Approval Year
Substance Class |
Protein
Created
by
admin
on
Edited
Tue Apr 01 16:27:49 GMT 2025
by
admin
on
Tue Apr 01 16:27:49 GMT 2025
|
Protein Sub Type | |
Sequence Type | COMPLETE |
Record UNII |
FZW85LW99M
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Record Status |
Validated (UNII)
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Record Version |
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-
Download
Name | Type | Language | ||
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Common Name | English | ||
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Preferred Name | English | ||
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Common Name | English | ||
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Common Name | English |
Code System | Code | Type | Description | ||
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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
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PRIMARY | |||
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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 | |||
|
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 |
Linkage Type | Residue Index | |||
---|---|---|---|---|
COORDINATION COMPOUND | 1_421 | 1_424 | 1_438 | 1_441 |
COORDINATION COMPOUND | 1_457 | 1_463 | 1_473 | 1_476 |
Related Record | Type | Details | ||
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET | |||
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET |
Ki
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AGONIST -> TARGET |
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AGONIST -> TARGET |
EC50
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AGONIST -> TARGET |
Selective Nonsteroidal Glucocorticoid Receptor Modulator
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET | |||
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INHIBITOR -> TARGET |
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
IC50
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
BINDING
IC50
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MODULATOR->TARGET |
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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AGONIST -> TARGET |
LPS-induced TNF-? release in peripheral blood mononuclear cells. Efficacy, maximum response relative to Dexamethasone (100%)=75%
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PARTIAL AGONIST->TARGET |
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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AGONIST -> TARGET |
BINDING
IC50
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
Luciferase transactivation assay in CV-1 (African green monkey kidney) cells transfected with hGR.alpha. expression vectors
AGONIST
EC50
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INHIBITOR -> TARGET |
BINDING
IC50
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
EC50
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INHIBITOR -> TARGET |
Ki
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PARTIAL AGONIST->TARGET | |||
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AGONIST -> TARGET |
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AGONIST -> TARGET | |||
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AGONIST -> TARGET |
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AGONIST -> TARGET |
BINDING
Ki
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RADIOLIGAND->TARGET |
Kd
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AGONIST -> TARGET | |||
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
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AGONIST -> TARGET |
25-30 times more potent than cortisol
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INHIBITOR -> TARGET | |||
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
6?-OH-21-desDFZ exhibited minimal binding to the human glucocorticoid receptor (<15%) at concentration up to 1 ?M.
MINOR
Ki
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AGONIST -> TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
BINDING
IC50
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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 |
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MOL_WEIGHT | CHEMICAL |
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