Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | nuclear receptor subfamily 1, group H, member 3 | Starlite/ChEMBL | References |
Homo sapiens | retinoid X receptor, alpha | References | |
Homo sapiens | nuclear receptor subfamily 1, group H, member 2 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
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 |
Schistosoma mansoni | retinoic acid receptor RXR | Get druggable targets OG5_130073 | All targets in OG5_130073 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_134445 | All targets in OG5_134445 |
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 |
Brugia malayi | ecdysteroid receptor | 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 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | ecdysteroid receptor | retinoid X receptor, alpha | 435 aa | 352 aa | 23.9 % |
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 |
---|---|---|---|---|
Schistosoma mansoni | retinoic acid receptor RXR | 0.015 | 0.6429 | 1 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.015 | 0.6429 | 1 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0216 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0216 | 1 | 1 |
Echinococcus multilocularis | retinoic acid receptor rxr beta a retinoic acid receptor rxr alpha a retinoic acid receptor rxr alpha | 0.0129 | 0.5297 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Cp (ADMET) | = 6.6 uM | Plasma concentration in mouse at 30 mg/kg, po measured at 4 hrs post dose | ChEMBL. | 25435151 |
EC50 (binding) | = 38 nM | Transactivation of LXR (unknown origin) expressed in human HeLa cells by ABCA1 LXREx3 reporter assay | ChEMBL. | 25435151 |
EC50 (binding) | = 230 nM | Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay | ChEMBL. | 25435151 |
EC50 (binding) | = 320 nM | Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay | ChEMBL. | 25435151 |
Efficacy (binding) | = 65 % | Transactivation of LXR (unknown origin) expressed in human HeLa cells by ABCA1 LXREx3 reporter assay relative to 1-(2,4-difluorobenzyl)-2-oxo-6-(4-phenoxyphenyl)-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile | ChEMBL. | 25435151 |
Efficacy (binding) | = 66 % | Transactivation of LXRalpha (unknown origin) expressed in CV1 cells by luciferase reporter gene assay relative to 1-(2,4-difluorobenzyl)-2-oxo-6-(4-phenoxyphenyl)-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile | ChEMBL. | 25435151 |
Efficacy (binding) | = 95 % | Transactivation of LXRbeta (unknown origin) expressed in CV1 cells by luciferase reporter gene assay relative to 1-(2,4-difluorobenzyl)-2-oxo-6-(4-phenoxyphenyl)-4-(trifluoromethyl)-1,2-dihydropyridine-3-carbonitrile | ChEMBL. | 25435151 |
Ki (binding) | = 31 nM | Binding affinity to LXRbeta-RXRalpha heterodimer (unknown origin) expressed in insect cells by scintillation proximity assay | ChEMBL. | 25435151 |
Ki (binding) | = 300 nM | Binding affinity to LXRalpha-RXRalpha heterodimer (unknown origin) expressed in insect cells by scintillation proximity assay | ChEMBL. | 25435151 |
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.