Assay Detail
Binding
CHEMBL4048640
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length N-terminal GST-tagged recombinant human MNK2 expressed in baculovirus expression system using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins followed by ATP addition measured after 40 mins by ADP-Glo assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
MAP kinase-interacting serine/threonine-protein kinase 2 (CHEMBL4204) ↗| Type | SINGLE PROTEIN |
| 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 | 8.59 | 9.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4094975 | — | — | 1 | 9.89 |
| CHEMBL4067557 | — | — | 1 | 9.85 |
| CHEMBL4086747 | — | — | 1 | 9.44 |
| CHEMBL4076439 | — | — | 1 | 9.17 |
| CHEMBL4065802 | — | — | 1 | 9.00 |
| CHEMBL4073443 | TOMIVOSERTIB | 2.0 | 1 | 9.00 |
| CHEMBL4084102 | — | — | 1 | 8.92 |
| CHEMBL4064839 | — | — | 1 | 8.92 |
| CHEMBL4073743 | — | — | 1 | 8.74 |
| CHEMBL4086319 | — | — | 1 | 8.64 |
| CHEMBL4091862 | — | — | 1 | 8.59 |
| CHEMBL4100554 | — | — | 1 | 8.24 |
| CHEMBL4094080 | — | — | 1 | 8.11 |
| CHEMBL4062387 | — | — | 1 | 7.72 |
| CHEMBL4099497 | — | — | 1 | 7.35 |
| CHEMBL4071021 | — | — | 1 | 7.24 |
| CHEMBL4086042 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4094975 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL4067557 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL4086747 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL4076439 | — | IC50 | = | 0.68 | nM | 9.17 |
| CHEMBL4065802 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4073443 | TOMIVOSERTIB | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4084102 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4064839 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4073743 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4086319 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4091862 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL4100554 | — | IC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4094080 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4062387 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4099497 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4071021 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4086042 | — | IC50 | = | 61.0 | nM | 7.21 |