Assay Detail
Binding
CHEMBL710955
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Inhibition of ERK-phosphorylation by Raf-MEK-ERK in coupled ELISA
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Expert |
Target
Serine/threonine-protein kinase RAF and Dual specificity mitogen-activated protein kinase kinase 1 (Raf/MEK) (CHEMBL2111351) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships of 3-cyano-4-(phenoxyanilino)quinolines as MEK (MAPKK) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.53 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL414139 | — | — | 1 | 8.62 |
| CHEMBL95002 | — | — | 1 | 8.10 |
| CHEMBL31733 | — | — | 1 | 8.05 |
| CHEMBL97714 | — | — | 1 | 7.75 |
| CHEMBL94965 | — | — | 1 | 7.55 |
| CHEMBL97463 | — | — | 1 | 7.22 |
| CHEMBL98131 | — | — | 1 | 7.05 |
| CHEMBL30763 | — | — | 1 | 7.02 |
| CHEMBL330388 | — | — | 1 | 7.01 |
| CHEMBL98130 | — | — | 1 | 6.90 |
| CHEMBL94956 | — | — | 1 | - |
| CHEMBL419333 | — | — | 1 | - |
| CHEMBL286244 | — | — | 1 | - |
| CHEMBL94586 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL414139 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL95002 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL31733 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL97714 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL94965 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL97463 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL98131 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL30763 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL330388 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL98130 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL94956 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL419333 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL286244 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL94586 | — | IC50 | > | 10000.0 | nM | - |