Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | hypocretin (orexin) receptor 2 | Starlite/ChEMBL | No references |
Homo sapiens | hypocretin (orexin) receptor 1 | Starlite/ChEMBL | No references |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Echinococcus granulosus | neuropeptide receptor | Get druggable targets OG5_127863 | All targets in OG5_127863 |
Schistosoma japonicum | ko:K04209 neuropeptide Y receptor, invertebrate, putative | Get druggable targets OG5_127863 | All targets in OG5_127863 |
Echinococcus multilocularis | G protein coupled receptor 139 | Get druggable targets OG5_127863 | All targets in OG5_127863 |
Echinococcus multilocularis | neuropeptide receptor | Get druggable targets OG5_127863 | All targets in OG5_127863 |
Schistosoma mansoni | neuropeptide receptor | Get druggable targets OG5_127863 | All targets in OG5_127863 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus granulosus | sex peptide receptor | hypocretin (orexin) receptor 1 | 425 aa | 350 aa | 23.4 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Onchocerca volvulus | Vesicular acetylcholine transporter homolog | 0.5161 | 0.7564 | 0.5 |
Loa Loa (eye worm) | vesicular acetylcholine transporter unc-17 | 0.5161 | 0.7564 | 0.5111 |
Echinococcus granulosus | vesicular acetylcholine transporter | 0.5161 | 0.7564 | 1 |
Echinococcus multilocularis | vesicular acetylcholine transporter | 0.5161 | 0.7564 | 1 |
Schistosoma mansoni | vesicular acetylcholine transporter | 0.5161 | 0.7564 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 25 nM | BindingDB_Patents: In Vitro Assay. Chinese hamster ovary (CHO) cells expressing the human orexin-1 receptor and the human orexin-2 receptor, respectively, are grown in culture medium (Ham F-12 with L-Glutamine) containing 300 ug/ml G418, 100 U/ml penicillin, 100 ug/ml streptomycin and 10% heat inactivated fetal calf serum (FCS). The cells are seeded at 20'000 cells/well into 384-well black clear bottom sterile plates (Greiner). The seeded plates are incubated overnight at 37 C. in 5% CO2.Human orexin-A as an agonist is prepared as 1 mM stock solution in MeOH: water (1:1), diluted in HBSS containing 0.1% bovine serum albumin (BSA), NaHCO3: 0.375 g/l and 20 mM HEPES for use in the assay at a final concentration of 3 nM.Antagonists are prepared as 10 mM stock solution in DMSO, then diluted in 384-well plates using DMSO followed by a transfer of the dilutions into in HBSS containing 0.1% bovine serum albumin (BSA), NaHCO3: 0.375 g/l and 20 mM HEPES. On the day of the assay, 50 ul of staining buffer. | ChEMBL. | No reference |
IC50 (binding) | = 73 nM | In Vitro Assay | BINDINGDB. | 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.