Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | glutamate receptor, ionotropic, AMPA 1 | References | |
Homo sapiens | cytochrome P450, family 1, subfamily A, polypeptide 2 | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus granulosus | Glutamate receptor ionotropic kainate 2 | glutamate receptor, ionotropic, AMPA 1 | 906 aa | 779 aa | 33.5 % |
Brugia malayi | Cytochrome P450 family protein | cytochrome P450, family 1, subfamily A, polypeptide 2 | 516 aa | 470 aa | 26.2 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | glutamate receptor 4 | 0.0051 | 0.3651 | 0.3651 |
Echinococcus multilocularis | glutamate receptor 2 | 0.0087 | 1 | 1 |
Echinococcus multilocularis | Glutamate receptor, ionotropic kainate 2 | 0.0036 | 0.1012 | 0.1012 |
Echinococcus multilocularis | glutamate receptor, ionotrophic, AMPA 3 | 0.0087 | 1 | 1 |
Echinococcus multilocularis | Glutamate receptor, ionotropic kainate 2 | 0.0036 | 0.1012 | 0.1012 |
Echinococcus granulosus | Glutamate receptor ionotropic kainate 2 | 0.0036 | 0.1012 | 0.1012 |
Brugia malayi | Glutamate receptor 1 precursor | 0.0081 | 0.8988 | 0.5 |
Echinococcus granulosus | glutamate receptor 4 | 0.0051 | 0.3651 | 0.3651 |
Brugia malayi | Glutamate receptor 2 precursor | 0.0081 | 0.8988 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0051 | 0.3651 | 0.4062 |
Schistosoma mansoni | glutamate receptor NMDA | 0.0036 | 0.1012 | 1 |
Echinococcus granulosus | glutamate receptor subunit protein glur | 0.0062 | 0.5626 | 0.5626 |
Echinococcus granulosus | Glutamate receptor ionotropic kainate 2 | 0.0036 | 0.1012 | 0.1012 |
Loa Loa (eye worm) | hypothetical protein | 0.0051 | 0.3651 | 0.4062 |
Echinococcus granulosus | glutamate receptor 2 | 0.0076 | 0.8025 | 0.8025 |
Echinococcus multilocularis | glutamate receptor subunit protein glur | 0.0062 | 0.5626 | 0.5626 |
Loa Loa (eye worm) | hypothetical protein | 0.0051 | 0.3651 | 0.4062 |
Echinococcus granulosus | glutamate receptor 1 | 0.0051 | 0.3651 | 0.3651 |
Echinococcus multilocularis | Glutamate receptor, ionotropic kainate 2 | 0.0036 | 0.1012 | 0.1012 |
Echinococcus granulosus | glutamate receptor ionotrophic AMPA 3 | 0.0087 | 1 | 1 |
Echinococcus granulosus | Glutamate receptor ionotropic kainate 2 | 0.0036 | 0.1012 | 0.1012 |
Echinococcus multilocularis | glutamate receptor 2 | 0.0076 | 0.8025 | 0.8025 |
Echinococcus multilocularis | glutamate receptor 2 | 0.0081 | 0.8988 | 0.8988 |
Loa Loa (eye worm) | glutamate receptor 1 | 0.0081 | 0.8988 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (ADMET) | = 230 nM | Inhibition of human CYP1A2 | ChEMBL. | 27067148 |
IC50 (binding) | = 353 nM | Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cells coexpressing TARP gamma-8 and human EAAT3 assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutamate addition by fluo-4 AM dye based fluorescence imaging plate reader method | ChEMBL. | 27067148 |
IC50 (binding) | > 83300 nM | Antagonist activity at human iGluA1 receptor flip isoform expressed in CHO-S cells assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutamate addition by fluo-4 NW dye based fluorescence imaging plate reader method | ChEMBL. | 27067148 |
IC50 (binding) | > 83300 nM | Antagonist activity at human iGluA1 receptor flop isoform expressed in CHO-S cells coexpressing TARP gamma-2 assessed as inhibition of glutamate-induced increase in intracellular calcium levels after 2 mins followed by cyclothiazide/glutamate addition by fluo-4 AM dye based fluorescence imaging plate reader method | ChEMBL. | 27067148 |
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.