Assay Detail
Binding
CHEMBL4735409
Review assay metadata, readout intent, target linkage, and publication context from the same page.
ATP-competitive inhibition of recombinant human full-length N-terminal GST-fused MNK1 (1 to 424 residues) expressed in baculovirus expression system using GRSRSRSRSR as substrate and varying levels of ATP by ADP-glo luminescence assay
2
Total Activities
2
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
Discovery of indazole-pyridinone derivatives as a novel class of potent and selective MNK1/2 kinase inhibitors that protecting against endotoxin-induced septic shock.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 2 | 7.86 | 7.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4752141 | — | — | 1 | 7.87 |
| CHEMBL4764756 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4752141 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL4764756 | — | Ki | = | 14.1 | nM | 7.85 |