Assay Detail
Binding
CHEMBL3705652
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Reductase Assay : The following procedure was followed using a HMG-CoA Reductase assay kit obtained from Sigma-Aldrich (catalogue number CS1090). The assay is based on the spectrophotometric measurement of the decrease in absorbance at 340 nm of NADPH in solution. A decrease in absorbance is caused by the oxidation of NADPH by the catalytic subunit of HMGR in the presence of the substrate HMG-CoA. Effective inhibition of the HMG-CoA leads to a reduction in oxidation of NADPH which in turn leads to a smaller reduction in the absorbance at 340 nm over time.
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL402) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Use of rosuvastatin lactols as medicaments
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 8.47 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3963593 | — | — | 1 | 9.00 |
| CHEMBL3985556 | — | — | 1 | 9.00 |
| CHEMBL3677709 | — | — | 1 | 8.70 |
| CHEMBL3906659 | — | — | 1 | 8.70 |
| CHEMBL3896765 | — | — | 1 | 8.70 |
| CHEMBL3677708 | — | — | 1 | 8.52 |
| CHEMBL1496 | ROSUVASTATIN | 4.0 | 1 | 8.40 |
| CHEMBL3677707 | — | — | 1 | 8.40 |
| CHEMBL3971241 | — | — | 1 | 8.10 |
| CHEMBL3971439 | — | — | 1 | 8.00 |
| CHEMBL3684074 | — | — | 1 | 7.66 |
| CHEMBL3941657 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3963593 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3985556 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3677709 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3906659 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3896765 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3677708 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1496 | ROSUVASTATIN | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3677707 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3971241 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3971439 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3684074 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3941657 | — | IC50 | < | 1.0 | nM | - |