Assay Detail
Binding
CHEMBL3706229
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Reductase Activity Assay: The HMGR activity was performed using HMG-CoA reductase assay kit from Sigma-Aldrich with the human recombinant protein or 100 μg total cell lysates from A549 cells. Lovastatin was used as a positive control, and SAHA as a negative control. HMGR activity under defined assay conditions, containing NADPH and HMG-CoA substrate in a final volume of 0.2 mL of 100 mM potassium phosphatate buffer (120 mM KCI, 1 mM EDTA, 5 mM DTT, pH 7.4), were initiated in the presence or absence (control) of test compounds dissolved in dimethylsulfoxide (DMSO). The rates of NADPH consumption were monitored every 20 seconds, for up to 10 minutes, by spectrophotometer at 37° C. and 340 nm.
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | A549 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
3-hydroxy-3-methylglutaryl-coenzyme A reductase (CHEMBL402) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.37 | 7.53 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL503 | LOVASTATIN | 4.0 | 1 | 7.53 |
| CHEMBL3704922 | — | — | 1 | 7.44 |
| CHEMBL2347010 | — | — | 1 | 7.44 |
| CHEMBL3704923 | — | — | 1 | 7.27 |
| CHEMBL2347011 | — | — | 1 | 7.27 |
| CHEMBL2347005 | — | — | 1 | 7.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL503 | LOVASTATIN | IC50 | = | 29.5 | nM | 7.53 |
| CHEMBL3704922 | — | IC50 | = | 36.5 | nM | 7.44 |
| CHEMBL2347010 | — | IC50 | = | 36.5 | nM | 7.44 |
| CHEMBL3704923 | — | IC50 | = | 53.8 | nM | 7.27 |
| CHEMBL2347011 | — | IC50 | = | 53.8 | nM | 7.27 |
| CHEMBL2347005 | — | IC50 | = | 54.1 | nM | 7.27 |