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 |
---|---|---|---|---|
Schistosoma mansoni | Tr4/Tr2 (homologue) | 0.0085 | 0.5 | 0.5 |
Echinococcus granulosus | ecdysone induced protein 78C | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-41 | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor-like 1 | 0.0085 | 0.5 | 0.5 |
Onchocerca volvulus | Protein ultraspiracle homolog | 0.0085 | 0.5 | 0.5 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0085 | 0.5 | 0.5 |
Brugia malayi | steroid hormone receptor | 0.0085 | 0.5 | 0.5 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0085 | 0.5 | 0.5 |
Echinococcus granulosus | hepatocyte nuclear factor 4 alpha | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-49 | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-1 | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0085 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0085 | 0.5 | 0.5 | |
Echinococcus multilocularis | ecdysone induced protein 78C | 0.0085 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0085 | 0.5 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-31 | 0.0085 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor nor-1/nor-2 | 0.0085 | 0.5 | 0.5 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.0085 | 0.5 | 0.5 |
Onchocerca volvulus | Steroid hormone receptor family member cnr14 homolog | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Steroid receptor seven-up type 2 | 0.0085 | 0.5 | 0.5 |
Echinococcus granulosus | COUP TF:Svp nuclear hormone receptor | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0085 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | 0.0085 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0085 | 0.5 | 0.5 |
Echinococcus multilocularis | COUP TF:Svp nuclear hormone receptor | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-40 | 0.0085 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-14 | 0.0085 | 0.5 | 0.5 |
Brugia malayi | nuclear hormone receptor | 0.0085 | 0.5 | 0.5 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.0085 | 0.5 | 0.5 |
Schistosoma mansoni | RAR-like nuclear receptor | 0.0085 | 0.5 | 0.5 |
Schistosoma mansoni | coup transcription factor | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear Hormone Receptor family member | 0.0085 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor | 0.0085 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0085 | 0.5 | 0.5 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-41 | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-1 | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-31 | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-3 | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-14 | 0.0085 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0085 | 0.5 | 0.5 |
Echinococcus multilocularis | Nuclear hormone receptor family member nhr 41 | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0085 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.0085 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 alpha | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0085 | 0.5 | 0.5 |
Echinococcus granulosus | Nuclear hormone receptor family member nhr 41 | 0.0085 | 0.5 | 0.5 |
Echinococcus multilocularis | hepatocyte nuclear factor 4 alpha | 0.0085 | 0.5 | 0.5 |
Schistosoma mansoni | FTZ-F1 nuclear receptor-like protein | 0.0085 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 nuclear receptor protein | 0.0085 | 0.5 | 0.5 |
Brugia malayi | photoreceptor-specific nuclear receptor | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0085 | 0.5 | 0.5 |
Loa Loa (eye worm) | steroid hormone receptor | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-49 | 0.0085 | 0.5 | 0.5 |
Brugia malayi | nuclear receptor NHR-88 | 0.0085 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0085 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-40 | 0.0085 | 0.5 | 0.5 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.0085 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 alpha | 0.0085 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 6.2 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.