Assay Detail
Binding
CHEMBL1787314
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HMG-CoA reductase in Sprague-Dawley rat liver microsomes using [14C]HMG-CoA as substrate preincubated for 0.5 hrs before substrate addition measured after 0.75 hrs by beta scintillation counting
22
Total Activities
22
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 | Autocuration |
Target
3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL3247) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
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 | 22 | 8.39 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL251188 | — | — | 1 | 9.00 |
| CHEMBL1782561 | — | — | 1 | 8.92 |
| CHEMBL1782560 | — | — | 1 | 8.92 |
| CHEMBL1782559 | — | — | 1 | 8.92 |
| CHEMBL1782556 | — | — | 1 | 8.92 |
| CHEMBL1782555 | — | — | 1 | 8.92 |
| CHEMBL1782551 | — | — | 1 | 8.85 |
| CHEMBL1782062 | — | — | 1 | 8.82 |
| CHEMBL1782552 | — | — | 1 | 8.77 |
| CHEMBL1496 | ROSUVASTATIN | 4.0 | 1 | 8.51 |
| CHEMBL1782558 | — | — | 1 | 8.47 |
| CHEMBL1782563 | — | — | 1 | 8.43 |
| CHEMBL1782562 | — | — | 1 | 8.39 |
| CHEMBL1782554 | — | — | 1 | 8.31 |
| CHEMBL1782565 | — | — | 1 | 8.31 |
| CHEMBL1782557 | — | — | 1 | 8.15 |
| CHEMBL1782553 | — | — | 1 | 8.14 |
| CHEMBL1782564 | — | — | 1 | 8.14 |
| CHEMBL1782550 | — | — | 1 | 8.10 |
| CHEMBL1782549 | — | — | 1 | 7.58 |
| CHEMBL1782548 | — | — | 1 | 7.03 |
| CHEMBL1782547 | — | — | 1 | 6.91 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL251188 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1782561 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1782560 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1782559 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1782556 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1782555 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1782551 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL1782062 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL1782552 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1496 | ROSUVASTATIN | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL1782558 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL1782563 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL1782562 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL1782554 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL1782565 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL1782557 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1782553 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL1782564 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL1782550 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL1782549 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1782548 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL1782547 | — | IC50 | = | 123.0 | nM | 6.91 |