Assay Detail
Functional
CHEMBL895599
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MEK in mouse colon 26 carcinoma cells assessed as inhibition of ERK phosphorylation by ELISA
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Dual specificity mitogen-activated protein kinase kinase; MEK1/2 (CHEMBL2111289) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
4-anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.16 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL244488 | — | — | 1 | 8.70 |
| CHEMBL442235 | — | — | 1 | 8.40 |
| CHEMBL234887 | — | — | 1 | 8.30 |
| CHEMBL243457 | — | — | 1 | 7.68 |
| CHEMBL396548 | — | — | 1 | 7.52 |
| CHEMBL105442 | CI-1040 | 2.0 | 1 | 7.34 |
| CHEMBL397811 | — | — | 1 | 7.20 |
| CHEMBL387574 | — | — | 1 | 7.17 |
| CHEMBL393283 | — | — | 1 | 7.03 |
| CHEMBL234890 | — | — | 1 | 7.02 |
| CHEMBL391975 | — | — | 1 | 6.96 |
| CHEMBL235780 | — | — | 1 | 6.92 |
| CHEMBL233627 | — | — | 1 | 6.82 |
| CHEMBL395231 | — | — | 1 | 6.75 |
| CHEMBL237257 | — | — | 1 | 6.37 |
| CHEMBL396631 | — | — | 1 | 6.20 |
| CHEMBL233626 | — | — | 1 | 5.41 |
| CHEMBL234237 | — | — | 1 | - |
| CHEMBL237469 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL244488 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL442235 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL234887 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL243457 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL396548 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL105442 | CI-1040 | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL397811 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL387574 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL393283 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL234890 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL391975 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL235780 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL233627 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL395231 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL237257 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL396631 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL233626 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL234237 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL237469 | — | IC50 | > | 5000.0 | nM | - |