Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | Glutamate receptor ionotropic kainate 3 | Starlite/ChEMBL | References |
Rattus norvegicus | Glutamate receptor ionotropic kainate 1 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus multilocularis | glutamate receptor, ionotrophic, AMPA 3 | Glutamate receptor ionotropic kainate 3 | 919 aa | 969 aa | 27.6 % |
Drosophila melanogaster | Glutamate receptor IA | Glutamate receptor ionotropic kainate 1 | 949 aa | 913 aa | 34.5 % |
Drosophila melanogaster | NMDA receptor 2 | Glutamate receptor ionotropic kainate 3 | 919 aa | 833 aa | 23.1 % |
Onchocerca volvulus | Glutamate receptor ionotropic kainate 3 | 919 aa | 920 aa | 31.4 % | |
Onchocerca volvulus | Putative 39S ribosomal protein L45, mitochondrial | Glutamate receptor ionotropic kainate 3 | 919 aa | 834 aa | 31.7 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | glutamate receptor ionotropic kainate | 0.0097 | 0.0067 | 0.0067 |
Echinococcus multilocularis | glutamate (NMDA) receptor subunit | 0.0061 | 0.0015 | 0.0015 |
Echinococcus granulosus | glutamate receptor 2 | 0.0072 | 0.0032 | 0.0032 |
Schistosoma mansoni | kinase | 0.0185 | 0.0192 | 0.0177 |
Schistosoma mansoni | glutamate receptor kainate | 0.0135 | 0.0121 | 0.0106 |
Echinococcus multilocularis | Glutamate receptor, ionotropic kainate 2 | 0.0147 | 0.0138 | 0.0138 |
Echinococcus granulosus | glutamate NMDA receptor subunit | 0.0061 | 0.0015 | 0.0015 |
Echinococcus multilocularis | dual specificity mitogen activated protein | 0.0185 | 0.0192 | 0.0192 |
Echinococcus granulosus | glutamate receptor ionotrophic AMPA 3 | 0.0072 | 0.0032 | 0.0032 |
Echinococcus multilocularis | glutamate receptor 2 | 0.0072 | 0.0032 | 0.0032 |
Echinococcus multilocularis | Glutamate receptor, ionotropic kainate 2 | 0.0147 | 0.0138 | 0.0138 |
Echinococcus granulosus | Glutamate receptor ionotropic kainate 2 | 0.0147 | 0.0138 | 0.0138 |
Echinococcus multilocularis | dual specificity mitogen activated protein | 0.7107 | 1 | 1 |
Loa Loa (eye worm) | STE/STE7/MEK4 protein kinase | 0.0185 | 0.0192 | 0.0177 |
Brugia malayi | Serine/threonine-protein kinase F42G10.2 | 0.0185 | 0.0192 | 0.0177 |
Loa Loa (eye worm) | STE/STE7/MEK7 protein kinase | 0.7107 | 1 | 1 |
Onchocerca volvulus | Kinase homolog | 0.0185 | 0.0192 | 0.5 |
Echinococcus granulosus | Glutamate receptor ionotropic kainate 2 | 0.0147 | 0.0138 | 0.0138 |
Echinococcus multilocularis | Glutamate receptor, ionotropic kainate 2 | 0.0147 | 0.0138 | 0.0138 |
Echinococcus granulosus | Glutamate receptor ionotropic kainate 2 | 0.0147 | 0.0138 | 0.0138 |
Schistosoma mansoni | glutamate receptor NMDA | 0.0072 | 0.0032 | 0.0016 |
Echinococcus granulosus | dual specificity mitogen activated protein | 0.7107 | 1 | 1 |
Echinococcus granulosus | glutamate receptor ionotropic kainate | 0.0097 | 0.0067 | 0.0067 |
Echinococcus granulosus | dual specificity mitogen activated protein | 0.0185 | 0.0192 | 0.0192 |
Schistosoma mansoni | glutamate receptor kainate | 0.0135 | 0.0121 | 0.0106 |
Schistosoma mansoni | protein kinase | 0.7107 | 1 | 1 |
Echinococcus multilocularis | glutamate receptor 2 | 0.0061 | 0.0015 | 0.0015 |
Echinococcus granulosus | glutamate receptor ionotropic kainate 3 | 0.0097 | 0.0067 | 0.0067 |
Loa Loa (eye worm) | STE/STE7/MEK7 protein kinase | 0.7107 | 1 | 1 |
Echinococcus multilocularis | glutamate receptor, ionotrophic, AMPA 3 | 0.0072 | 0.0032 | 0.0032 |
Echinococcus multilocularis | Glutamate receptor, ionotropic kainate 3 | 0.0097 | 0.0067 | 0.0067 |
Echinococcus multilocularis | NMDA receptor | 0.0097 | 0.0067 | 0.0067 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 300 uM | Inhibition of human EAAT2 expressed in HEK293 cells by [3H]-D-Asp uptake assay | ChEMBL. | 23414088 |
IC50 (binding) | > 1000 uM | Inhibition of human EAAT3 expressed in HEK293 cells by [3H]-D-Asp uptake assay | ChEMBL. | 23414088 |
IC50 (binding) | > 1000 uM | Inhibition of human EAAT1 expressed in HEK293 cells by [3H]-D-Asp uptake assay | ChEMBL. | 23414088 |
Ki (binding) | = 0.82 uM | Displacement of [3H]-(2S,4R)-4-methylglutamic acid from full length recombinant rat GluKK1(Q)1b receptor expressed in sf9 cells by liquid scintillation counting | ChEMBL. | 23414088 |
Ki (binding) | = 2.81 uM | Displacement of [3H]-(2S,4R)-4-methylglutamic acid from full length recombinant rat GluK3 receptor expressed in sf9 cells by liquid scintillation counting | ChEMBL. | 23414088 |
Ki (binding) | = 28.4 uM | Displacement of [3H]-(2S,4R)-4-methylglutamic acid from full length recombinant rat GluKK2(VCR) receptor expressed in sf9 cells by liquid scintillation counting | ChEMBL. | 23414088 |
Ki (binding) | > 100 uM | Displacement of [3H]AMPA from full length recombinant rat GluKA2(R) receptor expressed in sf9 cells by liquid scintillation counting | ChEMBL. | 23414088 |
Ki (binding) | > 100 uM | Displacement of [3H]CGP39653 from NMDA receptor in rat brain cortex after 60 mins by Packard TopCount microplate scintillator counting | ChEMBL. | 23414088 |
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.