Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | Voltage-gated calcium channel alpha2/delta subunit 1 | Starlite/ChEMBL | References |
Sus scrofa | Voltage-dependent calcium channel alpha2delta subunit | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Echinococcus granulosus | voltage dependent calcium channel subunit | Get druggable targets OG5_133164 | All targets in OG5_133164 |
Echinococcus multilocularis | voltage dependent calcium channel subunit | Get druggable targets OG5_133164 | All targets in OG5_133164 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus granulosus | voltage dependent calcium channel subunit | Voltage-gated calcium channel alpha2/delta subunit 1 | 1091 aa | 1030 aa | 23.2 % |
Echinococcus multilocularis | voltage dependent calcium channel subunit | Voltage-gated calcium channel alpha2/delta subunit 1 | 1091 aa | 984 aa | 23.7 % |
Onchocerca volvulus | Voltage-gated calcium channel alpha2/delta subunit 1 | 1091 aa | 1104 aa | 23.7 % | |
Brugia malayi | Cache domain containing protein | Voltage-gated calcium channel alpha2/delta subunit 1 | 1091 aa | 1090 aa | 23.4 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | voltage dependent calcium channel subunit | 0.071 | 1 | 1 |
Treponema pallidum | methyl-accepting chemotaxis protein (mcp2-1) | 0.0657 | 0.9034 | 0.5 |
Schistosoma mansoni | dihydropyridine-sensitive l-type calcium channel | 0.031 | 0.2632 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = 100 % | Protection against audiogenically induced tonic seizure in DBA/2 mouse at 30 mg/kg, po | ChEMBL. | 15946842 |
Activity (functional) | = 100 % | Protection against audiogenically induced tonic seizure in DBA/2 mouse at 30 mg/kg, po | ChEMBL. | 15946842 |
AUC (ADMET) | = 5.2 ug.hr/ml | AUC in rat | ChEMBL. | 15946842 |
CL (ADMET) | = 10.6 ml/min.Kg | Clearance in rat | ChEMBL. | 15946842 |
F (ADMET) | = 85 % | Oral bioavailability in rat | ChEMBL. | 15946842 |
IC50 (binding) | = 100 nM | Displacement of [3H]gabapentin from alpha2delta calcium channel in pig brain membrane | ChEMBL. | 15946842 |
IC50 (binding) | = 100 nM | Displacement of [3H]gabapentin from alpha2-delta calcium channel in pig brain | ChEMBL. | 17489571 |
IC50 (binding) | = 100 nM | Displacement of [3H]gabapentin from alpha2delta calcium channel in pig brain membrane | ChEMBL. | 15946842 |
IC50 (functional) | = 5.7 uM | Inhibition of potassium-evoked [3H]norepinephrine release from rat neocortex | ChEMBL. | 15946842 |
IC50 (functional) | = 5.7 uM | Inhibition of potassium-evoked [3H]norepinephrine release from rat neocortex | ChEMBL. | 15946842 |
T1/2 (ADMET) | = 1 hr | Plasma half life in rat | ChEMBL. | 15946842 |
Vdss (ADMET) | = 0.38 L/Kg | Volume of distribution in rat | ChEMBL. | 15946842 |
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.
2 literature references were collected for this gene.