Assay Detail
Binding
CHEMBL2016104
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MEK1-mediated ERK1 phosphorylation using IPTTPITTYFFFK-5FAM-COOH as substrate by fluorescent polarization assay
21
Total Activities
21
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
Design and synthesis of orally available MEK inhibitors with potent in vivo antitumor efficacy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.49 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2012893 | — | — | 1 | 8.05 |
| CHEMBL2012894 | — | — | 1 | 7.96 |
| CHEMBL2012890 | — | — | 1 | 7.85 |
| CHEMBL2012891 | — | — | 1 | 7.77 |
| CHEMBL1169814 | — | — | 1 | 7.75 |
| CHEMBL2012896 | — | — | 1 | 7.75 |
| CHEMBL2012892 | — | — | 1 | 7.70 |
| CHEMBL2012902 | — | — | 1 | 7.60 |
| CHEMBL2012907 | — | — | 1 | 7.54 |
| CHEMBL2012899 | — | — | 1 | 7.50 |
| CHEMBL2012901 | — | — | 1 | 7.44 |
| CHEMBL2012908 | — | — | 1 | 7.42 |
| CHEMBL2012905 | — | — | 1 | 7.41 |
| CHEMBL2012900 | — | — | 1 | 7.39 |
| CHEMBL2012898 | — | — | 1 | 7.28 |
| CHEMBL2012895 | — | — | 1 | 7.27 |
| CHEMBL2012903 | — | — | 1 | 7.24 |
| CHEMBL2012906 | — | — | 1 | 7.16 |
| CHEMBL2012897 | — | — | 1 | 7.12 |
| CHEMBL2012904 | — | — | 1 | 7.03 |
| CHEMBL2012909 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2012893 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL2012894 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2012890 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2012891 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL1169814 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2012896 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2012892 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL2012902 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2012907 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2012899 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL2012901 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL2012908 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2012905 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2012900 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2012898 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL2012895 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL2012903 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL2012906 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2012897 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL2012904 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL2012909 | — | IC50 | = | 109.0 | nM | 6.96 |