Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | 5-hydroxytryptamine (serotonin) receptor 2A, 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 2C, 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 granulosus | guanine nucleotide binding protein Gs subunit | 0.0047 | 0.0193 | 0.0217 |
Schistosoma mansoni | norepinephrine/norepinephrine 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 |
Brugia malayi | hypothetical protein | 0.0232 | 0.3713 | 0.3713 |
Entamoeba histolytica | hypothetical protein | 0.0037 | 0 | 0.5 |
Brugia malayi | GTP-binding regulatory protein Gs alpha-S chain, putative | 0.0047 | 0.0193 | 0.0193 |
Schistosoma mansoni | sodium/chloride dependent transporter | 0.0073 | 0.0681 | 0.0764 |
Echinococcus multilocularis | guanine nucleotide binding protein G(s) subunit | 0.0047 | 0.0193 | 0.0217 |
Echinococcus multilocularis | leukotriene A 4 hydrolase | 0.0504 | 0.8914 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0073 | 0.0681 | 0.0559 |
Schistosoma mansoni | leukotriene A4 hydrolase (M01 family) | 0.0504 | 0.8914 | 1 |
Loa Loa (eye worm) | norepinephrine transporter | 0.0073 | 0.0681 | 0.0559 |
Brugia malayi | Sodium:neurotransmitter symporter family protein | 0.0073 | 0.0681 | 0.0681 |
Loa Loa (eye worm) | hypothetical protein | 0.0073 | 0.0681 | 0.0559 |
Loa Loa (eye worm) | hypothetical protein | 0.0073 | 0.0681 | 0.0559 |
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 |
Echinococcus granulosus | leukotriene A 4 hydrolase | 0.0504 | 0.8914 | 1 |
Echinococcus granulosus | serotonin transporter | 0.0073 | 0.0681 | 0.0764 |
Treponema pallidum | sodium- and chloride- dependent transporter | 0.0073 | 0.0681 | 0.5 |
Echinococcus multilocularis | guanine nucleotide binding protein G(s) subunit | 0.0047 | 0.0193 | 0.0217 |
Schistosoma mansoni | Guanine nucleotide-binding protein G(s) subunit alpha (Adenylate cyclase-stimulating G alpha protein) | 0.0047 | 0.0193 | 0.0217 |
Onchocerca volvulus | 0.0073 | 0.0681 | 0.5 | |
Echinococcus multilocularis | serotonin transporter | 0.0073 | 0.0681 | 0.0764 |
Entamoeba histolytica | hypothetical protein | 0.0037 | 0 | 0.5 |
Loa Loa (eye worm) | leukotriene A4 hydrolase | 0.0504 | 0.8914 | 1 |
Entamoeba histolytica | hypothetical protein | 0.0037 | 0 | 0.5 |
Loa Loa (eye worm) | serotonin transporter b | 0.0073 | 0.0681 | 0.0559 |
Echinococcus granulosus | guanine nucleotide binding protein Gs subunit | 0.0047 | 0.0193 | 0.0217 |
Loa Loa (eye worm) | solute carrier family 6 member 4 | 0.0073 | 0.0681 | 0.0559 |
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.