Assay Detail
Binding
CHEMBL4048639
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length GST-tagged recombinant human MNK1 expressed in insect cells using Ac-TATKSGSTTKNR-NH2 as substrate preincubated for 5 mins followed by ATP addition measured after 40 mins by ADP-Glo assay
25
Total Activities
25
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 1 (CHEMBL4718) ↗| 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 | 25 | 7.54 | 9.29 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4073743 | — | — | 1 | 9.29 |
| CHEMBL4076439 | — | — | 1 | 9.19 |
| CHEMBL4094975 | — | — | 1 | 9.06 |
| CHEMBL4065802 | — | — | 1 | 8.85 |
| CHEMBL4094080 | — | — | 1 | 8.82 |
| CHEMBL4064839 | — | — | 1 | 8.80 |
| CHEMBL4100554 | — | — | 1 | 8.72 |
| CHEMBL4067557 | — | — | 1 | 8.66 |
| CHEMBL4073443 | TOMIVOSERTIB | 2.0 | 1 | 8.62 |
| CHEMBL4086319 | — | — | 1 | 8.57 |
| CHEMBL4084102 | — | — | 1 | 8.48 |
| CHEMBL4091862 | — | — | 1 | 8.19 |
| CHEMBL4062387 | — | — | 1 | 8.00 |
| CHEMBL4077341 | — | — | 1 | 7.64 |
| CHEMBL4099497 | — | — | 1 | 7.55 |
| CHEMBL1241463 | — | — | 1 | 7.22 |
| CHEMBL4071021 | — | — | 1 | 7.22 |
| CHEMBL4086042 | — | — | 1 | 7.00 |
| CHEMBL4071844 | — | — | 1 | 6.16 |
| CHEMBL1240591 | — | — | 1 | 5.75 |
| CHEMBL4065855 | — | — | 1 | 5.52 |
| CHEMBL4101302 | — | — | 1 | 5.42 |
| CHEMBL4063216 | — | — | 1 | 5.33 |
| CHEMBL1241462 | — | — | 1 | 5.26 |
| CHEMBL4091092 | — | — | 1 | 5.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4073743 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL4076439 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL4094975 | — | IC50 | = | 0.88 | nM | 9.06 |
| CHEMBL4065802 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4094080 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4064839 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4100554 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4067557 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4073443 | TOMIVOSERTIB | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4086319 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4084102 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4091862 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL4062387 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4077341 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4099497 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1241463 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4071021 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4086042 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4071844 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL1240591 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4065855 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4101302 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL4063216 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL1241462 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4091092 | — | IC50 | = | 6400.0 | nM | 5.19 |