Assay Detail
Binding
CHEMBL4048641
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MNK1/2 in human HCT116 cells assessed as decrease in eIF4E phosphorylation at Ser209 after 2 hrs by HTRF assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
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 | 17 | 7.48 | 10.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4086747 | — | — | 1 | 10.08 |
| CHEMBL4073743 | — | — | 1 | 9.51 |
| CHEMBL4094975 | — | — | 1 | 9.21 |
| CHEMBL4076439 | — | — | 1 | 9.10 |
| CHEMBL4064839 | — | — | 1 | 8.74 |
| CHEMBL4073443 | TOMIVOSERTIB | 2.0 | 1 | 8.22 |
| CHEMBL4067557 | — | — | 1 | 7.92 |
| CHEMBL4086319 | — | — | 1 | 7.91 |
| CHEMBL4065802 | — | — | 1 | 7.62 |
| CHEMBL4084102 | — | — | 1 | 7.14 |
| CHEMBL4094080 | — | — | 1 | 6.92 |
| CHEMBL4062387 | — | — | 1 | 6.80 |
| CHEMBL4100554 | — | — | 1 | 6.37 |
| CHEMBL4091862 | — | — | 1 | 6.24 |
| CHEMBL4071021 | — | — | 1 | 5.42 |
| CHEMBL4086042 | — | — | 1 | 5.36 |
| CHEMBL4099497 | — | — | 1 | 4.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4086747 | — | IC50 | = | 0.084 | nM | 10.08 |
| CHEMBL4073743 | — | IC50 | = | 0.31 | nM | 9.51 |
| CHEMBL4094975 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL4076439 | — | IC50 | = | 0.79 | nM | 9.10 |
| CHEMBL4064839 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4073443 | TOMIVOSERTIB | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4067557 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4086319 | — | IC50 | = | 12.3 | nM | 7.91 |
| CHEMBL4065802 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4084102 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL4094080 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4062387 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4100554 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL4091862 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL4071021 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4086042 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4099497 | — | IC50 | = | 28000.0 | nM | 4.55 |