Assay Detail
Functional
CHEMBL1787316
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Inhibition of cholesterol synthesis in rat L6 cells assessed as reduction of [14C]-cholesterol level using [14C]-acetic acid preincubated for 3 hrs before addition of [14C]-acetic acid by scintillation counting
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | L6 |
| 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 | 5.85 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1782552 | — | — | 1 | 6.75 |
| CHEMBL1782562 | — | — | 1 | 6.65 |
| CHEMBL1496 | ROSUVASTATIN | 4.0 | 1 | 6.60 |
| CHEMBL1782559 | — | — | 1 | 6.35 |
| CHEMBL1782553 | — | — | 1 | 6.27 |
| CHEMBL1782556 | — | — | 1 | 6.27 |
| CHEMBL1782551 | — | — | 1 | 6.20 |
| CHEMBL251188 | — | — | 1 | 6.14 |
| CHEMBL1782563 | — | — | 1 | 6.05 |
| CHEMBL1782558 | — | — | 1 | 5.79 |
| CHEMBL1782560 | — | — | 1 | 5.56 |
| CHEMBL1782550 | — | — | 1 | 5.52 |
| CHEMBL1782554 | — | — | 1 | 5.31 |
| CHEMBL1782561 | — | — | 1 | 5.31 |
| CHEMBL1782555 | — | — | 1 | 5.19 |
| CHEMBL1782557 | — | — | 1 | 4.97 |
| CHEMBL1782062 | — | — | 1 | 4.57 |
| CHEMBL1782564 | — | — | 1 | - |
| CHEMBL1782565 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1782552 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL1782562 | — | IC50 | = | 224.0 | nM | 6.65 |
| CHEMBL1496 | ROSUVASTATIN | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL1782559 | — | IC50 | = | 444.0 | nM | 6.35 |
| CHEMBL1782553 | — | IC50 | = | 532.0 | nM | 6.27 |
| CHEMBL1782556 | — | IC50 | = | 538.0 | nM | 6.27 |
| CHEMBL1782551 | — | IC50 | = | 632.0 | nM | 6.20 |
| CHEMBL251188 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL1782563 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL1782558 | — | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL1782560 | — | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL1782550 | — | IC50 | = | 3030.0 | nM | 5.52 |
| CHEMBL1782554 | — | IC50 | = | 4850.0 | nM | 5.31 |
| CHEMBL1782561 | — | IC50 | = | 4870.0 | nM | 5.31 |
| CHEMBL1782555 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL1782557 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL1782062 | — | IC50 | = | 27200.0 | nM | 4.57 |
| CHEMBL1782564 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL1782565 | — | IC50 | > | 100000.0 | nM | - |