Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | potassium channel, subfamily K, member 3 | No references |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | Twik (KCNK-like) family of potassium channels, alpha subunit 28 | potassium channel, subfamily K, member 3 | 394 aa | 450 aa | 24.2 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.0231 | 1 | 1 |
Echinococcus multilocularis | Two pore potassium channel protein sup 9 | 0.0231 | 1 | 0.5 |
Echinococcus granulosus | Two pore potassium channel protein sup 9 | 0.0231 | 1 | 0.5 |
Schistosoma mansoni | twik family of potassium channels-related | 0.0231 | 1 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0231 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 804 nM | BindingDB_Patents: Inhibition Assay. Human TASK-1 channels were expressed in Xenopus oocytes. For this purpose, oocytes were isolated from Xenopus laevis and defoliculated. Subsequently, TASK- 1 -encoding RNA synthesized in vitro was injected into oocytes. After two days of TASK-1 protein expression, TASK-1 currents were measured by two-microelectrode voltage clamp. Data were acquired and analyzed using a TEC-10cx amplifier (NPI Electronic, Tamm, Germany) connected to an ITC-16 interface (Instrutech Corp., Long Island, USA) and Pulse software (HEKA Elektronik, Lambrecht, Germany). Oocytes were clamped to -90 mV and TASK-1 mediated currents were measured during 500 ms voltage pulses to 40 mV. Oocytes were continuously superfused with ND96 buffer containing: NaCI 96 mM, KCI2 mM, CaCI21.8 mM, MgCI21 mM, HEPES 5 mM (pH adjusted to 7.4 with NaOH). | ChEMBL. | No reference |
IC50 (binding) | = 804 nM | BindingDB_Patents: Inhibition Assay. Human TASK-1 channels were expressed in Xenopus oocytes. For this purpose, oocytes were isolated from Xenopus laevis and defoliculated. Subsequently, TASK- 1 -encoding RNA synthesized in vitro was injected into oocytes. After two days of TASK-1 protein expression, TASK-1 currents were measured by two-microelectrode voltage clamp. Data were acquired and analyzed using a TEC-10cx amplifier (NPI Electronic, Tamm, Germany) connected to an ITC-16 interface (Instrutech Corp., Long Island, USA) and Pulse software (HEKA Elektronik, Lambrecht, Germany). Oocytes were clamped to -90 mV and TASK-1 mediated currents were measured during 500 ms voltage pulses to 40 mV. Oocytes were continuously superfused with ND96 buffer containing: NaCI 96 mM, KCI2 mM, CaCI21.8 mM, MgCI21 mM, HEPES 5 mM (pH adjusted to 7.4 with NaOH). | 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.