Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | nuclear receptor subfamily 1, group H, member 3 | Starlite/ChEMBL | No references |
Homo sapiens | nuclear receptor subfamily 1, group H, member 2 | Starlite/ChEMBL | No references |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_134445 | All targets in OG5_134445 |
Onchocerca volvulus | Bile acid receptor homolog | Get druggable targets OG5_134445 | All targets in OG5_134445 |
Brugia malayi | ecdysteroid receptor | Get druggable targets OG5_134445 | All targets in OG5_134445 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | photoreceptor-specific nuclear receptor | nuclear receptor subfamily 1, group H, member 3 | 387 aa | 321 aa | 28.0 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus granulosus | FTZ F1 alpha | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | Tr4/Tr2 (homologue) | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | RAR-like nuclear receptor | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | FTZ-F1 nuclear receptor-like protein | 0.0022 | 0 | 0.5 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0207 | 1 | 1 |
Echinococcus multilocularis | Nuclear hormone receptor family member nhr 41 | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | COUP TF:Svp nuclear hormone receptor | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | COUP TF:Svp nuclear hormone receptor | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | coup transcription factor | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor nor-1/nor-2 | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.0022 | 0 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0207 | 1 | 1 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | Nuclear hormone receptor family member nhr 41 | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | ecdysone induced protein 78C | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | hepatocyte nuclear factor 4 alpha | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | FTZ F1 alpha | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | hepatocyte nuclear factor 4 alpha | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | ecdysone induced protein 78C | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | FTZ F1 nuclear receptor protein | 0.0022 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Ki (binding) | = 20 nM | BindingDB_Patents: Radioligand Binding Assay. Compounds of the invention were assessed in a competition binding assay where different concentrations of compounds were incubated with the LXR ligand binding domain (LBD) in the presence of radiolabeled LXR ligand [3H]TO901317. The amount of the LXR-LBD that complexed with [3H]T0901317 was measured by scintillation proximity assay (SPA) employing non-specific binding of LXR-LBD to poly-lysine coated Yttrium silicate beads. Partially purified LXR alpha or beta LBD protein (15-45 nM) was incubated at rt for 30 min with 15 nM [3H]TO901317 (25-40 Ci/mmol) and different concentrations of test compounds in 80 uL of phosphate buffered saline (PBS) buffer containing 2.5% DMSO, 1% glycerol, 2 mM EDTA, 2 mM CHAPS and 5 mM DTT in 96-well plates. Poly-lysine SPA beads (50 ug) were added to each well and the total volume was adjusted to 120 uL. The plates were shaken on an orbital shaker for 20 min and then allowed to settle for 10 more minutes at rt. | ChEMBL. | No reference |
Ki (binding) | > 2500 nM | BindingDB_Patents: Radioligand Binding Assay. Compounds of the invention were assessed in a competition binding assay where different concentrations of compounds were incubated with the LXR ligand binding domain (LBD) in the presence of radiolabeled LXR ligand [3H]TO901317. The amount of the LXR-LBD that complexed with [3H]T0901317 was measured by scintillation proximity assay (SPA) employing non-specific binding of LXR-LBD to poly-lysine coated Yttrium silicate beads. Partially purified LXR alpha or beta LBD protein (15-45 nM) was incubated at rt for 30 min with 15 nM [3H]TO901317 (25-40 Ci/mmol) and different concentrations of test compounds in 80 uL of phosphate buffered saline (PBS) buffer containing 2.5% DMSO, 1% glycerol, 2 mM EDTA, 2 mM CHAPS and 5 mM DTT in 96-well plates. Poly-lysine SPA beads (50 ug) were added to each well and the total volume was adjusted to 120 uL. The plates were shaken on an orbital shaker for 20 min and then allowed to settle for 10 more minutes at rt. | 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.