Assay Detail
Binding
CHEMBL691934
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Inhibition of HMG-CoA reductase activity in partially purified rat liver
23
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL3247) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Inhibitors of cholesterol biosynthesis. 3. Tetrahydro-4-hydroxy-6-[2-(1H-pyrrol-1-yl)ethyl]-2H-pyran-2-one inhibitors of HMG-CoA reductase. 2. Effects of introducing substituents at positions three and four of the pyrrole nucleus.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.87 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333687 | ATORVASTATIN LACTONE | — | 3 | 8.15 |
| CHEMBL121658 | — | — | 1 | 7.55 |
| CHEMBL332165 | — | — | 1 | 7.55 |
| CHEMBL54440 | MEVASTATIN | 2.0 | 1 | 7.52 |
| CHEMBL331453 | — | — | 1 | 7.40 |
| CHEMBL330753 | — | — | 1 | 7.34 |
| CHEMBL122219 | — | — | 1 | 7.30 |
| CHEMBL120949 | — | — | 1 | 7.15 |
| CHEMBL333361 | — | — | 1 | 6.92 |
| CHEMBL331952 | — | — | 1 | 6.85 |
| CHEMBL330777 | — | — | 1 | 6.77 |
| CHEMBL123357 | — | — | 1 | 6.75 |
| CHEMBL420354 | — | — | 1 | 6.70 |
| CHEMBL104044 | — | — | 1 | 6.64 |
| CHEMBL331411 | — | — | 1 | 6.55 |
| CHEMBL120897 | — | — | 1 | 6.51 |
| CHEMBL333478 | — | — | 1 | 6.46 |
| CHEMBL123986 | — | — | 1 | 6.46 |
| CHEMBL333206 | — | — | 1 | 6.10 |
| CHEMBL420337 | — | — | 1 | 6.05 |
| CHEMBL123811 | — | — | 1 | 5.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333687 | ATORVASTATIN LACTONE | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL333687 | ATORVASTATIN LACTONE | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL121658 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL332165 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL54440 | MEVASTATIN | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL331453 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL330753 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL122219 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL120949 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL333361 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL331952 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL330777 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL123357 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL420354 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL104044 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL331411 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL120897 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL333478 | — | IC50 | = | 347.0 | nM | 6.46 |
| CHEMBL123986 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL333687 | ATORVASTATIN LACTONE | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL333206 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL420337 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL123811 | — | IC50 | = | 4000.0 | nM | 5.40 |