Compound Detail
CHEMBL1504
TRIAMCINOLONE ACETONIDE 💊 Approved Drug
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💊 Approved Drug
CC1(C)O[C@@H]2C[C@H]3[C@@H]4CCC5=CC(=O)C=C[C@]5(C)[C@@]4(F)[C@@H](O)C[C@]3(C)[C@]2(C(=O)CO)O1
Basic Information
| ChEMBL ID | CHEMBL1504 |
| Name | TRIAMCINOLONE ACETONIDE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | YNDXUCZADRHECN-JNQJZLCISA-N |
| Therapeutic | ✓ Yes |
3
Targets
5
Activities
2
Assay Types
18
PK Parameters
20
Publications
30
Known Names
20
Indications
1
Mechanisms
Molecular Properties
434.5
MW (Da)
2.42
ALogP
6
HBA
2
HBD
93.1
PSA (Ų)
0.69
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1960 |
| Availability | OTC |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Glucocorticoid receptor agonist | AGONIST | Glucocorticoid receptor | ✓ | ✓ |
Indications
Anemia Arthritis, Gouty Arthritis, Rheumatoid Asthma Bursitis Bursitis Dermatitis Multiple Sclerosis Mycoses Nasal Obstruction Osteoarthritis Pain Rhinitis, Allergic, Seasonal Rhinitis, Allergic, Seasonal Serum Sickness Skin Diseases Tennis Elbow Tennis Elbow Tenosynovitis Tuberculosis, Pulmonary
Activity Summary
IC50 3 meas. best 8.36
Ki 2 meas. best 8.7
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Glucocorticoid receptor CHEMBL2034 | Ki | 8.7 | 8.7 | 2.0 | 1 |
| Glucocorticoid receptor CHEMBL2034 | IC50 | 8.36 | 8.36 | 4.4 | 1 |
| Progesterone receptor CHEMBL1909044 | Ki | 7.64 | 7.64 | 23.0 | 1 |
| Progesterone receptor CHEMBL1909044 | IC50 | 6.75 | 6.75 | 179.0 | 1 |
| NIH3T3 CHEMBL614822 | IC50 | 5.6 | 5.6 | 2500.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 1.4 | ng.hr.mL-1 | Homo sapiens |
| AUC | 1.4 | ng.hr.mL-1 | Homo sapiens |
| CL | 9.4 | mL.min-1.kg-1 | Homo sapiens |
| CL | 45.2 | L/hr | Homo sapiens |
| Cmax | 1.151 | nM | Homo sapiens |
| Cmax | 1.151 | nM | Homo sapiens |
| Fu | 0.2 | - | Homo sapiens |
| MRT | 2.5 | hr | Homo sapiens |
| T1/2 | 2.4 | hr | Homo sapiens |
| T1/2 | 0.2 | hr | Homo sapiens |
| T1/2 | 2.167 | hr | Homo sapiens |
| T1/2 | 3.55 | hr | Homo sapiens |
| T1/2 | 3.1 | hr | Homo sapiens |
| T1/2 | 3.1 | hr | Homo sapiens |
| T1/2 | 1.467 | hr | Homo sapiens |
| Tmax | 1.5 | hr | Homo sapiens |
| Tmax | 1.5 | hr | Homo sapiens |
| Vd | 99.5 | L | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Glucocorticoid receptor | Ki | = | 2.006 | nM | 8.7 | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | - |
| Glucocorticoid receptor | IC50 | = | 4.414 | nM | 8.36 | DRUGMATRIX: Glucocorticoid radioligand binding (ligand: [3H] Dexamethasone) | - |
| Progesterone receptor | Ki | = | 23.0 | nM | 7.64 | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | - |
| Progesterone receptor | IC50 | = | 179.0 | nM | 6.75 | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | - |
| NIH3T3 | IC50 | = | 2500.0 | nM | 5.6 | Inhibition of NIH 3T3 cell growth required to induce 50% of maximum response usi... | 11855992 |
Literature References
Data from ChEMBL 36 via Core Engine