Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | transient receptor potential cation channel, subfamily M, member 8 | Starlite/ChEMBL | No references |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus granulosus | transient receptor potential cation channel | transient receptor potential cation channel, subfamily M, member 8 | 1104 aa | 1115 aa | 24.8 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Mycobacterium ulcerans | thymidylate synthase | 0.0378 | 0.5 | 0.5 |
Plasmodium vivax | bifunctional dihydrofolate reductase-thymidylate synthase, putative | 0.0378 | 0.5 | 0.5 |
Echinococcus granulosus | thymidylate synthase | 0.0378 | 0.5 | 0.5 |
Mycobacterium leprae | PROBABLE THYMIDYLATE SYNTHASE THYA (TS) (TSASE) | 0.0378 | 0.5 | 0.5 |
Schistosoma mansoni | bifunctional dihydrofolate reductase-thymidylate synthase | 0.0378 | 0.5 | 0.5 |
Echinococcus multilocularis | thymidylate synthase | 0.0378 | 0.5 | 0.5 |
Plasmodium falciparum | bifunctional dihydrofolate reductase-thymidylate synthase | 0.0378 | 0.5 | 0.5 |
Toxoplasma gondii | bifunctional dihydrofolate reductase-thymidylate synthase | 0.0378 | 0.5 | 0.5 |
Trypanosoma cruzi | dihydrofolate reductase-thymidylate synthase | 0.0378 | 0.5 | 0.5 |
Mycobacterium tuberculosis | Probable thymidylate synthase ThyA (ts) (TSASE) | 0.0378 | 0.5 | 0.5 |
Loa Loa (eye worm) | thymidylate synthase | 0.0378 | 0.5 | 0.5 |
Leishmania major | dihydrofolate reductase-thymidylate synthase | 0.0378 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0378 | 0.5 | 0.5 | |
Trypanosoma brucei | dihydrofolate reductase-thymidylate synthase | 0.0378 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 2.1 nM | BindingDB_Patents: Inhibition Assay. The functional activity of compounds was determined by measuring changes in intracellular calcium concentration using a Ca2+ sensitive fluorescent dye. The changes in fluorescent signal were monitored by the cell imaging technology by Hamamatsu Photonics's Functional Drug Screening System (FDSS). Increases in intracellular Ca2+ concentration were readily detected upon activation with menthol.HEK293 cells stably expressing human TRPM8 were grown in flasks. On assay day, the culture medium was removed, and cells were washed with phosphate-buffered saline (PBS) and harvested with PBS containing 2 mM ethylenediaminetetraacetic acid, disodium salt (EDTA, 2Na). The cells were then incubated with assay buffer containing 3 uM Fura-2AM and 0.01% Pluronic F-127 for 60 min. Subsequently, suspended 20,000 to 50,000 cells per well were incubated with test compound (at varying concentrations) in each well for 20 min at 37 C. | 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.