Assay Detail
Binding
CHEMBL4380948
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MNK1/MNK2 in human HeLa cells overexpressing eIF4E assessed as reduction in eIF4E phosphorylation at Ser209 residue after 2 hrs by Alphascreen SureFly assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HeLa |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
MAP kinase-interacting serine/threonine-protein kinase 1/2 (CHEMBL3883293) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Stepwise Evolution of Fragment Hits against MAPK Interacting Kinases 1 and 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.17 | 6.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4442209 | — | — | 1 | 6.80 |
| CHEMBL4587832 | — | — | 1 | 6.70 |
| CHEMBL4569209 | — | — | 1 | 6.50 |
| CHEMBL4462099 | — | — | 1 | 6.43 |
| CHEMBL4443472 | — | — | 1 | 6.41 |
| CHEMBL4587472 | — | — | 1 | 6.24 |
| CHEMBL4457274 | — | — | 1 | 6.12 |
| CHEMBL4450463 | — | — | 1 | 6.07 |
| CHEMBL4588193 | — | — | 1 | 6.03 |
| CHEMBL4441602 | — | — | 1 | 5.77 |
| CHEMBL4586717 | — | — | 1 | 5.72 |
| CHEMBL4465294 | — | — | 1 | 5.70 |
| CHEMBL4440223 | — | — | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4442209 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4587832 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4569209 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4462099 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4443472 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4587472 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4457274 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4450463 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL4588193 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4441602 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4586717 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4465294 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4440223 | — | IC50 | = | 2200.0 | nM | 5.66 |