U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Approval Year

Substance Class Protein
Protein Sub Type
Sequence Type COMPLETE
Record UNII
FZW85LW99M
Record Status Validated (UNII)
Record Version
Subunit 0

Related Record Type Details
INHIBITOR -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
enhanced-affinity glucocorticoid
AGONIST
AGONIST -> TARGET
AGONIST -> TARGET
EC50
4.68 NANOMOLAR (average)
AGONIST -> TARGET
Selective Nonsteroidal Glucocorticoid Receptor Modulator
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
BINDING
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
IC50
0.45 NANOMOLAR [0.38 to 0.52] (average)
AGONIST -> TARGET
AGONIST -> TARGET
BINDING
IC50
69 NANOMOLAR (average)
MODULATOR->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
LPS-induced TNF-α release in peripheral blood mononuclear cells. Efficacy, maximum response relative to Dexamethasone (100%)=75%
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
BINDING
IC50
1.8 NANOMOLAR (average)
AGONIST -> TARGET
AGONIST -> TARGET
Luciferase transactivation assay in CV-1 (African green monkey kidney) cells transfected with hGR.alpha. expression vectors
AGONIST
EC50
4.37 NANOMOLAR (average)
Emax = 1.28
INHIBITOR -> TARGET
BINDING
IC50
3 NANOMOLAR (average)
AGONIST -> TARGET
INHIBITOR -> TARGET
Ki
0.9 NANOMOLAR (average)
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
BINDING
Ki
10 NANOMOLAR (average)
RADIOLIGAND->TARGET
Kd
1.5 NANOMOLAR (average)
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
6β-OH-21-desDFZ exhibited minimal binding to the human glucocorticoid receptor (<15%) at concentration up to 1 μM.
MINOR
Ki
[>1] MICROMOLAR (average)
INHIBITOR -> TARGET
INHIBITOR -> TARGET
BINDING
IC50
1.736 MICROMOLAR (average)
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT CHEMICAL