Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | eukaryotic translation initiation factor 4E | Starlite/ChEMBL | No references |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | eukaryotic translation initiation factor 4E-1 | eukaryotic translation initiation factor 4E | 237 aa | 190 aa | 44.2 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Trichomonas vaginalis | eukaryotic translation initiation factor 4E, putative | 0.0042 | 1 | 0.5 |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Trichomonas vaginalis | eukaryotic translation initiation factor 4E, putative | 0.0042 | 1 | 0.5 |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Leishmania major | eukaryotic translation initiation factor-like | 0.0042 | 1 | 0.5 |
Trichomonas vaginalis | eukaryotic translation initiation factor 4E, putative | 0.0042 | 1 | 0.5 |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Trypanosoma brucei | Eukaryotic translation initiation factor 4E-1 | 0.0042 | 1 | 0.5 |
Onchocerca volvulus | Neuropeptide F receptor homolog | 0.0008 | 0 | 0.5 |
Echinococcus multilocularis | eukaryotic translation initiation factor 4E | 0.0042 | 1 | 1 |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Trypanosoma cruzi | Eukaryotic translation initiation factor 4E-1 | 0.0042 | 1 | 0.5 |
Leishmania major | eukaryotic translation initiation factor-like protein | 0.0042 | 1 | 0.5 |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Entamoeba histolytica | eukaryotic translation initiation factor 4E, putative | 0.0042 | 1 | 0.5 |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Onchocerca volvulus | Dopamine\/Ecdysteroid receptor homolog | 0.0008 | 0 | 0.5 |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Schistosoma mansoni | eukaryotic translation initiation factor 4e | 0.0042 | 1 | 1 |
Trypanosoma cruzi | Eukaryotic translation initiation factor 4E-1 | 0.0042 | 1 | 0.5 |
Trichomonas vaginalis | eukaryotic translation initiation factor 4E, putative | 0.0042 | 1 | 0.5 |
Toxoplasma gondii | eukaryotic initiation factor-4E, putative | 0.0042 | 1 | 0.5 |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Entamoeba histolytica | eukaryotic translation initiation factor 4E, putative | 0.0042 | 1 | 0.5 |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Echinococcus granulosus | eukaryotic translation initiation factor 4E | 0.0042 | 1 | 1 |
Loa Loa (eye worm) | translation initiation factor 4E | 0.0042 | 1 | 1 |
Onchocerca volvulus | 0.0008 | 0 | 0.5 | |
Leishmania major | eukaryotic translation initiation factor eIF-4E, putative | 0.0042 | 1 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 1400 nM | BindingDB_Patents: Binding Assay. Human eIF4E (aa 28-217) with a C-terminal His tag (HH-eIF4E) was expressed in E. coli in inclusion bodies. The protein was solubilized with 8 M urea and purified under denaturing conditions using nickel-charged HisTrap HP columns (GE Healthcare). The protein was refolded by diluting to approximately 0.25 mg/mL with 6 M urea, 20 mM Hepes pH 7.0, 500 mM NaCl, 1 mM DTT, 1 mM EDTA, and 0.5 M arginine»HCl, and then dialyzing overnight into the same buffer without the urea. The protein was further dialyzed into 20 mM Hepes pH 6.5, 50 mM NaCl, 1 mM EDTA, and 1 mM DTT, filtered, and then concentrated using Hitrap SP sepharose FF columns (GE Healthcare). The protein was dialyzed into 20 mM Hepes pH 7.0, 500 mM NaCl, 5 mM DTT, and 10% glycerol and stored at -80 °C until use. Test compounds (1.6 mM stock in DMSO) were diluted 3 fold in series in DMSO. Compound solutions were diluted 4 fold in Assay Buffer (50 mM sodium phosphate, pH 6.5, 50 mM KC1, 1 mM DTT and 0.5 mg/mL gammaglobulin). | ChEMBL. | No reference |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.