Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | nuclear receptor subfamily 1, group H, member 2 | References | |
Homo sapiens | retinoid X receptor, alpha | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Schistosoma japonicum | ko:K08524 nuclear receptor, subfamily 2, group B, member 1, putative | Get druggable targets OG5_130073 | All targets in OG5_130073 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | Get druggable targets OG5_130073 | All targets in OG5_130073 |
Schistosoma mansoni | retinoic acid receptor RXR | Get druggable targets OG5_130073 | All targets in OG5_130073 |
Echinococcus multilocularis | retinoic acid receptor rxr beta a retinoic acid receptor rxr alpha a retinoic acid receptor rxr alpha | Get druggable targets OG5_130073 | All targets in OG5_130073 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | ecdysteroid receptor | retinoid X receptor, alpha | 435 aa | 352 aa | 23.9 % |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (binding) | = 5 nM | Agonist activity at LXR-beta in human HeLa cells assessed as induction of ABCA1 by beta-galactosidase/luciferase reporter gene assay | LITERATURE. | 27994765 |
EC50 (binding) | = 42 nM | Agonist activity at LXR-beta in human whole blood assessed as ABCA1 gene induction by measuring ABCA1 mRNA level after 4 hrs by SYBR-Green dye-based Q-PCR analysis | LITERATURE. | 27994765 |
EC50 (binding) | = 140 nM | Agonist activity at human LXR-beta expressed in African green monkey CV1 cells measured after 18 to 20 hrs by luciferase reporter gene assay | LITERATURE. | 27994765 |
Efficacy (binding) | = 43 % | Agonist activity at LXR-beta in human HeLa cells assessed as induction of ABCA1 by beta-galactosidase/luciferase reporter gene assay relative to control | LITERATURE. | 27994765 |
Efficacy (binding) | = 51 % | Agonist activity at LXR-beta in human whole blood assessed as ABCA1 gene induction by measuring ABCA1 mRNA level after 4 hrs by SYBR-Green dye-based Q-PCR analysis relative to pan agonist 2-(4-(5-(5-cyano-1-(2,4-difluorobenzyl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridin-2-yl)thiophen-2-yl)-3-methylphenyl)acetic acid | LITERATURE. | 27994765 |
Efficacy (binding) | = 54 % | Agonist activity at human LXR-beta expressed in African green monkey CV1 cells measured after 18 to 20 hrs by luciferase reporter gene assay relative to pan agonist 1-(2,4-difluorobenzyl)-2-oxo-6-(4-phenoxyphenyl)-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile | LITERATURE. | 27994765 |
Ki (binding) | = 11 nM | Displacement of [3H]-24,25-epoxycholesterol from human LXRbeta/RXRalpha expressed in baculovirus infected Sf9 cells by scintillation proximity analysis | LITERATURE. | 27994765 |
Ki (binding) | = 75 nM | Displacement of [3H]-24,25-epoxycholesterol from human LXRalpha/RXRalpha expressed in baculovirus infected Sf9 cells by scintillation proximity analysis | LITERATURE. | 27994765 |
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.
1 literature reference was collected for this gene.