Assay Detail
Binding
CHEMBL2379959
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Inhibition of MEK1 (unknown origin) after 2 hrs by fluorescence assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of allosteric MEK inhibitors. Part 1: Venturing into underexplored SAR territories.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.34 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | 8.15 |
| CHEMBL2376674 | — | — | 1 | 7.89 |
| CHEMBL2376666 | — | — | 1 | 7.85 |
| CHEMBL2376661 | — | — | 1 | 7.82 |
| CHEMBL2376675 | — | — | 1 | 7.80 |
| CHEMBL2376662 | — | — | 1 | 7.75 |
| CHEMBL2376663 | — | — | 1 | 7.68 |
| CHEMBL2375372 | — | — | 1 | 7.68 |
| CHEMBL2376664 | — | — | 1 | 7.68 |
| CHEMBL2376665 | — | — | 1 | 7.66 |
| CHEMBL2376676 | — | — | 1 | 7.58 |
| CHEMBL2376684 | — | — | 1 | 7.55 |
| CHEMBL2376667 | — | — | 1 | 7.50 |
| CHEMBL2376660 | — | — | 1 | 7.44 |
| CHEMBL2376673 | — | — | 1 | 7.37 |
| CHEMBL2376686 | — | — | 1 | 7.32 |
| CHEMBL2376683 | — | — | 1 | 7.27 |
| CHEMBL2376671 | — | — | 1 | 7.20 |
| CHEMBL2376668 | — | — | 1 | 7.20 |
| CHEMBL2376672 | — | — | 1 | 7.16 |
| CHEMBL2376680 | — | — | 1 | 7.14 |
| CHEMBL2376669 | — | — | 1 | 7.13 |
| CHEMBL2376682 | — | — | 1 | 7.12 |
| CHEMBL1614701 | SELUMETINIB | 4.0 | 1 | 7.10 |
| CHEMBL2376678 | — | — | 1 | 7.02 |
| CHEMBL2376670 | — | — | 1 | 7.02 |
| CHEMBL2376681 | — | — | 1 | 7.00 |
| CHEMBL2376677 | — | — | 1 | 6.74 |
| CHEMBL2376685 | — | — | 1 | 6.27 |
| CHEMBL2376679 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL507361 | MIRDAMETINIB | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL2376674 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL2376666 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2376661 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2376675 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL2376662 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2376663 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2375372 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2376664 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2376665 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2376676 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2376684 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2376667 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2376660 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2376673 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2376686 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL2376683 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2376671 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2376668 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL2376672 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2376680 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL2376669 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2376682 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL1614701 | SELUMETINIB | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL2376678 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL2376670 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL2376681 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL2376677 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL2376685 | — | IC50 | = | 539.0 | nM | 6.27 |
| CHEMBL2376679 | — | IC50 | = | 1000.0 | nM | 6.00 |