Assay Detail
Binding
CHEMBL3857946
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HMG-CoA reductase in rat liver microsomes assessed as reduction in [14C]-HMG-CoA conversion to [14C]-mevalonic acid after 15 mins by column filtration method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Microsomes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL3247) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
The "Cyclopropyl Fragment" is a Versatile Player that Frequently Appears in Preclinical/Clinical Drug Molecules.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 8.06 | 8.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1201753 | PITAVASTATIN | 4.0 | 1 | 8.39 |
| CHEMBL3951152 | — | — | 1 | 7.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1201753 | PITAVASTATIN | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL3951152 | — | IC50 | = | 19.0 | nM | 7.72 |