Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | solute carrier family 8 (sodium/calcium exchanger), member 1 | Starlite/ChEMBL | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Plasmodium falciparum | choline kinase | 0.0257 | 1 | 1 |
Giardia lamblia | Ethanolamine kinase, putative | 0.0025 | 0 | 0.5 |
Schistosoma mansoni | sodium/calcium exchanger | 0.0091 | 0.2855 | 1 |
Brugia malayi | Sodium/calcium exchanger protein | 0.0036 | 0.0499 | 0.0499 |
Echinococcus multilocularis | sodium calcium exchanger | 0.0091 | 0.2855 | 0.2855 |
Trichomonas vaginalis | choline/ethanolamine kinase, putative | 0.0025 | 0 | 0.5 |
Entamoeba histolytica | choline/ethanolamine kinase, putative | 0.0025 | 0 | 0.5 |
Trypanosoma cruzi | choline ethanolamine kinase, putative | 0.0025 | 0 | 0.5 |
Toxoplasma gondii | phosphotransferase enzyme family protein | 0.0257 | 1 | 1 |
Echinococcus multilocularis | choline:ethanolamine kinase | 0.0257 | 1 | 1 |
Leishmania major | choline/ethanolamine kinase, putative | 0.0025 | 0 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0036 | 0.0499 | 0.0499 |
Plasmodium vivax | choline kinase, putative | 0.0257 | 1 | 1 |
Trypanosoma cruzi | choline kinase | 0.0025 | 0 | 0.5 |
Echinococcus granulosus | choline:ethanolamine kinase | 0.0257 | 1 | 1 |
Trypanosoma brucei | choline/ethanolamine kinase | 0.0025 | 0 | 0.5 |
Loa Loa (eye worm) | solute carrier family 8 | 0.0091 | 0.2855 | 0.2855 |
Onchocerca volvulus | 0.0025 | 0 | 0.5 | |
Echinococcus granulosus | sodium calcium exchanger | 0.0091 | 0.2855 | 0.2855 |
Trypanosoma brucei | choline kinase | 0.0025 | 0 | 0.5 |
Onchocerca volvulus | Putative choline\/ethanolamine kinase | 0.0025 | 0 | 0.5 |
Entamoeba histolytica | choline/ethanolamine kinase, putative | 0.0025 | 0 | 0.5 |
Loa Loa (eye worm) | choline/ethanolamine kinase | 0.0257 | 1 | 1 |
Leishmania major | choline kinase | 0.0025 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 1200 nM | BindingDB_Patents: Reverse Mode Assay. The assay is based on the monitoring of intracellular Ca2+concentrations using the calcium-sensitive dye Fluo-4. CHO cells expressing NCX1 were loaded with the dye by means of the acetoxymethyl ester Fluo-4 AM (Invitrogen, F14202), which is cleaved intracellularly by esterase activity to yield the charged species of free Fluo-4. After an preincubation period with the test compound, Gramicidine (Sigma, G5002) was added. Gramicidine is an ionophor for Na+ions mediating an increase of intracellular Na+ions. Consequently, intracellular Na+ions are exchanged against extracellular Ca2+ions (Ca2+influx, reverse mode). The intracellular elevation of Ca2+ ions was detected by measuring the fluorescence of Fluo-4 at a wavelength of 520 nm by a FLIPR device.Briefly, for the reverse mode transport assay 18000 cells per well were seeded into a 96 well microplate (Corning COSTAR 3904) and incubated overnight in culture medium (1x Nut Mix F12 (Ham) (Gibco, 21765-029); 10% (v/v) fetal calf serum. | 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.