Assay Detail
Binding
CHEMBL2092007
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MEK1-mediated ERK1 phosphorylation after 30 mins by HTRF assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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 |
|---|---|---|---|
| IC50 | 11 | 7.27 | 7.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2087076 | — | — | 1 | 7.89 |
| CHEMBL2087080 | — | — | 1 | 7.82 |
| CHEMBL2087461 | — | — | 1 | 7.82 |
| CHEMBL2087462 | — | — | 1 | 7.70 |
| CHEMBL2087077 | — | — | 1 | 7.60 |
| CHEMBL2087078 | — | — | 1 | 7.46 |
| CHEMBL2087081 | — | — | 1 | 7.10 |
| CHEMBL2087082 | — | — | 1 | 7.03 |
| CHEMBL2087079 | — | — | 1 | 6.90 |
| CHEMBL2087460 | — | — | 1 | 5.34 |
| CHEMBL2087083 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2087076 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2087080 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2087461 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2087462 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2087077 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2087078 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL2087081 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL2087082 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL2087079 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL2087460 | — | IC50 | = | 4546.0 | nM | 5.34 |
| CHEMBL2087083 | — | IC50 | > | 10000.0 | nM | - |