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 |
---|---|---|---|---|
Brugia malayi | Steroid receptor seven-up type 2 | 0.0012 | 0.5 | 0.5 |
Schistosoma mansoni | Tr4/Tr2 (homologue) | 0.0012 | 0.5 | 0.5 |
Brugia malayi | nuclear hormone receptor | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear Hormone Receptor family member | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0012 | 0.5 | 0.5 |
Echinococcus granulosus | COUP TF:Svp nuclear hormone receptor | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-41 | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-14 | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0012 | 0.5 | 0.5 |
Onchocerca volvulus | Protein ultraspiracle homolog | 0.0012 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 alpha | 0.0012 | 0.5 | 0.5 |
Echinococcus multilocularis | ecdysone induced protein 78C | 0.0012 | 0.5 | 0.5 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.0012 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0012 | 0.5 | 0.5 |
Onchocerca volvulus | Steroid hormone receptor family member cnr14 homolog | 0.0012 | 0.5 | 0.5 |
Brugia malayi | nuclear receptor NHR-88 | 0.0012 | 0.5 | 0.5 |
Brugia malayi | steroid hormone receptor | 0.0012 | 0.5 | 0.5 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0012 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-1 | 0.0012 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0012 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0012 | 0.5 | 0.5 | |
Schistosoma mansoni | RAR-like nuclear receptor | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0012 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-49 | 0.0012 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 nuclear receptor protein | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0012 | 0.5 | 0.5 |
Echinococcus granulosus | Nuclear hormone receptor family member nhr 41 | 0.0012 | 0.5 | 0.5 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.0012 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0012 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | 0.0012 | 0.5 | 0.5 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-31 | 0.0012 | 0.5 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-49 | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-31 | 0.0012 | 0.5 | 0.5 |
Echinococcus granulosus | hepatocyte nuclear factor 4 alpha | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor-like 1 | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-40 | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | steroid hormone receptor | 0.0012 | 0.5 | 0.5 |
Schistosoma mansoni | FTZ-F1 nuclear receptor-like protein | 0.0012 | 0.5 | 0.5 |
Echinococcus multilocularis | Nuclear hormone receptor family member nhr 41 | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-3 | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-40 | 0.0012 | 0.5 | 0.5 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.0012 | 0.5 | 0.5 |
Echinococcus multilocularis | hepatocyte nuclear factor 4 alpha | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-14 | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-1 | 0.0012 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0012 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0012 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor nor-1/nor-2 | 0.0012 | 0.5 | 0.5 |
Echinococcus granulosus | ecdysone induced protein 78C | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-41 | 0.0012 | 0.5 | 0.5 |
Echinococcus multilocularis | COUP TF:Svp nuclear hormone receptor | 0.0012 | 0.5 | 0.5 |
Brugia malayi | photoreceptor-specific nuclear receptor | 0.0012 | 0.5 | 0.5 |
Schistosoma mansoni | coup transcription factor | 0.0012 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 alpha | 0.0012 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0012 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0012 | 0.5 | 0.5 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.0012 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0012 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 0.9 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.