Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | potassium voltage-gated channel, subfamily H (eag-related), member 2 | Starlite/ChEMBL | References |
Homo sapiens | adrenoceptor beta 3 | Starlite/ChEMBL | References |
Homo sapiens | adrenoceptor beta 2, surface | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = 93 % | Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation at 10'-10 to 10'-5 M after 30 mins by time-resolved fluorescence assay relative to R-(-)isoproterenol | ChEMBL. | 24437735 |
EC50 (functional) | = 0.15 nM | Agonist activity at human beta-3 adrenergic receptor expressed in CHO cells assessed as increase in intracellular cAMP accumulation after 30 mins by time-resolved fluorescence assay | ChEMBL. | 24437735 |
IC50 (binding) | = 8451 nM | Displacement of [125I]-cyanopindolol from recombinant human beta-2 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysis | ChEMBL. | 24437735 |
IC50 (binding) | > 20000 nM | Displacement of [125I]-cyanopindolol from recombinant human beta-1 adrenergic receptor expressed in CHO cell membranes after 1 hr by scintillation counting analysis | ChEMBL. | 24437735 |
IC50 (binding) | = 1.5 uM | Inhibition of human ERG | ChEMBL. | 24437735 |
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.