Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | 5-hydroxytryptamine (serotonin) receptor 2C, G protein-coupled | Starlite/ChEMBL | References |
Homo sapiens | solute carrier family 6 (neurotransmitter transporter), member 4 | Starlite/ChEMBL | References |
Homo sapiens | 5-hydroxytryptamine (serotonin) receptor 2A, G protein-coupled | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | Sodium:neurotransmitter symporter family protein | solute carrier family 6 (neurotransmitter transporter), member 4 | 630 aa | 574 aa | 31.5 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | leukotriene A 4 hydrolase | 0.0504 | 0.8914 | 1 |
Schistosoma mansoni | Guanine nucleotide-binding protein G(s) subunit alpha (Adenylate cyclase-stimulating G alpha protein) | 0.0047 | 0.0193 | 0.0217 |
Schistosoma mansoni | norepinephrine/norepinephrine transporter | 0.0073 | 0.0681 | 0.0764 |
Loa Loa (eye worm) | hypothetical protein | 0.0073 | 0.0681 | 0.0559 |
Echinococcus multilocularis | serotonin transporter | 0.0073 | 0.0681 | 0.0764 |
Loa Loa (eye worm) | hypothetical protein | 0.0073 | 0.0681 | 0.0559 |
Brugia malayi | hypothetical protein | 0.0232 | 0.3713 | 0.3713 |
Echinococcus multilocularis | guanine nucleotide binding protein G(s) subunit | 0.0047 | 0.0193 | 0.0217 |
Loa Loa (eye worm) | leukotriene A4 hydrolase | 0.0504 | 0.8914 | 1 |
Echinococcus granulosus | serotonin transporter | 0.0073 | 0.0681 | 0.0764 |
Loa Loa (eye worm) | norepinephrine transporter | 0.0073 | 0.0681 | 0.0559 |
Schistosoma mansoni | leukotriene A4 hydrolase (M01 family) | 0.0504 | 0.8914 | 1 |
Entamoeba histolytica | hypothetical protein | 0.0037 | 0 | 0.5 |
Echinococcus granulosus | guanine nucleotide binding protein Gs subunit | 0.0047 | 0.0193 | 0.0217 |
Entamoeba histolytica | hypothetical protein | 0.0037 | 0 | 0.5 |
Onchocerca volvulus | 0.0073 | 0.0681 | 0.5 | |
Loa Loa (eye worm) | hypothetical protein | 0.0073 | 0.0681 | 0.0559 |
Brugia malayi | Sodium:neurotransmitter symporter family protein | 0.0073 | 0.0681 | 0.0681 |
Echinococcus granulosus | leukotriene A 4 hydrolase | 0.0504 | 0.8914 | 1 |
Entamoeba histolytica | hypothetical protein | 0.0037 | 0 | 0.5 |
Schistosoma mansoni | Guanine nucleotide-binding protein G(s) subunit alpha (Adenylate cyclase-stimulating G alpha protein) | 0.0047 | 0.0193 | 0.0217 |
Loa Loa (eye worm) | serotonin transporter b | 0.0073 | 0.0681 | 0.0559 |
Entamoeba histolytica | hypothetical protein | 0.0037 | 0 | 0.5 |
Treponema pallidum | sodium- and chloride- dependent transporter | 0.0073 | 0.0681 | 0.5 |
Loa Loa (eye worm) | solute carrier family 6 member 4 | 0.0073 | 0.0681 | 0.0559 |
Brugia malayi | GTP-binding regulatory protein Gs alpha-S chain, putative | 0.0047 | 0.0193 | 0.0193 |
Echinococcus granulosus | guanine nucleotide binding protein Gs subunit | 0.0047 | 0.0193 | 0.0217 |
Schistosoma mansoni | sodium/chloride dependent transporter | 0.0073 | 0.0681 | 0.0764 |
Schistosoma mansoni | Guanine nucleotide-binding protein G(s) subunit alpha (Adenylate cyclase-stimulating G alpha protein) | 0.0047 | 0.0193 | 0.0217 |
Echinococcus multilocularis | guanine nucleotide binding protein G(s) subunit | 0.0047 | 0.0193 | 0.0217 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = 49.12 cm | Locomotor activity in mouse assessed as distance traveled by animal in horizontal locomotion at 25 mg/kg, po after 60 mins measured for 30 mins by spontaneous locomotor activity | ChEMBL. | 20637635 |
IC50 (binding) | = 64 nM | Displacement of [3H]mesulergine from human recombinant 5HT2C expressed in CHOK1 cells | ChEMBL. | 20637635 |
IC50 (binding) | = 152 nM | Displacement of [3H]ketanserin from human recombinant 5HT2A expressed in CHOK1 cells | ChEMBL. | 20637635 |
IC50 (binding) | = 7096 nM | Displacement of [3H]imipramine from human SERT expressed in HEK293 cells | ChEMBL. | 20637635 |
Inhibition (functional) | = 210 % | Antidepressant activity in mouse assessed as inhibition of mobility at 25 mg/kg, po after 60 mins by forced swim test assay | ChEMBL. | 20637635 |
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.