Assay Detail
Functional
CHEMBL975203
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Inhibition of cholesterol synthesis in rat hepatocytes assessed as incorporation of [14C]acetate into cholesterol
23
Total Activities
23
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
(3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1h-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid (BMS-644950): a rationally designed orally efficacious 3-hydroxy-3-methylglutaryl coenzyme-a reductase inhibitor with reduced myotoxicity potential.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.47 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1496 | ROSUVASTATIN | 4.0 | 1 | 9.22 |
| CHEMBL468631 | — | — | 1 | 9.00 |
| CHEMBL468768 | — | — | 1 | 8.92 |
| CHEMBL498360 | — | — | 1 | 8.89 |
| CHEMBL466547 | — | — | 1 | 8.85 |
| CHEMBL511255 | — | — | 1 | 8.85 |
| CHEMBL466546 | — | — | 1 | 8.82 |
| CHEMBL468204 | — | — | 1 | 8.72 |
| CHEMBL1477 | CERIVASTATIN | 4.0 | 1 | 8.64 |
| CHEMBL1487 | ATORVASTATIN | 4.0 | 1 | 8.60 |
| CHEMBL525188 | — | — | 1 | 8.60 |
| CHEMBL467782 | — | — | 1 | 8.43 |
| CHEMBL468205 | — | — | 1 | 8.43 |
| CHEMBL466326 | — | — | 1 | 8.40 |
| CHEMBL495463 | — | — | 1 | 8.27 |
| CHEMBL498161 | — | — | 1 | 8.26 |
| CHEMBL1064 | SIMVASTATIN | 4.0 | 1 | 8.21 |
| CHEMBL511574 | — | — | 1 | 8.12 |
| CHEMBL466352 | — | — | 1 | 8.11 |
| CHEMBL468862 | — | — | 1 | 8.11 |
| CHEMBL496100 | — | — | 1 | 8.05 |
| CHEMBL468632 | — | — | 1 | 7.86 |
| CHEMBL1144 | PRAVASTATIN | 4.0 | 1 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1496 | ROSUVASTATIN | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL468631 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL468768 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL498360 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL466547 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL511255 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL466546 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL468204 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1477 | CERIVASTATIN | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL1487 | ATORVASTATIN | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL525188 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL467782 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL468205 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL466326 | — | IC50 | = | 3.95 | nM | 8.40 |
| CHEMBL495463 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL498161 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL1064 | SIMVASTATIN | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL511574 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL466352 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL468862 | — | IC50 | = | 7.7 | nM | 8.11 |
| CHEMBL496100 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL468632 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL1144 | PRAVASTATIN | IC50 | = | 29.0 | nM | 7.54 |