Compound Detail
CHEMBL103
PROGESTERONE 💊 Approved Drug
Enter ChEMBL ID:
Free Research Context
This compound will appear in recent viewed items on the research home for this browser.
Research home
View demo workspace
💊 Approved Drug
CC(=O)[C@H]1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C
Basic Information
| ChEMBL ID | CHEMBL103 |
| Name | PROGESTERONE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | RJKFOVLPORLFTN-LEKSSAKUSA-N |
| Therapeutic | ✓ Yes |
34
Targets
131
Activities
4
Assay Types
5
PK Parameters
20
Publications
22
Known Names
20
Indications
1
Mechanisms
Molecular Properties
314.5
MW (Da)
4.72
ALogP
2
HBA
0
HBD
34.1
PSA (Ų)
0.70
QED
0
Ro5 Violations
1
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1976 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Progesterone receptor agonist | AGONIST | Progesterone receptor | ✓ | ✓ |
Indications
Amenorrhea Endometrial Hyperplasia Uterine Hemorrhage Alzheimer Disease Angina, Unstable Bone Diseases Bone Diseases, Metabolic Brain Injuries Breast Neoplasms Breast Neoplasms Breast Neoplasms Cardiovascular Diseases Coronary Disease Diabetes Mellitus Epilepsy Hypercholesterolemia Hypertension Infertility Infertility, Female Leiomyoma
ATC Classification
G03DA04
progesterone
Level 1: GENITO URINARY SYSTEM AND SEX HORMONES
Level 2: SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
Drug Warnings
Black Box Warning
cardiotoxicity
Black Box Warning
vascular toxicity
Black Box Warning
neurotoxicity
Black Box Warning
respiratory toxicity
Black Box Warning
carcinogenicity
Activity Summary
IC50 54 meas. best 9.7
Ki 42 meas. best 8.47
EC50 30 meas. best 10.0
Kd 5 meas. best 9.41
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Progesterone receptor CHEMBL208 | EC50 | 10.0 | 8.6817 | 0.1 | 24 |
| Progesterone receptor CHEMBL208 | IC50 | 9.7 | 8.5575 | 0.2 | 4 |
| Mineralocorticoid receptor CHEMBL1994 | Kd | 9.41 | 9.41 | 0.4 | 1 |
| Unchecked CHEMBL612545 | IC50 | 8.47 | 5.9267 | 3.4 | 3 |
| Progesterone receptor CHEMBL208 | Ki | 8.47 | 8.4446 | 3.4 | 13 |
| Progesterone receptor CHEMBL1909044 | Ki | 8.44 | 8.44 | 3.6 | 1 |
| Estrogen receptor CHEMBL2094114 | Kd | 8.41 | 8.41 | 3.9 | 1 |
| Progesterone receptor CHEMBL3456 | IC50 | 8.22 | 8.22 | 6.0 | 2 |
| Androgen receptor CHEMBL1871 | Ki | 8.07 | 7.9829 | 8.5 | 7 |
| Progesterone receptor CHEMBL3456 | Ki | 7.98 | 7.98 | 10.4 | 1 |
| Androgen receptor CHEMBL1871 | IC50 | 7.86 | 7.5017 | 13.7 | 6 |
| Mineralocorticoid receptor CHEMBL1994 | IC50 | 7.85 | 7.784 | 14.0 | 5 |
| Fatty acid-binding protein, liver CHEMBL5738 | Ki | 7.57 | 7.57 | 27.0 | 1 |
| Progesterone receptor CHEMBL1909044 | IC50 | 7.55 | 7.55 | 28.0 | 1 |
| Glucocorticoid receptor CHEMBL2034 | Ki | 7.52 | 7.42 | 30.5 | 7 |
| Androgen receptor CHEMBL3056 | IC50 | 7.43 | 7.43 | 37.0 | 1 |
| Corticosteroid-binding globulin CHEMBL2421 | Ki | 7.38 | 7.38 | 41.7 | 1 |
| Sex hormone-binding globulin CHEMBL3305 | Kd | 6.94 | 6.94 | 114.8 | 1 |
| Androgen receptor CHEMBL3072 | Ki | 6.84 | 6.84 | 143.0 | 1 |
| Androgen receptor CHEMBL3072 | IC50 | 6.67 | 6.24 | 214.0 | 2 |
| Sigma non-opioid intracellular receptor 1 CHEMBL3602 | Kd | 6.62 | 6.62 | 239.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | Ki | 6.58 | 6.235 | 260.0 | 2 |
| Glucocorticoid receptor CHEMBL2034 | IC50 | 6.48 | 6.48 | 330.0 | 1 |
| Unchecked CHEMBL612545 | Kd | 6.36 | 6.36 | 441.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL4153 | Ki | 6.18 | 6.18 | 660.0 | 2 |
| Solute carrier family 22 member 2 CHEMBL1770032 | IC50 | 5.8 | 5.8 | 1600.0 | 1 |
| P2X purinoceptor 3 CHEMBL2998 | IC50 | 5.8 | 5.8 | 1600.0 | 1 |
| Steroid 5-alpha-reductase CHEMBL2096664 | IC50 | 5.8 | 5.69 | 1600.0 | 2 |
| G-protein coupled bile acid receptor 1 CHEMBL5409 | EC50 | 5.56 | 5.56 | 2770.0 | 1 |
| Solute carrier family 22 member 1 CHEMBL5685 | IC50 | 5.52 | 5.52 | 3050.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | IC50 | 5.51 | 5.51 | 3055.0 | 1 |
| Solute carrier family 22 member 3 CHEMBL2073673 | IC50 | 5.37 | 5.37 | 4280.0 | 1 |
| C-8 sterol isomerase ERG2 CHEMBL3224 | Ki | 5.35 | 5.35 | 4430.0 | 1 |
| Cytochrome P450 2C9 CHEMBL3397 | Ki | 5.26 | 5.26 | 5500.0 | 1 |
| Plasmodium falciparum CHEMBL364 | IC50 | 5.2 | 4.9457 | 6309.6 | 7 |
| Unchecked CHEMBL612545 | Ki | 5.17 | 4.91 | 6703.0 | 2 |
| Solute carrier family 22 member 3 CHEMBL1770033 | IC50 | 4.98 | 4.98 | 10500.0 | 1 |
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 4.97 | 4.6567 | 10600.0 | 3 |
| Sterol O-acyltransferase 1 CHEMBL2782 | IC50 | 4.77 | 4.77 | 17000.0 | 1 |
| Bile salt export pump CHEMBL6020 | IC50 | 4.76 | 4.76 | 17300.0 | 1 |
| Breast cancer cell line CHEMBL614788 | EC50 | 4.73 | 4.69 | 18700.0 | 2 |
| Fatty acid-binding protein, intestinal CHEMBL4879 | Ki | 4.7 | 4.7 | 20000.0 | 1 |
| Unchecked CHEMBL612545 | EC50 | 4.68 | 4.53 | 21000.0 | 2 |
| ATP-dependent translocase ABCB1 CHEMBL4302 | EC50 | 4.67 | 4.67 | 21200.0 | 1 |
| Solute carrier family 22 member 2 CHEMBL1743122 | IC50 | 4.57 | 4.57 | 26700.0 | 1 |
| Monoclonal antibody (mAb) CHEMBL613294 | Ki | 4.44 | 4.44 | 36000.0 | 1 |
| ATP-dependent translocase ABCB1 CHEMBL4302 | IC50 | 4.32 | 4.204 | 47863.0 | 5 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| Cmax | 193.0 | nM | Homo sapiens |
| F | 20.0 | % | Homo sapiens |
| Fu | 0.67 | - | Homo sapiens |
| T1/2 | 240.0 | hr | - |
| T1/2 | 0.4167 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine