Assay Detail
Binding
CHEMBL3637765
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Mnk1a (unknown origin) using TAMRA-labeled eIF4E peptide as substrate incubated for 10 mins followed by addition of ATP measured after 90 mins by IMAP TR-FRET analysis
14
Total Activities
13
Compounds Tested
2
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
An integrated approach for discovery of highly potent and selective Mnk inhibitors: Screening, synthesis and SAR analysis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 6.28 | 6.97 |
| IC50 | 1 | 6.06 | 6.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3632744 | — | — | 1 | 6.97 |
| CHEMBL3632742 | — | — | 1 | 6.73 |
| CHEMBL3632747 | — | — | 1 | 6.50 |
| CHEMBL3416305 | — | — | 1 | 6.29 |
| CHEMBL1240885 | — | — | 2 | 6.06 |
| CHEMBL3632745 | — | — | 1 | 6.03 |
| CHEMBL3632743 | — | — | 1 | 5.99 |
| CHEMBL3632740 | — | — | 1 | 5.72 |
| CHEMBL3632737 | — | — | 1 | - |
| CHEMBL3632738 | — | — | 1 | - |
| CHEMBL3632739 | — | — | 1 | - |
| CHEMBL3632741 | — | — | 1 | - |
| CHEMBL3632746 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3632744 | — | Ki | = | 106.0 | nM | 6.97 |
| CHEMBL3632742 | — | Ki | = | 186.0 | nM | 6.73 |
| CHEMBL3632747 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL3416305 | — | Ki | = | 507.0 | nM | 6.29 |
| CHEMBL1240885 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL3632745 | — | Ki | = | 933.0 | nM | 6.03 |
| CHEMBL1240885 | — | Ki | = | 1010.0 | nM | 6.00 |
| CHEMBL3632743 | — | Ki | = | 1020.0 | nM | 5.99 |
| CHEMBL3632740 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL3632737 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3632738 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3632739 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3632741 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3632746 | — | Ki | > | 10000.0 | nM | - |