Assay Detail
Binding
CHEMBL3269909
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of NF-kappaB transactivation in TNF-alpha-stimulated human K562 cells preincubated for 2 hrs followed by TNF-alpha challenge measured after 6 hrs by dual luciferase reporter gene assay
18
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | K562 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Nuclear factor NF-kappa-B complex (CHEMBL2094258) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Homo sapiens |
Publication
Bis(4-hydroxy-2H-chromen-2-one): synthesis and effects on leukemic cell lines proliferation and NF-κB regulation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.14 | 7.52 |
| Inhibition | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL552054 | — | — | 1 | 7.52 |
| CHEMBL512054 | ALTERSOLANOL A | — | 1 | 6.10 |
| CHEMBL417799 | SANGUINARIUM | 2.0 | 1 | 5.70 |
| CHEMBL15192 | LAPACHONE | 2.0 | 1 | 5.40 |
| CHEMBL2392435 | — | — | 1 | 5.34 |
| CHEMBL514498 | HETERONEMIN | — | 1 | 5.30 |
| CHEMBL464443 | GONIOTHALAMIN | — | 1 | 5.16 |
| CHEMBL140 | CURCUMIN | 3.0 | 1 | 5.10 |
| CHEMBL251958 | FLAVOKAWAIN C | — | 1 | 5.10 |
| CHEMBL3264622 | — | — | 1 | 4.96 |
| CHEMBL3264621 | — | — | 2 | 4.76 |
| CHEMBL7747 | 4-HYDROXYCHALCONE | — | 1 | 4.62 |
| CHEMBL105496 | 4-METHOXY CHALCONE | — | 1 | 4.54 |
| CHEMBL129795 | ISOLIQUIRITIGENIN | — | 1 | 4.50 |
| CHEMBL144686 | HOMOBUTEIN | — | 1 | 4.42 |
| CHEMBL128000 | BUTEIN | — | 1 | 4.42 |
| CHEMBL45068 | PHLORETIN | — | 1 | 4.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL552054 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL512054 | ALTERSOLANOL A | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL417799 | SANGUINARIUM | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL15192 | LAPACHONE | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2392435 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL514498 | HETERONEMIN | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL464443 | GONIOTHALAMIN | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL140 | CURCUMIN | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL251958 | FLAVOKAWAIN C | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL3264622 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3264621 | — | IC50 | = | 17500.0 | nM | 4.76 |
| CHEMBL7747 | 4-HYDROXYCHALCONE | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL105496 | 4-METHOXY CHALCONE | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL129795 | ISOLIQUIRITIGENIN | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL144686 | HOMOBUTEIN | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL128000 | BUTEIN | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL45068 | PHLORETIN | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL3264621 | — | Inhibition | - | % | - |