Assay Detail
Binding
CHEMBL975202
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of HMGR in rat hepatic microsomes assessed as conversion of [14C]HMG-CoA to [14C]mevalonic acid
23
Total Activities
23
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
(3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1h-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid (BMS-644950): a rationally designed orally efficacious 3-hydroxy-3-methylglutaryl coenzyme-a reductase inhibitor with reduced myotoxicity potential.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.45 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL466547 | — | — | 1 | 9.30 |
| CHEMBL466546 | — | — | 1 | 9.05 |
| CHEMBL468632 | — | — | 1 | 9.05 |
| CHEMBL466326 | — | — | 1 | 8.85 |
| CHEMBL468205 | — | — | 1 | 8.74 |
| CHEMBL495463 | — | — | 1 | 8.66 |
| CHEMBL511255 | — | — | 1 | 8.64 |
| CHEMBL498360 | — | — | 1 | 8.62 |
| CHEMBL468768 | — | — | 1 | 8.60 |
| CHEMBL525188 | — | — | 1 | 8.60 |
| CHEMBL511574 | — | — | 1 | 8.54 |
| CHEMBL467782 | — | — | 1 | 8.52 |
| CHEMBL1496 | ROSUVASTATIN | 4.0 | 1 | 8.51 |
| CHEMBL466352 | — | — | 1 | 8.43 |
| CHEMBL468631 | — | — | 1 | 8.38 |
| CHEMBL1064 | SIMVASTATIN | 4.0 | 1 | 8.37 |
| CHEMBL1487 | ATORVASTATIN | 4.0 | 1 | 8.21 |
| CHEMBL468862 | — | — | 1 | 8.16 |
| CHEMBL496100 | — | — | 1 | 8.15 |
| CHEMBL1477 | CERIVASTATIN | 4.0 | 1 | 8.01 |
| CHEMBL468204 | — | — | 1 | 7.91 |
| CHEMBL1144 | PRAVASTATIN | 4.0 | 1 | 7.50 |
| CHEMBL498161 | — | — | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL466547 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL466546 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL468632 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL466326 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL468205 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL495463 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL511255 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL498360 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL468768 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL525188 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL511574 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL467782 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1496 | ROSUVASTATIN | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL466352 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL468631 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL1064 | SIMVASTATIN | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1487 | ATORVASTATIN | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL468862 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL496100 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1477 | CERIVASTATIN | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL468204 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL1144 | PRAVASTATIN | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL498161 | — | IC50 | = | 33.0 | nM | 7.48 |