Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | coactivator-associated arginine methyltransferase 1 | References | |
Homo sapiens | protein arginine methyltransferase 6 | References | |
Homo sapiens | protein arginine methyltransferase 3 | References | |
Homo sapiens | protein arginine methyltransferase 8 | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Plasmodium falciparum | histone-arginine methyltransferase CARM1, putative | protein arginine methyltransferase 6 | 375 aa | 353 aa | 25.8 % |
Toxoplasma gondii | histone arginine methyltransferase PRMT3 | protein arginine methyltransferase 3 | 469 aa | 431 aa | 30.9 % |
Toxoplasma gondii | histone arginine methyltransferase PRMT4/CARM1 | protein arginine methyltransferase 8 | 385 aa | 345 aa | 33.9 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Trypanosoma brucei | Protein arginine N-methyltransferase 1 catalytic subunit | 0.0092 | 0 | 0.5 |
Toxoplasma gondii | histone arginine methyltransferase PRMT4/CARM1 | 0.0195 | 0.3938 | 0.5 |
Brugia malayi | Carm1-pending protein | 0.0195 | 0.3938 | 1 |
Onchocerca volvulus | 0.014 | 0.1827 | 0.5 | |
Loa Loa (eye worm) | Carm1-pending protein | 0.0195 | 0.3938 | 1 |
Echinococcus multilocularis | histone arginine methyltransferase CARMER | 0.0195 | 0.3938 | 0.5 |
Entamoeba histolytica | hypothetical protein | 0.0092 | 0 | 0.5 |
Trypanosoma cruzi | arginine N-methyltransferase, putative | 0.0092 | 0 | 0.5 |
Entamoeba histolytica | arginine N-methyltransferase protein, putative | 0.0092 | 0 | 0.5 |
Schistosoma mansoni | protein arginine n-methyltransferase | 0.0195 | 0.3938 | 0.5 |
Trypanosoma cruzi | arginine N-methyltransferase, putative | 0.0092 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | Inhibition of PRMT7 (unknown origin) assessed as inhibition of methylation activity measured after 3 hrs using [3H]-SAM by scintillation proximity assay | LITERATURE. | 27584694 | |
IC50 (binding) | Inhibition of PRMT5 (unknown origin) assessed as inhibition of methylation activity measured after 3 hrs using [3H]-SAM by scintillation proximity assay | LITERATURE. | 27584694 | |
IC50 (binding) | = 27 nM | Inhibition of human full length PRMT4 (1 to 608 residues) expressed in 293F cells assessed as inhibition of methylation activity preincubated with protein followed by addition of biotin labeled histone H3 (1 to 25) peptide as substrate and [3H]-SAM measured after 3 hrs by scintillation proximity assay | LITERATURE. | 27584694 |
IC50 (binding) | = 30 nM | Inhibition of human full length PRMT6 (1 to 375 residues) expressed in baculovirus expression system assessed as inhibition of methylation activity preincubated with protein followed by addition of biotin labeled histone H4 (1 to 24) peptide as substrate and [3H]-SAM measured after 3 hrs by scintillation proximity assay | LITERATURE. | 27584694 |
IC50 (binding) | = 573 nM | Inhibition of PRMT8 (unknown origin) assessed as inhibition of methylation activity measured after 3 hrs using [3H]-SAM by scintillation proximity assay | LITERATURE. | 27584694 |
IC50 (binding) | = 1970 nM | Inhibition of PRMT3 (unknown origin) assessed as inhibition of methylation activity measured after 3 hrs using [3H]-SAM by scintillation proximity assay | LITERATURE. | 27584694 |
IC50 (binding) | > 5800 nM | Inhibition of PRMT1 (unknown origin) assessed as inhibition of methylation activity measured after 3 hrs using [3H]-SAM by scintillation proximity assay | LITERATURE. | 27584694 |
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.
1 literature reference was collected for this gene.