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 |
Schistosoma mansoni | histone J3 methyltransferase | 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 japonicum | ko:K05302 histone-lysine N-methyltransferase [EC2.1.1.43], putative | 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 |
Echinococcus multilocularis | histone h3 methyltransferase | Get druggable targets OG5_130680 | All targets in OG5_130680 |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | hypothetical protein | 0.0064 | 0.3278 | 0.2658 |
Onchocerca volvulus | 0.0064 | 0.3278 | 0.5 | |
Brugia malayi | Muscle positioning protein 4 | 0.0064 | 0.3278 | 0.3078 |
Onchocerca volvulus | 0.0064 | 0.3278 | 0.5 | |
Toxoplasma gondii | hypothetical protein | 0.002 | 0 | 0.5 |
Trypanosoma brucei | Histone-lysine N-methyltransferase, H3 lysine-76 specific | 0.002 | 0 | 0.5 |
Echinococcus multilocularis | histone h3 methyltransferase | 0.0155 | 1 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0064 | 0.3278 | 0.3078 |
Onchocerca volvulus | 0.0064 | 0.3278 | 0.5 | |
Leishmania major | histone-lysine N-methyltransferase, putative | 0.002 | 0 | 0.5 |
Schistosoma mansoni | histone J3 methyltransferase | 0.0155 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0155 | 1 | 1 |
Onchocerca volvulus | 0.0064 | 0.3278 | 0.5 | |
Trypanosoma cruzi | histone-lysine N-methyltransferase, putative | 0.002 | 0 | 0.5 |
Leishmania major | hypothetical protein, conserved | 0.002 | 0 | 0.5 |
Echinococcus granulosus | histone h3 methyltransferase | 0.0155 | 1 | 0.5 |
Trypanosoma cruzi | Histone methylation protein DOT1, putative | 0.002 | 0 | 0.5 |
Trypanosoma cruzi | Histone-lysine N-methyltransferase, H3 lysine-76 specific | 0.002 | 0 | 0.5 |
Loa Loa (eye worm) | DOMON domain-containing protein | 0.0064 | 0.3278 | 0.3078 |
Trypanosoma brucei | Histone methylation protein DOT1, putative | 0.002 | 0 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0064 | 0.3278 | 0.3078 |
Leishmania major | hypothetical protein, conserved | 0.002 | 0 | 0.5 |
Trypanosoma cruzi | Histone methylation protein DOT1, putative | 0.002 | 0 | 0.5 |
Brugia malayi | SEA domain containing protein | 0.0064 | 0.3278 | 0.3078 |
Onchocerca volvulus | 0.0064 | 0.3278 | 0.5 | |
Trypanosoma brucei | histone-lysine n-methyltransferase | 0.002 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
CLH (ADMET) | = 0.36 uL/min | Intrinsic clearance in human liver microsomes assessed per mg of protein | ChEMBL. | 23879463 |
CLH (ADMET) | = 0.36 uL/min | Intrinsic clearance in human liver microsomes measured per gram of protein at 200 uM measured after 1 by LC/MS/MS method | ChEMBL. | 23795283 |
IC50 (functional) | = 0.2 uM | Induction of histone methylation in human MV4-11 cells assessed as H3K79 methylation after 4 days by Western blot analysis | ChEMBL. | 23795283 |
Ki (binding) | = 1.1 nM | Competitive inhibition of recombinant human DOT1L using adenosine/deazaadenosine as substrate and SAM cofactor | ChEMBL. | 23879463 |
Ki (binding) | = 0.0011 uM | Inhibition of human recombinant DOT1L (catalytic domain 1 to 472) using [3H]-SAM by scintillation containing | ChEMBL. | 23795283 |
Ki (binding) | > 50 uM | Inhibition of SUV39H1 (unknown origin) | ChEMBL. | 23795283 |
Ki (binding) | > 50 uM | Inhibition of CARM1 (unknown origin) | ChEMBL. | 23795283 |
Ki (binding) | > 50 uM | Inhibition of PRMT1 (unknown origin) | ChEMBL. | 23795283 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 23795283 |
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.