Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | HMG-CoA reductase | Starlite/ChEMBL | References |
Homo sapiens | 3-hydroxy-3-methylglutaryl-CoA reductase | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Change (functional) | = -46 % | Tested in vivo for hypocholesterolemic activity by measuring its ability to decrease serum total cholesterol, after oral administration of 5 mg/kg body wt. per day in normolipemic NZW rabbits | ChEMBL. | 1656041 |
IC50 (functional) | = 0.5 nM | Inhibition of the incorporation of sodium [14C]-acetate into cholesterol in HEP G2 cells. | ChEMBL. | 1656041 |
IC50 (functional) | = 0.5 nM | Inhibition of the incorporation of sodium [14C]-acetate into cholesterol in HEP G2 cells. | ChEMBL. | 1656041 |
IC50 (binding) | = 6 nM | In vitro inhibition of HMG-CoA reductase in solubilized rat liver. | ChEMBL. | 1656041 |
IC50 (binding) | = 6 nM | In vitro inhibition of HMG-CoA reductase in solubilized rat liver. | ChEMBL. | 1656041 |
IC50 (functional) | > 10 uM | In vitro inhibition of Cu2+ catalyzed LDL oxidation | ChEMBL. | 1656041 |
Inhibition (functional) | < 10 % | In vitro inhibition of microsomal lipid peroxidation at 10e-5 M conc. | ChEMBL. | 1656041 |
Inhibition (functional) | = 41 % | In vitro inhibition of Cu2+ catalyzed LDL oxidation at 10e-5 M conc. | ChEMBL. | 1656041 |
Relative potency (binding) | = 113 | Potency of the compound relative to mevinolin was determined with respect to IC50. Mevinolin was assigned a value of 100 | ChEMBL. | 1656041 |
Relative potency (functional) | = 10000 | Inhibition of HMG-CoA reductase compared to mevinolin. | ChEMBL. | 1656041 |
Relative potency (functional) | << 0.1 | Compound was tested for inhibition of microsomal lipid peroxidation and the potency relative to terbufucine was determined | ChEMBL. | 1656041 |
Relative potency (functional) | = 0.1 | Compound was tested for inhibition of Cu2+ catalyzed LDL oxidation and the potency relative to terbufucine was determined | ChEMBL. | 1656041 |
Relative potency (binding) | = 113 | Potency of the compound relative to mevinolin was determined with respect to IC50. Mevinolin was assigned a value of 100 | ChEMBL. | 1656041 |
Relative potency (functional) | = 10000 | Inhibition of HMG-CoA reductase compared to mevinolin. | ChEMBL. | 1656041 |
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.