Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | DOT1-like histone H3K79 methyltransferase | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Brugia malayi | Histone-lysine N-methyltransferase, H3 lysine-79 specific | Get druggable targets OG5_130680 | All targets in OG5_130680 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_130680 | All targets in OG5_130680 |
Schistosoma mansoni | histone J3 methyltransferase | Get druggable targets OG5_130680 | All targets in OG5_130680 |
Echinococcus multilocularis | histone h3 methyltransferase | Get druggable targets OG5_130680 | All targets in OG5_130680 |
Echinococcus granulosus | histone h3 methyltransferase | Get druggable targets OG5_130680 | All targets in OG5_130680 |
Schistosoma japonicum | ko:K05302 histone-lysine N-methyltransferase [EC2.1.1.43], putative | Get druggable targets OG5_130680 | All targets in OG5_130680 |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.0155 | 0.5 | 0.5 |
Schistosoma mansoni | histone J3 methyltransferase | 0.0155 | 0.5 | 0.5 |
Echinococcus multilocularis | histone h3 methyltransferase | 0.0155 | 0.5 | 0.5 |
Echinococcus granulosus | histone h3 methyltransferase | 0.0155 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 120 nM | Inhibition of GST-tagged human DOT1L amino acid 1 to 472 expressed in Escherichia coli BL21 (DE3) using [3H]-SAM as substrate preincubated for 10 mins before substrate addition measured after 30 mins by scintillation counter | ChEMBL. | 22975593 |
IC50 (binding) | = 120 nM | Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactor | ChEMBL. | 23879463 |
IC50 (binding) | > 100 uM | Inhibition of human CARM1 expressed in Escherichia coli BL21 (DE3) using [3H]-SAM as substrate preincubated for 10 mins before substrate addition measured after 30 mins by scintillation counter | ChEMBL. | 22975593 |
IC50 (binding) | > 100 uM | Inhibition of SUV39H1 using [3H]-SAM as substrate preincubated for 10 mins before substrate addition measured after 30 mins by scintillation counter | ChEMBL. | 22975593 |
IC50 (binding) | > 100 uM | Inhibition of G9a using [3H]-SAM as substrate preincubated for 10 mins before substrate addition measured after 30 mins by scintillation counter | ChEMBL. | 22975593 |
IC50 (binding) | > 100 uM | Inhibition of PRMT1 using [3H]-SAM as substrate preincubated for 10 mins before substrate addition measured after 30 mins by scintillation counter | ChEMBL. | 22975593 |
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.
2 literature references were collected for this gene.