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 |
---|---|---|---|---|
Loa Loa (eye worm) | acetylcholinesterase 1 | 0.3237 | 1 | 0.5 |
Echinococcus multilocularis | acetylcholinesterase | 0.3237 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.3237 | 1 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.3237 | 1 | 0.5 |
Echinococcus granulosus | acetylcholinesterase | 0.3237 | 1 | 1 |
Echinococcus granulosus | acetylcholinesterase | 0.3237 | 1 | 1 |
Loa Loa (eye worm) | carboxylesterase | 0.3237 | 1 | 0.5 |
Echinococcus multilocularis | acetylcholinesterase | 0.3237 | 1 | 1 |
Brugia malayi | Carboxylesterase family protein | 0.3237 | 1 | 0.5 |
Echinococcus granulosus | carboxylesterase 5A | 0.3237 | 1 | 1 |
Schistosoma mansoni | family S9 non-peptidase homologue (S09 family) | 0.3237 | 1 | 0.5 |
Echinococcus multilocularis | carboxylesterase 5A | 0.3237 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 187 nM | BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors 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 level 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 the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity. | ChEMBL. | No reference |
IC50 (binding) | = 187 nM | BindingDB_Patents: Functional Assay. Determination of antagonistic activity of compounds of the general formula 1 towards 5-HT6 receptors. Compounds of the general formula 1 were tested for their ability to prevent 5-HT6 receptors 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 level 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 the compounds was estimated by their ability to reduce the level of intracellular cAMP induced by serotonin. Table 4 presents IC50 values for the compounds of general formula 1 in the setting of functional assay for serotonin 5-HT6 receptor inhibition. The data given testify their moderate or high antagonistic activity. | ChEMBL. | No reference |
Ki (functional) | = 8.1 | 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.