Assay Detail
Binding
CHEMBL5503542
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Mnk1 (unknown origin) incubated for 60 mins in presence of ATP/substrateby HTRF assay
27
Total Activities
27
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
Design, synthesis and biological evaluation of 4-(indolin-1-yl)-6-substituted-pyrido[3,2-d]pyrimidine derivatives as Mnk1/2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.74 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5558538 | — | — | 1 | 9.10 |
| CHEMBL5505875 | — | — | 1 | 8.74 |
| CHEMBL5527964 | — | — | 1 | 8.70 |
| CHEMBL5558584 | — | — | 1 | 8.62 |
| CHEMBL5527844 | — | — | 1 | 8.40 |
| CHEMBL5557092 | — | — | 1 | 8.38 |
| CHEMBL5549825 | — | — | 1 | 8.29 |
| CHEMBL5555268 | — | — | 1 | 8.19 |
| CHEMBL5556149 | — | — | 1 | 8.16 |
| CHEMBL5556368 | — | — | 1 | 8.08 |
| CHEMBL5558014 | — | — | 1 | 7.91 |
| CHEMBL5517719 | — | — | 1 | 7.82 |
| CHEMBL5556644 | — | — | 1 | 7.80 |
| CHEMBL5518130 | — | — | 1 | 7.79 |
| CHEMBL5558554 | — | — | 1 | 7.62 |
| CHEMBL5556811 | — | — | 1 | 7.57 |
| CHEMBL5532210 | — | — | 1 | 7.46 |
| CHEMBL5532477 | — | — | 1 | 7.43 |
| CHEMBL5558353 | — | — | 1 | 7.40 |
| CHEMBL5505919 | — | — | 1 | 7.31 |
| CHEMBL5555338 | — | — | 1 | 7.19 |
| CHEMBL5555088 | — | — | 1 | 7.09 |
| CHEMBL5559298 | — | — | 1 | 7.09 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.00 |
| CHEMBL5532431 | — | — | 1 | 6.93 |
| CHEMBL5557205 | — | — | 1 | 6.69 |
| CHEMBL1240885 | — | — | 1 | 6.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5558538 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL5505875 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5527964 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5558584 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5527844 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5557092 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL5549825 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL5555268 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5556149 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL5556368 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL5558014 | — | IC50 | = | 12.4 | nM | 7.91 |
| CHEMBL5517719 | — | IC50 | = | 15.3 | nM | 7.82 |
| CHEMBL5556644 | — | IC50 | = | 15.7 | nM | 7.80 |
| CHEMBL5518130 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL5558554 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5556811 | — | IC50 | = | 26.8 | nM | 7.57 |
| CHEMBL5532210 | — | IC50 | = | 34.9 | nM | 7.46 |
| CHEMBL5532477 | — | IC50 | = | 36.9 | nM | 7.43 |
| CHEMBL5558353 | — | IC50 | = | 39.5 | nM | 7.40 |
| CHEMBL5505919 | — | IC50 | = | 48.5 | nM | 7.31 |
| CHEMBL5555338 | — | IC50 | = | 64.1 | nM | 7.19 |
| CHEMBL5555088 | — | IC50 | = | 81.3 | nM | 7.09 |
| CHEMBL5559298 | — | IC50 | = | 81.2 | nM | 7.09 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 99.5 | nM | 7.00 |
| CHEMBL5532431 | — | IC50 | = | 117.9 | nM | 6.93 |
| CHEMBL5557205 | — | IC50 | = | 203.9 | nM | 6.69 |
| CHEMBL1240885 | — | IC50 | = | 628.2 | nM | 6.20 |