Assay Detail
Binding
CHEMBL4189498
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MNK1/2 in human HeLa cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by AlphaScreen assay
24
Total Activities
24
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 | Intermediate |
Target
MAP kinase-interacting serine/threonine-protein kinase 1/2 (CHEMBL3883293) ↗| Type | PROTEIN FAMILY |
| Organism | Homo sapiens |
Publication
Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 6.24 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4209905 | — | — | 1 | 6.89 |
| CHEMBL4209496 | — | — | 1 | 6.72 |
| CHEMBL4208772 | — | — | 1 | 6.66 |
| CHEMBL4204438 | — | — | 1 | 6.64 |
| CHEMBL4213168 | — | — | 1 | 6.49 |
| CHEMBL4211649 | TINODASERTIB | 2.0 | 1 | 6.49 |
| CHEMBL4203889 | — | — | 1 | 6.38 |
| CHEMBL4216109 | — | — | 1 | 6.37 |
| CHEMBL4216991 | — | — | 1 | 6.36 |
| CHEMBL4208246 | — | — | 1 | 6.19 |
| CHEMBL4213819 | — | — | 1 | 6.13 |
| CHEMBL4211757 | — | — | 1 | 6.12 |
| CHEMBL4213023 | — | — | 1 | 6.09 |
| CHEMBL4212480 | — | — | 1 | 5.97 |
| CHEMBL4212307 | — | — | 1 | 5.92 |
| CHEMBL4216093 | — | — | 1 | 5.88 |
| CHEMBL4202593 | — | — | 1 | 5.79 |
| CHEMBL4206349 | — | — | 1 | 5.72 |
| CHEMBL4212200 | — | — | 1 | 5.70 |
| CHEMBL4217366 | — | — | 1 | - |
| CHEMBL4214092 | — | — | 1 | - |
| CHEMBL4204506 | — | — | 1 | - |
| CHEMBL4208890 | — | — | 1 | - |
| CHEMBL4208627 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4209905 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4209496 | — | IC50 | = | 189.0 | nM | 6.72 |
| CHEMBL4208772 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4204438 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL4213168 | — | IC50 | = | 326.0 | nM | 6.49 |
| CHEMBL4211649 | TINODASERTIB | IC50 | = | 321.0 | nM | 6.49 |
| CHEMBL4203889 | — | IC50 | = | 421.0 | nM | 6.38 |
| CHEMBL4216109 | — | IC50 | = | 431.0 | nM | 6.37 |
| CHEMBL4216991 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4208246 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL4213819 | — | IC50 | = | 748.0 | nM | 6.13 |
| CHEMBL4211757 | — | IC50 | = | 759.0 | nM | 6.12 |
| CHEMBL4213023 | — | IC50 | = | 819.0 | nM | 6.09 |
| CHEMBL4212480 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL4212307 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL4216093 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL4202593 | — | IC50 | = | 1630.0 | nM | 5.79 |
| CHEMBL4206349 | — | IC50 | = | 1920.0 | nM | 5.72 |
| CHEMBL4212200 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL4217366 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4214092 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4204506 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4208890 | — | IC50 | > | 2500.0 | nM | - |
| CHEMBL4208627 | — | IC50 | > | 2500.0 | nM | - |