Assay Detail
Functional
CHEMBL4048727
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vivo inhibition of MNK1/2 in human TMD8 cells xenografted in NOD SCID mouse assessed as reduction in eIF4E phosphorylation at Ser209 administered as po qd for 14 days measured over 24 hrs post last dose by Western blot method
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Structure-based Design of Pyridone-Aminal eFT508 Targeting Dysregulated Translation by Selective Mitogen-activated Protein Kinase Interacting Kinases 1 and 2 (MNK1/2) Inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 1 | 7.80 | 7.80 |
| IC90 | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4073443 | TOMIVOSERTIB | 2.0 | 2 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4073443 | TOMIVOSERTIB | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL4073443 | TOMIVOSERTIB | IC90 | = | 376.0 | nM | - |