Assay Detail
Binding
CHEMBL672143
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Inhibitory activity against Dual specificity mitogen-activated protein kinase kinase using coupled MEK assay (which uses activated Raf to activate an inactivate GST-MEK)
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
MEK (MAPKK) inhibitors. Part 2: structure-activity relationships of 4-anilino-3-cyano-6,7-dialkoxyquinolines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.48 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL29714 | — | — | 1 | 8.96 |
| CHEMBL414139 | — | — | 1 | 8.62 |
| CHEMBL30728 | — | — | 1 | 8.57 |
| CHEMBL31806 | — | — | 1 | 8.44 |
| CHEMBL30359 | — | — | 1 | 8.38 |
| CHEMBL288081 | — | — | 1 | 8.36 |
| CHEMBL31733 | — | — | 1 | 8.21 |
| CHEMBL30790 | — | — | 1 | 7.85 |
| CHEMBL281662 | — | — | 1 | 7.75 |
| CHEMBL31143 | — | — | 1 | 7.70 |
| CHEMBL282361 | — | — | 1 | 7.68 |
| CHEMBL31497 | — | — | 1 | 7.58 |
| CHEMBL287852 | — | — | 1 | 7.54 |
| CHEMBL31384 | — | — | 1 | 7.37 |
| CHEMBL30763 | — | — | 1 | 7.22 |
| CHEMBL30516 | — | — | 1 | 7.00 |
| CHEMBL31149 | — | — | 1 | 6.96 |
| CHEMBL31639 | — | — | 1 | 6.80 |
| CHEMBL30540 | — | — | 1 | 6.72 |
| CHEMBL282976 | — | — | 1 | 6.70 |
| CHEMBL30597 | — | — | 1 | 6.55 |
| CHEMBL279758 | — | — | 1 | 6.28 |
| CHEMBL30268 | — | — | 1 | 6.26 |
| CHEMBL285956 | — | — | 1 | 5.96 |
| CHEMBL286244 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL29714 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL414139 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL30728 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL31806 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL30359 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL288081 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL31733 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL30790 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL281662 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL31143 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL282361 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL31497 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL287852 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL31384 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL30763 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL30516 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL31149 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL31639 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL30540 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL282976 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL30597 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL279758 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL30268 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL285956 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL286244 | — | IC50 | > | 10000.0 | nM | - |