Assay Detail
Binding
CHEMBL2051182
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Competitive inhibition of [3H]m7-GTP binding to human FLAG-His6 tagged eIF4E expressed in Escherichia coli by scintillation proximity assay
26
Total Activities
26
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
Eukaryotic translation initiation factor 4E (CHEMBL4848) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-guided design, synthesis, and evaluation of guanine-derived inhibitors of the eIF4E mRNA-cap interaction.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.80 | 7.80 |
| Ki | 1 | 7.55 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2046918 | — | — | 1 | 7.80 |
| CHEMBL1094973 | — | — | 1 | 7.55 |
| CHEMBL2046906 | — | — | 1 | 7.39 |
| CHEMBL2046915 | — | — | 1 | 7.29 |
| CHEMBL2046910 | — | — | 1 | 7.25 |
| CHEMBL2046905 | — | — | 1 | 7.23 |
| CHEMBL2046916 | — | — | 1 | 7.02 |
| CHEMBL2046912 | — | — | 1 | 6.93 |
| CHEMBL2046908 | — | — | 1 | 6.90 |
| CHEMBL2046917 | — | — | 1 | 6.80 |
| CHEMBL2046920 | — | — | 1 | 5.87 |
| CHEMBL2046907 | — | — | 1 | 5.80 |
| CHEMBL2046909 | — | — | 1 | 5.59 |
| CHEMBL2046921 | — | — | 1 | 5.50 |
| CHEMBL2046914 | — | — | 1 | 5.44 |
| CHEMBL2046903 | — | — | 1 | 5.27 |
| CHEMBL2046913 | — | — | 1 | 5.18 |
| CHEMBL1095620 | — | — | 1 | 5.00 |
| CHEMBL1097198 | — | — | 1 | 4.85 |
| CHEMBL1094975 | — | — | 1 | 4.81 |
| CHEMBL2046904 | — | — | 1 | 4.37 |
| CHEMBL2046902 | — | — | 1 | 4.31 |
| CHEMBL1095941 | — | — | 1 | 4.26 |
| CHEMBL1097199 | — | — | 1 | 4.25 |
| CHEMBL2046911 | — | — | 1 | 4.07 |
| CHEMBL2046919 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2046918 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1094973 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2046906 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL2046915 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2046910 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL2046905 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL2046916 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL2046912 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL2046908 | — | IC50 | = | 125.0 | nM | 6.90 |
| CHEMBL2046917 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2046920 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL2046907 | — | IC50 | = | 1590.0 | nM | 5.80 |
| CHEMBL2046909 | — | IC50 | = | 2570.0 | nM | 5.59 |
| CHEMBL2046921 | — | IC50 | = | 3140.0 | nM | 5.50 |
| CHEMBL2046914 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL2046903 | — | IC50 | = | 5350.0 | nM | 5.27 |
| CHEMBL2046913 | — | IC50 | = | 6580.0 | nM | 5.18 |
| CHEMBL1095620 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1097198 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL1094975 | — | IC50 | = | 15500.0 | nM | 4.81 |
| CHEMBL2046904 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL2046902 | — | IC50 | = | 49300.0 | nM | 4.31 |
| CHEMBL1095941 | — | IC50 | = | 54500.0 | nM | 4.26 |
| CHEMBL1097199 | — | IC50 | = | 56800.0 | nM | 4.25 |
| CHEMBL2046911 | — | IC50 | = | 85400.0 | nM | 4.07 |
| CHEMBL2046919 | — | IC50 | = | 300000.0 | nM | - |