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
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Preferred Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
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 | |||
|
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 | ||
|---|---|---|---|---|
|
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 | |||
|
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 | |||
|
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
|
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 |
|