Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | glutamate receptor, metabotropic 5 | Starlite/ChEMBL | References |
Rattus norvegicus | Metabotropic glutamate receptor 5 | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | < 70 % | Induction of rat mGluR5 activation expressed in HEK293A cells assessed as maximal response in presence of glutamate | ChEMBL. | 18550372 |
Activity (binding) | = 73 % | Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay relative to glutamate | ChEMBL. | 23947773 |
EC50 (binding) | = 6.75 | Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay | ChEMBL. | 23947773 |
EC50 (binding) | = 10 nM | Effective concentration against metabotropic glutamate receptor 5 of human transfected into CHO cells | ChEMBL. | 15537338 |
EC50 (binding) | = 10 nM | Effective concentration against metabotropic glutamate receptor 5 of human transfected into CHO cells | ChEMBL. | 15537338 |
EC50 (binding) | = 20 nM | Effective concentration against metabotropic glutamate receptor 5 of rat | ChEMBL. | 15537338 |
EC50 (binding) | = 20 nM | Effective concentration against metabotropic glutamate receptor 5 of rat | ChEMBL. | 15537338 |
EC50 (binding) | = 27 nM | Positive allosteric modulation of human mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay | ChEMBL. | 24050755 |
EC50 (binding) | = 77 nM | Activity at mGluR5 assessed as potentiation of glutamate-induced calcium flux in rat astrocytes | ChEMBL. | 16722652 |
EC50 (binding) | = 77 nM | Activity at mGluR5 assessed as potentiation of glutamate-induced calcium flux in rat astrocytes | ChEMBL. | 16722652 |
EC50 (binding) | = 98 nM | Positive allosteric modulation of rat mGluR5 stably expressed in CHO cells assessed as Ca2+ flux by FLIPR assay | ChEMBL. | 24050755 |
EC50 (binding) | = 176 nM | Positive allosteric modulation of human mGluR5a transfected in HEK293 cells by calcium mobilization assay | ChEMBL. | 23947773 |
Ki (binding) | = 3760 nM | Displacement of [3H]methoxyPEPy from rat mGluR5 expressed in HEK293 cells | ChEMBL. | 16722652 |
Ki (binding) | = 3760 nM | Displacement of [3H]methoxyPEPy from rat mGluR5 expressed in HEK293 cells | ChEMBL. | 16722652 |
Ki (binding) | = 0.25 uM | Displacement of [3H]-MPEP from human mGluR5 | ChEMBL. | 21067920 |
Potentiation (functional) | = 4 | Fold potentiation in CHO cells overexpressing human metabotropic glutamate receptor 5 | ChEMBL. | 15537338 |
Potentiation (functional) | = 4.3 | Fold potentiation towards rat metabotropic glutamate receptor 5 | ChEMBL. | 15537338 |
Potentiation (functional) | = 4 | Fold potentiation in CHO cells overexpressing human metabotropic glutamate receptor 5 | ChEMBL. | 15537338 |
Potentiation (functional) | = 4.3 | Fold potentiation towards rat metabotropic glutamate receptor 5 | ChEMBL. | 15537338 |
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.
5 literature references were collected for this gene.