U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Approval Year

Substance Class Protein
Created
by admin
on Tue Apr 01 16:27:49 GMT 2025
Edited
by admin
on Tue Apr 01 16:27:49 GMT 2025
Protein Sub Type
Sequence Type COMPLETE
Record UNII
FZW85LW99M
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
GLUCOCORTICOID RECEPTOR
Common Name English
GR
Preferred Name English
NUCLEAR RECEPTOR SUBFAMILY 3 GROUP C MEMBER 1
Common Name English
GRL
Common Name English
Code System Code Type Description
PHAROS
P04150
Created by admin on Tue Apr 01 16:27:49 GMT 2025 , Edited by admin on Tue Apr 01 16:27:49 GMT 2025
PRIMARY
UNIPROT
P04150
Created by admin on Tue Apr 01 16:27:49 GMT 2025 , Edited by admin on Tue Apr 01 16:27:49 GMT 2025
PRIMARY
FDA UNII
FZW85LW99M
Created by admin on Tue Apr 01 16:27:49 GMT 2025 , Edited by admin on Tue Apr 01 16:27:49 GMT 2025
PRIMARY
Related Record Type Details
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AGONIST -> TARGET
INHIBITOR -> TARGET
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Selective Nonsteroidal Glucocorticoid Receptor Modulator
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
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MODULATOR->TARGET
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PARTIAL AGONIST->TARGET
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Luciferase transactivation assay in CV-1 (African green monkey kidney) cells transfected with hGR.alpha. expression vectors
AGONIST
EC50
INHIBITOR -> TARGET
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AGONIST -> TARGET
AGONIST -> TARGET
EC50
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Ki
PARTIAL AGONIST->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
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RADIOLIGAND->TARGET
Kd
AGONIST -> TARGET
INHIBITOR -> TARGET
INHIBITOR -> TARGET
AGONIST -> TARGET
INHIBITOR -> TARGET
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25-30 times more potent than cortisol
INHIBITOR -> TARGET
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INHIBITOR -> TARGET
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6?-OH-21-desDFZ exhibited minimal binding to the human glucocorticoid receptor (<15%) at concentration up to 1 ?M.
MINOR
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Structural Modifications

Modification Type Location Site Location Type Residue Modified Extent Fragment Name Fragment Approval
AMINO ACID SUBSTITUTION [1_480] [1_492] [1_494] [1_495] N6-ACETYLLYSINE 470AD5VY1X
AMINO ACID SUBSTITUTION [1_113] [1_134] [1_141] [1_203] [1_211] [1_226] [1_267] [1_404] DEXFOSFOSERINE VI4F0K069V
AMINO_ACID_SUBSTITUTION [1_457] [1_463] [1_473] [1_476] SITE_SPECIFIC C4-TYPE ZINC FINGER C56TF4V7OP
AMINO_ACID_SUBSTITUTION [1_421] [1_424] [1_438] [1_441] SITE_SPECIFIC C4-TYPE ZINC FINGER C56TF4V7OP
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT CHEMICAL