Compound Detail
CHEMBL1473
FLUTICASONE PROPIONATE 💊 Approved Drug
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💊 Approved Drug
CCC(=O)O[C@]1(C(=O)SCF)[C@H](C)C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@@]21C
Basic Information
| ChEMBL ID | CHEMBL1473 |
| Name | FLUTICASONE PROPIONATE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | WMWTYOKRWGGJOA-CENSZEJFSA-N |
| Therapeutic | ✓ Yes |
7
Targets
15
Activities
2
Assay Types
23
PK Parameters
20
Publications
30
Known Names
20
Indications
1
Mechanisms
Molecular Properties
500.6
MW (Da)
4.43
ALogP
6
HBA
1
HBD
80.7
PSA (Ų)
0.58
QED
1
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1990 |
| Availability | OTC |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Glucocorticoid receptor agonist | AGONIST | Glucocorticoid receptor | ✓ | ✓ |
Indications
Asthma Bronchitis, Chronic Dermatitis, Atopic Emphysema Lung Diseases, Obstructive Nasal Obstruction Nasal Polyps Nasal Polyps Pulmonary Disease, Chronic Obstructive Rhinitis, Allergic, Seasonal Rhinitis, Allergic, Seasonal Skin Diseases Bronchiolitis Obliterans Chronic Disease Eosinophilic Esophagitis Respiratory Sounds Rhinitis, Allergic, Perennial Sinusitis Adenomatous Polyposis Coli Blepharitis
ATC Classification
D07AC17
fluticasone
Level 1: DERMATOLOGICALS
Level 2: CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
R01AD08
fluticasone
Level 1: RESPIRATORY SYSTEM
Level 2: NASAL PREPARATIONS
R01AD58
fluticasone, combinations
Level 1: RESPIRATORY SYSTEM
Level 2: NASAL PREPARATIONS
R03BA05
fluticasone
Level 1: RESPIRATORY SYSTEM
Level 2: DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
Activity Summary
IC50 12 meas. best 10.4
EC50 3 meas. best 9.15
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Glucocorticoid receptor CHEMBL2034 | IC50 | 10.4 | 9.846 | 0.0 | 5 |
| PBMC CHEMBL613107 | IC50 | 10.0 | 10.0 | 0.1 | 1 |
| Glucocorticoid receptor CHEMBL3368 | IC50 | 9.85 | 9.075 | 0.1 | 2 |
| Unchecked CHEMBL612545 | IC50 | 9.82 | 9.82 | 0.1 | 1 |
| Glucocorticoid receptor CHEMBL2034 | EC50 | 9.15 | 9.055 | 0.7 | 2 |
| Glucocorticoid receptor CHEMBL3368 | EC50 | 9.12 | 9.12 | 0.8 | 1 |
| Blood CHEMBL613416 | IC50 | 8.03 | 8.03 | 9.3 | 1 |
| Progesterone receptor CHEMBL208 | IC50 | 7.68 | 7.68 | 21.0 | 1 |
| Mineralocorticoid receptor CHEMBL1994 | IC50 | 6.83 | 6.83 | 149.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 100116.0 | ng.hr.mL-1 | Rattus norvegicus |
| CL | 17.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 51.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 300.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 56000.0 | mL.min-1.g-1 | Rattus norvegicus |
| CL | 1800000.0 | mL.min-1.g-1 | Rattus norvegicus |
| CL | 107.15 | uL.min-1.(10^6cells)-1 | Rattus norvegicus |
| CL | 150.0 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 103.0 | mL.min-1.kg-1 | Rattus norvegicus |
| Cmax | 24.0 | nM | Rattus norvegicus |
| F | 2.0 | % | Rattus norvegicus |
| F | 0.1 | % | Rattus norvegicus |
| Fu | 0.1 | - | Homo sapiens |
| MRT | 3.9 | hr | Homo sapiens |
| MRT | 6.0 | hr | Rattus norvegicus |
| T1/2 | 6.0 | hr | Homo sapiens |
| T1/2 | 1.1 | hr | Rattus norvegicus |
| T1/2 | 9.067 | hr | Homo sapiens |
| T1/2 | 0.01433 | hr | Homo sapiens |
| T1/2 | 0.2667 | hr | Homo sapiens |
| T1/2 | 0.9667 | hr | Homo sapiens |
| T1/2 | 3.3 | hr | Rattus norvegicus |
| T1/2 | 4.5 | hr | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine