U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Approval Year

Unknown
149124
Substance Class Protein
Created
by admin
on Tue Apr 01 19:00:23 GMT 2025
Edited
by admin
on Tue Apr 01 19:00:23 GMT 2025
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
ER-ALPHA
Preferred 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
NR3A1
Common Name English
Code System Code Type Description
FDA UNII
SIDP85PFD6
Created by admin on Tue Apr 01 19:00:24 GMT 2025 , Edited by admin on Tue Apr 01 19:00:24 GMT 2025
PRIMARY
UNIPROT
P03372
Created by admin on Tue Apr 01 19:00:24 GMT 2025 , Edited by admin on Tue Apr 01 19:00:24 GMT 2025
PRIMARY
Glycosylation Type HUMAN
Glycosylation Link Type Site
O 1_10
Related Record Type Details
Structure of RWJ-443931
MODULATOR->TARGET
Structure of ELACESTRANT
INHIBITOR, RECEPTOR DEGRADER->TARGET
Structure of METHYLPIPERIDINOPYRAZOLE
INHIBITOR -> TARGET
ANTAGONIST
Structure of BAZEDOXIFENE
INHIBITOR -> TARGET
Structure of LSZ-102
INHIBITOR, RECEPTOR DEGRADER->TARGET
Selective estrogen receptor degrader (SERD)
IC50
Structure of NALOXONE
INHIBITOR -> TARGET
Structure of TTC-352
PARTIAL AGONIST->TARGET
Structure of DANAZOL
AGONIST -> TARGET
Structure of Fispemifene
MODULATOR->TARGET
Structure of ESTETROL ANHYDROUS
AGONIST -> TARGET
Ki
Structure of ARZOXIFENE
DEGRADER, SELECTIVE->TARGET
EC50
Structure of ESTRADIOL
AGONIST -> TARGET
Binding Assay
IC50
Structure of DCW-234
AGONIST -> TARGET
Structure of IDOXIFENE
MODULATOR->TARGET
Structure of 7-DESMETHYLORMELOXIFENE, (-)-
MODULATOR->TARGET
Structure of [3H] Estradiol
LIGAND->TARGET
Binding Assay
Kd
Structure of FULVESTRANT
DEGRADER, SELECTIVE->TARGET
Selective estrogen receptor degrader (SERD)
BINDING
IC50
Structure of TAMOXIFEN
INHIBITOR -> TARGET
Binding Assay
IC50
Structure of BRILANESTRANT
DEGRADER, SELECTIVE->TARGET
Degrades 91% of Fulvestrant control
EC50
Structure of OSPEMIFENE
INHIBITOR -> TARGET
Structure of Taragarestrant
INHIBITOR, RECEPTOR DEGRADER->TARGET
LEADS TO DEGRADATION OF RECEPTOR
Structure of H3B-6545 FREE BASE
INHIBITOR -> TARGET
IRREVERSIBLE INHIBITOR
Structure of CHF-4227
INHIBITOR -> TARGET
Structure of DIETHYLSTILBESTROL
INHIBITOR -> TARGET
Binding Assay
IC50
Structure of DIENESTROL
AGONIST -> TARGET
Structure of BRILANESTRANT
INHIBITOR -> TARGET
Binding assay
IC50
Structure of GIREDESTRANT
INHIBITOR, RECEPTOR DEGRADER->TARGET
induction of an inactive conformation of the ER ligand-binding domain (LBD) and 2) induces ER? (WT and mutant) degradation.
IC50
Structure of PIPENDOXIFENE
DEGRADER, SELECTIVE->TARGET
87% efficacy relative to Fulvestrant
EC50
Structure of 8.BETA.-VE2
AGONIST -> TARGET
Structure of Vepdegestrant
INHIBITOR, RECEPTOR DEGRADER->TARGET
IN MCF7 CELLS
DC50
Structure of ZB-716
DEGRADER->TARGET
Structure of RALOXIFENE
AGONIST -> TARGET
Structure of 7-DESMETHYLORMELOXIFENE
MODULATOR->TARGET
Structure of BIFLURANOL
AGONIST -> TARGET
IC50
Structure of LASOFOXIFENE
AGONIST -> TARGET
Structure of 8-PRENYLNARINGENIN
AGONIST -> TARGET
Structure of GDC-0927
INHIBITOR, RECEPTOR DEGRADER->TARGET
Selective estrogen receptor degrader
Structure of 7.ALPHA.-METHYLESTRADIOL
AGONIST -> TARGET
Structure of FULVESTRANT
DEGRADER, SELECTIVE->TARGET
100% Degradation as control
EC50
Structure of AMCENESTRANT
INHIBITOR, RECEPTOR DEGRADER->TARGET
ANTAGONIST
IC50
Structure of MIPROXIFENE
MODULATOR->TARGET
Structure of ZB-716
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
Structure of IMLUNESTRANT
INHIBITOR, RECEPTOR DEGRADER->TARGET
Selective Estrogen Receptor Degrader
Structure of QUINESTROL
AGONIST -> TARGET
Structure of RINTODESTRANT
INHIBITOR, RECEPTOR DEGRADER->TARGET
Selective estrogen receptor degrader
Structure of FULVESTRANT
INHIBITOR -> TARGET
IC50
Structure of ARZOXIFENE
INHIBITOR -> TARGET
serm Competitive binding with estrogen
IC50
AFIMOXIFENE
INHIBITOR -> TARGET
Structure of PHTPP
INHIBITOR -> TARGET
ANTAGONIST
Structure of TIBOLONE
AGONIST -> TARGET
Structure of EQUOL
AGONIST -> TARGET
Structure of PRINABEREL
LIGAND->BINDER
Structure of ACOLBIFENE
INHIBITOR -> TARGET
Structure of MESTRANOL
AGONIST -> TARGET
NORGESTIMATE
AGONIST -> TARGET
Structure of ENDOXIFEN
INHIBITOR -> TARGET
Inhibitory effect of on the activation of estrogen receptor by estradiol.
IC50
Structure of CAMIZESTRANT
INHIBITOR, RECEPTOR DEGRADER->TARGET
SERD
IC50
Structure of 16.ALPHA.-LE2
AGONIST -> TARGET
Structure of GNE-149
INHIBITOR, RECEPTOR DEGRADER->TARGET
MCF-7 cells SERD
IC50
Structure of PIPENDOXIFENE
INHIBITOR -> TARGET
Transcription inhibition
IC50

Structural Modifications

Modification Type Location Site Location Type Residue Modified Extent Fragment Name Fragment Approval
AMINO_ACID_SUBSTITUTION [1_260] SITE_SPECIFIC N,N-DIMETHYLARGININE 63CV1GEK3Y
AMINO_ACID_SUBSTITUTION [1_221] [1_227] [1_237] [1_240] SITE_SPECIFIC C4-TYPE ZINC FINGER C56TF4V7OP
AMINO_ACID_SUBSTITUTION [1_537] SITE_SPECIFIC TYROSINE O-PHOSPHATE 2R86C98KDX
AMINO_ACID_SUBSTITUTION [1_447] SITE_SPECIFIC S-PALMITOYL CYSTEINE 08WQ73S7SV
AMINO_ACID_SUBSTITUTION [1_185] [1_188] [1_202] [1_205] SITE_SPECIFIC C4-TYPE ZINC FINGER C56TF4V7OP
AMINO_ACID_SUBSTITUTION [1_104] [1_106] [1_118] [1_167] SITE_SPECIFIC DEXFOSFOSERINE VI4F0K069V
Name Property Type Amount Referenced Substance Defining Parameters References
MOL_WEIGHT CHEMICAL
NIH
NCATS
PRIVACY NOTICE
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966