Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | enhancer of zeste 2 polycomb repressive complex 2 subunit | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Echinococcus granulosus | histone lysine N methyltransferase Ez | Get druggable targets OG5_129164 | All targets in OG5_129164 |
Schistosoma mansoni | enhancer of zeste ezh | Get druggable targets OG5_129164 | All targets in OG5_129164 |
Brugia malayi | SET domain containing protein | Get druggable targets OG5_129164 | All targets in OG5_129164 |
Loa Loa (eye worm) | SET domain-containing protein | Get druggable targets OG5_129164 | All targets in OG5_129164 |
Echinococcus multilocularis | histone lysine N methyltransferase E(z) | Get druggable targets OG5_129164 | All targets in OG5_129164 |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus granulosus | histone lysine N methyltransferase Ez | 0.0114 | 0.5 | 0.5 |
Echinococcus multilocularis | histone lysine N methyltransferase E(z) | 0.0114 | 0.5 | 0.5 |
Schistosoma mansoni | enhancer of zeste ezh | 0.0114 | 0.5 | 0.5 |
Loa Loa (eye worm) | SET domain-containing protein | 0.0114 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | = 7 uM | Inhibition of EZH2 in human HeLa cells assessed as reduction in H3K27me3 level | ChEMBL. | 24900844 |
EC50 (binding) | = 7 uM | Inhibition of EZH2 in human HeLa cells assessed as reduction of H3K27me3 and H3K27me2 level after 96 hrs by ELISA method | ChEMBL. | 25406853 |
IC50 (binding) | = 0.032 uM | Inhibition of wild type EZH2 (unknown origin) | ChEMBL. | 24900844 |
IC50 (binding) | = 0.032 uM | Inhibition of EZH2 (unknown origin) using biotinylated nucleosome, H3K27me3 activator and [3H]-SAM incubated for 60 mins by top-count based method | ChEMBL. | 26189078 |
IC50 (binding) | = 9.5 uM | Inhibition of EZH2 in human KARPAS422 cells assessed as global reduction in H3K27me3 level after 10 days by ELISA-based assay | ChEMBL. | 24900844 |
IC50 (binding) | = 13.4 uM | Inhibition of EZH2 in human KARPAS422 cells assessed as global reduction in H3K27me3 level after 7 days by ELISA-based assay | ChEMBL. | 24900844 |
IC50 (binding) | = 58.3 uM | Inhibition of EZH2 in human KARPAS422 cells assessed as global reduction in H3K27me3 level after 4 days by ELISA-based assay | ChEMBL. | 24900844 |
permeability (ADMET) | = 0.19 ucm/s | Passive permeability from apical to basolateral side in human Caco2 cells | ChEMBL. | 24900844 |
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.
3 literature references were collected for this gene.