Assay Detail
Binding
CHEMBL3820565
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of purified MEK1 (unknown origin) assessed as reduction in phosphorylation of inactive Erk2 incubated for 30 mins by Kinase-Glo luminescent kinase assay
7
Total Activities
7
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 Bifunctional Oncogenic Target Inhibitors against Allosteric Mitogen-Activated Protein Kinase (MEK1) and Phosphatidylinositol 3-Kinase (PI3K).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 8.97 | 10.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3819302 | — | — | 1 | 10.82 |
| CHEMBL3818677 | — | — | 1 | 10.72 |
| CHEMBL3819622 | — | — | 1 | 9.30 |
| CHEMBL244488 | — | — | 1 | 7.89 |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | 7.82 |
| CHEMBL3819520 | — | — | 1 | 7.25 |
| CHEMBL3818606 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3819302 | — | IC50 | = | 0.015 | nM | 10.82 |
| CHEMBL3818677 | — | IC50 | = | 0.019 | nM | 10.72 |
| CHEMBL3819622 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL244488 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL507361 | MIRDAMETINIB | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3819520 | — | IC50 | = | 56.7 | nM | 7.25 |
| CHEMBL3818606 | — | IC50 | = | 0.00715 | nM | - |