◎ Sugi Atlas

Atlas / Drug / Estrogen

Estrogen

drug
On this page

Summary

Estrogen (CHEMBL592868) is a phase-3 clinical-stage small molecule targeting SLC36A1, GPER1, and KCNMA1; indicated across 5 conditions including heart disorder and breast neoplasm.

At a glance

  • Status: Max clinical phase 3 (not approved)
  • Modality: Small molecule
  • Targets: 6 (SLC36A1, GPER1, KCNMA1…)
  • Indications: 5 conditions
  • Clinical trials: 69
  • Chemistry: 310.4 Da · C21H26O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL592868
NameEstrogen
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID21628493
Molecular formulaC21H26O2
Molecular weight310.4
InChIKeyGJUHUIXJLZINMA-MJCUULBUSA-N

SMILES: CC#C[C@@]1(CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2CCC4=C3C=CC(=C4)O)C)O

IUPAC name: (8R,9S,13S,14S,17S)-13-methyl-17-prop-1-ynyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthrene-3,17-diol

Also known as: Estrogen, estrogen, ESTROGEN

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

GeneTargetActionpAffinityCancer dependencyUniProt
SLC36A1Proton-coupled Amino acid Transporter 1Inhibition5.20.2%Q7Z2H8
GPER1GPERFull agonist8.50.2%Q99527
KCNMA1KCa1.15.60.1%Q12791
NR1I2Pregnane X receptorAgonist0.3%O75469
ESR1Estrogen receptor-αAgonist9.821.7%P03372
ESR2Estrogen receptor-βAgonist9.340.2%Q92731

Broader ChEMBL bioactivity targets: 1 (assay-derived). Sample: Estrogen receptor.

Bioactivity

ChEMBL activities: 1 potent at pChembl ≥ 5 of 1 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
ESR110.55EC500.03nMCHEMBL_ACT_3103528

Target pathways

Aggregated over 6 target gene(s): SLC36A1, GPER1, KCNMA1, NR1I2, ESR1, ESR2.

Top Reactome pathways

37 total, by targets touching each:

PathwayTargetsGenes
Nuclear Receptor transcription pathway3ESR1, ESR2, NR1I2
PIP3 activates AKT signaling2ESR1, ESR2
Constitutive Signaling by Aberrant PI3K in Cancer2ESR1, ESR2
SUMOylation of intracellular receptors2ESR1, NR1I2
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling2ESR1, ESR2
ESR-mediated signaling2ESR1, ESR2
Extra-nuclear estrogen signaling2ESR1, ESR2
Hemostasis1KCNMA1
Neuronal System1KCNMA1
Nuclear signaling by ERBB41ESR1
Ca2+ activated K+ channels1KCNMA1
Potassium Channels1KCNMA1
Amino acid transport across the plasma membrane1SLC36A1
Peptide ligand-binding receptors1GPER1
Transport of small molecules1SLC36A1
Nitric oxide stimulates guanylate cyclase1KCNMA1
Platelet homeostasis1KCNMA1
cGMP effects1KCNMA1
G alpha (i) signalling events1GPER1
R-HSA-4253931SLC36A1
SLC-mediated transmembrane transport1SLC36A1
Proton-coupled neutral amino acid transporters1SLC36A1
Ovarian tumor domain proteases1ESR1
TFAP2 (AP-2) family regulates transcription of growth factors and their receptors1ESR1
RUNX1 regulates estrogen receptor mediated transcription1ESR1
RUNX1 regulates transcription of genes involved in WNT signaling1ESR1
Regulation of RUNX2 expression and activity1ESR1
Estrogen-dependent gene expression1ESR1
GPER1 signaling1GPER1
Sensory processing of sound1KCNMA1

Dominant GO biological processes

GO termTargets
positive regulation of transcription by RNA polymerase II4
signal transduction4
cellular response to estradiol stimulus3
negative regulation of transcription by RNA polymerase II3
regulation of DNA-templated transcription3
positive regulation of DNA-templated transcription3
monoatomic ion transport2
positive regulation of cytosolic calcium ion concentration2
positive regulation of gene expression2
negative regulation of gene expression2
cell differentiation2
nuclear receptor-mediated steroid hormone signaling pathway2
vasodilation2
positive regulation of apoptotic process2
steroid hormone receptor signaling pathway2

Indications & clinical

Indications

5 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

IndicationTrial phaseMONDOEFO
heart disorder3MONDO:0005267EFO:0003777
breast neoplasm3MONDO:0021100EFO:0003869
Alzheimer disease3MONDO:0004975MONDO:0004975

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 69.

Phase distribution

PhaseTrials
Not specified24
PHASE415
PHASE313
PHASE211
PHASE1/PHASE22
EARLY_PHASE12
PHASE2/PHASE31
PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT05221021PHASE4RECRUITINGVaginal Estradiol vs Oral Beta-3 Agonist for Overactive Bladder Syndrome
NCT05562518PHASE4ACTIVE_NOT_RECRUITINGGRACE-trial: a Randomized Active-controlled Trial for vulvovaGinal atRophy in breAst Cancer Patients on Endocrine Therapy.
NCT05704036PHASE4RECRUITINGEstrogen Supplementation and Bone Health in Women With CF
NCT07420218PHASE4NOT_YET_RECRUITINGMenopausal Hormones and Sympathetic Activation
NCT00229450PHASE4COMPLETEDEstrogen and Perimenopausal Depression
NCT01295892PHASE4COMPLETEDChronic Effects of Estrogen in Microcirculation
NCT01833663PHASE4COMPLETEDEffectiveness and Safety Study of Solifenacin Succinate and Solifenacin Succinate + Estrogen to Treat OAB in Postmenopausal Women
NCT02427386PHASE4COMPLETEDHomeopathic Treatment of Chronic Pelvic Pain in Women With Endometriosis
NCT02835846PHASE4COMPLETEDInvestigation of the Effect of the Female Urinary Microbiome on Incontinence
NCT02969590PHASE4COMPLETEDRegulation of Cervical Mucus Secretion
NCT03032848PHASE4COMPLETEDVaginal Estrogens Comparative Trial on Pelvic Organ Prolapse Patients
NCT03120715PHASE4UNKNOWNPregnancy Outcome of Women Using Low Molecular Weight Heparin Before Frozen-thawed Embryo Transfer
NCT03996057PHASE4WITHDRAWNMethenamine in a Non-antibiotic, Multimodal Approach to UTI Prevention
NCT04043520PHASE4UNKNOWNBioenergetic Effects of Aging and Menopause (BEAM)
NCT05753098PHASE4COMPLETEDEffect of Sildenafil Citrate Compared to Estrogen as Adjuvant Therapy for Unexplained Infertility
NCT06851754PHASE3RECRUITINGHormone Replacement Therapy in Adolescents With Premature Ovarian Insufficiency
NCT00000176PHASE3COMPLETEDAlzheimer’s Disease Prevention Trial
NCT00000177PHASE3COMPLETEDEstrogen Hormone Protocol
NCT00000430PHASE3TERMINATEDLow-Dose Hormone Replacement Therapy and Alendronate for Osteoporosis
NCT00000482PHASE3COMPLETEDCoronary Drug Project
NCT00026039PHASE3COMPLETEDWomen’s Estrogen for Stroke Trial (WEST)
NCT00029159PHASE3COMPLETEDThe Effect of Androgen and Growth Hormone on Height and Learning in Girls With Turner Syndrome
NCT00043069PHASE3COMPLETEDCalcium With or Without Estrogen and/or Risedronate in Preventing Osteoporosis in Patients With Prostate Cancer
NCT00386022PHASE2/PHASE3UNKNOWNThe Effects of Aging and Estrogen on the Pituitary
NCT00827151PHASE3WITHDRAWNBone Mass Accrual in Adolescent Athletes
NCT01501422PHASE3COMPLETEDEffect of Estrogen Therapy on Objective Sleep Quality in Postmenopausal Women
NCT02419729PHASE3COMPLETEDEvaluation of Fractional CO2 Laser Treatment Efficacy and Comparison to Vaginal Estrogen Therapy in Postmenopausal Women With Vulvovaginal Atrophy
NCT03568708PHASE3COMPLETEDPrimary Ovarian Insufficiency: Phenotype and Optimal Treatment
NCT05658874PHASE3TERMINATEDA Multidisciplinary, Multimodal Bundled Care Approach to Chronic Pelvic Pain
NCT03663543PHASE1/PHASE2ACTIVE_NOT_RECRUITINGIntravenous Estrogen in Kidney Transplant Study
NCT03875378PHASE2RECRUITINGTransdermal Estrogen in Women With Anorexia Nervosa
NCT06271551PHASE2NOT_YET_RECRUITINGTransdermal Estradiol and Exercise in Mitigating Adverse Effects of Androgen Deprivation Therapy for Prostate Cancer Radiation Therapy
NCT06318403PHASE2NOT_YET_RECRUITINGEstradiol Supplementation and Rotator Cuff Repair
NCT07466498PHASE2NOT_YET_RECRUITINGEstrogen to Improve Quality of Life for Men With Newly Diagnosed or Recurrent Metastatic Hormone Sensitive Prostate Cancer, EQUIP Trial
NCT00001752PHASE2COMPLETEDVascular and Metabolic Effects of Hormone Therapy Combined With L-Arginine in Postmenopausal Women
NCT00001890PHASE2COMPLETEDEffects of Hormone Therapy on the Immune Systems of Postmenopausal Women With Chronic Infections
NCT00005768PHASE2UNKNOWNEstrogen Modulation of Mood and Cognition Following Monoaminergic Depletion in Post-Menopausal Women
NCT00006399PHASE2COMPLETEDEffects of Estrogen on Memory in Post-Menopausal Women and Patients With Alzheimer’s Disease
NCT00018343PHASE2COMPLETEDAlzheimer’s Disease and Aging: Therapeutic Potential of Estrogen
NCT00332553PHASE2COMPLETEDStudy of Hot Flashes and Night Sweats in Postmenopausal Women Receiving Combination Raloxifene and Oral Estrogen

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

427 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
ESTRADIOLChEMBL + PubChemPhase 4 (approved)ESR1, ESR2, GPER1, KCNMA1
FulvestrantChEMBL + PubChemPhase 4 (approved)ESR1, ESR2, GPER1, NR1I2
RaloxifeneChEMBL + PubChemPhase 4 (approved)ESR1, ESR2, GPER1, NR1I2
TamoxifenChEMBL + PubChemPhase 4 (approved)ESR1, ESR2, GPER1, NR1I2
BOSENTANChEMBL + PubChemPhase 4 (approved)ESR1, ESR2, NR1I2
BITHIONOLChEMBLPhase 4 (approved)ESR1, ESR2, NR1I2
DIETHYLSTILBESTROLChEMBLPhase 4 (approved)ESR1, ESR2, NR1I2
ETHINYL ESTRADIOLChEMBLPhase 4 (approved)ESR1, ESR2, NR1I2
LASOFOXIFENEChEMBLPhase 4 (approved)ESR1, ESR2, NR1I2
MIFEPRISTONEChEMBLPhase 4 (approved)ESR1, ESR2, NR1I2
FidaxomicinPubChemApprovedESR1, ESR2, NR1I2
PyrazinamidePubChemApprovedESR1, ESR2, NR1I2
CANNABIDIOLChEMBL + PubChemPhase 4 (approved)KCNMA1, NR1I2
ALECTINIBChEMBLPhase 4 (approved)ESR1, NR1I2
BAZEDOXIFENEChEMBLPhase 4 (approved)ESR1, ESR2
BENZBROMARONEChEMBLPhase 4 (approved)ESR1, NR1I2
BUTOCONAZOLEChEMBLPhase 4 (approved)ESR1, NR1I2
CANDESARTAN CILEXETILChEMBLPhase 4 (approved)ESR1, NR1I2
CEFEPIMEChEMBLPhase 4 (approved)ESR1, NR1I2
CEFTAZIDIMEChEMBLPhase 4 (approved)ESR1, NR1I2
CISPLATINChEMBLPhase 4 (approved)ESR1, ESR2
DANAZOLChEMBLPhase 4 (approved)ESR1, NR1I2
DAUNORUBICINChEMBLPhase 4 (approved)ESR1, NR1I2
DEMECLOCYCLINEChEMBLPhase 4 (approved)ESR2, NR1I2
DESOGESTRELChEMBLPhase 4 (approved)ESR1, NR1I2
DINOPROSTONEChEMBLPhase 4 (approved)ESR1, NR1I2
ELACESTRANTChEMBLPhase 4 (approved)ESR1, ESR2
ESTETROLChEMBLPhase 4 (approved)ESR1, ESR2
ESTRIOLChEMBLPhase 4 (approved)ESR1, ESR2
ESTRONEChEMBLPhase 4 (approved)ESR1, ESR2
HEXACHLOROPHENEChEMBLPhase 4 (approved)ESR1, ESR2
ISOCONAZOLEChEMBLPhase 4 (approved)ESR1, NR1I2
LYMECYCLINEChEMBLPhase 4 (approved)ESR1, NR1I2
MASOPROCOLChEMBLPhase 4 (approved)ESR1, NR1I2
MEDROXYPROGESTERONEChEMBLPhase 4 (approved)ESR1, ESR2
PHENOLPHTHALEINChEMBLPhase 4 (approved)ESR1, ESR2
SERTRALINEChEMBLPhase 4 (approved)ESR1, NR1I2
SPIRONOLACTONEChEMBLPhase 4 (approved)ESR1, ESR2
ACOLBIFENEChEMBLPhase 3ESR1, ESR2
AFIMOXIFENEChEMBLPhase 3ESR1, ESR2
AMCENESTRANTChEMBLPhase 3ESR1, ESR2
ARZOXIFENEChEMBLPhase 3ESR1, ESR2
BENSERAZIDEChEMBLPhase 3ESR1, ESR2
SURAMINChEMBLPhase 3ESR1, NR1I2
ALFATRADIOLChEMBLPhase 2ESR1, ESR2
AUS-131ChEMBLPhase 2ESR1, ESR2
BENZETHONIUMChEMBLPhase 2ESR1, NR1I2
BRILANESTRANTChEMBLPhase 2ESR1, ESR2
CEPHACETRILEChEMBLPhase 2ESR1, NR1I2
CLEMIZOLEChEMBLPhase 2ESR1, NR1I2
DAIDZEINChEMBLPhase 2ESR1, ESR2
DOMIPHENChEMBLPhase 2ESR1, NR1I2
ERTEBERELChEMBLPhase 2ESR1, ESR2
GENISTEINChEMBLPhase 2ESR1, ESR2
GESTRINONEChEMBLPhase 2ESR1, NR1I2
GTX-758ChEMBLPhase 2ESR1, ESR2
IDOXIFENEChEMBLPhase 2ESR1, ESR2
LEVORMELOXIFENEChEMBLPhase 2ESR1, ESR2
MOXESTROLChEMBLPhase 2ESR1, ESR2
PIPENDOXIFENEChEMBLPhase 2ESR1, ESR2

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.2
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot