Assay Detail
Binding
CHEMBL769165
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of kinase activity of Raf/MEK/ERK kinase cascade in ELISA
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Expert |
Target
Serine/threonine-protein kinase RAF and Dual specificity mitogen-activated protein kinase kinase 1 (Raf/MEK) (CHEMBL2111351) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Aldisine alkaloids from the Philippine sponge Stylissa massa are potent inhibitors of mitogen-activated protein kinase kinase-1 (MEK-1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.01 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.60 |
| CHEMBL359106 | — | — | 1 | 8.52 |
| CHEMBL361708 | HYMENIALDISINE | — | 1 | 8.22 |
| CHEMBL440356 | — | — | 1 | 6.27 |
| CHEMBL255465 | DEBROMOHYMENIALDISINE | — | 1 | 6.05 |
| CHEMBL151430 | — | — | 1 | 5.89 |
| CHEMBL35482 | — | — | 1 | 5.55 |
| CHEMBL397591 | OROIDIN | — | 1 | - |
| CHEMBL356164 | — | — | 1 | - |
| CHEMBL357047 | ALDISIN | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL359106 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL361708 | HYMENIALDISINE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL440356 | — | IC50 | = | 539.0 | nM | 6.27 |
| CHEMBL255465 | DEBROMOHYMENIALDISINE | IC50 | = | 881.0 | nM | 6.05 |
| CHEMBL151430 | — | IC50 | = | 1288.0 | nM | 5.89 |
| CHEMBL35482 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL397591 | OROIDIN | IC50 | > | 2500.0 | nM | - |
| CHEMBL356164 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL357047 | ALDISIN | IC50 | > | 2500.0 | nM | - |