Assay Detail
Binding
CHEMBL731425
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MEK1 phosphorylation by activated human recombinant Raf
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗| Type | SINGLE PROTEIN |
| 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 | 5.93 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.60 |
| CHEMBL397591 | OROIDIN | — | 1 | 5.60 |
| CHEMBL356164 | — | — | 1 | 5.60 |
| CHEMBL361708 | HYMENIALDISINE | — | 1 | 5.60 |
| CHEMBL255465 | DEBROMOHYMENIALDISINE | — | 1 | 5.60 |
| CHEMBL151430 | — | — | 1 | 5.60 |
| CHEMBL357047 | ALDISIN | — | 1 | 5.60 |
| CHEMBL440356 | — | — | 1 | 5.60 |
| CHEMBL359106 | — | — | 1 | 5.60 |
| CHEMBL35482 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL397591 | OROIDIN | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL356164 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL361708 | HYMENIALDISINE | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL255465 | DEBROMOHYMENIALDISINE | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL151430 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL357047 | ALDISIN | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL440356 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL359106 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL35482 | — | IC50 | > | 10000.0 | nM | - |