Assay Detail
Binding
CHEMBL2092012
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MEK1-mediated ERK1 phosphorylation in human A375 cells after 2 hrs by immunoblotting method
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | A-375 |
| 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 novel allosteric mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors possessing bidentate Ser212 interactions.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 8.56 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2087076 | — | — | 1 | 9.40 |
| CHEMBL2087461 | — | — | 1 | 9.05 |
| CHEMBL2087462 | — | — | 1 | 8.96 |
| CHEMBL2087081 | — | — | 1 | 8.82 |
| CHEMBL2087082 | — | — | 1 | 8.62 |
| CHEMBL2087080 | — | — | 1 | 8.43 |
| CHEMBL2087079 | — | — | 1 | 8.19 |
| CHEMBL2087078 | — | — | 1 | 8.14 |
| CHEMBL2087077 | — | — | 1 | 7.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2087076 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL2087461 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL2087462 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2087081 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2087082 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL2087080 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL2087079 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL2087078 | — | EC50 | = | 7.2 | nM | 8.14 |
| CHEMBL2087077 | — | EC50 | = | 34.0 | nM | 7.47 |