Assay Detail
Binding
CHEMBL4822879
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-fused human full length recombinant MNK2 (1 to 465 residues) expressed in baculovirus-infected Sf21 cells using TATKSGSTTKNR as substrate preincubated with enzyme and substrate for 10 mins followed by ATP addition and measured after 40 mins by ADP-glo luminescence assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf21 |
| 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
Design, synthesis and biological evaluation of imidazopyridazine derivatives containing isoquinoline group as potent MNK1/2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.88 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4858035 | — | — | 1 | 8.82 |
| CHEMBL4857770 | — | — | 1 | 8.60 |
| CHEMBL4865340 | — | — | 1 | 8.54 |
| CHEMBL4864827 | — | — | 1 | 8.49 |
| CHEMBL4878199 | — | — | 1 | 8.47 |
| CHEMBL4872637 | — | — | 1 | 8.28 |
| CHEMBL4862069 | — | — | 1 | 8.18 |
| CHEMBL4852274 | — | — | 1 | 8.05 |
| CHEMBL4211649 | TINODASERTIB | 2.0 | 1 | 8.03 |
| CHEMBL4862651 | — | — | 1 | 7.80 |
| CHEMBL4857509 | — | — | 1 | 7.73 |
| CHEMBL4865426 | — | — | 1 | 7.71 |
| CHEMBL4869957 | — | — | 1 | 7.59 |
| CHEMBL4879113 | — | — | 1 | 7.57 |
| CHEMBL4869672 | — | — | 1 | 7.29 |
| CHEMBL4848427 | — | — | 1 | 6.67 |
| CHEMBL4862514 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4858035 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4857770 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4865340 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4864827 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4878199 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4872637 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4862069 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL4852274 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL4211649 | TINODASERTIB | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4862651 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL4857509 | — | IC50 | = | 18.5 | nM | 7.73 |
| CHEMBL4865426 | — | IC50 | = | 19.4 | nM | 7.71 |
| CHEMBL4869957 | — | IC50 | = | 25.7 | nM | 7.59 |
| CHEMBL4879113 | — | IC50 | = | 26.7 | nM | 7.57 |
| CHEMBL4869672 | — | IC50 | = | 51.2 | nM | 7.29 |
| CHEMBL4848427 | — | IC50 | = | 215.8 | nM | 6.67 |
| CHEMBL4862514 | — | IC50 | = | 635.7 | nM | 6.20 |