Assay Detail
Binding
CHEMBL5349478
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Inhibition of MEK1 (unknown origin)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optically activated MEK1/2 inhibitors (Opti-MEKi) as potential antimelanoma agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 8.46 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5433950 | — | — | 1 | 9.15 |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | 9.00 |
| CHEMBL2146883 | COBIMETINIB | 4.0 | 1 | 8.38 |
| CHEMBL3187723 | BINIMETINIB | 4.0 | 1 | 7.92 |
| CHEMBL1614701 | SELUMETINIB | 4.0 | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5433950 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL507361 | MIRDAMETINIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL2146883 | COBIMETINIB | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3187723 | BINIMETINIB | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1614701 | SELUMETINIB | IC50 | = | 14.0 | nM | 7.85 |