Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | dopamine receptor D2 | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | = 0.3 nM | Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay | ChEMBL. | 22845053 |
EC50 (functional) | = 0.8 nM | Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay | ChEMBL. | 22845053 |
ED50 (functional) | > 8 uM kg-1 | post-synaptic dopamine autoreceptor antagonist activity evaluated by inhibition of the apomorphine-induced stereotyped behavior in mice. | ChEMBL. | 9513593 |
ED50 (functional) | > 8 uM kg-1 | post-synaptic dopamine autoreceptor antagonist activity evaluated by inhibition of the apomorphine-induced stereotyped behavior in mice. | ChEMBL. | 9513593 |
Emax (functional) | = 89 % | Agonist activity at D2L receptor in human HTLA cells assessed as beta arrestin recruitment at 6 uM after 18 hrs by luminescence assay relative to Quinpirole | ChEMBL. | 22845053 |
Emax (functional) | = 93 % | Agonist activity at human D2L receptor expressed in HEK293T cells coexpressing Gi subunit assessed as inhibition of isoproterenol-stimulated cAMP production by luminescence assay relative to quinpirole | ChEMBL. | 22845053 |
Ki (binding) | = 5.5 nM | Displacement of [3H]N-methylspiperone from human D2L receptor expressed in CHO cells after 1.5 hrs by microbeta counting method | ChEMBL. | 22845053 |
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.
2 literature references were collected for this gene.