Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | Transient receptor potential cation channel subfamily M member 8 | Starlite/ChEMBL | References |
Rattus norvegicus | Transient receptor potential cation channel subfamily A member 1 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Schistosoma mansoni | transient receptor potential cation channel subfamily m member | Transient receptor potential cation channel subfamily M member 8 | 1104 aa | 1070 aa | 24.6 % |
Echinococcus granulosus | transient receptor potential cation channel | Transient receptor potential cation channel subfamily M member 8 | 1104 aa | 1098 aa | 25.1 % |
Echinococcus multilocularis | transient receptor potential cation channel | Transient receptor potential cation channel subfamily M member 8 | 1104 aa | 1095 aa | 25.2 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | ankyrin repeat protein | 0.0192 | 0.968 | 0.968 |
Echinococcus granulosus | transient receptor potential cation channel | 0.0198 | 0.9985 | 1 |
Echinococcus multilocularis | transient receptor potential cation channel | 0.0006 | 0.0015 | 0.0015 |
Schistosoma mansoni | transient receptor potential cation channel subfamily A member | 0.0192 | 0.968 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0006 | 0.0015 | 1 |
Echinococcus multilocularis | short transient receptor potential channel 6 | 0.0006 | 0.0015 | 0.0015 |
Echinococcus granulosus | transient receptor potential cation channel | 0.0006 | 0.0015 | 0.0015 |
Brugia malayi | olfactory channel protein osm-9 | 0.0006 | 0.0015 | 0.5 |
Echinococcus granulosus | short transient receptor potential channel 6 | 0.0006 | 0.0015 | 0.0015 |
Schistosoma mansoni | transient receptor potential channel | 0.0006 | 0.0015 | 0.0016 |
Echinococcus granulosus | ankyrin repeat protein | 0.0192 | 0.968 | 0.9695 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (binding) | = 4.7 uM | Activation of rat TRPA1 expressed in HEK293 cells assessed as stimulation of intracellular Ca2+ levels | ChEMBL. | 22503249 |
Efficacy (binding) | < 10 % | Activation of rat TRPM8 expressed in HEK293 cells assessed as stimulation of intracellular Ca2+ levels relative to 4 uM ionomycin | ChEMBL. | 22503249 |
Efficacy (binding) | = 162.8 % | Activation of rat TRPA1 expressed in HEK293 cells assessed as stimulation of intracellular Ca2+ levels relative to 100 uM allyl isothiocyanate | ChEMBL. | 22503249 |
IC50 (binding) | = 5.8 uM | Inhibition of rat TRPM8 expressed in HEK293 cells assessed as reduction in 0.25 uM icilin-stimulated increase in intracellular Ca2+ levels | ChEMBL. | 22503249 |
IC50 (binding) | = 7.2 uM | Inhibition of rat TRPA1 expressed in HEK293 cells assessed as reduction in 100 uM allyl isothiocyanate-stimulated increase in intracellular Ca2+ levels | ChEMBL. | 22503249 |
IC50 (binding) | = 13.9 uM | Inhibition of rat TRPM8 expressed in HEK293 cells assessed as reduction in 20 uM menthol-stimulated increase in intracellular Ca2+ levels | ChEMBL. | 22503249 |
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.