Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | HMG-CoA reductase | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = -41 % | Reduction of LDL level in chow fed Hartley guinea pig serum at 20 mg/kg/day, po for 7 days relative to rosuvastatin | ChEMBL. | 18072721 |
ED50 (functional) | = 3.6 mg kg-1 | Reduction of LDL level in po dosed Hartley guinea pig plasma after 7 days | ChEMBL. | 18072721 |
IC50 (functional) | = 0.9 nM | Inhibition of cholesterol synthesis in rat hepatocytes | ChEMBL. | 18072721 |
IC50 (binding) | = 1.9 nM | Inhibition of HMG-CoA redcutase in Sprague-Dawley rat liver microsomes | ChEMBL. | 18072721 |
IC50 (binding) | = 1.9 nM | Inhibition of HMG-CoA redcutase in Sprague-Dawley rat liver microsomes | ChEMBL. | 18072721 |
IC50 (functional) | = 730 nM | Inhibition of cholesterol synthesis in rat L6 cells | ChEMBL. | 18072721 |
Inhibition (functional) | = -74 % | Inhibition of cholesterol synthesis in Goldern Syrian hamster blood at 10 mg/kg, po after 2 to 4 hrs relative to control | ChEMBL. | 18072721 |
Inhibition (functional) | = -15 % | Inhibition of cholesterol synthesis in Golden Syrian hamster blood at 10 mg/kg, po after 4 to 6 hrs relative to control | ChEMBL. | 18072721 |
Ratio IC50 (functional) | = 810 | Ratio of IC50 for cholesterol synthesis in rat myocytes to rat hepatocytes | ChEMBL. | 18072721 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.
1 literature reference was collected for this gene.