Assay Detail
Binding
CHEMBL5588080
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Inhibition of MEK1 (unknown origin)
8
Total Activities
8
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
Design, Synthesis, and Biological Evaluation of 5-Amino-4-fluoro-1<i>H</i>-benzo[<i>d</i>]imidazole-6-carboxamide Derivatives as Novel and Potential MEK/RAF Complex Inhibitors Based on the "Clamp" Strategy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.42 | 8.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5596553 | — | — | 1 | 8.10 |
| CHEMBL5597316 | — | — | 1 | 7.55 |
| CHEMBL5597799 | — | — | 1 | 7.38 |
| CHEMBL5596257 | — | — | 1 | 7.13 |
| CHEMBL5597586 | — | — | 1 | 6.92 |
| CHEMBL5598115 | — | — | 1 | - |
| CHEMBL3187723 | BINIMETINIB | 4.0 | 1 | - |
| CHEMBL3264002 | AVUTOMETINIB | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5596553 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5597316 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5597799 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5596257 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL5597586 | — | IC50 | = | 119.0 | nM | 6.92 |
| CHEMBL5598115 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL3187723 | BINIMETINIB | IC50 | - | — | - | |
| CHEMBL3264002 | AVUTOMETINIB | IC50 | - | — | - |