Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | retinoid X receptor, alpha | Starlite/ChEMBL | References |
Rattus norvegicus | Retinoid X receptor alpha | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Schistosoma mansoni | retinoic acid receptor RXR | 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 japonicum | ko:K08524 nuclear receptor, subfamily 2, group B, member 1, putative | 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 |
---|---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | Retinoid X receptor alpha | 467 aa | 401 aa | 28.2 % |
Brugia malayi | ecdysteroid receptor | retinoid X receptor, alpha | 435 aa | 352 aa | 23.9 % |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-31 | Retinoid X receptor alpha | 467 aa | 400 aa | 25.8 % |
Onchocerca volvulus | Retinoid X receptor alpha | 467 aa | 435 aa | 31.5 % | |
Onchocerca volvulus | DnaJ subfamily C member 16 homolog | Retinoid X receptor alpha | 467 aa | 391 aa | 29.4 % |
Onchocerca volvulus | Retinoid X receptor alpha | 467 aa | 379 aa | 25.1 % | |
Loa Loa (eye worm) | hypothetical protein | Retinoid X receptor alpha | 467 aa | 390 aa | 29.5 % |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | < 1 % | Agonist activity at Gal4-fused human RAR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity at 1 uM treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay | ChEMBL. | 24801499 |
Activity (binding) | < 5 % | Agonist activity at human RXRalpha LBD expressed in HEK293 cells transfected with Gal4 reporter assessed as increase of transcription at 10'-6 M by dual luciferase reporter assay relative to control | ChEMBL. | 26331194 |
EC50 (binding) | = 160 nM | Agonist activity at Gal4-fused human RXR-alpha expressed in HEK293 cells assessed as receptor-mediated transcriptional activity treated 24 hrs after transfection measured 48 hrs post-transfection by dual luciferase reporter assay | ChEMBL. | 24801499 |
EC50 (binding) | > 1000 nM | Agonist activity at RXR-alpha in rat R3KE cells infected with oncogene KLF4-ER assessed as inhibition of KLF4-mediated oncogenic transformation | ChEMBL. | 24801499 |
Kd (binding) | = 8 nM | Binding affinity to human RXR-alpha-ligand binding domain homodimers by fluorescence quenching method | ChEMBL. | 24801499 |
Kd (binding) | = 1.86 uM | Agonist activity at human RXR-alpha-ligand binding domain homodimers assessed as coactivator recruitment by measuring GRIP1 binding to receptor by isothermal titration calorimetry | ChEMBL. | 24801499 |
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.