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Report error Found 114 Enz. Inhib. hit(s) for PDB: 1M2Z
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  0.690nMAssay Description:Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  1.10nMAssay Description:Binding affinity to glucocorticoid receptor-LBD (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  1.10nMAssay Description:Displacement of GS-red from GRapha by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  1.10nMAssay Description:Displacement of [3H]DEX from human glucocorticoid receptorMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  1.10nMAssay Description:Displacement of FITC-dexamethasone from human recombinant glucocorticoid receptor alpha by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  1.20nMAssay Description:Displacement of GS-red from human glucocorticoid receptor by fluorescent polarization assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  1.20nMAssay Description:Binding affinity to glucocorticoid receptor (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  1.20nMAssay Description:Binding affinity to glucocorticoid receptor (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  1.20nMAssay Description:Binding affinity to glucocorticoid receptor (unknown origin) by fluorescence assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  1.5nMAssay Description:Binding affinity to human glucocorticoid receptor by radioligand displacement assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  2.10nM ΔG°:  -46.0kJ/mole IC50:  1.40nM EC50:  0.200nMpH: 7.5 T: 4°CAssay Description:Competitive Ligand Binding Assay- The Ki values were determined by the application of the Cheng-Prusoff equation: Ki=IC50/(1+[L]/Kd) where [L] is the...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  2.20nMAssay Description:Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrsMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  5.5nMAssay Description:Binding affinity was determined for human glucocorticoid receptor(hGR).More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  6.70nMMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataKi:  6.80nMMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
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
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  0.5nMAssay Description:Agonist activity at glucocorticoid receptor in HFF assessed as inhibition of IL-1-induced IL-6 production after 24 hrsMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  0.508nMAssay Description:Antagonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity a...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  0.510nMAssay Description:Transrepression activity at glucocorticoid receptor in HFF assessed as inhibition of IL-1-induced IL-6 production after 18 to 24 hrs by ELISAMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
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
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
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
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  1nMAssay Description:Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  1nMAssay Description:Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  1nMAssay Description:Agonist activity at GR in human A549 cells by NF-kappaB transrepression assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  1.17nMAssay Description:Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  1.20nMAssay 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(Rat)
University of Tennessee

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  1.30nMAssay 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
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  1.58nMAssay Description:Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human HeLa cells assessed as inhibition of TPA-induced coll...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  1.60nMAssay Description:Transrepression activity at glucocorticoid receptorin human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by lucifer...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
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
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  2.10nMAssay Description:The potency of binding to gucocorticoid receptor by small molecule compounds was measured with the PolarScreen™ Glucocorticoid Receptor Competitor As...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  2.40nMAssay Description:Agonist activity at GAL4 DNA-binding domain fused GR (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lact...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  2.5nMAssay Description:Binding affinity to human glucocorticoid receptor by radioligand displacement assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  2.5nMAssay Description:Binding affinity to recombinant human glucocorticoid receptor expressed in baculovirus infected sf9 cellsMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  2.51nMAssay Description:Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-8...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  3nMAssay Description:Displacement of TAMRA-labeled dexamethasone from glucocorticoid receptor (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  3nMAssay Description:Displacement of TAMRA labeled Dexamethasone at human glucocorticoid receptor in insect cellMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  3nMAssay Description:Modulation of glucocorticoid receptor (unknown origin) transfected in human HeLa cells assessed as transrepression by measuring inhibition of PMA-ind...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
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
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  3nMAssay Description:Binding affinity to human glucocorticoid receptor by radioligand displacement assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  3nMAssay Description:Inhibition of tetramethylrhodamine labeled dexamethosone binding to GR by FP assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  3.40nMAssay Description:Inhibition of human GRMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  3.40nMAssay Description:Binding affinity to glucocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluore...More data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  3.5nMAssay Description:Displacement of TAMRA-labeled dexamethasone from glucocorticoid receptor (unknown origin) by fluorescence polarization competitive binding assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  3.5nMAssay Description:Binding affinity to human GRMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  3.80nMAssay Description:Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM9 cellsMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  3.80nMAssay Description:Displacement of [3H]dexamethasone from GR receptor in human IM9 cellsMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
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
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  4nMAssay Description:Binding affinity to glucocorticoid receptor (unknown origin) by Lanthascreen TR-FRET competition binding assayMore data for this Ligand-Target Pair
TargetGlucocorticoid receptor(Human)
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM18207((1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dih...)
Affinity DataIC50:  4.10nMAssay Description:Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrsMore data for this Ligand-Target Pair
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