Assay Detail
Binding
CHEMBL5523077
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of eIF4E phosphorylation at ser209 residue in human HeLa cells incubated for 2 hrs by HTRF assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Eukaryotic translation initiation factor 4E (CHEMBL4848) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Development of an Imidazopyridazine-Based MNK1/2 Inhibitor for the Treatment of Lymphoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.61 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4073443 | TOMIVOSERTIB | 2.0 | 1 | 8.27 |
| CHEMBL5561277 | — | — | 1 | 7.28 |
| CHEMBL5561300 | — | — | 1 | 7.15 |
| CHEMBL5561635 | — | — | 1 | 7.04 |
| CHEMBL5559028 | — | — | 1 | 7.04 |
| CHEMBL5532369 | — | — | 1 | 6.96 |
| CHEMBL5561551 | — | — | 1 | 6.93 |
| CHEMBL5563273 | — | — | 1 | 6.91 |
| CHEMBL5557794 | — | — | 1 | 6.89 |
| CHEMBL5556268 | — | — | 1 | 6.84 |
| CHEMBL5560751 | — | — | 1 | 6.67 |
| CHEMBL5537096 | — | — | 1 | 6.58 |
| CHEMBL5559255 | — | — | 1 | 6.57 |
| CHEMBL5560868 | — | — | 1 | 6.48 |
| CHEMBL5567858 | — | — | 1 | 6.44 |
| CHEMBL5562512 | — | — | 1 | 6.40 |
| CHEMBL5560746 | — | — | 1 | 6.21 |
| CHEMBL4211649 | TINODASERTIB | 2.0 | 1 | 6.19 |
| CHEMBL5557736 | — | — | 1 | 6.14 |
| CHEMBL5561655 | — | — | 1 | 5.95 |
| CHEMBL5556823 | — | — | 1 | 5.83 |
| CHEMBL5559044 | — | — | 1 | 4.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4073443 | TOMIVOSERTIB | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5561277 | — | IC50 | = | 52.5 | nM | 7.28 |
| CHEMBL5561300 | — | IC50 | = | 71.5 | nM | 7.15 |
| CHEMBL5561635 | — | IC50 | = | 91.5 | nM | 7.04 |
| CHEMBL5559028 | — | IC50 | = | 90.5 | nM | 7.04 |
| CHEMBL5532369 | — | IC50 | = | 110.8 | nM | 6.96 |
| CHEMBL5561551 | — | IC50 | = | 118.6 | nM | 6.93 |
| CHEMBL5563273 | — | IC50 | = | 122.2 | nM | 6.91 |
| CHEMBL5557794 | — | IC50 | = | 128.9 | nM | 6.89 |
| CHEMBL5556268 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL5560751 | — | IC50 | = | 213.1 | nM | 6.67 |
| CHEMBL5537096 | — | IC50 | = | 261.7 | nM | 6.58 |
| CHEMBL5559255 | — | IC50 | = | 269.4 | nM | 6.57 |
| CHEMBL5560868 | — | IC50 | = | 334.5 | nM | 6.48 |
| CHEMBL5567858 | — | IC50 | = | 364.1 | nM | 6.44 |
| CHEMBL5562512 | — | IC50 | = | 397.7 | nM | 6.40 |
| CHEMBL5560746 | — | IC50 | = | 617.3 | nM | 6.21 |
| CHEMBL4211649 | TINODASERTIB | IC50 | = | 646.2 | nM | 6.19 |
| CHEMBL5557736 | — | IC50 | = | 721.8 | nM | 6.14 |
| CHEMBL5561655 | — | IC50 | = | 1114.5 | nM | 5.95 |
| CHEMBL5556823 | — | IC50 | = | 1495.0 | nM | 5.83 |
| CHEMBL5559044 | — | IC50 | = | 24463.0 | nM | 4.61 |