Assay Detail
Binding
CHEMBL691937
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to inhibit HMG-CoA reductase (HMGR) by CoA reductase inhibition screen (COR) in rats
36
Total Activities
36
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. 1. trans-6-(2-pyrrol-1-ylethyl)-4-hydroxypyran-2-ones, a novel series of HMG-CoA reductase inhibitors. 1. Effects of structural modifications at the 2- and 5-positions of the pyrrole nucleus.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 36 | 5.24 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54440 | MEVASTATIN | 2.0 | 1 | 7.60 |
| CHEMBL104044 | — | — | 1 | 6.64 |
| CHEMBL322366 | — | — | 1 | 6.20 |
| CHEMBL319870 | — | — | 1 | 5.75 |
| CHEMBL104595 | — | — | 1 | 5.75 |
| CHEMBL107753 | — | — | 1 | 5.66 |
| CHEMBL265305 | — | — | 1 | 5.64 |
| CHEMBL106062 | — | — | 1 | 5.58 |
| CHEMBL430472 | — | — | 1 | 5.58 |
| CHEMBL104295 | — | — | 1 | 5.58 |
| CHEMBL104660 | — | — | 1 | 5.55 |
| CHEMBL322656 | — | — | 1 | 5.50 |
| CHEMBL323019 | — | — | 1 | 5.50 |
| CHEMBL317885 | — | — | 1 | 5.44 |
| CHEMBL320352 | — | — | 1 | 5.40 |
| CHEMBL321564 | — | — | 1 | 5.27 |
| CHEMBL104031 | — | — | 1 | 5.25 |
| CHEMBL321914 | — | — | 1 | 5.24 |
| CHEMBL106167 | — | — | 1 | 5.20 |
| CHEMBL104703 | — | — | 1 | 5.05 |
| CHEMBL322724 | — | — | 1 | 5.04 |
| CHEMBL104866 | — | — | 1 | 4.96 |
| CHEMBL105654 | — | — | 1 | 4.92 |
| CHEMBL106720 | — | — | 1 | 4.89 |
| CHEMBL280437 | — | — | 1 | 4.80 |
| CHEMBL107995 | — | — | 1 | 4.64 |
| CHEMBL317854 | — | — | 1 | 4.60 |
| CHEMBL104639 | — | — | 1 | 4.60 |
| CHEMBL319905 | — | — | 1 | 4.55 |
| CHEMBL104405 | — | — | 1 | 4.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54440 | MEVASTATIN | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL104044 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL322366 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL319870 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL104595 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL107753 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL265305 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL106062 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL430472 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL104295 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL104660 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL322656 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL323019 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL317885 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL320352 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL321564 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL104031 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL321914 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL106167 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL104703 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL322724 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL104866 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL105654 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL106720 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL280437 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL107995 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL104639 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL317854 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL319905 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL104405 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL321930 | — | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL318596 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL105511 | — | IC50 | = | 63000.0 | nM | 4.20 |
| CHEMBL323256 | — | IC50 | = | 87000.0 | nM | 4.06 |
| CHEMBL317403 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL322367 | — | IC50 | > | 100000.0 | nM | - |