Compound Detail
CHEMBL1370
BUDESONIDE 💊 Approved Drug
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💊 Approved Drug
CCCC1O[C@@H]2C[C@H]3[C@@H]4CCC5=CC(=O)C=C[C@]5(C)[C@H]4[C@@H](O)C[C@]3(C)[C@]2(C(=O)CO)O1
Basic Information
| ChEMBL ID | CHEMBL1370 |
| Name | BUDESONIDE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | VOVIALXJUBGFJZ-KWVAZRHASA-N |
| Therapeutic | ✓ Yes |
20
Targets
49
Activities
3
Assay Types
23
PK Parameters
20
Publications
30
Known Names
20
Indications
1
Mechanisms
Molecular Properties
430.5
MW (Da)
2.72
ALogP
6
HBA
2
HBD
93.1
PSA (Ų)
0.71
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1994 |
| Availability | OTC |
| Chirality | Racemic |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Glucocorticoid receptor agonist | AGONIST | Glucocorticoid receptor | ✓ | ✓ |
Indications
Asthma Bronchitis, Chronic Colitis, Ulcerative Crohn Disease Emphysema Esophageal Diseases Glomerulonephritis, IGA Lung Diseases, Obstructive Nasal Obstruction Pulmonary Disease, Chronic Obstructive Rhinitis, Allergic, Perennial Rhinitis, Allergic, Seasonal Rhinitis, Allergic, Seasonal Altitude Sickness Bronchiolitis Obliterans Syndrome Bronchopulmonary Dysplasia Colitis, Collagenous Colitis, Lymphocytic Colitis, Microscopic Eosinophilic Esophagitis
ATC Classification
A07EA06
budesonide
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
D07AC09
budesonide
Level 1: DERMATOLOGICALS
Level 2: CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
R01AD05
budesonide
Level 1: RESPIRATORY SYSTEM
Level 2: NASAL PREPARATIONS
R03BA02
budesonide
Level 1: RESPIRATORY SYSTEM
Level 2: DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
Drug Warnings
Black Box Warning
infectious disease
Activity Summary
IC50 40 meas. best 9.92
EC50 5 meas. best 8.7
Ki 4 meas. best 8.89
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| ADMET CHEMBL612558 | IC50 | 9.92 | 9.705 | 0.1 | 2 |
| Glucocorticoid receptor CHEMBL2034 | IC50 | 9.3 | 8.784 | 0.5 | 5 |
| RAW264.7 CHEMBL612557 | IC50 | 9.09 | 9.09 | 0.8 | 1 |
| Unchecked CHEMBL612545 | IC50 | 9.05 | 6.81 | 0.9 | 2 |
| PBMC CHEMBL613107 | IC50 | 9.02 | 9.02 | 1.0 | 1 |
| Glucocorticoid receptor CHEMBL2034 | Ki | 8.89 | 8.79 | 1.3 | 2 |
| Glucocorticoid receptor CHEMBL2034 | EC50 | 8.7 | 8.4425 | 2.0 | 4 |
| Glucocorticoid receptor CHEMBL3368 | IC50 | 8.54 | 8.54 | 2.9 | 1 |
| Mineralocorticoid receptor CHEMBL1994 | EC50 | 8.32 | 8.32 | 4.8 | 1 |
| Blood CHEMBL613416 | IC50 | 8.07 | 8.07 | 8.5 | 1 |
| Mineralocorticoid receptor CHEMBL1994 | IC50 | 7.85 | 7.85 | 14.0 | 1 |
| Progesterone receptor CHEMBL1909044 | Ki | 7.57 | 7.57 | 27.0 | 1 |
| Progesterone receptor CHEMBL208 | IC50 | 7.55 | 7.55 | 28.0 | 1 |
| Progesterone receptor CHEMBL1909044 | IC50 | 6.68 | 6.68 | 210.0 | 1 |
| Androgen receptor CHEMBL3072 | IC50 | 6.15 | 5.97 | 710.0 | 2 |
| Androgen receptor CHEMBL3072 | Ki | 5.96 | 5.96 | 1090.0 | 1 |
| Plasmodium falciparum CHEMBL364 | IC50 | 5.8 | 5.4429 | 1584.9 | 7 |
| Matrix metalloproteinase-9 CHEMBL321 | IC50 | 5.7 | 5.7 | 1989.0 | 1 |
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 4.58 | 4.58 | 26200.0 | 1 |
| Interleukin-5 receptor subunit alpha CHEMBL4523198 | IC50 | 4.58 | 4.58 | 26200.0 | 1 |
| Interleukin-5 CHEMBL1163111 | IC50 | 4.58 | 4.5763 | 26200.0 | 8 |
| Interleukin-5 CHEMBL1169600 | IC50 | 4.57 | 4.57 | 26800.0 | 1 |
| ATP-binding cassette sub-family C member 4 CHEMBL1743128 | IC50 | 4.43 | 4.43 | 37000.0 | 1 |
| Bile salt export pump CHEMBL6020 | IC50 | 4.34 | 4.34 | 46000.0 | 1 |
| ATP-binding cassette sub-family C member 3 CHEMBL5918 | IC50 | 4.26 | 4.26 | 54500.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 12.92 | ng.hr.mL-1 | Homo sapiens |
| AUC | 6.501 | ng.hr.mL-1 | Homo sapiens |
| AUClast | 11.6 | hr.nmol/ml | Rattus norvegicus |
| AUClast | 110.03 | hr.nmol/g | Rattus norvegicus |
| CL | 20.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 19.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 20.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 20.0 | mL.min-1.kg-1 | Homo sapiens |
| Cmax | 5.0 | nM | Homo sapiens |
| Cmax | 127.0 | nM | Rattus norvegicus |
| Cmax | 18.67 | nmol/g | Rattus norvegicus |
| F | 11.0 | % | Homo sapiens |
| Fu | 0.13 | - | Homo sapiens |
| Fu | 0.13 | - | Homo sapiens |
| MRT | 3.2 | hr | Homo sapiens |
| PPB | 85.0 | % | Homo sapiens |
| T1/2 | 2.8 | hr | Homo sapiens |
| T1/2 | 0.1833 | hr | Homo sapiens |
| T1/2 | 0.6667 | hr | Homo sapiens |
| T1/2 | 1.183 | hr | Homo sapiens |
| Tmax | 0.5 | hr | Homo sapiens |
| Vd | 2.2 | L.kg-1 | Homo sapiens |
| Vd | 2.2 | L.kg-1 | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine