Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | 3-hydroxy-3-methylglutaryl-CoA reductase | Starlite/ChEMBL | References |
Rattus norvegicus | HMG-CoA reductase | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Change (functional) | = 3 % | Tested in vivo for hypocholesterolemic activity by measuring its ability to decrease serum LDL-cholesterol, after oral administration of 25 mg/kg per day for 14 days in male beagle dogs. | ChEMBL. | 1656041 |
IC50 (binding) | = 17 nM | In vitro inhibition of HMG-CoA reductase in solubilized rat liver. | ChEMBL. | 1656041 |
IC50 (binding) | = 17 nM | In vitro inhibition of HMG-CoA reductase in solubilized rat liver. | ChEMBL. | 1656041 |
IC50 (functional) | = 55 nM | Inhibition of the incorporation of sodium [14C]-acetate into cholesterol in HEP G2 cells. | ChEMBL. | 1656041 |
IC50 (functional) | = 55 nM | Inhibition of the incorporation of sodium [14C]-acetate into cholesterol in HEP G2 cells. | ChEMBL. | 1656041 |
Relative potency (binding) | = 43 | Inhibition of HMG-CoA reductase compared to mevinolin. | ChEMBL. | 1656041 |
Relative potency (functional) | = 90 | Inhibition of HMG-CoA reductase compared to mevinolin. | ChEMBL. | 1656041 |
Relative potency (binding) | = 43 | Inhibition of HMG-CoA reductase compared to mevinolin. | ChEMBL. | 1656041 |
Relative potency (functional) | = 90 | 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.