Assay Detail
Binding
CHEMBL675993
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory activity against Dual specificity mitogen-activated protein kinase kinase using direct MEK assay (which by-passes the need for activated Raf by using an activated 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 | 6.79 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL29714 | — | — | 1 | 8.24 |
| CHEMBL414139 | — | — | 1 | 8.15 |
| CHEMBL30728 | — | — | 1 | 7.85 |
| CHEMBL288081 | — | — | 1 | 7.70 |
| CHEMBL30359 | — | — | 1 | 7.64 |
| CHEMBL31733 | — | — | 1 | 7.47 |
| CHEMBL31806 | — | — | 1 | 7.44 |
| CHEMBL30790 | — | — | 1 | 7.37 |
| CHEMBL31143 | — | — | 1 | 7.18 |
| CHEMBL281662 | — | — | 1 | 7.14 |
| CHEMBL31497 | — | — | 1 | 7.09 |
| CHEMBL287852 | — | — | 1 | 7.00 |
| CHEMBL30763 | — | — | 1 | 6.80 |
| CHEMBL31384 | — | — | 1 | 6.68 |
| CHEMBL30516 | — | — | 1 | 6.60 |
| CHEMBL282361 | — | — | 1 | 6.52 |
| CHEMBL31149 | — | — | 1 | 6.50 |
| CHEMBL30540 | — | — | 1 | 6.19 |
| CHEMBL31639 | — | — | 1 | 5.92 |
| CHEMBL30597 | — | — | 1 | 5.89 |
| CHEMBL30268 | — | — | 1 | 5.66 |
| CHEMBL279758 | — | — | 1 | 5.52 |
| CHEMBL282976 | — | — | 1 | 5.48 |
| CHEMBL285956 | — | — | 1 | 5.02 |
| CHEMBL286244 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL29714 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL414139 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL30728 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL288081 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL30359 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL31733 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL31806 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL30790 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL31143 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL281662 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL31497 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL287852 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL30763 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL31384 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL30516 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL282361 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL31149 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL30540 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL31639 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL30597 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL30268 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL279758 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL282976 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL285956 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL286244 | — | IC50 | > | 10000.0 | nM | - |