OralTopicalDosed ingredientTherapeutic flag
Cosmetic cross-reference
Estradiol
CAS 50-28-2
Estradiol (CAS 50-28-2) is a Phase 4 pharmaceutical compound with 18 bioactivity targets and 3,453 adverse event associations.
SOURCE
NLM DailyMed
Label records
1
SOURCE
EMBL-EBI ChEMBL
Bioactivity
32
SOURCE
DrugCentral
Adverse signals
3,453
SOURCE
IUPHAR/BPS
PubMed IDs
9
SOURCE
EMBL-EBI ChEMBL
B25820EEF0F0
Compound Identity
Matched identifiers and naming fields for the pharmaceutical compound record.
Primary Name
Estradiol
CAS Number
50-28-2
UNII
4TI98Z838E
InChIKey
VOXZDWNPVJITMN-ZBRFXRBCSA-N
ChEMBL ID
CHEMBL135
Molecule Type
Small molecule
Source Match
EMBL-EBI ChEMBL (INCHIKEY)
Synonyms and normalized names
ESTROGENS, ESTERIFIEDESTRADIOL CYPIONATEDepo-estradiolEstringVagifemEstraceAloraCombipatchMenestVivelleDelestrogenClimaraEstrogelFemringMenostarElestrinDivigelEvamist
black box warningdosed ingredientnatural productoraltherapeutic flagtopical
SOURCE
EMBL-EBI ChEMBL
B25820EEF0F0
Clinical Development Phase
Highest clinical development phase rendered from the matched compound identifier rows.
Phase 4 (Approved)
Approved or marketed human pharmaceutical use is represented in the source phase field.
ChEMBL CHEMBL135 | Small molecule
SOURCE
Ingredients table / CosIng profile
same-CAS cross-reference
Cross-Reference to Cosmetics
Same-CAS ingredient record found in the cosmetics vertical.
SOURCE
NLM DailyMed
1 label row
Drug Label Active Ingredients
Active ingredient and active moiety rows from source drug product labels.
| Product | Ingredient | Active Moiety | Effective |
|---|---|---|---|
| Estradiol Gel | ESTRADIOL 4TI98Z838E |
ESTRADIOL | 20260429 |
SOURCE
EMBL-EBI ChEMBL
32 bioactivity rows
Bioactivity & Target Interactions
Target-level activity records with assay counts, activity type, and measured value where present.
| Target | Activity | Value | Assays | Organism |
|---|---|---|---|---|
| - | IC50 | 6121.81648108108 nM | 184 | - |
| - | EC50 | 349.42539565891474 nM | 129 | - |
| - | AC50 | 16726.440983606557 nM | 122 | - |
| - | Potency | 20413.572619047616 nM | 62 | - |
| - | Ki | 1534.5677441860464 nM | 43 | - |
| - | Kd | 110.40340625 nM | 32 | - |
| - | EC50 | 0.4875 ug.mL-1 | 4 | - |
| - | Kd | 100 | 3 | - |
| Sodium-dependent serotonin transporter Transporter |
Ki | 5.243 | - | Homo sapiens |
| Aldehyde oxidase Enzyme |
IC50 | 6.538 | - | Homo sapiens |
| Glucocorticoid receptor Nuclear hormone receptor |
Ki | 4.725 | - | Homo sapiens |
| Sodium-dependent dopamine transporter Transporter |
Ki | 4.926 | - | Homo sapiens |
| Estrogen receptor Nuclear hormone receptor |
EC50 | 10.3 | - | Homo sapiens |
| Androgen receptor Nuclear hormone receptor |
IC50 | 7.72 | - | Homo sapiens |
| Calcium-activated potassium channel subunit alpha-1 Ion channel |
EC50 | 5.6 | - | Homo sapiens |
| Estrogen receptor beta Nuclear hormone receptor |
EC50 | 9.7 | - | Homo sapiens |
| G-protein coupled estrogen receptor 1 GPCR |
EC50 | 9.52 | - | Homo sapiens |
| Corticosteroid-binding globulin Secreted |
Ki | 5 | - | Homo sapiens |
| Steryl-sulfatase Enzyme |
IC50 | 4.08 | - | Homo sapiens |
| Sex hormone-binding globulin Secreted |
Kd | 8.83 | - | Homo sapiens |
| Steroid hormone receptor ERR1 Nuclear hormone receptor |
IC50 | 8.44 | - | Homo sapiens |
| Steroid hormone receptor ERR2 Nuclear hormone receptor |
IC50 | 8.49 | - | Homo sapiens |
| Androgen receptor Transcription factor |
IC50 | 6.39 | - | Rattus norvegicus |
| Arachidonate 15-lipoxygenase Enzyme |
IC50 | 4.947 | - | Oryctolagus cuniculus |
| Progesterone receptor Transcription factor |
Ki | 5.372 | - | Bos taurus |
| Estrogen receptor Transcription factor |
IC50 | 8.72 | - | Rattus norvegicus |
| Estrogen receptor beta Transcription factor |
IC50 | 8.77 | - | Rattus norvegicus |
| Estrogen receptor beta Transcription factor |
IC50 | 8.64 | - | Mus musculus |
| Estrogen receptor Transcription factor |
IC50 | 8.66 | - | Mus musculus |
| Cytochrome P450 1B1 Enzyme |
Ki | 5.72 | - | Homo sapiens |
| Estrogen receptor Transcription factor |
IC50 | 9.45 | - | Rattus norvegicus |
| Alpha-synuclein Transporter |
IC50 | 4.22 | - | Homo sapiens |
SOURCE
DrugCentral
80 associations
Adverse Event Associations
DrugCentral / FAERS disproportionality signal rows matched to this compound.
| Reaction PT | Drug AE | LLR | MedDRA |
|---|---|---|---|
| Product adhesion issue | 1080 | 4293.469 | 10069889 |
| Hot flush | 768 | 1099.39 | 10060800 |
| Application site rash | 278 | 921.05 | 10003054 |
| Application site erythema | 237 | 581.401 | 10003041 |
| Meningioma | 211 | 553.996 | 10027191 |
| Application site pruritus | 206 | 534.442 | 10003053 |
| Product quality issue | 437 | 497.418 | 10069327 |
| Application site irritation | 144 | 427.908 | 10003046 |
| Vulvovaginal discomfort | 140 | 425.22 | 10047786 |
| Death | 239 | 316.331 | 10011906 |
| Wrong technique in product usage process | 428 | 272.136 | 10076573 |
| Menopausal symptoms | 99 | 258.174 | 10027304 |
| Vulvovaginal pain | 98 | 251.614 | 10069055 |
| Vaginal haemorrhage | 216 | 250.116 | 10046910 |
| Vulvovaginal burning sensation | 84 | 227.299 | 10067641 |
| Application site reaction | 75 | 222.497 | 10003055 |
| Schizoaffective disorder | 104 | 211.701 | 10039621 |
| Blood oestrogen decreased | 49 | 202.282 | 10005687 |
| Vulvovaginal dryness | 85 | 200.386 | 10047791 |
| Pneumonia viral | 135 | 199.321 | 10035737 |
| Migraine | 416 | 197.867 | 10027599 |
| Toxicity to various agents | 141 | 178.63 | 10070863 |
| Breast tenderness | 80 | 175.73 | 10006313 |
| Pemphigus | 13 | 172.3 | 10034280 |
| Soft tissue disorder | 93 | 171.866 | 10061366 |
| Vaginal discharge | 111 | 166.639 | 10046901 |
| Acute kidney injury | 225 | 166.027 | 10069339 |
| Application site pain | 95 | 161.495 | 10003051 |
| Feeling abnormal | 538 | 160.717 | 10016322 |
| Headache | 1480 | 159.297 | 10019211 |
| Ovarian hyperstimulation syndrome | 79 | 159.165 | 10033266 |
| Product physical issue | 98 | 149.612 | 10071134 |
| Febrile neutropenia | 51 | 146.607 | 10016288 |
| Neutropenia | 100 | 146.337 | 10029354 |
| Product complaint | 134 | 140.371 | 10069902 |
| Application site vesicles | 60 | 139.575 | 10048941 |
| Hysterectomy | 98 | 139.376 | 10021151 |
| Vaginal infection | 91 | 135.496 | 10046914 |
| Hand deformity | 17 | 135.021 | 10061194 |
| Colitis microscopic | 106 | 130.521 | 10056979 |
| Thrombocytopenia | 94 | 129.933 | 10043554 |
| Hormone level abnormal | 63 | 129.008 | 10061210 |
| Breast cancer | 203 | 125.218 | 10006187 |
| Glossodynia | 32 | 123.171 | 10018388 |
| Drug abuse | 18 | 120.448 | 10013654 |
| Intermenstrual bleeding | 84 | 118.112 | 10022559 |
| Sepsis | 109 | 117.018 | 10040047 |
| Application site burn | 45 | 116.971 | 10065059 |
| Postmenopausal haemorrhage | 52 | 113.344 | 10055870 |
| Application site urticaria | 34 | 113.313 | 10050104 |
Association rows are source-linked signal records, not incidence rates or clinical causality claims.
SOURCE
IUPHAR/BPS
6 interactions
IUPHAR Ligand-Target Data
Curated ligand-target interaction rows with action, affinity, and literature identifiers.
| Target | Action | Affinity | PubMed |
|---|---|---|---|
| Estrogen receptor-α ESR1 |
Agonist | 9.819999694824219 pKi | 9048584 |
| Estrogen receptor-β ESR2 |
Agonist | 9.34 pKi | 9048584 |
| GPER GPER1 |
Full agonist | 8.199999809265137 pKi | 15705806|15539556 |
| K Ca 1.1 KCNMA1 |
Activator | 5.6 pEC50 | 10489376 |
| Pregnane X receptor NR1I2 |
Agonist | - | 10628745 |
| Proton-coupled Amino acid Transporter 1 SLC36A1 |
Inhibition | 5.0 pIC50 | 32835702 |
SOURCE
PharmGKB
3 phenotype rows
Pharmacogenomics
Drug-gene phenotype annotations and evidence levels from PharmGKB-mapped rows.
- rs1864729
Allele A is associated with increased plasma level of estradiol in women with Breast Neoplasms as compared to allele G.
Evidence: -; PMID 23518928
NFE2L2 (PA31588) rs6721961
Allele T is associated with increased risk of venous thromboembolism when treated with estradiol as compared to genotype CC.
Evidence: -; PMID 21107315
- rs11849538
-
Evidence: 3; PMID 1
SOURCE
NLM RxNorm
23 name rows
Drug Names / RxNorm
Normalized drug-name vocabulary rows, RxCUIs, and source abbreviations.
| Name | RxCUI | Type | Source |
|---|---|---|---|
| Estradiol | 4083 | SU | MTHSPL |
| estradiol | 4083 | SU | MTHSPL |
| ESTRADIOL | 4083 | SU | MTHSPL |
| ESTROGENS, ESTERIFIED | 214549 | SU | MTHSPL |
| ESTRADIOL CYPIONATE | 1000146 | SU | MTHSPL |
| estradiol | 4083 | IN | RXNORM |
| Depo-estradiol | 48876 | BN | RXNORM |
| Estring | 151720 | BN | RXNORM |
| Vagifem | 152483 | BN | RXNORM |
| Estrace | 202619 | BN | RXNORM |
| Alora | 215168 | BN | RXNORM |
| Combipatch | 216161 | BN | RXNORM |
| Menest | 218309 | BN | RXNORM |
| Vivelle | 220918 | BN | RXNORM |
| Delestrogen | 319865 | BN | RXNORM |
| Climara | 323984 | BN | RXNORM |
| Estrogel | 405052 | BN | RXNORM |
| Femring | 405070 | BN | RXNORM |
| Menostar | 545273 | BN | RXNORM |
| Elestrin | 706464 | BN | RXNORM |
| Divigel | 722259 | BN | RXNORM |
| Evamist | 728119 | BN | RXNORM |
| estradiol cypionate | 1000146 | PIN | RXNORM |
SOURCE
SIDER
80 side-effect rows
Side Effects
SIDER side-effect terms mapped to the drug or same-CAS compound identity.
| Side Effect | Drug Name | MedDRA Type | Concept ID |
|---|---|---|---|
| Abdominal bloating | estradiol | LLT | C1291077 |
| Abdominal bloating | estradiol | LLT | C1291077 |
| Abdominal bloating | estradiol | LLT | C1291077 |
| Abdominal cramps | estradiol | LLT | C0000729 |
| Abdominal cramps | estradiol | LLT | C0000729 |
| Abdominal cramps | estradiol | LLT | C0000729 |
| Abdominal discomfort | estradiol | LLT | C0232487 |
| Abdominal discomfort | estradiol | PT | C0232487 |
| Abdominal discomfort | estradiol | PT | C0232487 |
| Abdominal distension | estradiol | LLT | C0000731 |
| Abdominal distension | estradiol | PT | C0000731 |
| Abdominal distension | estradiol | PT | C0000731 |
| Abdominal distension | estradiol | PT | C0000731 |
| Abdominal distension | estradiol | PT | C0000731 |
| Abdominal distension | estradiol | PT | C0000731 |
| Abdominal pain | estradiol | PT | C0000737 |
| Abdominal pain | estradiol | LLT | C0000737 |
| Abdominal pain | estradiol | PT | C0000737 |
| Abdominal pain | estradiol | PT | C0000737 |
| Abdominal pain | estradiol | PT | C0000737 |
| Abdominal pain | estradiol | LLT | C0000737 |
| Abdominal pain | estradiol | PT | C0000737 |
| Abdominal pain lower | estradiol | LLT | C0232495 |
| Abdominal pain lower | estradiol | PT | C0232495 |
| Abdominal pain upper | estradiol | LLT | C0232492 |
| Abdominal pain upper | estradiol | PT | C0232492 |
| Abnormal vision | estradiol | LLT | C3665386 |
| Abnormal withdrawal bleeding | estradiol | LLT | C2609183 |
| Abnormal withdrawal bleeding | estradiol | PT | C2609183 |
| Abnormal withdrawal bleeding | estradiol | LLT | C2609183 |
| Abnormal withdrawal bleeding | estradiol | PT | C2609183 |
| Abnormal withdrawal bleeding | estradiol | LLT | C2609183 |
| Abnormal withdrawal bleeding | estradiol | PT | C2609183 |
| Accidental injury | estradiol | LLT | C0151736 |
| Ache | estradiol | LLT | C0234238 |
| Acne | estradiol | LLT | C0702166 |
| Acne | estradiol | PT | C0702166 |
| Acne | estradiol | LLT | C0702166 |
| Acne | estradiol | PT | C0702166 |
| Acute coronary syndrome | estradiol | PT | C0948089 |
| Acute coronary syndrome | estradiol | PT | C0948089 |
| Acute coronary syndrome | estradiol | PT | C0948089 |
| Affect lability | estradiol | PT | C0233472 |
| Agitation | estradiol | LLT | C0085631 |
| Agitation | estradiol | PT | C0085631 |
| Alanine aminotransferase increased | estradiol | LLT | C0151905 |
| Alanine aminotransferase increased | estradiol | PT | C0151905 |
| Allergic contact dermatitis | estradiol | LLT | C0162820 |
| Alopecia | estradiol | LLT | C0002170 |
| Alopecia | estradiol | PT | C0002170 |
| Amenorrhoea | estradiol | LLT | C0002453 |
| Amenorrhoea | estradiol | PT | C0002453 |
| Amnesia | estradiol | LLT | C0002622 |
| Amnesia | estradiol | PT | C0002622 |
| Anal pruritus | estradiol | LLT | C0033775 |
| Anal pruritus | estradiol | PT | C0033775 |
| Anaphylactic shock | estradiol | LLT | C0002792 |
| Anaphylactic shock | estradiol | PT | C0002792 |
| Anaphylactic shock | estradiol | PT | C0002792 |
| Anaphylactic shock | estradiol | LLT | C0002792 |
| Anaphylactic shock | estradiol | PT | C0002792 |
| Anaphylactic shock | estradiol | LLT | C0002792 |
| Anaphylactic shock | estradiol | PT | C0002792 |
| Anaphylactoid reaction | estradiol | LLT | C0340865 |
| Anaphylactoid reaction | estradiol | PT | C0340865 |
| Angioedema | estradiol | LLT | C0002994 |
| Angioedema | estradiol | PT | C0002994 |
| Angioedema | estradiol | LLT | C0002994 |
| Angioedema | estradiol | PT | C0002994 |
| Angioedema | estradiol | LLT | C0002994 |
| Angioedema | estradiol | PT | C0002994 |
| Angiopathy | estradiol | LLT | C0042373 |
| Angiopathy | estradiol | PT | C0042373 |
| Anorectal discomfort | estradiol | PT | C2242737 |
| Anxiety | estradiol | LLT | C0003467 |
| Anxiety | estradiol | PT | C0003467 |
| Anxiety | estradiol | PT | C0003467 |
| Anxiety | estradiol | LLT | C0003467 |
| Anxiety | estradiol | PT | C0003467 |
| Anxiety NEC | estradiol | LLT | C0853074 |
SOURCE
Rendered pharma page rows
FAQPage JSON-LD
Frequently Asked Questions
Short answers generated only from the same visible source-linked rows on this page.
What is Estradiol used for in pharmaceutical contexts?
Estradiol (CAS 50-28-2) appears in DailyMed active-ingredient label rows, including Estradiol Gel.
What are the known adverse events for Estradiol?
Estradiol has 3,453 DrugCentral/FAERS adverse event associations. Rendered reaction terms include Product adhesion issue, Hot flush, Application site rash, Application site erythema, Meningioma. Signal rows are source-linked records and should not be read as incidence rates or causality conclusions.
Is Estradiol also used in cosmetics?
Yes. The ingredients table has a same-CAS cosmetic profile for Estradiol with EU status "prohibited".
What clinical phase is Estradiol in?
Estradiol is rendered with ChEMBL max phase 4 (approved).
What bioactivity targets are documented for Estradiol?
Estradiol has 32 bioactivity rows in this page query. Rendered target entries include Sodium-dependent serotonin transporter, Aldehyde oxidase, Glucocorticoid receptor, Sodium-dependent dopamine transporter, Estrogen receptor.