Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | Metabotropic glutamate receptor 4 | Starlite/ChEMBL | References |
Homo sapiens | glutamate receptor, metabotropic 4 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Onchocerca volvulus | Cell death abnormality protein 8 homolog | Metabotropic glutamate receptor 4 | 912 aa | 874 aa | 39.1 % |
Schistosoma mansoni | metabotropic glutamate receptor | Metabotropic glutamate receptor 4 | 912 aa | 903 aa | 25.6 % |
Loa Loa (eye worm) | hypothetical protein | Metabotropic glutamate receptor 4 | 912 aa | 881 aa | 20.9 % |
Onchocerca volvulus | Golgi-associated plant pathogenesis-related protein 1 homolog | Metabotropic glutamate receptor 4 | 912 aa | 826 aa | 34.7 % |
Onchocerca volvulus | Metabotropic glutamate receptor 4 | 912 aa | 841 aa | 21.0 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Plasmodium vivax | protein kinase Crk2 | 0.0097 | 0.0947 | 0.5 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0097 | 0.0947 | 0.074 |
Loa Loa (eye worm) | CMGC/MAPK/ERK1 protein kinase | 0.0562 | 1 | 1 |
Leishmania major | mitogen activated protein kinase, putative,map kinase, putative | 0.0562 | 1 | 1 |
Brugia malayi | cell division control protein 2 homolog | 0.0097 | 0.0947 | 0.074 |
Echinococcus granulosus | mitogen activated protein kinase 3 | 0.0562 | 1 | 1 |
Echinococcus multilocularis | mitogen activated protein kinase 3 | 0.0562 | 1 | 1 |
Trypanosoma cruzi | mitogen activated protein kinase 4, putative | 0.0562 | 1 | 1 |
Entamoeba histolytica | cell division protein kinase 2, putative | 0.0097 | 0.0947 | 0.5 |
Echinococcus multilocularis | mitogen activated protein kinase | 0.0562 | 1 | 1 |
Trypanosoma cruzi | mitogen-activated protein kinase 11, putative | 0.0562 | 1 | 1 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0562 | 1 | 1 |
Giardia lamblia | Kinase, CMGC MAPK | 0.0562 | 1 | 1 |
Trypanosoma cruzi | mitogen activated protein kinase 2, putative | 0.0562 | 1 | 1 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0562 | 1 | 1 |
Toxoplasma gondii | CMGC kinase, MAPK family (ERK) MAPK-1 | 0.0562 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.015 | 0.1992 | 0.1992 |
Loa Loa (eye worm) | CMGC/CDK/CDK5 protein kinase | 0.0097 | 0.0947 | 0.0947 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0097 | 0.0947 | 0.074 |
Echinococcus granulosus | metabotropic glutamate receptor 5 | 0.015 | 0.1992 | 0.1153 |
Brugia malayi | Protein kinase domain containing protein | 0.0097 | 0.0947 | 0.074 |
Entamoeba histolytica | cell division protein kinase 2, putative | 0.0097 | 0.0947 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0562 | 1 | 1 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0562 | 1 | 1 |
Brugia malayi | metabotropic glutamate receptor subtype 5a (mGluR5a), putative | 0.0111 | 0.1219 | 0.1018 |
Echinococcus granulosus | metabotropic glutamate receptor 2 | 0.0102 | 0.1056 | 0.012 |
Echinococcus multilocularis | metabotropic glutamate receptor 5 | 0.015 | 0.1992 | 0.1153 |
Plasmodium falciparum | protein kinase 5 | 0.0097 | 0.0947 | 0.5 |
Trypanosoma brucei | protein kinase, putative | 0.0562 | 1 | 1 |
Brugia malayi | Metabotropic glutamate receptor precursor. | 0.0122 | 0.1442 | 0.1247 |
Schistosoma mansoni | metabotropic glutamate receptor | 0.0102 | 0.1056 | 0.0852 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0562 | 1 | 1 |
Loa Loa (eye worm) | CMGC/CDK/CDC2 protein kinase | 0.0097 | 0.0947 | 0.0947 |
Trypanosoma cruzi | mitogen-activated protein kinase 11, putative | 0.0562 | 1 | 1 |
Loa Loa (eye worm) | CMGC/CDK/CDC2 protein kinase | 0.0097 | 0.0947 | 0.0947 |
Loa Loa (eye worm) | glutamate receptor | 0.0122 | 0.1442 | 0.1442 |
Echinococcus multilocularis | metabotropic glutamate receptor 2 | 0.0102 | 0.1056 | 0.012 |
Leishmania major | mitogen activated protein kinase 4, putative;with=GeneDB:LmxM19.1440 | 0.0562 | 1 | 1 |
Schistosoma mansoni | metabotropic glutamate receptor 2 3 (mglur group 2) | 0.0139 | 0.1768 | 0.158 |
Loa Loa (eye worm) | hypothetical protein | 0.0091 | 0.083 | 0.083 |
Trypanosoma brucei | mitogen activated protein kinase 4, putative | 0.0562 | 1 | 1 |
Echinococcus granulosus | mitogen activated protein kinase | 0.0562 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | = 99.7 % | Positive allosteric modulation of human mGlu4 receptor expressed in CHO cells coexpressing Gqi5 assessed as potentiation of glutamate-induced calcium mobilization relative to (-)-PHCCC | ChEMBL. | 21966889 |
Activity (binding) | = 124.3 % | Positive allosteric modulation of rat mGlu4 receptor assessed as potentiation of glutamate-induced thallium flux relative to (-)-PHCCC | ChEMBL. | 21966889 |
EC50 (binding) | = 136 nM | Positive allosteric modulator activity at human mGlu4 receptor expressed in CHO cells expressing Gqi5 by calcium mobilization assay | ChEMBL. | 21966889 |
EC50 (binding) | = 165 nM | Positive allosteric modulator activity at rat mGlu4 receptor by thallium flux assay | ChEMBL. | 21966889 |
IC50 (ADMET) | > 30 uM | Inhibition of CYP1A2 in human liver microsomes using acetaminophen as substrate | ChEMBL. | 21966889 |
IC50 (ADMET) | > 30 uM | Inhibition of CYP2C9 in human liver microsomes using 4-hydroxydiclofenac as substrate | ChEMBL. | 21966889 |
IC50 (ADMET) | > 30 uM | Inhibition of CYP2D6 in human liver microsomes using dextrophan tartarate as substrate | ChEMBL. | 21966889 |
IC50 (ADMET) | > 30 uM | Inhibition of CYP3A4 in human liver microsomes using 1-hydroxymidazolam as substrate | ChEMBL. | 21966889 |
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.