Assay Detail
Binding
CHEMBL4189497
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged MNK2 (72 to 385 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) using JH3 peptide as substrate preincubated for 10 mins followed by substrate and ATP addition measured after 60 mins
26
Total Activities
26
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
Optimization of Selective Mitogen-Activated Protein Kinase Interacting Kinases 1 and 2 Inhibitors for the Treatment of Blast Crisis Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 6.69 | 7.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4216109 | — | — | 1 | 7.96 |
| CHEMBL4213168 | — | — | 1 | 7.60 |
| CHEMBL4208772 | — | — | 1 | 7.58 |
| CHEMBL4214092 | — | — | 1 | 7.51 |
| CHEMBL4203889 | — | — | 1 | 7.39 |
| CHEMBL4204438 | — | — | 1 | 7.14 |
| CHEMBL4211649 | TINODASERTIB | 2.0 | 1 | 7.07 |
| CHEMBL4209905 | — | — | 1 | 6.95 |
| CHEMBL4209496 | — | — | 1 | 6.85 |
| CHEMBL4208246 | — | — | 1 | 6.84 |
| CHEMBL4208890 | — | — | 1 | 6.80 |
| CHEMBL4204506 | — | — | 1 | 6.73 |
| CHEMBL4212480 | — | — | 1 | 6.71 |
| CHEMBL4211757 | — | — | 1 | 6.66 |
| CHEMBL4202593 | — | — | 1 | 6.47 |
| CHEMBL4217366 | — | — | 1 | 6.45 |
| CHEMBL4212200 | — | — | 1 | 6.41 |
| CHEMBL4212307 | — | — | 1 | 6.39 |
| CHEMBL4213023 | — | — | 1 | 6.38 |
| CHEMBL4213819 | — | — | 1 | 6.34 |
| CHEMBL4216991 | — | — | 1 | 6.30 |
| CHEMBL4208627 | — | — | 1 | 6.29 |
| CHEMBL4216093 | — | — | 1 | 6.13 |
| CHEMBL4208112 | — | — | 1 | 5.97 |
| CHEMBL4206349 | — | — | 1 | 5.84 |
| CHEMBL4202639 | — | — | 1 | 5.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4216109 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4213168 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4208772 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4214092 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4203889 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4204438 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4211649 | TINODASERTIB | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4209905 | — | IC50 | = | 113.0 | nM | 6.95 |
| CHEMBL4209496 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4208246 | — | IC50 | = | 143.0 | nM | 6.84 |
| CHEMBL4208890 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4204506 | — | IC50 | = | 187.0 | nM | 6.73 |
| CHEMBL4212480 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL4211757 | — | IC50 | = | 217.0 | nM | 6.66 |
| CHEMBL4202593 | — | IC50 | = | 336.0 | nM | 6.47 |
| CHEMBL4217366 | — | IC50 | = | 355.0 | nM | 6.45 |
| CHEMBL4212200 | — | IC50 | = | 389.0 | nM | 6.41 |
| CHEMBL4212307 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4213023 | — | IC50 | = | 415.0 | nM | 6.38 |
| CHEMBL4213819 | — | IC50 | = | 454.0 | nM | 6.34 |
| CHEMBL4216991 | — | IC50 | = | 502.0 | nM | 6.30 |
| CHEMBL4208627 | — | IC50 | = | 515.0 | nM | 6.29 |
| CHEMBL4216093 | — | IC50 | = | 742.0 | nM | 6.13 |
| CHEMBL4208112 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL4206349 | — | IC50 | = | 1430.0 | nM | 5.84 |
| CHEMBL4202639 | — | IC50 | = | 5170.0 | nM | 5.29 |