Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | 5-hydroxytryptamine (serotonin) receptor 6, G protein-coupled | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Echinococcus multilocularis | tm gpcr rhodopsin gpcr rhodopsin superfamily | Get druggable targets OG5_145685 | All targets in OG5_145685 |
Echinococcus granulosus | tm gpcr rhodopsin | Get druggable targets OG5_145685 | All targets in OG5_145685 |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | metabotropic glutamate receptor 2 3 (mglur group 2) | 0.0047 | 0.0127 | 0.0448 |
Loa Loa (eye worm) | hypothetical protein | 0.0051 | 0.0167 | 1 |
Echinococcus multilocularis | metabotropic glutamate receptor 5 | 0.0051 | 0.0167 | 0.0167 |
Plasmodium falciparum | sortilin | 0.0438 | 0.4164 | 0.5 |
Schistosoma mansoni | hypothetical protein | 0.0107 | 0.0752 | 0.2641 |
Echinococcus granulosus | sortilin | 0.0438 | 0.4164 | 0.4164 |
Schistosoma mansoni | hypothetical protein | 0.0128 | 0.0962 | 0.3382 |
Schistosoma mansoni | sortilin | 0.031 | 0.2845 | 1 |
Plasmodium vivax | sortilin, putative | 0.0438 | 0.4164 | 0.5 |
Schistosoma mansoni | hypothetical protein | 0.0107 | 0.0752 | 0.2641 |
Toxoplasma gondii | sortilin, putative | 0.0438 | 0.4164 | 0.5 |
Echinococcus multilocularis | sortilin | 0.0438 | 0.4164 | 0.4164 |
Echinococcus granulosus | metabotropic glutamate receptor 5 | 0.0051 | 0.0167 | 0.0167 |
Brugia malayi | Metabotropic glutamate receptor precursor. | 0.0041 | 0.0069 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 4 nM | BindingDB_Patents: Lance cAMP Assay. Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin. | ChEMBL. | No reference |
IC50 (binding) | = 4 nM | BindingDB_Patents: Lance cAMP Assay. Determination of antagonistic activity of compounds of general formula 1 towards 5-HT6 receptors. Compounds of general formula 1 were tested for their ability to prevent 5-HT6 receptor activation by serotonin. HEK 293 cells (cells of human embryo's kidney) with artificially expressed 5-HT6 receptor, activation of which by serotonin leads to increasing the concentration of intracellular cAMP were used. The content of intracellular cAMP was determined using reagent kit LANCE cAMP (PerkinElmer) according to the method described by the manufacturer of the kit [http://las.perkinelmer.com/content/Manuals/MAN_LANCEcAMP384KitUser.pdf]. Effectiveness of compounds was estimated by their ability to reduce the content of intracellular cAMP induced by serotonin. | ChEMBL. | No reference |
Ki (functional) | = 9.22 | Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced cAMP accumulation after 2 hrs | ChEMBL. | 21277782 |
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.