Assay Detail
Functional
CHEMBL1787315
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of cholesterol synthesis in rat hepatocytes assessed as reduction of [14C]-cholesterol level using [14C]-acetic acid preincubated for 4 hrs before addition of [14C]-acetic acid by liquid scintillation counting
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | Hepatocyte |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Discovery of novel hepatoselective HMG-CoA reductase inhibitors for treating hypercholesterolemia: a bench-to-bedside case study on tissue selective drug distribution.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 9.63 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1782552 | — | — | 1 | 10.00 |
| CHEMBL1782554 | — | — | 1 | 10.00 |
| CHEMBL1782557 | — | — | 1 | 10.00 |
| CHEMBL1782559 | — | — | 1 | 10.00 |
| CHEMBL1782562 | — | — | 1 | 10.00 |
| CHEMBL1782556 | — | — | 1 | 9.70 |
| CHEMBL1782555 | — | — | 1 | 9.70 |
| CHEMBL1782561 | — | — | 1 | 9.70 |
| CHEMBL1782551 | — | — | 1 | 9.70 |
| CHEMBL1782563 | — | — | 1 | 9.70 |
| CHEMBL1496 | ROSUVASTATIN | 4.0 | 1 | 9.52 |
| CHEMBL1782553 | — | — | 1 | 9.52 |
| CHEMBL1782550 | — | — | 1 | 9.52 |
| CHEMBL1782564 | — | — | 1 | 9.40 |
| CHEMBL1782560 | — | — | 1 | 9.30 |
| CHEMBL1782565 | — | — | 1 | 9.30 |
| CHEMBL1782558 | — | — | 1 | 9.15 |
| CHEMBL251188 | — | — | 1 | 9.05 |
| CHEMBL1782062 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1782552 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1782554 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1782557 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1782559 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1782562 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL1782556 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1782555 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1782561 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1782551 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1782563 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL1496 | ROSUVASTATIN | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1782553 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1782550 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL1782564 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL1782560 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1782565 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL1782558 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL251188 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL1782062 | — | IC50 | - | — | - |