Assay Detail
Binding
CHEMBL5523071
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant MNK1 (unknown origin) using TATKSGSTTKNR as substrate preincubated for 15 mins followed by ATP addition and measured after 1 hr by ADP-glo kinase assay
44
Total Activities
44
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
Development of an Imidazopyridazine-Based MNK1/2 Inhibitor for the Treatment of Lymphoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 7.90 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5561655 | — | — | 1 | 8.96 |
| CHEMBL5560868 | — | — | 1 | 8.74 |
| CHEMBL4073443 | TOMIVOSERTIB | 2.0 | 1 | 8.72 |
| CHEMBL5532369 | — | — | 1 | 8.68 |
| CHEMBL5565212 | — | — | 1 | 8.55 |
| CHEMBL5566841 | — | — | 1 | 8.55 |
| CHEMBL5557736 | — | — | 1 | 8.54 |
| CHEMBL5560746 | — | — | 1 | 8.51 |
| CHEMBL5556268 | — | — | 1 | 8.49 |
| CHEMBL5561551 | — | — | 1 | 8.44 |
| CHEMBL5567858 | — | — | 1 | 8.42 |
| CHEMBL5561277 | — | — | 1 | 8.41 |
| CHEMBL5537096 | — | — | 1 | 8.40 |
| CHEMBL5559028 | — | — | 1 | 8.36 |
| CHEMBL5557794 | — | — | 1 | 8.28 |
| CHEMBL5563273 | — | — | 1 | 8.27 |
| CHEMBL5561300 | — | — | 1 | 8.24 |
| CHEMBL5557853 | — | — | 1 | 8.21 |
| CHEMBL5562512 | — | — | 1 | 8.21 |
| CHEMBL5560751 | — | — | 1 | 8.17 |
| CHEMBL5561635 | — | — | 1 | 8.15 |
| CHEMBL5559255 | — | — | 1 | 8.09 |
| CHEMBL5558680 | — | — | 1 | 8.07 |
| CHEMBL5559044 | — | — | 1 | 8.05 |
| CHEMBL5559431 | — | — | 1 | 7.67 |
| CHEMBL5560378 | — | — | 1 | 7.66 |
| CHEMBL4211649 | TINODASERTIB | 2.0 | 1 | 7.65 |
| CHEMBL5568181 | — | — | 1 | 7.61 |
| CHEMBL5560962 | — | — | 1 | 7.51 |
| CHEMBL5556823 | — | — | 1 | 7.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5561655 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5560868 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4073443 | TOMIVOSERTIB | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5532369 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5565212 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5566841 | — | IC50 | = | 2.81 | nM | 8.55 |
| CHEMBL5557736 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5560746 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5556268 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5561551 | — | IC50 | = | 3.61 | nM | 8.44 |
| CHEMBL5567858 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL5561277 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL5537096 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5559028 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5557794 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5563273 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5561300 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL5557853 | — | IC50 | = | 6.13 | nM | 8.21 |
| CHEMBL5562512 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5560751 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL5561635 | — | IC50 | = | 7.01 | nM | 8.15 |
| CHEMBL5559255 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL5558680 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5559044 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5559431 | — | IC50 | = | 21.4 | nM | 7.67 |
| CHEMBL5560378 | — | IC50 | = | 21.7 | nM | 7.66 |
| CHEMBL4211649 | TINODASERTIB | IC50 | = | 22.4 | nM | 7.65 |
| CHEMBL5568181 | — | IC50 | = | 24.4 | nM | 7.61 |
| CHEMBL5560962 | — | IC50 | = | 30.9 | nM | 7.51 |
| CHEMBL5556823 | — | IC50 | = | 33.1 | nM | 7.48 |
| CHEMBL5559368 | — | IC50 | = | 54.5 | nM | 7.26 |
| CHEMBL5561218 | — | IC50 | = | 126.8 | nM | 6.90 |
| CHEMBL5559460 | — | IC50 | = | 150.6 | nM | 6.82 |
| CHEMBL5561011 | — | IC50 | = | 174.7 | nM | 6.76 |
| CHEMBL5555402 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL5568529 | — | IC50 | = | 252.3 | nM | 6.60 |
| CHEMBL5555120 | — | IC50 | = | 250.3 | nM | 6.60 |
| CHEMBL5549927 | — | IC50 | = | 255.4 | nM | 6.59 |
| CHEMBL5567832 | — | IC50 | = | 272.0 | nM | 6.57 |
| CHEMBL5561390 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5566077 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5556376 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5532420 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5555454 | — | IC50 | > | 500.0 | nM | - |