Assay Detail
Binding
CHEMBL4220448
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MEK1 (unknown origin) using Ser/Thr 03 peptide substrate after 4 hrs by fluorescence assay
15
Total Activities
15
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
Discovery of EBI-1051: A novel and orally efficacious MEK inhibitor with benzofuran scaffold.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.87 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4229260 | — | — | 1 | 8.47 |
| CHEMBL4228425 | — | — | 1 | 8.41 |
| CHEMBL4225654 | — | — | 1 | 8.24 |
| CHEMBL4226300 | — | — | 1 | 8.22 |
| CHEMBL4225401 | — | — | 1 | 8.15 |
| CHEMBL4228161 | — | — | 1 | 8.12 |
| CHEMBL1614701 | SELUMETINIB | 4.0 | 1 | 8.05 |
| CHEMBL4228999 | — | — | 1 | 7.97 |
| CHEMBL4225180 | — | — | 1 | 7.67 |
| CHEMBL4225400 | — | — | 1 | 7.53 |
| CHEMBL4228687 | — | — | 1 | 7.20 |
| CHEMBL4227816 | — | — | 1 | 6.36 |
| CHEMBL4226967 | — | — | 1 | - |
| CHEMBL4227199 | — | — | 1 | - |
| CHEMBL4224923 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4229260 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4228425 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4225654 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4226300 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4225401 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4228161 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL1614701 | SELUMETINIB | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4228999 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL4225180 | — | IC50 | = | 21.5 | nM | 7.67 |
| CHEMBL4225400 | — | IC50 | = | 29.8 | nM | 7.53 |
| CHEMBL4228687 | — | IC50 | = | 62.8 | nM | 7.20 |
| CHEMBL4227816 | — | IC50 | = | 441.0 | nM | 6.36 |
| CHEMBL4226967 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4227199 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL4224923 | — | IC50 | > | 1000.0 | nM | - |