Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled | Starlite/ChEMBL | References |
Homo sapiens | 5-hydroxytryptamine (serotonin) receptor 2C, G protein-coupled | Starlite/ChEMBL | References |
Homo sapiens | 5-hydroxytryptamine (serotonin) receptor 2B, G protein-coupled | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Echinococcus multilocularis | conserved hypothetical protein | Get druggable targets OG5_144688 | All targets in OG5_144688 |
Brugia malayi | Serotonin receptor | Get druggable targets OG5_135430 | All targets in OG5_135430 |
Echinococcus granulosus | hypothetical protein | Get druggable targets OG5_144688 | All targets in OG5_144688 |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Mycobacterium ulcerans | L-lysine aminotransferase | 0.0244 | 0.2411 | 0.3314 |
Entamoeba histolytica | protein kinase, putative | 0.0106 | 0.0661 | 0.5 |
Wolbachia endosymbiont of Brugia malayi | O-methyltransferase | 0.0063 | 0.0115 | 0.5 |
Mycobacterium leprae | PROBABLE METHYLTRANSFERASE | 0.0063 | 0.0115 | 0.5 |
Mycobacterium tuberculosis | Probable L-lysine-epsilon aminotransferase Lat (L-lysine aminotransferase) (lysine 6-aminotransferase) | 0.0244 | 0.2411 | 0.3748 |
Schistosoma mansoni | o-methyltransferase | 0.0063 | 0.0115 | 1 |
Loa Loa (eye worm) | IRE protein kinase | 0.0106 | 0.0661 | 1 |
Entamoeba histolytica | protein kinase, putative | 0.0106 | 0.0661 | 0.5 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0054 | 0 | 0.5 |
Mycobacterium tuberculosis | Probable catechol-O-methyltransferase | 0.0546 | 0.6239 | 1 |
Onchocerca volvulus | 0.0063 | 0.0115 | 0.5 | |
Brugia malayi | Serotonin receptor | 0.0564 | 0.6474 | 1 |
Mycobacterium ulcerans | O-methyltransferase | 0.0609 | 0.7041 | 1 |
Echinococcus multilocularis | conserved hypothetical protein | 0.0833 | 0.9891 | 1 |
Trichomonas vaginalis | serine threonine-protein kinase, putative | 0.0054 | 0 | 0.5 |
Schistosoma mansoni | o-methyltransferase | 0.0063 | 0.0115 | 1 |
Onchocerca volvulus | 0.0063 | 0.0115 | 0.5 | |
Brugia malayi | Ribonuclease 2-5A family protein | 0.0106 | 0.0661 | 0.0858 |
Brugia malayi | 4-aminobutyrate aminotransferase, mitochondrial precursor | 0.0244 | 0.2411 | 0.361 |
Schistosoma mansoni | o-methyltransferase | 0.0063 | 0.0115 | 1 |
Schistosoma mansoni | o-methyltransferase | 0.0063 | 0.0115 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
ID50 (functional) | > 5 mg kg-1 | Dose required to reverse mCPP induced hypolocomotion by 50% at 7 mg/kg, ip administration 30 min pretest | ChEMBL. | 10969986 |
Ki (binding) | = -8.8 | Binding affinity towards human cloned 5-hydroxytryptamine 2C receptor of HEK293 cells by displacement of [3H]-mesulergine | ChEMBL. | 10969986 |
Ki (binding) | = -7.4 | Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]-5-HT | ChEMBL. | 10969986 |
Ki (binding) | = -6.6 | Binding affinity towards human cloned 5-hydroxytryptamine 2A receptor of HEK293 cells by displacement of [3H]-ketanserin | ChEMBL. | 10969986 |
Log Ki (binding) | = 6.6 | Binding affinity towards human cloned 5-hydroxytryptamine 2A receptor of HEK293 cells by displacement of [3H]-ketanserin | ChEMBL. | 10969986 |
Log Ki (binding) | = 7.4 | Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]-5-HT | ChEMBL. | 10969986 |
Log Ki (binding) | = 8.8 | Binding affinity towards human cloned 5-hydroxytryptamine 2C receptor of HEK293 cells by displacement of [3H]-mesulergine | ChEMBL. | 10969986 |
Selectivity (binding) | = 25 | Selectivity expressed as ratio of serotonin 5-HT2C receptor over serotonin 5-HT2B receptor | ChEMBL. | 10969986 |
Selectivity (binding) | = 160 | Selectivity expressed as ratio of serotonin 5-HT2C receptor over serotonin 5-HT2A receptor | ChEMBL. | 10969986 |
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.