Assay Detail
Binding
CHEMBL692516
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Inhibition of HMG-CoA reductase in rat liver microsomes
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL3247) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Total synthesis and biological evaluation of structural analogues of compactin and dihydromevinolin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.20 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL293944 | — | — | 1 | 9.00 |
| CHEMBL3350219 | — | — | 1 | 8.80 |
| CHEMBL54440 | MEVASTATIN | 2.0 | 1 | 7.89 |
| CHEMBL54045 | — | — | 1 | 7.50 |
| CHEMBL299644 | — | — | 1 | 6.50 |
| CHEMBL55028 | — | — | 1 | 6.20 |
| CHEMBL55303 | — | — | 1 | 6.20 |
| CHEMBL3350220 | — | — | 1 | 5.70 |
| CHEMBL2115471 | — | — | 1 | 5.70 |
| CHEMBL2115055 | — | — | 1 | 5.40 |
| CHEMBL416308 | — | — | 1 | 5.30 |
| CHEMBL53758 | — | — | 1 | 5.15 |
| CHEMBL2115472 | — | — | 1 | 5.00 |
| CHEMBL291954 | — | — | 1 | 4.60 |
| CHEMBL2115058 | — | — | 1 | 4.10 |
| CHEMBL2115056 | — | — | 1 | - |
| CHEMBL56180 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL293944 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3350219 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL54440 | MEVASTATIN | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL54045 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL299644 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL55028 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL55303 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL3350220 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2115471 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2115055 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL416308 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL53758 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL2115472 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL291954 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL2115058 | — | IC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL2115056 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL56180 | — | IC50 | = | 110000.0 | nM | - |