Assay Detail
Binding
CHEMBL692133
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Tested in vitro for the inhibition of HMG-CoA reductase from partially purified microsomal preparations.
14
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Canis lupus familiaris |
| Subcellular | Microsome |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL402) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Inhibitors of cholesterol biosynthesis. 6. trans-6-[2-(2-N-heteroaryl-3,5-disubstituted- pyrazol-4-yl)ethyl/ethenyl]tetrahydro-4-hydroxy-2H-pyran-2-ones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.59 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2367472 | — | — | 2 | 8.15 |
| CHEMBL2367478 | — | — | 1 | 8.15 |
| CHEMBL2367477 | — | — | 2 | 8.10 |
| CHEMBL2367470 | — | — | 1 | 7.77 |
| CHEMBL503 | LOVASTATIN | 4.0 | 1 | 7.70 |
| CHEMBL303515 | LOVASTATIN SODIUM | — | 1 | 7.70 |
| CHEMBL1144 | PRAVASTATIN | 4.0 | 1 | 7.52 |
| CHEMBL690 | PRAVASTATIN SODIUM | 4.0 | 1 | 7.52 |
| CHEMBL64962 | — | — | 1 | 7.40 |
| CHEMBL2367471 | — | — | 1 | 7.23 |
| CHEMBL2367475 | — | — | 1 | 7.21 |
| CHEMBL65037 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2367472 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2367478 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2367477 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2367470 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL503 | LOVASTATIN | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL303515 | LOVASTATIN SODIUM | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2367477 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1144 | PRAVASTATIN | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL690 | PRAVASTATIN SODIUM | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL64962 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL2367471 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL2367475 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL2367472 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL65037 | — | IC50 | = | 110.0 | nM | 6.96 |