Assay Detail
Binding
CHEMBL1936645
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Inhibition of human MEK using fluorescein-labelled Erk-tide as substrate after 20 mins by IMAP assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Dual specificity mitogen-activated protein kinase kinase; MEK1/2 (CHEMBL2111289) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Fused thiophene derivatives as MEK inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.31 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1933935 | — | — | 1 | 8.22 |
| CHEMBL1933934 | — | — | 1 | 8.15 |
| CHEMBL1933937 | — | — | 1 | 8.10 |
| CHEMBL1933928 | — | — | 1 | 8.05 |
| CHEMBL1933932 | — | — | 1 | 8.05 |
| CHEMBL1933923 | — | — | 1 | 7.89 |
| CHEMBL1933938 | — | — | 1 | 7.85 |
| CHEMBL1933931 | — | — | 1 | 7.85 |
| CHEMBL1933929 | — | — | 1 | 7.75 |
| CHEMBL1933936 | — | — | 1 | 7.66 |
| CHEMBL1933926 | — | — | 1 | 7.55 |
| CHEMBL1933076 | — | — | 1 | 7.38 |
| CHEMBL1933927 | — | — | 1 | 6.70 |
| CHEMBL1933924 | — | — | 1 | 6.65 |
| CHEMBL1933930 | — | — | 1 | 6.52 |
| CHEMBL1933933 | — | — | 1 | 6.51 |
| CHEMBL1933925 | — | — | 1 | 6.34 |
| CHEMBL1933921 | — | — | 1 | 6.02 |
| CHEMBL1933922 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1933935 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1933934 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL1933937 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1933928 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1933932 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL1933923 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1933938 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1933931 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1933929 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1933936 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL1933926 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1933076 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL1933927 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL1933924 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL1933930 | — | IC50 | = | 305.0 | nM | 6.52 |
| CHEMBL1933933 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL1933925 | — | IC50 | = | 456.0 | nM | 6.34 |
| CHEMBL1933921 | — | IC50 | = | 946.0 | nM | 6.02 |
| CHEMBL1933922 | — | IC50 | = | 2617.0 | nM | 5.58 |