Tamoxifen
CAS 10540-29-1
Tamoxifen (CAS 10540-29-1) is a Phase 4 pharmaceutical compound with 65 bioactivity targets and 1,598 adverse event associations.
Compound Identity
Matched identifiers and naming fields for the pharmaceutical compound record.
Clinical Development Phase
Highest clinical development phase rendered from the matched compound identifier rows.
Bioactivity & Target Interactions
Target-level activity records with assay counts, activity type, and measured value where present.
| Target | Activity | Value | Assays | Organism |
|---|---|---|---|---|
| - | IC50 | 14827.782802850355 nM | 420 | - |
| - | AC50 | 18384.081714285716 nM | 105 | - |
| - | GI50 | 8070.906190476191 nM | 63 | - |
| - | Potency | 25652.495402298853 nM | 60 | - |
| - | Ki | 4102.770931034483 nM | 58 | - |
| - | EC50 | 19281.505 nM | 22 | - |
| - | IC50 | 6.5175 ug.mL-1 | 16 | - |
| - | MIC | 38.18181818181818 ug.mL-1 | 11 | - |
| - | GI50 | 10 ug.mL-1 | 1 | - |
| - | Kd | 1 nM | 1 | - |
| Adenosine receptor A1 GPCR |
Ki | 4.858 | - | Homo sapiens |
| Sodium/potassium-transporting ATPase subunit alpha-2 Ion channel |
IC50 | 4.807 | - | Sus scrofa |
| Beta-1 adrenergic receptor GPCR |
Ki | 5.001 | - | Homo sapiens |
| Prostaglandin G/H synthase 2 Enzyme |
IC50 | 4.46 | - | Homo sapiens |
| Prostaglandin G/H synthase 1 Enzyme |
IC50 | 5.357 | - | Homo sapiens |
| Mu-type opioid receptor GPCR |
Ki | 5.146 | - | Homo sapiens |
| D(1A) dopamine receptor GPCR |
Ki | 5.372 | - | Homo sapiens |
| D(2) dopamine receptor GPCR |
Ki | 5.335 | - | Homo sapiens |
| Adenosine receptor A2a GPCR |
Ki | 5.4 | - | Homo sapiens |
| Alpha-2A adrenergic receptor GPCR |
Ki | 6.139 | - | Homo sapiens |
| Sigma non-opioid intracellular receptor 1 Membrane receptor |
Ki | 7.5 | - | Homo sapiens |
| Potassium voltage-gated channel subfamily H member 2 Ion channel |
IC50 | 5.8 | - | Homo sapiens |
| 3-beta-hydroxysteroid-Delta(8),Delta(7)-isomerase Enzyme |
Ki | 8.301 | - | Homo sapiens |
| Multidrug resistance protein 1 Transporter |
Ki | 7 | - | Homo sapiens |
| Sodium-dependent serotonin transporter Transporter |
Ki | 5.907 | - | Homo sapiens |
| Sodium-dependent noradrenaline transporter Transporter |
Ki | 5.836 | - | Homo sapiens |
| 5-hydroxytryptamine receptor 1A GPCR |
Ki | 5.158 | - | Homo sapiens |
| 5-hydroxytryptamine receptor 2A GPCR |
Ki | 5.863 | - | Homo sapiens |
| 5-hydroxytryptamine receptor 2B GPCR |
Ki | 5.877 | - | Homo sapiens |
| 5-hydroxytryptamine receptor 2C GPCR |
Ki | 6.618 | - | Homo sapiens |
| 5-hydroxytryptamine receptor 6 GPCR |
Ki | 5.98 | - | Homo sapiens |
| Alpha-2B adrenergic receptor GPCR |
Ki | 5.794 | - | Homo sapiens |
| D(3) dopamine receptor GPCR |
Ki | 6.439 | - | Homo sapiens |
| Histamine H2 receptor GPCR |
Ki | 5.034 | - | Homo sapiens |
| Muscarinic acetylcholine receptor M1 GPCR |
Ki | 6.167 | - | Homo sapiens |
| Muscarinic acetylcholine receptor M2 GPCR |
Ki | 5.557 | - | Homo sapiens |
| Muscarinic acetylcholine receptor M3 GPCR |
Ki | 6.201 | - | Homo sapiens |
| Muscarinic acetylcholine receptor M4 GPCR |
Ki | 6.173 | - | Homo sapiens |
| Muscarinic acetylcholine receptor M5 GPCR |
Ki | 5.731 | - | Homo sapiens |
| Aldehyde oxidase Enzyme |
IC50 | 5.658 | - | Homo sapiens |
| Beta-3 adrenergic receptor GPCR |
Ki | 5.238 | - | Homo sapiens |
| Sodium-dependent dopamine transporter Transporter |
Ki | 5.835 | - | Homo sapiens |
| Adenosine receptor A3 GPCR |
Ki | 5.679 | - | Homo sapiens |
| Nuclear receptor subfamily 1 group I member 2 Nuclear hormone receptor |
Ki | 7.456 | - | Homo sapiens |
| D(4) dopamine receptor GPCR |
Ki | 5.407 | - | Homo sapiens |
| Alpha-1D adrenergic receptor GPCR |
Ki | 5.611 | - | Homo sapiens |
| Kappa-type opioid receptor GPCR |
Ki | 5.204 | - | Homo sapiens |
| Estrogen receptor Nuclear hormone receptor |
Ki | 7.51 | - | Homo sapiens |
| Progesterone receptor Nuclear hormone receptor |
IC50 | 6.89 | - | Homo sapiens |
| Delta-type opioid receptor GPCR |
Ki | 5.328 | - | Homo sapiens |
Adverse Event Associations
DrugCentral / FAERS disproportionality signal rows matched to this compound.
| Reaction PT | Drug AE | LLR | MedDRA |
|---|---|---|---|
| Metastases to bone | 753 | 2218.542 | 10027452 |
| Malignant neoplasm progression | 1053 | 1784.654 | 10051398 |
| Metastases to liver | 495 | 1194.816 | 10027457 |
| Metastases to lung | 311 | 760.029 | 10027458 |
| Breast cancer recurrent | 183 | 636.496 | 10006198 |
| Metastases to lymph nodes | 225 | 597.144 | 10027459 |
| Breast cancer metastatic | 217 | 586.99 | 10055113 |
| Disease progression | 548 | 432.1 | 10061818 |
| Neoplasm progression | 289 | 420.169 | 10061309 |
| Breast cancer | 254 | 387.542 | 10006187 |
| Osteonecrosis of jaw | 208 | 268.244 | 10064658 |
| Metastases to central nervous system | 150 | 265.721 | 10059282 |
| Metastasis | 116 | 259.581 | 10062194 |
| PIK3CA-activated mutation | 62 | 230.597 | 10081234 |
| Metastases to spine | 88 | 220.463 | 10027468 |
| Hot flush | 194 | 188.818 | 10060800 |
| Tumour marker increased | 76 | 183.863 | 10048621 |
| Uterine polyp | 57 | 178.739 | 10046811 |
| Endometrial hyperplasia | 47 | 175.717 | 10014755 |
| Bone lesion | 81 | 166.055 | 10061728 |
| Metastases to pleura | 53 | 159.248 | 10027463 |
| Bone disorder | 118 | 158.832 | 10005956 |
| Metastases to skin | 53 | 156.255 | 10027465 |
| Carbohydrate antigen 15-3 increased | 45 | 144.234 | 10051415 |
| Osteonecrosis | 125 | 135.474 | 10031264 |
| Metastases to the mediastinum | 38 | 133.136 | 10027469 |
| Hormone receptor positive breast cancer | 34 | 131 | 10083234 |
| Hepatic lesion | 68 | 129.577 | 10061998 |
| Pseudocirrhosis | 35 | 126.042 | 10076501 |
| Metastases to peritoneum | 56 | 119.941 | 10051676 |
| Neuropathy peripheral | 275 | 119.227 | 10029331 |
| Sarcoma uterus | 19 | 113.379 | 10039497 |
| Endometrial hypertrophy | 26 | 109.969 | 10014756 |
| Bone pain | 151 | 106.516 | 10006002 |
| Endometrial cancer | 43 | 105.153 | 10014733 |
| Acute myeloid leukaemia | 106 | 102.343 | 10000880 |
| Second primary malignancy | 77 | 100.864 | 10039801 |
| Contraindicated product administered | 6 | 98.175 | 10078504 |
| Hysteroscopy | 17 | 97.337 | 10050125 |
| Tonsillar disorder | 34 | 95.862 | 10053477 |
| Uterine cancer | 45 | 94.732 | 10046766 |
| Breast mass | 55 | 93.287 | 10006272 |
| Invasive ductal breast carcinoma | 49 | 89.296 | 10073095 |
| Pulmonary mass | 95 | 88.514 | 10056342 |
| Lymphoedema | 67 | 88.373 | 10025282 |
| Device related thrombosis | 37 | 85.325 | 10077455 |
| Nail disorder | 64 | 83.164 | 10028694 |
| Systemic lupus erythematosus | 7 | 81.099 | 10042945 |
| Blood uric acid decreased | 28 | 79.27 | 10005860 |
| Therapeutic product effect decreased | 9 | 79.257 | 10082201 |
Association rows are source-linked signal records, not incidence rates or clinical causality claims.
IUPHAR Ligand-Target Data
Curated ligand-target interaction rows with action, affinity, and literature identifiers.
| Target | Action | Affinity | PubMed |
|---|---|---|---|
| Estrogen receptor-α ESR1 |
Agonist | 7.820000171661377 pKi | 9048584 |
| Estrogen receptor-α ESR1 |
Antagonist | 7.800000190734863 pKi | 9048584 |
| Estrogen receptor-β ESR2 |
Agonist | 7.16 pKi | 9048584 |
| Estrogen receptor-β ESR2 |
Antagonist | 7.17 pKi | 9048584 |
| GPER GPER1 |
Full agonist | 6.0 pKi | 15539556 |
| Maxi Cl - | Activator | - | - |
| VRAC | Channel blocker | - | - |
Pharmacogenomics
Drug-gene phenotype annotations and evidence levels from PharmGKB-mapped rows.
Drug Names / RxNorm
Normalized drug-name vocabulary rows, RxCUIs, and source abbreviations.
| Name | RxCUI | Type | Source |
|---|---|---|---|
| TAMOXIFEN | 10324 | SU | MTHSPL |
| Tamoxifen | 10324 | SU | MTHSPL |
| Tamoxifen Citrate | 40137 | SU | MTHSPL |
| TAMOXIFEN CITRATE | 40137 | SU | MTHSPL |
| tamoxifen | 10324 | IN | RXNORM |
| tamoxifen citrate | 40137 | PIN | RXNORM |
Side Effects
SIDER side-effect terms mapped to the drug or same-CAS compound identity.
| Side Effect | Drug Name | MedDRA Type | Concept ID |
|---|---|---|---|
| Abdominal cramps | tamoxifen | LLT | C0000729 |
| Abdominal discomfort | tamoxifen | PT | C0232487 |
| Abdominal pain | tamoxifen | PT | C0000737 |
| Abdominal pain | tamoxifen | LLT | C0000737 |
| Abdominal pain | tamoxifen | PT | C0000737 |
| Accidental exposure to product | tamoxifen | PT | C3544060 |
| Accidental ingestion | tamoxifen | LLT | C0857807 |
| Accidental injury | tamoxifen | LLT | C0151736 |
| Acute coronary syndrome | tamoxifen | PT | C0948089 |
| Adenocarcinoma | tamoxifen | LLT | C0001418 |
| Adenocarcinoma | tamoxifen | PT | C0001418 |
| Alanine aminotransferase increased | tamoxifen | LLT | C0151905 |
| Alanine aminotransferase increased | tamoxifen | PT | C0151905 |
| Alopecia | tamoxifen | LLT | C0002170 |
| Alopecia | tamoxifen | PT | C0002170 |
| Alopecia | tamoxifen | LLT | C0002170 |
| Alopecia | tamoxifen | PT | C0002170 |
| Amenorrhoea | tamoxifen | LLT | C0002453 |
| Amenorrhoea | tamoxifen | PT | C0002453 |
| Anaemia | tamoxifen | LLT | C0002871 |
| Anaemia | tamoxifen | PT | C0002871 |
| Angina pectoris | tamoxifen | LLT | C0002962 |
| Angina pectoris | tamoxifen | PT | C0002962 |
| Angioedema | tamoxifen | LLT | C0002994 |
| Angioedema | tamoxifen | PT | C0002994 |
| Angioedema | tamoxifen | LLT | C0002994 |
| Angioedema | tamoxifen | PT | C0002994 |
| Ankle edema | tamoxifen | LLT | C0235439 |
| Anorexia | tamoxifen | LLT | C0003123 |
| Anxiety | tamoxifen | LLT | C0003467 |
| Anxiety | tamoxifen | PT | C0003467 |
| Appetite absent | tamoxifen | LLT | C1971624 |
| Arrhythmia | tamoxifen | LLT | C0003811 |
| Arrhythmia | tamoxifen | PT | C0003811 |
| Arthralgia | tamoxifen | LLT | C0003862 |
| Arthralgia | tamoxifen | PT | C0003862 |
| Arthritis | tamoxifen | LLT | C0003864 |
| Arthritis | tamoxifen | PT | C0003864 |
| Arthropathy | tamoxifen | LLT | C0022408 |
| Arthropathy | tamoxifen | PT | C0022408 |
| Aspartate aminotransferase increased | tamoxifen | LLT | C0151904 |
| Aspartate aminotransferase increased | tamoxifen | PT | C0151904 |
| Asthenia | tamoxifen | LLT | C0004093 |
| Asthenia | tamoxifen | PT | C0004093 |
| Asthenia | tamoxifen | PT | C0004093 |
| Back pain | tamoxifen | LLT | C0004604 |
| Back pain | tamoxifen | PT | C0004604 |
| Benign neoplasm | tamoxifen | LLT | C0086692 |
| Benign neoplasm | tamoxifen | PT | C0086692 |
| Blindness | tamoxifen | LLT | C0456909 |
| Blindness | tamoxifen | PT | C0456909 |
| Blindness | tamoxifen | LLT | C0456909 |
| Blindness | tamoxifen | PT | C0456909 |
| Blister | tamoxifen | LLT | C0005758 |
| Blister | tamoxifen | PT | C0005758 |
| Blood bilirubin increased | tamoxifen | LLT | C0311468 |
| Blood bilirubin increased | tamoxifen | PT | C0311468 |
| Blood creatinine increased | tamoxifen | PT | C0235431 |
| Blood triglycerides increased | tamoxifen | PT | C0853692 |
| Bone pain | tamoxifen | LLT | C0151825 |
| Bone pain | tamoxifen | PT | C0151825 |
| Breast cancer male | tamoxifen | LLT | C0238033 |
| Breast cancer male | tamoxifen | PT | C0238033 |
| Breast feeding | tamoxifen | LLT | C0006147 |
| Breast feeding | tamoxifen | PT | C0006147 |
| Breast neoplasm | tamoxifen | LLT | C1458155 |
| Breast neoplasm | tamoxifen | PT | C1458155 |
| Breast pain | tamoxifen | LLT | C0024902 |
| Breast pain | tamoxifen | PT | C0024902 |
| Bronchitis | tamoxifen | LLT | C0006277 |
| Bronchitis | tamoxifen | PT | C0006277 |
| Cardiovascular disorder | tamoxifen | LLT | C0007222 |
| Cardiovascular disorder | tamoxifen | PT | C0007222 |
| Cataract | tamoxifen | LLT | C0086543 |
| Cataract | tamoxifen | PT | C0086543 |
| Cataract | tamoxifen | PT | C0086543 |
| Cataract specified | tamoxifen | LLT | C0151547 |
| Chest pain | tamoxifen | LLT | C0008031 |
| Chest pain | tamoxifen | PT | C0008031 |
| Cholestasis | tamoxifen | LLT | C0008370 |
Frequently Asked Questions
Short answers generated only from the same visible source-linked rows on this page.
What is Tamoxifen used for in pharmaceutical contexts?
Tamoxifen (CAS 10540-29-1) is rendered as a pharmaceutical compound from the matched source rows; no DailyMed product-name rows are present in this page query.
What are the known adverse events for Tamoxifen?
Tamoxifen has 1,598 DrugCentral/FAERS adverse event associations. Rendered reaction terms include Metastases to bone, Malignant neoplasm progression, Metastases to liver, Metastases to lung, Breast cancer recurrent. Signal rows are source-linked records and should not be read as incidence rates or causality conclusions.
Is Tamoxifen also used in cosmetics?
No same-CAS cosmetics profile is rendered from the ingredients-table cross-reference for Tamoxifen.
What clinical phase is Tamoxifen in?
Tamoxifen is rendered with ChEMBL max phase 4 (approved).
What bioactivity targets are documented for Tamoxifen?
Tamoxifen has 77 bioactivity rows in this page query. Rendered target entries include Adenosine receptor A1, Sodium/potassium-transporting ATPase subunit alpha-2, Beta-1 adrenergic receptor, Prostaglandin G/H synthase 2, Prostaglandin G/H synthase 1.