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Approval Year

Substance Class Protein
Created
by admin
on Thu Jul 06 17:54:14 UTC 2023
Edited
by admin
on Thu Jul 06 17:54:14 UTC 2023
Protein Type RECEPTOR
Protein Sub Type
Sequence Type COMPLETE
Record UNII
SIDP85PFD6
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ESTROGEN RECEPTOR
Common Name English
ESR1
Common Name English
ESTROGEN RECEPTOR ALPHA
Common Name English
NUCLEAR RECEPTOR SUBFAMILY 3 GROUP A MEMBER 1
Common Name English
ESR
Common Name English
ESTRADIOL RECEPTOR
Common Name English
ER-ALPHA
Common Name English
NR3A1
Common Name English
Code System Code Type Description
FDA UNII
SIDP85PFD6
Created by admin on Thu Jul 06 17:54:17 UTC 2023 , Edited by admin on Thu Jul 06 17:54:17 UTC 2023
PRIMARY
UNIPROT
P03372
Created by admin on Thu Jul 06 17:54:17 UTC 2023 , Edited by admin on Thu Jul 06 17:54:17 UTC 2023
PRIMARY
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
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
DEGRADER->TARGET
AGONIST -> TARGET
AGONIST -> TARGET
AGONIST -> TARGET
INHIBITOR, RECEPTOR DEGRADER->TARGET
Selective estrogen receptor degrader
AGONIST -> TARGET
DEGRADER, SELECTIVE->TARGET
100% Degradation as control
EC50
INHIBITOR, RECEPTOR DEGRADER->TARGET
ANTAGONIST
IC50
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
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