Assay Detail
Binding
CHEMBL4666433
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal DYKDDDDK-tagged MNK1(1 to 424 residues) expressed in baculovirus expression system using TATKSGSTTKNR as substrate preincubated for 10 mins followed by ATP addition and measured after 40 mins by luminescence based assay
29
Total Activities
29
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
Design, synthesis and biological evaluation of pyridone-aminal derivatives as MNK1/2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.14 | 8.48 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4073443 | TOMIVOSERTIB | 2.0 | 1 | 8.48 |
| CHEMBL4757546 | — | — | 1 | 8.15 |
| CHEMBL4796087 | — | — | 1 | 8.06 |
| CHEMBL4780209 | — | — | 1 | 7.98 |
| CHEMBL4754824 | — | — | 1 | 7.68 |
| CHEMBL4787265 | — | — | 1 | 7.29 |
| CHEMBL4740694 | — | — | 1 | 7.28 |
| CHEMBL4793971 | — | — | 1 | 7.26 |
| CHEMBL4741081 | — | — | 1 | 7.16 |
| CHEMBL4797669 | — | — | 1 | 6.90 |
| CHEMBL4760245 | — | — | 1 | 6.80 |
| CHEMBL4751127 | — | — | 1 | 6.62 |
| CHEMBL4784364 | — | — | 1 | 6.41 |
| CHEMBL4741111 | — | — | 1 | 6.38 |
| CHEMBL4757777 | — | — | 1 | 6.33 |
| CHEMBL4743829 | — | — | 1 | 6.32 |
| CHEMBL4752750 | — | — | 1 | 6.32 |
| CHEMBL4747129 | — | — | 1 | - |
| CHEMBL4791921 | — | — | 1 | - |
| CHEMBL4791161 | — | — | 1 | - |
| CHEMBL4776154 | — | — | 1 | - |
| CHEMBL4746641 | — | — | 1 | - |
| CHEMBL4792146 | — | — | 1 | - |
| CHEMBL4797682 | — | — | 1 | - |
| CHEMBL4752964 | — | — | 1 | - |
| CHEMBL4747093 | — | — | 1 | - |
| CHEMBL4747663 | — | — | 1 | - |
| CHEMBL4757325 | — | — | 1 | - |
| CHEMBL4754789 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4073443 | TOMIVOSERTIB | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4757546 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4796087 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL4780209 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL4754824 | — | IC50 | = | 20.7 | nM | 7.68 |
| CHEMBL4787265 | — | IC50 | = | 51.2 | nM | 7.29 |
| CHEMBL4740694 | — | IC50 | = | 52.3 | nM | 7.28 |
| CHEMBL4793971 | — | IC50 | = | 55.2 | nM | 7.26 |
| CHEMBL4741081 | — | IC50 | = | 68.9 | nM | 7.16 |
| CHEMBL4797669 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL4760245 | — | IC50 | = | 159.8 | nM | 6.80 |
| CHEMBL4751127 | — | IC50 | = | 239.8 | nM | 6.62 |
| CHEMBL4784364 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4741111 | — | IC50 | = | 422.0 | nM | 6.38 |
| CHEMBL4757777 | — | IC50 | = | 466.0 | nM | 6.33 |
| CHEMBL4743829 | — | IC50 | = | 479.0 | nM | 6.32 |
| CHEMBL4752750 | — | IC50 | = | 476.0 | nM | 6.32 |
| CHEMBL4747129 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4791921 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4791161 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4776154 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4746641 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4792146 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4797682 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4752964 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4747093 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4747663 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4757325 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL4754789 | — | IC50 | > | 500.0 | nM | - |