Compound Detail
CHEMBL1201753
PITAVASTATIN 💊 Approved Drug
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💊 Approved Drug
O=C(O)C[C@H](O)C[C@H](O)/C=C/c1c(C2CC2)nc2ccccc2c1-c1ccc(F)cc1
Basic Information
| ChEMBL ID | CHEMBL1201753 |
| Name | PITAVASTATIN |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | VGYFMXBACGZSIL-MCBHFWOFSA-N |
| Therapeutic | ✓ Yes |
2
Targets
3
Activities
2
Assay Types
12
PK Parameters
20
Publications
5
Known Names
11
Indications
Molecular Properties
421.5
MW (Da)
4.52
ALogP
4
HBA
3
HBD
90.7
PSA (Ų)
0.50
QED
0
Ro5 Violations
8
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2009 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Indications
Cardiovascular Diseases Coronary Disease Diabetes Mellitus, Type 1 Diabetes Mellitus, Type 2 Hypercholesterolemia Hyperlipidemias Lipid Metabolism Disorders Breast Neoplasms Influenza, Human Metabolic Syndrome Renal Insufficiency
ATC Classification
C10AA08
pitavastatin
Level 1: CARDIOVASCULAR SYSTEM
Level 2: LIPID MODIFYING AGENTS
Activity Summary
EC50 2 meas. best 6.92
IC50 1 meas. best 8.39
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase CHEMBL3247 | IC50 | 8.39 | 8.39 | 4.1 | 1 |
| Nuclear receptor subfamily 4 group A member 2 CHEMBL5002 | EC50 | 6.92 | 6.92 | 120.0 | 2 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 7.11 | uL.min-1.(10^6cells)-1 | Rattus norvegicus |
| CL | 14.5 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 3.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 1705.0 | uL.min-1.(10^6cells)-1 | Rattus norvegicus |
| CL | 7.1 | uL.min-1.(10^6cells)-1 | Rattus norvegicus |
| CL | 31.0 | mL.min-1.kg-1 | Homo sapiens |
| CL | 7.1 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 17.8 | mL.min-1.kg-1 | Macaca fascicularis |
| CL | 5.6 | mL.min-1.kg-1 | Homo sapiens |
| Fu | 8e-05 | - | Rattus norvegicus |
| Fu | 0.000263 | - | Macaca fascicularis |
| Fu | 8e-05 | - | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase | IC50 | = | 4.1 | nM | 8.39 | Inhibition of HMG-CoA reductase in rat liver microsomes assessed as reduction in... | 27299736 |
| Nuclear receptor subfamily 4 group A member 2 | EC50 | = | 120.0 | nM | 6.92 | Agonist activity at human Nurr1 measured by Gal4-Nurr1 hybrid reporter gene assa... | 35797147 |
| Nuclear receptor subfamily 4 group A member 2 | EC50 | = | 120.0 | nM | 6.92 | Agonist activity at Gal4-fused human full length Nurr1 transfected in human HEK2... | 37751901 |
Literature References
Data from ChEMBL 36 via Core Engine