Assay Detail
Binding
CHEMBL4735374
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full-length N-terminal GST-fused MNK2 (1 to 465 residues) expressed in baculovirus expression system using GRSRSRSRSR as substrate measured after 2 hrs by ADP-glo luminescence assay
28
Total Activities
28
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 2 (CHEMBL4204) ↗| 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 |
|---|---|---|---|
| IC50 | 28 | 7.33 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4752141 | — | — | 1 | 8.40 |
| CHEMBL4787269 | — | — | 1 | 8.30 |
| CHEMBL4764756 | — | — | 1 | 8.22 |
| CHEMBL4785028 | — | — | 1 | 8.10 |
| CHEMBL4743561 | — | — | 1 | 7.92 |
| CHEMBL4757431 | — | — | 1 | 7.68 |
| CHEMBL4755524 | — | — | 1 | 7.50 |
| CHEMBL4746396 | — | — | 1 | 7.50 |
| CHEMBL4795993 | — | — | 1 | 7.43 |
| CHEMBL4791136 | — | — | 1 | 7.42 |
| CHEMBL4749973 | — | — | 1 | 7.40 |
| CHEMBL4750622 | — | — | 1 | 7.37 |
| CHEMBL4789590 | — | — | 1 | 7.12 |
| CHEMBL4752921 | — | — | 1 | 7.11 |
| CHEMBL4759018 | — | — | 1 | 7.08 |
| CHEMBL4762761 | — | — | 1 | 7.01 |
| CHEMBL4752471 | — | — | 1 | 7.00 |
| CHEMBL4790632 | — | — | 1 | 6.97 |
| CHEMBL4763087 | — | — | 1 | 6.47 |
| CHEMBL4793486 | — | — | 1 | 5.97 |
| CHEMBL4776712 | — | — | 1 | 5.95 |
| CHEMBL4793538 | — | — | 1 | - |
| CHEMBL4746326 | — | — | 1 | - |
| CHEMBL4752505 | — | — | 1 | - |
| CHEMBL4765071 | — | — | 1 | - |
| CHEMBL4758288 | — | — | 1 | - |
| CHEMBL4757267 | — | — | 1 | - |
| CHEMBL4763764 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4752141 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4787269 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4764756 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4785028 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4743561 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4757431 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4755524 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4746396 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4795993 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4791136 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4749973 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4750622 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4789590 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4752921 | — | IC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4759018 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4762761 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4752471 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4790632 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL4763087 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4793486 | — | IC50 | = | 1073.0 | nM | 5.97 |
| CHEMBL4776712 | — | IC50 | = | 1112.0 | nM | 5.95 |
| CHEMBL4793538 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4746326 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4752505 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4765071 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4758288 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4757267 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4763764 | — | IC50 | > | 2000.0 | nM | - |