMineralocorticoid receptor(Human)
Boehringer Ingelheim Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 33nMAssay Description:Inhibition of human MRMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
TargetGlucocorticoid receptor(Human)
Glaxosmithkline

Curated by ChEMBL
LigandPNGBDBM18207(dexamethasone (tetramethyl-rhodamine conjugated ) ...)
Affinity DataIC50: 3nMAssay Description:Inhibition of tetramethylrhodamine labeled dexamethasone binding to GR by FP assayMore data for this Ligand-Target Pair
In DepthDetails Article
PubMed
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