Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | opioid receptor, kappa 1 | Starlite/ChEMBL | References |
Homo sapiens | opioid receptor, mu 1 | Starlite/ChEMBL | References |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (functional) | = 9.7 nM | Antagonist activity assessed as inhibition of loperamide-stimulated [35S]GTPgammaS binding to human mu opioid receptor expressed in CHO cells | ChEMBL. | 17149859 |
IC50 (functional) | = 9.7 nM | Antagonist activity assessed as inhibition of loperamide-stimulated [35S]GTPgammaS binding to human mu opioid receptor expressed in CHO cells | ChEMBL. | 17149859 |
Inhibition (binding) | = 55 % | Inhibition of [3H]diprenorphine binding to human cloned delta opioid receptor expressed in CHO cells at 10 uM | ChEMBL. | 17149859 |
Inhibition (binding) | = 55 % | Inhibition of [3H]diprenorphine binding to human cloned delta opioid receptor expressed in CHO cells at 10 uM | ChEMBL. | 17149859 |
Ki (binding) | = 21 nM | Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells | ChEMBL. | 17149859 |
Ki (binding) | = 21 nM | Displacement of [3H]diprenorphine from human cloned mu opioid receptor expressed in CHO cells | ChEMBL. | 17149859 |
Ki (binding) | = 24 nM | Displacement of [3H]diprenorphine from human cloned kappa opioid receptor expressed in CHO cells | ChEMBL. | 17149859 |
Ki (binding) | = 24 nM | Displacement of [3H]diprenorphine from human cloned kappa opioid receptor expressed in CHO cells | ChEMBL. | 17149859 |
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.