Assay Detail
Binding
CHEMBL898453
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Inhibition of rat microsomal HMG-CoA reductase assessed as inhibition of cholesterol synthesis after 30 mins
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL3247) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Discovery of pyrrole-based hepatoselective ligands as potent inhibitors of HMG-CoA reductase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.34 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL398403 | — | — | 1 | 9.07 |
| CHEMBL237814 | — | — | 1 | 8.80 |
| CHEMBL237596 | — | — | 1 | 8.80 |
| CHEMBL262322 | — | — | 1 | 8.62 |
| CHEMBL427854 | — | — | 1 | 8.55 |
| CHEMBL1477 | CERIVASTATIN | 4.0 | 1 | 8.55 |
| CHEMBL1496 | ROSUVASTATIN | 4.0 | 1 | 8.44 |
| CHEMBL235472 | — | — | 1 | 8.43 |
| CHEMBL392897 | — | — | 1 | 8.33 |
| CHEMBL235712 | — | — | 1 | 8.32 |
| CHEMBL235709 | — | — | 1 | 8.28 |
| CHEMBL394937 | — | — | 1 | 7.92 |
| CHEMBL1064 | SIMVASTATIN | 4.0 | 1 | 7.75 |
| CHEMBL391241 | — | — | 1 | 7.68 |
| CHEMBL237597 | — | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL398403 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL237814 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL237596 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL262322 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL427854 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL1477 | CERIVASTATIN | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL1496 | ROSUVASTATIN | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL235472 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL392897 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL235712 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL235709 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL394937 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1064 | SIMVASTATIN | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL391241 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL237597 | — | IC50 | = | 30.0 | nM | 7.52 |