Assay Detail
Binding
CHEMBL688750
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Inhibitory activity against washed rat liver microsomal HMG-CoA reductase (HMGR)
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Liver |
| Subcellular | Microsomal |
| 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. 1. 3,5-Dihydroxy-7-(N-imidazolyl)-6-heptenoates and -heptanoates, a novel series of HMG-CoA reductase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 46 | 7.59 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL333760 | — | — | 1 | 9.00 |
| CHEMBL331048 | — | — | 1 | 9.00 |
| CHEMBL121727 | — | — | 1 | 9.00 |
| CHEMBL120932 | — | — | 1 | 8.70 |
| CHEMBL331899 | — | — | 1 | 8.70 |
| CHEMBL332201 | — | — | 1 | 8.70 |
| CHEMBL121309 | — | — | 1 | 8.59 |
| CHEMBL121756 | — | — | 1 | 8.52 |
| CHEMBL431659 | — | — | 1 | 8.52 |
| CHEMBL121610 | — | — | 1 | 8.40 |
| CHEMBL333003 | — | — | 1 | 8.30 |
| CHEMBL122957 | — | — | 1 | 8.15 |
| CHEMBL332797 | — | — | 1 | 8.10 |
| CHEMBL123127 | — | — | 1 | 8.05 |
| CHEMBL333307 | — | — | 1 | 7.89 |
| CHEMBL332580 | — | — | 1 | 7.77 |
| CHEMBL431842 | — | — | 1 | 7.70 |
| CHEMBL332912 | — | — | 1 | 7.66 |
| CHEMBL333479 | — | — | 1 | 7.62 |
| CHEMBL120860 | — | — | 1 | 7.54 |
| CHEMBL121602 | — | — | 1 | 7.52 |
| CHEMBL333717 | — | — | 1 | 7.51 |
| CHEMBL121122 | — | — | 1 | 7.51 |
| CHEMBL332202 | — | — | 1 | 7.50 |
| CHEMBL121230 | — | — | 1 | 7.42 |
| CHEMBL120908 | — | — | 1 | 7.42 |
| CHEMBL123253 | — | — | 1 | 7.39 |
| CHEMBL123354 | — | — | 1 | 7.37 |
| CHEMBL122725 | — | — | 1 | 7.25 |
| CHEMBL330995 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL333760 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL121727 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL331048 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL120932 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL331899 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL332201 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL121309 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL121756 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL431659 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL121610 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL333003 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL122957 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL332797 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL123127 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL333307 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL332580 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL431842 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL332912 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL333479 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL120860 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL121602 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL333717 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL121122 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL332202 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL120908 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL121230 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL123253 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL123354 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL122725 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL330995 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL420899 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL120869 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL123487 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL330981 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL332125 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL332244 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL331923 | — | IC50 | = | 201.0 | nM | 6.70 |
| CHEMBL121052 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL331675 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL120971 | — | IC50 | = | 418.0 | nM | 6.38 |
| CHEMBL1161659 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL122713 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL1161663 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL123417 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL434224 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL333437 | — | IC50 | > | 1000.0 | nM | - |