Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | transient receptor potential cation channel, subfamily V, member 1 | Starlite/ChEMBL | No references |
Rattus norvegicus | Vanilloid receptor | Starlite/ChEMBL | No references |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Ki (binding) | = 7.7 nM | BindingDB_Patents: FLIPR Assay. The FLIPR protocol consists of two substance additions. Initially, the compounds to be tested (10 uM) are pipeted onto the cells and the Ca2+ influx is compared with the control (capsaicin 10 uM). Information is gained therefrom in percentage activation relative to the Ca2+ signal after addition of 10 uM of capsaicin (CP). After incubation for 5 minutes, 100 nM of capsaicin are applied and the influx of Ca2+ is likewise determined. Desensitizing agonists and antagonists lead to suppression of the Ca2+ influx. The percentage inhibition is calculated in comparison with the maximum inhibition achieved with 10 uM of capsaicin. | ChEMBL. | No reference |
Ki (binding) | = 7.9 nM | BindingDB_Patents: FLIPR Assay. The FLIPR protocol consists of two substance additions. Initially, the compounds to be tested (10 uM) are pipeted onto the cells and the Ca2+ influx is compared with the control (capsaicin 10 uM). Information is gained therefrom in percentage activation relative to the Ca2+ signal after addition of 10 uM of capsaicin (CP). After incubation for 5 minutes, 100 nM of capsaicin are applied and the influx of Ca2+ is likewise determined. Desensitizing agonists and antagonists lead to suppression of the Ca2+ influx. The percentage inhibition is calculated in comparison with the maximum inhibition achieved with 10 uM of capsaicin. | ChEMBL. | No reference |
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.