Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | Metabotropic glutamate receptor 3 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Onchocerca volvulus | Golgi-associated plant pathogenesis-related protein 1 homolog | Metabotropic glutamate receptor 3 | 879 aa | 827 aa | 35.9 % |
Loa Loa (eye worm) | hypothetical protein | Metabotropic glutamate receptor 3 | 879 aa | 782 aa | 21.0 % |
Onchocerca volvulus | Metabotropic glutamate receptor 3 | 879 aa | 784 aa | 21.6 % | |
Onchocerca volvulus | Cell death abnormality protein 8 homolog | Metabotropic glutamate receptor 3 | 879 aa | 867 aa | 43.3 % |
Schistosoma mansoni | metabotropic glutamate receptor | Metabotropic glutamate receptor 3 | 879 aa | 894 aa | 27.4 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | hypothetical protein | 0.0232 | 0.3758 | 0.4175 |
Onchocerca volvulus | 0.0487 | 0.9 | 0.5 | |
Mycobacterium leprae | PROBABLE THYMIDYLATE SYNTHASE THYA (TS) (TSASE) | 0.0487 | 0.9 | 1 |
Brugia malayi | metabotropic glutamate receptor subtype 5a (mGluR5a), putative | 0.0055 | 0.0137 | 0.0152 |
Brugia malayi | thymidylate synthase | 0.0487 | 0.9 | 1 |
Echinococcus multilocularis | metabotropic glutamate receptor 2 | 0.0051 | 0.0051 | 0.0057 |
Mycobacterium tuberculosis | Probable thymidylate synthase ThyA (ts) (TSASE) | 0.0487 | 0.9 | 1 |
Chlamydia trachomatis | dihydrofolate reductase | 0.0049 | 0 | 0.5 |
Trypanosoma cruzi | dihydrofolate reductase-thymidylate synthase | 0.0536 | 1 | 1 |
Schistosoma mansoni | bifunctional dihydrofolate reductase-thymidylate synthase | 0.0487 | 0.9 | 1 |
Loa Loa (eye worm) | glutamate receptor | 0.0061 | 0.0255 | 0.0283 |
Toxoplasma gondii | bifunctional dihydrofolate reductase-thymidylate synthase | 0.0536 | 1 | 0.5 |
Brugia malayi | Metabotropic glutamate receptor precursor. | 0.0061 | 0.0255 | 0.0283 |
Loa Loa (eye worm) | hypothetical protein | 0.0075 | 0.0545 | 0.0605 |
Echinococcus multilocularis | metabotropic glutamate receptor 5 | 0.0075 | 0.0545 | 0.0605 |
Echinococcus granulosus | metabotropic glutamate receptor 5 | 0.0075 | 0.0545 | 0.0605 |
Echinococcus granulosus | metabotropic glutamate receptor 2 | 0.0051 | 0.0051 | 0.0057 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0232 | 0.3758 | 0.5 |
Echinococcus granulosus | thymidylate synthase | 0.0487 | 0.9 | 1 |
Mycobacterium ulcerans | thymidylate synthase | 0.0487 | 0.9 | 1 |
Loa Loa (eye worm) | thymidylate synthase | 0.0487 | 0.9 | 1 |
Mycobacterium tuberculosis | Hypothetical protein | 0.0232 | 0.3758 | 0.4175 |
Plasmodium vivax | bifunctional dihydrofolate reductase-thymidylate synthase, putative | 0.0536 | 1 | 0.5 |
Echinococcus multilocularis | thymidylate synthase | 0.0487 | 0.9 | 1 |
Plasmodium falciparum | bifunctional dihydrofolate reductase-thymidylate synthase | 0.0536 | 1 | 0.5 |
Schistosoma mansoni | metabotropic glutamate receptor 2 3 (mglur group 2) | 0.0069 | 0.0427 | 0.0474 |
Trypanosoma brucei | dihydrofolate reductase-thymidylate synthase | 0.0536 | 1 | 0.5 |
Schistosoma mansoni | metabotropic glutamate receptor | 0.0051 | 0.0051 | 0.0057 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | = 1.6 % | Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells after 2.5 mins by calcium mobilization assay relative to glutamate | ChEMBL. | 23718281 |
IC50 (binding) | = 5.56 | Negative allosteric modulation of rat mGlu3 receptor transfected in human TREX cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins | ChEMBL. | 23718281 |
IC50 (functional) | 2.049017216 uM | PubChem BioAssay. Modulation of the Metabotropic Glutamate Receptor mGluR3 (Negative Allosteric Modulators mGlu3 Galpha15 Calcium Potency). (Class of assay: confirmatory) | ChEMBL. | No reference |
IC50 (binding) | > 30 uM | Negative allosteric modulation of rat mGlu2 receptor transfected in HEK293 cells assessed as inhibition of glutamate-induced calcium mobilization after 2.5 mins | ChEMBL. | 23718281 |
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.