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Found 95 Enz. Inhib. hit(s) with Target = 'Glucocorticoid receptor' and Ligand = 'BDBM19190'
TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  1.10nMAssay Description:Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cellsMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  1.5nMAssay Description:Displacement of FITC-dexamethasone from human recombinant glucocorticoid receptor alpha by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  1.5nMAssay Description:Displacement of GS-red from GRapha by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  1.5nMAssay Description:Displacement of GS-red from glucocorticoid receptor by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  2.40nMAssay Description:Binding affinity towards glucocorticoid receptor (GR) by displacing [3H]-DexamethasoneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  2.40nMAssay Description:Displacement of [3H]DEX from human glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  2.40nMAssay Description:Inhibition of dihydrofolate reductase DHFR in Pneumocystis carinii.More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  2.40nMAssay Description:Binding affinity for glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  5.30nMAssay Description:Displacement of radiolabeled dexamethasone from glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  5.30nMAssay Description:Displacement of radiolabeled dexamethasone from GRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  5.30nMAssay Description:Displacement of radiolabeled Dexamethasone from glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  5.30nMAssay Description:Displacement of radiolabeled dexamethasone from glucocorticoid receptor expressed in baculovirusMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  5.30nMAssay Description:Displacement of radiolabeled dexamethasone from GRMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataKi:  5.30nMAssay Description:Displacement of radiolabeled dexamethasone from glucocorticoid receptor expressed in baculovirusMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  0.526nMAssay Description:The glucocorticoid receptor fluorescence polarization ligand binding (GRFP) assay is used to evaluate direct binding of testing compounds to full-len...More data for this Ligand-Target Pair
In DepthDetails US PatentDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50: >1nMAssay Description:Antagonist activity at glucocorticoid receptor assessed as inhibition of dexamethasone-induced glucose response element transcriptional transactivati...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  2.10nMAssay Description:Transcriptional repression activity in HEP G2 cells expressing glucocorticoid receptor compared to dexamethasoneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  2.10nMAssay Description:Inhibition of transcriptional repression in CV-1 cells expressing glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  3.80nMAssay Description:Repression activity of GR ligand with interleukin-6 receptor in native cell assay using dexamethasone was determined as maximal potencyMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  4.10nMAssay Description:Activity at GR assessed as repression of TNFalpha and IL 1beta induced E-selectin responseMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  4.10nMAssay Description:Agonist activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcr...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  4.10nMAssay Description:Transrepression activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of TNFalpha/IL1beta-stimulated NFkappaB-dependent E-s...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  4.10nMAssay Description:Transrepression activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  4.10nMAssay Description:Transrepression activity at glucocorticoid receptor in TNFalpha/IL1beta-stimulated human HepG2 cells assessed as inhibition of NFkappaB-dependent E-s...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  4.10nMAssay Description:Activity at glucocorticoid receptor assessed as repression of TNFalpha and IL1 beta-induced E-selectin expressionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  6nMAssay 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 ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  6.10nMAssay Description:Binding affinity to GR (unknown origin) by FP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  6.60nMAssay 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
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  7nMAssay 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 ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  7nMAssay Description:Binding affinity to human glucocorticoid receptor by fluorescence polariztion competitive binding assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  7nMAssay Description:Displacement of fluormone RED from human full length glucocorticoid receptor after 4 hrs by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  7.70nMAssay Description:Transrepression activity at glucocorticoid receptor in human H292 cells assessed as inhibition of TNF-stimulated IL-8 productionMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  8nMAssay Description:Transcriptional activation in CV-1 cells expressing glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  8nMAssay Description:Inhibition of transcriptional repression in CV-1 cells expressing glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  8.5nMAssay 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
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  8.51nMAssay Description:Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  12.6nMAssay Description:Displacement of fluorescent labelled Dexamethasone from glucocorticoid receptorMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  13nMAssay Description:Displacement of [3H]dexamethasone from GR in human IM9 cells after 6 hrs by scintillation counting methodMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  13.8nMAssay Description:Inhibition of human glucocorticoid receptor alpha by displacement of [3H]-dexamethasoneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  13.8nM EC50:  4.5nMpH: 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 ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  13.8nM EC50:  4.5nMpH: 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 ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  15nMAssay 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 ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  15nMAssay Description:Inhibition of tetramethylrhodamine labeled dexamethosone binding to GR by FP assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  15nMAssay 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
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  15nMAssay Description:Displacement of TAMRA-labeled dexamethasone from glucocorticoid receptor (unknown origin) by fluorescence polarization assayMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  23nMAssay Description:Transrepression activity at glucocorticoid receptor in human NHDF cells assessed as inhibition of IL-1beta-stimulated AP1 dependent IL-6 repression b...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  23nMAssay Description:Transrepression activity at GR expressed in NHDF cells assessed as IL-1beta-mediated IL-6 transcription by ELISAMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  23nMAssay Description:Transrepression activity at glucocorticoid receptor in IL-1beta-stimulated human HepG2 cells assessed as inhibition of AP1 response element-induced I...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  23nMAssay Description:Agonist activity at human GR expressed in NHDF cells assessed as inhibition of IL-6 production by ELISA relative to dexamethasoneMore data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

TargetGlucocorticoid receptor(Homo sapiens (Human))
Eli Lilly

Curated by ChEMBL
LigandPNGBDBM19190((1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-...)
Affinity DataIC50:  40nMAssay Description:Transrepression activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of PMA-stimulated gene e...More data for this Ligand-Target Pair
In DepthDetails ArticlePubMedDrugBank

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