Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | HMG-CoA reductase | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = 14 % | Percent increase in plasma HDL-cholesterol in dog was determined after oral administration of a dose of 20 mg/kg for 14 days | ChEMBL. | 2153213 |
Activity (functional) | = 34 % | Percent decrease in total plasma cholesterol in rabbit was determined after oral administration of a dose of 20 mg/kg for 10 days | ChEMBL. | 2153213 |
Activity (functional) | = 48 % | Percent decrease in plasma LDL-cholesterol in dog was determined after oral administration of a dose of 20 mg/kg for 14 days | ChEMBL. | 2153213 |
IC50 (binding) | < 0.01 nM | Inhibition of cellular HMG-CoA reductase in cultures of hepatic cells (HEP G2, a human hepatoma cell line) | ChEMBL. | 2153213 |
IC50 (binding) | = 3 nM | In vitro inhibition of HMG-CoA reductase of rat liver | ChEMBL. | 2153213 |
IC50 (binding) | = 3 nM | In vitro inhibition of HMG-CoA reductase of rat liver | ChEMBL. | 2153213 |
IC50 (binding) | = 6 nM | In vitro inhibition of HMG-CoA reductase of rat liver | ChEMBL. | 2153213 |
Inhibition (functional) | = 5.6 % | Inhibition of hepatic cholesterol de novo synthesis in male rats after po administration | ChEMBL. | 2153213 |
Relative potency (binding) | = 257 | In vitro inhibition of solubilized, partially purified rat liver HMG-CoA reductase relative to mevinolin | ChEMBL. | 2153213 |
Relative potency (binding) | = 128 | In vitro inhibition of solubilized, partially purified rat liver HMG-CoA reductase relative to mevinolin | ChEMBL. | 2153213 |
Relative potency (functional) | = 250 | Inhibition of hepatic cholesterol de novo synthesis in male rats after po administration, relative to mevinolin | ChEMBL. | 2153213 |
Relative potency (binding) | = 257 | In vitro inhibition of solubilized, partially purified rat liver HMG-CoA reductase relative to mevinolin | ChEMBL. | 2153213 |
Relative potency (binding) | > 500 | Inhibition of cellular HMG-CoA reductase in cultures of hepatic cells (HEP G2, a human hepatoma cell line) relative to mevinolin | ChEMBL. | 2153213 |
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.