Compound Detail
CHEMBL1201139
MEGESTROL ACETATE 💊 Approved Drug
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💊 Approved Drug
CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C=C(C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C
Basic Information
| ChEMBL ID | CHEMBL1201139 |
| Name | MEGESTROL ACETATE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | RQZAXGRLVPAYTJ-GQFGMJRRSA-N |
| Therapeutic | ✓ Yes |
5
Targets
8
Activities
2
Assay Types
1
PK Parameters
20
Publications
13
Known Names
20
Indications
1
Mechanisms
Molecular Properties
384.5
MW (Da)
4.58
ALogP
4
HBA
0
HBD
60.4
PSA (Ų)
0.65
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1971 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Progesterone receptor agonist | AGONIST | Progesterone receptor | ✓ | ✓ |
Indications
Acquired Immunodeficiency Syndrome Anorexia Cachexia Neoplasms Neoplasms Primary Immunodeficiency Diseases Breast Neoplasms Breast Neoplasms Endometrial Neoplasms Endometrial Neoplasms Endometrial Neoplasms Endometrial Neoplasms Hot Flashes Liver Neoplasms Adrenal Cortex Neoplasms Carcinoma in Situ Dementia Head and Neck Neoplasms HIV Wasting Syndrome Pulmonary Disease, Chronic Obstructive
ATC Classification
G03AC05
megestrol
Level 1: GENITO URINARY SYSTEM AND SEX HORMONES
Level 2: SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
G03DB02
megestrol
Level 1: GENITO URINARY SYSTEM AND SEX HORMONES
Level 2: SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
L02AB01
megestrol
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ENDOCRINE THERAPY
Activity Summary
IC50 5 meas. best 7.96
Ki 3 meas. best 8.84
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Progesterone receptor CHEMBL1909044 | Ki | 8.84 | 8.84 | 1.4 | 1 |
| Glucocorticoid receptor CHEMBL2034 | Ki | 8.06 | 8.06 | 8.8 | 1 |
| Progesterone receptor CHEMBL1909044 | IC50 | 7.96 | 7.96 | 11.0 | 1 |
| Glucocorticoid receptor CHEMBL2034 | IC50 | 7.72 | 7.72 | 19.0 | 1 |
| Androgen receptor CHEMBL3072 | Ki | 7.7 | 7.7 | 20.0 | 1 |
| Androgen receptor CHEMBL3072 | IC50 | 7.52 | 7.52 | 30.0 | 1 |
| Cytochrome P450 2C9 CHEMBL3397 | IC50 | 5.0 | 5.0 | 10000.0 | 1 |
| Bile salt export pump CHEMBL6020 | IC50 | 4.75 | 4.75 | 17800.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 13785.04 | ng.hr.mL-1 | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine