Compound Detail
CHEMBL717
MEDROXYPROGESTERONE 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@H](C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C
Basic Information
| ChEMBL ID | CHEMBL717 |
| Name | MEDROXYPROGESTERONE ACETATE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | PSGAAPLEWMOORI-PEINSRQWSA-N |
| Therapeutic | ✓ Yes |
20
Targets
82
Activities
4
Assay Types
1
PK Parameters
20
Publications
30
Known Names
20
Indications
1
Mechanisms
Molecular Properties
386.5
MW (Da)
4.66
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 | 1959 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Progesterone receptor agonist | AGONIST | Progesterone receptor | ✓ | ✓ |
Indications
Carcinoma, Renal Cell Carcinoma, Renal Cell Endometriosis Hyperplasia Neoplasms Uterine Hemorrhage Bone Diseases Cardiovascular Diseases Coronary Disease Diabetes Mellitus Endometrial Neoplasms Endometrial Neoplasms Heart Diseases Hot Flashes Hypercholesterolemia Hypertension Infertility Kidney Neoplasms Lupus Erythematosus, Systemic Menopause
ATC Classification
G03AC06
medroxyprogesterone
Level 1: GENITO URINARY SYSTEM AND SEX HORMONES
Level 2: SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
G03DA02
medroxyprogesterone
Level 1: GENITO URINARY SYSTEM AND SEX HORMONES
Level 2: SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
L02AB02
medroxyprogesterone
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ENDOCRINE THERAPY
Drug Warnings
Black Box Warning
neurotoxicity
Black Box Warning
vascular toxicity
Black Box Warning
cardiotoxicity
Black Box Warning
musculoskeletal toxicity
Black Box Warning
carcinogenicity
Black Box Warning
respiratory toxicity
Activity Summary
IC50 34 meas. best 8.65
Ki 24 meas. best 9.53
EC50 22 meas. best 10.0
Kd 2 meas. best 9.0
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Progesterone receptor CHEMBL208 | EC50 | 10.0 | 9.668 | 0.1 | 15 |
| Progesterone receptor CHEMBL1909044 | Ki | 9.53 | 9.53 | 0.3 | 1 |
| Progesterone receptor CHEMBL208 | Ki | 9.47 | 9.3925 | 0.3 | 8 |
| Androgen receptor CHEMBL1871 | Kd | 9.0 | 9.0 | 1.0 | 1 |
| Progesterone receptor CHEMBL1909044 | IC50 | 8.65 | 8.65 | 2.2 | 1 |
| Androgen receptor CHEMBL1871 | Ki | 8.54 | 8.54 | 2.9 | 5 |
| Androgen receptor CHEMBL3072 | Ki | 8.31 | 8.31 | 4.8 | 1 |
| Androgen receptor CHEMBL1871 | EC50 | 8.21 | 8.21 | 6.1 | 1 |
| Androgen receptor CHEMBL1871 | IC50 | 8.21 | 8.21 | 6.1 | 2 |
| Androgen receptor CHEMBL3056 | EC50 | 8.21 | 8.21 | 6.1 | 2 |
| Androgen receptor CHEMBL3072 | IC50 | 8.14 | 7.23 | 7.3 | 3 |
| Glucocorticoid receptor CHEMBL2034 | Ki | 8.06 | 7.91 | 8.6 | 6 |
| Glucocorticoid receptor CHEMBL2034 | EC50 | 8.0 | 8.0 | 10.0 | 3 |
| Glucocorticoid receptor CHEMBL2034 | IC50 | 8.0 | 7.9067 | 10.0 | 3 |
| Progesterone receptor CHEMBL208 | IC50 | 7.97 | 7.97 | 10.8 | 3 |
| Aldo-keto reductase family 1 member C3 CHEMBL4681 | IC50 | 6.55 | 6.2233 | 280.0 | 3 |
| Sex hormone-binding globulin CHEMBL3305 | Kd | 6.2 | 6.2 | 631.0 | 1 |
| Aldo-keto reductase family 1 member C1 CHEMBL5905 | IC50 | 6.16 | 5.955 | 700.0 | 2 |
| Estrogen receptor CHEMBL2093866 | EC50 | 6.03 | 6.03 | 924.0 | 1 |
| Estrogen receptor CHEMBL2093866 | IC50 | 6.03 | 6.03 | 924.0 | 2 |
| Mineralocorticoid receptor CHEMBL1994 | IC50 | 5.92 | 5.92 | 1197.0 | 3 |
| Aldo-keto reductase family 1 member C2 CHEMBL5847 | IC50 | 5.8 | 5.53 | 1600.0 | 3 |
| Unchecked CHEMBL612545 | Ki | 5.2 | 5.035 | 6305.0 | 2 |
| Unchecked CHEMBL612545 | IC50 | 5.11 | 4.97 | 7738.0 | 2 |
| Bile salt export pump CHEMBL6020 | IC50 | 4.8 | 4.8 | 15700.0 | 1 |
| ATP-binding cassette sub-family C member 4 CHEMBL1743128 | IC50 | 4.65 | 4.65 | 22500.0 | 1 |
| Histamine H2 receptor CHEMBL1941 | Ki | 4.56 | 4.56 | 27453.0 | 1 |
| Histamine H2 receptor CHEMBL1941 | IC50 | 4.55 | 4.55 | 27920.0 | 1 |
| AN3-CA CHEMBL1075392 | IC50 | 4.43 | 4.43 | 37100.0 | 1 |
| Ishikawa CHEMBL614649 | IC50 | 4.43 | 4.43 | 37000.0 | 1 |
| HEC-1-A CHEMBL4296424 | IC50 | 4.29 | 4.29 | 51800.0 | 1 |
| HEC-1B cell line CHEMBL614817 | IC50 | 4.22 | 4.22 | 60400.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 6.184 | ng.hr.mL-1 | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine