Assay Detail
Binding
CHEMBL873739
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Inhibition of MEK-1 activity
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of isothiazole-4-carboxamidines derivatives as a novel class of allosteric MEK1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 56 | 7.09 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL214613 | — | — | 1 | 7.70 |
| CHEMBL214734 | — | — | 1 | 7.70 |
| CHEMBL385446 | — | — | 1 | 7.58 |
| CHEMBL387184 | — | — | 1 | 7.57 |
| CHEMBL214614 | — | — | 1 | 7.57 |
| CHEMBL385905 | — | — | 1 | 7.55 |
| CHEMBL269696 | — | — | 1 | 7.52 |
| CHEMBL215193 | — | — | 1 | 7.52 |
| CHEMBL214901 | — | — | 1 | 7.50 |
| CHEMBL437331 | — | — | 1 | 7.48 |
| CHEMBL383858 | — | — | 1 | 7.47 |
| CHEMBL263039 | — | — | 1 | 7.47 |
| CHEMBL216449 | — | — | 1 | 7.47 |
| CHEMBL216325 | — | — | 1 | 7.46 |
| CHEMBL215038 | — | — | 1 | 7.43 |
| CHEMBL375609 | — | — | 1 | 7.42 |
| CHEMBL385059 | — | — | 1 | 7.40 |
| CHEMBL214587 | — | — | 1 | 7.40 |
| CHEMBL213992 | — | — | 1 | 7.38 |
| CHEMBL216832 | — | — | 1 | 7.36 |
| CHEMBL265478 | — | — | 1 | 7.36 |
| CHEMBL386230 | — | — | 1 | 7.35 |
| CHEMBL384012 | — | — | 1 | 7.34 |
| CHEMBL216833 | — | — | 1 | 7.34 |
| CHEMBL217414 | — | — | 1 | 7.28 |
| CHEMBL386469 | — | — | 1 | 7.25 |
| CHEMBL424897 | — | — | 1 | 7.24 |
| CHEMBL217310 | — | — | 1 | 7.24 |
| CHEMBL217832 | — | — | 1 | 7.24 |
| CHEMBL214683 | — | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL214613 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL214734 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL385446 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL387184 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL214614 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL385905 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL269696 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL215193 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL214901 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL437331 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL383858 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL263039 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL216449 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL216325 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL215038 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL375609 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL385059 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL214587 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL213992 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL216832 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL265478 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL386230 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL384012 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL216833 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL217414 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL386469 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL217310 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL217832 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL214683 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL424897 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL217415 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL211359 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL214816 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL217126 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL214032 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL214425 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL215012 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL384784 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL217130 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL217833 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL214977 | — | IC50 | = | 137.0 | nM | 6.86 |
| CHEMBL425980 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL385203 | — | IC50 | = | 145.0 | nM | 6.84 |
| CHEMBL214636 | — | IC50 | = | 147.0 | nM | 6.83 |
| CHEMBL217117 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL413636 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL216500 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL215011 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL253116 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL217416 | — | IC50 | = | 280.0 | nM | 6.55 |