Assay Detail
Functional
CHEMBL645952
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Ability to antagonise AP-1 transcriptional activity
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Target
Dual specificity mitogen-activated protein kinase kinase; MEK1/2 (CHEMBL2111289) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.03 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL95069 | — | — | 1 | 6.40 |
| CHEMBL34704 | — | — | 1 | 6.00 |
| CHEMBL329492 | — | — | 1 | 5.92 |
| CHEMBL97067 | — | — | 1 | 5.19 |
| CHEMBL97406 | — | — | 1 | 5.18 |
| CHEMBL330393 | — | — | 1 | 5.12 |
| CHEMBL318939 | — | — | 1 | 5.10 |
| CHEMBL316635 | — | — | 1 | 5.10 |
| CHEMBL317720 | — | — | 1 | 4.98 |
| CHEMBL329698 | — | — | 1 | 4.91 |
| CHEMBL95400 | — | — | 1 | 4.88 |
| CHEMBL97586 | — | — | 1 | 4.78 |
| CHEMBL97205 | — | — | 1 | 4.74 |
| CHEMBL94565 | — | — | 1 | 4.74 |
| CHEMBL95905 | — | — | 1 | 4.73 |
| CHEMBL95728 | — | — | 1 | 4.66 |
| CHEMBL97724 | — | — | 1 | 4.60 |
| CHEMBL316536 | — | — | 1 | 4.58 |
| CHEMBL330195 | — | — | 1 | 4.54 |
| CHEMBL316510 | — | — | 1 | 4.37 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL95069 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL34704 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL329492 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL97067 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL97406 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL330393 | — | IC50 | = | 7600.0 | nM | 5.12 |
| CHEMBL318939 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL316635 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL317720 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL329698 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL95400 | — | IC50 | = | 13300.0 | nM | 4.88 |
| CHEMBL97586 | — | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL97205 | — | IC50 | = | 18100.0 | nM | 4.74 |
| CHEMBL94565 | — | IC50 | = | 18400.0 | nM | 4.74 |
| CHEMBL95905 | — | IC50 | = | 18700.0 | nM | 4.73 |
| CHEMBL95728 | — | IC50 | = | 21700.0 | nM | 4.66 |
| CHEMBL97724 | — | IC50 | = | 25100.0 | nM | 4.60 |
| CHEMBL316536 | — | IC50 | = | 26200.0 | nM | 4.58 |
| CHEMBL330195 | — | IC50 | = | 28900.0 | nM | 4.54 |
| CHEMBL316510 | — | IC50 | = | 42500.0 | nM | 4.37 |