Assay Detail
Binding
CHEMBL941841
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Inhibition of HMG-CoA reductase in rat liver microsomes
41
Total Activities
41
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 | Intermediate |
Target
3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL3247) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Pyrazole inhibitors of HMG-CoA reductase: an attempt to dramatically reduce synthetic complexity through minimal analog re-design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 41 | 7.95 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL251153 | — | — | 1 | 8.70 |
| CHEMBL400644 | — | — | 1 | 8.68 |
| CHEMBL1496 | ROSUVASTATIN | 4.0 | 1 | 8.68 |
| CHEMBL251188 | — | — | 1 | 8.60 |
| CHEMBL250955 | — | — | 1 | 8.42 |
| CHEMBL400983 | — | — | 1 | 8.39 |
| CHEMBL250792 | — | — | 1 | 8.32 |
| CHEMBL399679 | — | — | 1 | 8.31 |
| CHEMBL250956 | — | — | 1 | 8.28 |
| CHEMBL400311 | — | — | 1 | 8.27 |
| CHEMBL249977 | — | — | 1 | 8.24 |
| CHEMBL400982 | — | — | 1 | 8.21 |
| CHEMBL250383 | — | — | 1 | 8.21 |
| CHEMBL428229 | — | — | 1 | 8.17 |
| CHEMBL447483 | — | — | 1 | 8.08 |
| CHEMBL249978 | — | — | 1 | 8.06 |
| CHEMBL266679 | — | — | 1 | 8.02 |
| CHEMBL250168 | — | — | 1 | 8.00 |
| CHEMBL250584 | — | — | 1 | 7.92 |
| CHEMBL438144 | — | — | 1 | 7.85 |
| CHEMBL249369 | — | — | 1 | 7.85 |
| CHEMBL251154 | — | — | 1 | 7.85 |
| CHEMBL437775 | — | — | 1 | 7.85 |
| CHEMBL248728 | — | — | 1 | 7.82 |
| CHEMBL250180 | — | — | 1 | 7.82 |
| CHEMBL398292 | — | — | 1 | 7.80 |
| CHEMBL250585 | — | — | 1 | 7.80 |
| CHEMBL250381 | — | — | 1 | 7.77 |
| CHEMBL248919 | — | — | 1 | 7.77 |
| CHEMBL250179 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL251153 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL400644 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1496 | ROSUVASTATIN | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL251188 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL250955 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL400983 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL250792 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL399679 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL250956 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL400311 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL249977 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL400982 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL250383 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL428229 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL447483 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL249978 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL266679 | — | IC50 | = | 9.5 | nM | 8.02 |
| CHEMBL250168 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL250584 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL437775 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL249369 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL438144 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL251154 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL248728 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL250180 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL398292 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL250585 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL250381 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL248919 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL250179 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL399536 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL249770 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL398289 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL250794 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL400757 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL249769 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL248727 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL249565 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL249368 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL400576 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL250382 | — | IC50 | = | 76.0 | nM | 7.12 |