Assay Detail
Binding
CHEMBL3889301
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Cellular Firefly Luciferase Assay (NFkB): The NF-kB activities of curcumin and analogs were determined by a cellular firefly luciferase assay. This assay utilized a commercially available cell line (Panomics 293T-luc cellular assay) developed for screening inhibitors of NF-kB. This cell line is stably transfected with a luciferase reporter controlled by an NF-kB dependent promoter. The cell is stimulated with tumor necrosis factor alpha (TNFalpha) which activates NF-kB. NF-kB then binds to one of six promoter regions on the cell's DNA leading to the production of a luciferase enzyme. Luciferin is added to the cell lysates and the luciferase enzyme catalyzes a cleavage of luciferin leading to the emission of light.
14
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Nuclear factor NF-kappa-B p105 subunit (CHEMBL3251) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Therapeutic curcumin derivatives
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.28 | 5.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1971185 | — | — | 2 | 5.47 |
| CHEMBL3577010 | — | — | 1 | 5.46 |
| CHEMBL17205 | CYCLOVALONE | 2.0 | 2 | 5.38 |
| CHEMBL559673 | — | — | 1 | 5.38 |
| CHEMBL476424 | — | — | 1 | 5.30 |
| CHEMBL560131 | — | — | 1 | 5.27 |
| CHEMBL557311 | — | — | 1 | 5.19 |
| CHEMBL1797794 | — | — | 2 | 5.17 |
| CHEMBL3929895 | — | — | 1 | 5.12 |
| CHEMBL3892642 | — | — | 1 | 5.09 |
| CHEMBL140 | CURCUMIN | 3.0 | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1971185 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL1971185 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL3577010 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL17205 | CYCLOVALONE | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL559673 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL17205 | CYCLOVALONE | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL476424 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL560131 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL557311 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL1797794 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL1797794 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL3929895 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL3892642 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL140 | CURCUMIN | IC50 | = | 8200.0 | nM | 5.09 |