Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 0.17 nM | Inhibitory activity against Opioid receptor kappa 1 in electrically stimulated guinea pig longitudinal ileal muscle (GPI) preparation. | ChEMBL. | 8648612 |
IC50 (binding) | = 1.2 nM | Inhibitory activity against Opioid receptor kappa 1 in electrically stimulated mouse vas deferens (MVD) preparation. | ChEMBL. | 8648612 |
Ki (binding) | = 0.31 nM | Binding affinity of the compound towards Opioid receptor kappa 1 in guinea pig brain | ChEMBL. | 8648612 |
Ki (binding) | = 18 nM | Binding affinity of the compound towards delta-1 opioid receptor in guinea pig brain | ChEMBL. | 8648612 |
Ki (binding) | = 43.8 nM | Binding affinity of the compound towards delta-2 opioid receptor in guinea pig brain | ChEMBL. | 8648612 |
Ki (binding) | = 286 nM | Binding affinity of the compound towards Opioid receptor mu 1 in guinea pig brain | ChEMBL. | 8648612 |
Recovery (functional) | = 39 % | Percent recovery of twitch height after 30-40 washes with buffer using smooth guinea pig ileal muscle | ChEMBL. | 8648612 |
Recovery (functional) | = 79 % | Percent recovery of twitch height after 30-40 washes with buffer using mouse vas deferens preparation | ChEMBL. | 8648612 |
Recovery (functional) | = 97 % | Percent recovery after treatment with 500 nM of NTX and removal of NTX by 40 washes with buffer using smooth guinea pig ileal muscle | ChEMBL. | 8648612 |
Selectivity ratio (binding) | = 58 | Selectivity ratio between delta-1 opioid receptor versus kappa opioid receptor | ChEMBL. | 8648612 |
Selectivity ratio (binding) | = 141 | Selectivity ratio between delta-2 opioid receptor versus kappa opioid receptor | ChEMBL. | 8648612 |
Selectivity ratio (binding) | = 922 | Selectivity ratio between mu opioid receptor versus kappa opioid receptor | ChEMBL. | 8648612 |
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.