Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Sat Dec 16 12:19:44 GMT 2023
by
admin
on
Sat Dec 16 12:19:44 GMT 2023
|
| Protein Type | RECEPTOR |
| Protein Sub Type | |
| Sequence Type | COMPLETE |
| Record UNII |
SIDP85PFD6
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
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Common Name | English | ||
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Common Name | English | ||
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Common Name | English | ||
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Common 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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SIDP85PFD6
Created by
admin on Sat Dec 16 12:19:48 GMT 2023 , Edited by admin on Sat Dec 16 12:19:48 GMT 2023
|
PRIMARY | |||
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P03372
Created by
admin on Sat Dec 16 12:19:48 GMT 2023 , Edited by admin on Sat Dec 16 12:19:48 GMT 2023
|
PRIMARY |
| Linkage Type | Residue Index | |||
|---|---|---|---|---|
| COORDINATION COMPOUND | 1_185 | 1_188 | 1_202 | 1_205 |
| COORDINATION COMPOUND | 1_221 | 1_227 | 1_237 | 1_240 |
| Glycosylation Type | HUMAN |
| Glycosylation Link Type | Site |
|---|---|
| O | 1_10 |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
MODULATOR->TARGET |
|
||
|
INHIBITOR, RECEPTOR DEGRADER->TARGET |
|
||
|
INHIBITOR -> TARGET |
ANTAGONIST
|
||
|
INHIBITOR -> TARGET | |||
|
INHIBITOR, RECEPTOR DEGRADER->TARGET |
Selective estrogen receptor degrader (SERD)
IC50
|
||
|
INHIBITOR -> TARGET |
|
||
|
PARTIAL AGONIST->TARGET | |||
|
|
AGONIST -> TARGET | |||
|
|
MODULATOR->TARGET |
|
||
|
AGONIST -> TARGET |
Ki
|
||
|
DEGRADER, SELECTIVE->TARGET |
EC50
|
||
|
AGONIST -> TARGET |
Binding Assay
IC50
|
||
|
AGONIST -> TARGET |
|
||
|
|
MODULATOR->TARGET |
|
||
|
DEGRADER, SELECTIVE->TARGET |
Selective estrogen receptor degrader (SERD)
BINDING
IC50
|
||
|
INHIBITOR -> TARGET |
Binding Assay
IC50
|
||
|
DEGRADER, SELECTIVE->TARGET |
Degrades 91% of Fulvestrant control
EC50
|
||
|
INHIBITOR -> TARGET | |||
|
|
INHIBITOR, RECEPTOR DEGRADER->TARGET |
LEADS TO DEGRADATION OF RECEPTOR
|
||
|
INHIBITOR -> TARGET | |||
|
INHIBITOR -> TARGET |
Binding Assay
IC50
|
||
|
AGONIST -> TARGET | |||
|
|
INHIBITOR -> TARGET |
Binding assay
IC50
|
||
|
|
INHIBITOR, RECEPTOR DEGRADER->TARGET |
induction of an inactive conformation of the ER ligand-binding domain (LBD) and 2) induces ERα (WT and mutant) degradation.
IC50
|
||
|
DEGRADER, SELECTIVE->TARGET |
87% efficacy relative to Fulvestrant
EC50
|
||
|
AGONIST -> TARGET |
|
||
|
INHIBITOR, RECEPTOR DEGRADER->TARGET |
IN MCF7 CELLS
DC50
|
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|
DEGRADER->TARGET |
|
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|
AGONIST -> TARGET | |||
|
|
MODULATOR->TARGET |
|
||
|
AGONIST -> TARGET | |||
|
|
AGONIST -> TARGET | |||
|
INHIBITOR, RECEPTOR DEGRADER->TARGET |
Selective estrogen receptor degrader
|
||
|
AGONIST -> TARGET |
|
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|
DEGRADER, SELECTIVE->TARGET |
100% Degradation as control
EC50
|
||
|
|
INHIBITOR, RECEPTOR DEGRADER->TARGET |
ANTAGONIST
IC50
|
||
|
MODULATOR->TARGET |
|
||
|
INHIBITOR -> TARGET |
In vitro and in vivo pharmacological studies of ZB716 demonstrate it is a pure antagonist of the
ER. It binds to the ER and degrades the protein in a dose-dependent manner.
IN-VITRO, IN-VIVO
|
||
|
INHIBITOR, RECEPTOR DEGRADER->TARGET |
Selective Estrogen Receptor Degrader
|
||
|
AGONIST -> TARGET | |||
|
INHIBITOR, RECEPTOR DEGRADER->TARGET |
Selective estrogen receptor degrader
|
||
|
INHIBITOR -> TARGET |
IC50
|
||
|
|
INHIBITOR -> TARGET |
serm Competitive binding with estrogen
IC50
|
||
|
INHIBITOR -> TARGET | |||
|
INHIBITOR -> TARGET |
ANTAGONIST
|
||
|
AGONIST -> TARGET | |||
|
|
AGONIST -> TARGET | |||
|
|
LIGAND->BINDER | |||
|
|
INHIBITOR -> TARGET |
|
||
|
AGONIST -> TARGET | |||
|
|
AGONIST -> TARGET | |||
|
INHIBITOR, RECEPTOR DEGRADER->TARGET |
SERD
IC50
|
||
|
AGONIST -> TARGET |
|
||
|
INHIBITOR -> TARGET |
Transcription inhibition
IC50
|
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT | CHEMICAL |
|