Compound Detail
CHEMBL2220442
FLUVASTATIN 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL2220442 |
| Name | FLUVASTATIN |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | FJLGEFLZQAZZCD-VAWYXSNFSA-N |
| Therapeutic | ✓ Yes |
11
Targets
16
Activities
3
Assay Types
23
PK Parameters
20
Publications
5
Known Names
12
Indications
Molecular Properties
411.5
MW (Da)
4.63
ALogP
4
HBA
3
HBD
82.7
PSA (Ų)
0.50
QED
0
Ro5 Violations
8
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1993 |
| Availability | Prescription |
| Chirality | Racemic |
Indications
Cardiovascular Diseases Erectile Dysfunction Hypercholesterolemia Lipid Metabolism Disorders Aortic Valve Stenosis Hepatitis C Hepatitis C, Chronic Nephritis, Hereditary Polyendocrinopathies, Autoimmune Prostatic Neoplasms, Castration-Resistant Paraganglioma Melanoma
ATC Classification
C10AA04
fluvastatin
Level 1: CARDIOVASCULAR SYSTEM
Level 2: LIPID MODIFYING AGENTS
Activity Summary
IC50 10 meas. best 9.45
EC50 5 meas. best 5.74
Kd 1 meas. best 4.96
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase CHEMBL402 | IC50 | 9.45 | 8.5 | 0.4 | 2 |
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase CHEMBL3247 | IC50 | 8.52 | 8.52 | 3.0 | 1 |
| HepG2 CHEMBL395 | IC50 | 7.55 | 7.55 | 28.0 | 1 |
| Cytochrome P450 2C9 CHEMBL3397 | IC50 | 6.4 | 6.4 | 400.0 | 1 |
| dengue virus type 2 CHEMBL613966 | EC50 | 5.74 | 5.74 | 1820.0 | 1 |
| Nuclear receptor subfamily 4 group A member 2 CHEMBL5002 | EC50 | 5.72 | 5.72 | 1900.0 | 3 |
| NAD-dependent protein deacylase sirtuin-6 CHEMBL2163182 | EC50 | 5.15 | 5.15 | 7100.0 | 1 |
| Retinoic acid receptor RXR-alpha CHEMBL2061 | Kd | 4.96 | 4.96 | 11040.0 | 1 |
| Bile salt export pump CHEMBL6020 | IC50 | 4.44 | 4.44 | 36100.0 | 3 |
| Hepatic sodium/bile acid cotransporter CHEMBL5287 | IC50 | 4.4 | 4.4 | 40000.0 | 1 |
| ATP-binding cassette sub-family C member 3 CHEMBL5918 | IC50 | 4.24 | 4.24 | 57000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 614.74 | ng.hr.mL-1 | Homo sapiens |
| CL | 16.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 16.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 5.0 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 16.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 16.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 32.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 35.0 | mL.min-1.kg-1 | Macaca |
| CL | 8.33 | mL.min-1.g-1 | Homo sapiens |
| CL | 3.0 | uL.min-1.(10^6cells)-1 | Rattus norvegicus |
| CL | 4.3 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 7.3 | mL.min-1.kg-1 | Homo sapiens |
| Cmax | 663.0 | nM | Homo sapiens |
| F | 49.0 | % | Homo sapiens |
| F | 24.0 | % | Homo sapiens |
| F | 95.0 | % | Homo sapiens |
| Fu | 0.0079 | - | Homo sapiens |
| Fu | 0.0079 | - | Homo sapiens |
| Fu | 9e-05 | - | Rattus norvegicus |
| Fu | 9.22e-05 | - | Homo sapiens |
| MRT | 0.44 | hr | Homo sapiens |
| T1/2 | 0.7 | hr | Homo sapiens |
| Vd | 0.35 | L.kg-1 | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine