Assay Detail
Binding
CHEMBL944783
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Inhibition of rat microsomal HMGCoA reductase
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| 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
Hepatoselectivity of statins: design and synthesis of 4-sulfamoyl pyrroles as HMG-CoA reductase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.25 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL401950 | — | — | 1 | 9.00 |
| CHEMBL253054 | — | — | 1 | 8.74 |
| CHEMBL252657 | — | — | 1 | 8.70 |
| CHEMBL429487 | — | — | 1 | 8.59 |
| CHEMBL402622 | — | — | 1 | 8.57 |
| CHEMBL437783 | — | — | 1 | 8.54 |
| CHEMBL1496 | ROSUVASTATIN | 4.0 | 1 | 8.43 |
| CHEMBL1487 | ATORVASTATIN | 4.0 | 1 | 8.42 |
| CHEMBL401949 | — | — | 1 | 8.35 |
| CHEMBL253258 | — | — | 1 | 8.31 |
| CHEMBL404671 | — | — | 1 | 8.24 |
| CHEMBL253055 | — | — | 1 | 8.21 |
| CHEMBL437790 | — | — | 1 | 8.19 |
| CHEMBL404672 | — | — | 1 | 8.10 |
| CHEMBL251863 | — | — | 1 | 8.08 |
| CHEMBL403430 | — | — | 1 | 8.07 |
| CHEMBL403646 | — | — | 1 | 8.05 |
| CHEMBL252854 | — | — | 1 | 8.03 |
| CHEMBL253053 | — | — | 1 | 8.01 |
| CHEMBL252855 | — | — | 1 | 7.89 |
| CHEMBL437795 | — | — | 1 | 7.82 |
| CHEMBL265899 | — | — | 1 | 7.75 |
| CHEMBL438884 | — | — | 1 | 7.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL401950 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL253054 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL252657 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL429487 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL402622 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL437783 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL1496 | ROSUVASTATIN | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL1487 | ATORVASTATIN | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL401949 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL253258 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL404671 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL253055 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL437790 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL404672 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL251863 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL403430 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL403646 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL252854 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL253053 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL252855 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL437795 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL265899 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL438884 | — | IC50 | = | 27.0 | nM | 7.57 |