Assay Detail
Binding
CHEMBL711119
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Non-competitive inhibition of the dual specificity kinase MEK
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.86 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL329492 | — | — | 1 | 6.52 |
| CHEMBL95069 | — | — | 1 | 6.52 |
| CHEMBL94971 | — | — | 1 | 6.40 |
| CHEMBL317720 | — | — | 1 | 6.30 |
| CHEMBL100473 | U-0126 | — | 1 | 6.30 |
| CHEMBL316510 | — | — | 1 | 6.16 |
| CHEMBL97406 | — | — | 1 | 6.05 |
| CHEMBL329698 | — | — | 1 | 6.05 |
| CHEMBL330393 | — | — | 1 | 6.05 |
| CHEMBL318939 | — | — | 1 | 5.96 |
| CHEMBL97724 | — | — | 1 | 5.85 |
| CHEMBL94565 | — | — | 1 | 5.72 |
| CHEMBL316635 | — | — | 1 | 5.72 |
| CHEMBL95400 | — | — | 1 | 5.70 |
| CHEMBL95728 | — | — | 1 | 5.68 |
| CHEMBL330195 | — | — | 1 | 5.68 |
| CHEMBL95057 | — | — | 1 | 5.68 |
| CHEMBL97067 | — | — | 1 | 5.55 |
| CHEMBL95905 | — | — | 1 | 5.50 |
| CHEMBL97586 | — | — | 1 | 5.35 |
| CHEMBL97205 | — | — | 1 | 5.32 |
| CHEMBL316536 | — | — | 1 | 4.87 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL329492 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL95069 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL94971 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL317720 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL100473 | U-0126 | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL316510 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL97406 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL329698 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL330393 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL318939 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL97724 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL94565 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL316635 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL95400 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL95728 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL330195 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL95057 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL97067 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL95905 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL97586 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL97205 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL316536 | — | IC50 | = | 13500.0 | nM | 4.87 |