Assay Detail
Binding
CHEMBL1686836
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Inhibition of MEK1 by IMAP assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Dual specificity mitogen-activated protein kinase kinase 1 (CHEMBL3587) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.07 | 8.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1684075 | — | — | 1 | 8.51 |
| CHEMBL1615025 | TAK-733 | 2.0 | 1 | 8.49 |
| CHEMBL1684070 | — | — | 1 | 8.49 |
| CHEMBL1684074 | — | — | 1 | 8.48 |
| CHEMBL1684067 | — | — | 1 | 8.42 |
| CHEMBL1684073 | — | — | 1 | 8.40 |
| CHEMBL1684063 | — | — | 1 | 8.34 |
| CHEMBL1684069 | — | — | 1 | 8.32 |
| CHEMBL1684062 | — | — | 1 | 8.31 |
| CHEMBL1684071 | — | — | 1 | 8.30 |
| CHEMBL1681812 | — | — | 1 | 8.23 |
| CHEMBL1684064 | — | — | 1 | 8.08 |
| CHEMBL1684072 | — | — | 1 | 8.07 |
| CHEMBL1684061 | — | — | 1 | 8.01 |
| CHEMBL1684068 | — | — | 1 | 7.80 |
| CHEMBL1684060 | — | — | 1 | 7.58 |
| CHEMBL1684065 | — | — | 1 | 7.28 |
| CHEMBL1684066 | — | — | 1 | 6.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1684075 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL1615025 | TAK-733 | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1684070 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL1684074 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL1684067 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL1684073 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL1684063 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL1684069 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL1684062 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL1684071 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1681812 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL1684064 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL1684072 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL1684061 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL1684068 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1684060 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL1684065 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL1684066 | — | IC50 | = | 740.0 | nM | 6.13 |