Compound Detail
CHEMBL1256391
PIRFENIDONE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1256391 |
| Name | PIRFENIDONE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | ISWRGOKTTBVCFA-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
2
Targets
8
Activities
1
Assay Types
20
PK Parameters
20
Publications
9
Known Names
20
Indications
1
Mechanisms
Molecular Properties
185.2
MW (Da)
2.15
ALogP
2
HBA
0
HBD
22.0
PSA (Ų)
0.67
QED
0
Ro5 Violations
1
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2011 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Unknown | - | - | ✓ | ✓ |
Indications
Idiopathic Pulmonary Fibrosis Immune System Diseases Lung Diseases Respiratory Tract Diseases Diabetic Foot Keloid Pneumoconiosis Pneumonia Respiratory Distress Syndrome Severe Acute Respiratory Syndrome Acute Lung Injury Alveolitis, Extrinsic Allergic Bronchiolitis Obliterans Burns Carcinoma, Squamous Cell Cardiomyopathy, Hypertrophic Glomerulosclerosis, Focal Segmental Heart Failure Leiomyoma Lung Diseases, Interstitial
ATC Classification
L04AX05
pirfenidone
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: IMMUNOSUPPRESSANTS
Activity Summary
IC50 8 meas. best 6.15
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| HFL1 CHEMBL612547 | IC50 | 6.15 | 6.15 | 710.0 | 1 |
| Transforming growth factor beta-1 proprotein/Mothers against decapentaplegic homolog 3 CHEMBL4296078 | IC50 | 5.84 | 5.84 | 1430.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 2722.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 649.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 650.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 3463.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 3464.0 | ng.hr.mL-1 | Rattus norvegicus |
| CL | 1231.17 | mL.min-1.kg-1 | Homo sapiens |
| CL | 1732.1 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 53.33 | mL.min-1.kg-1 | Rattus norvegicus |
| Cmax | 5506.67 | nM | Rattus norvegicus |
| Cmax | 5436.48 | nM | Rattus norvegicus |
| Cmax | 27387.57 | nM | Rattus norvegicus |
| F | 107.0 | % | Rattus norvegicus |
| T1/2 | 3.0 | hr | Homo sapiens |
| T1/2 | 1.9 | hr | Rattus norvegicus |
| T1/2 | 1.9 | hr | Rattus norvegicus |
| T1/2 | 0.096 | hr | Homo sapiens |
| T1/2 | 0.02433 | hr | Rattus norvegicus |
| T1/2 | 0.4 | hr | Rattus norvegicus |
| T1/2 | 0.4 | hr | Rattus norvegicus |
| Tmax | 0.3 | hr | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| HFL1 | IC50 | = | 710.0 | nM | 6.15 | Antifibrotic activity in HFL1 cells assessed as inhibition of cell viability aft... | 26896707 |
| Transforming growth factor beta-1 proprotein/Mothers against decapentaplegic homolog 3 | IC50 | = | 1430.0 | nM | 5.84 | Inhibition of TGF beta1/Smad3 signaling in mouse NIH/3T3 cells harboring CAGA pr... | 31606345 |
Literature References
Data from ChEMBL 36 via Core Engine