Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | RAR-related orphan receptor A | Starlite/ChEMBL | References |
Homo sapiens | nuclear receptor subfamily 1, group H, member 3 | Starlite/ChEMBL | References |
Homo sapiens | RAR-related orphan receptor C | Starlite/ChEMBL | References |
Homo sapiens | nuclear receptor subfamily 1, group H, member 2 | Starlite/ChEMBL | References |
Homo sapiens | RAR-related orphan receptor B | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Schistosoma japonicum | Ecdysone-induced protein 78C, putative | Get druggable targets OG5_134341 | All targets in OG5_134341 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_134445 | All targets in OG5_134445 |
Loa Loa (eye worm) | steroid hormone receptor | Get druggable targets OG5_134341 | All targets in OG5_134341 |
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 |
Echinococcus granulosus | thyroid hormone receptor alpha | Get druggable targets OG5_134341 | All targets in OG5_134341 |
Brugia malayi | steroid hormone receptor | Get druggable targets OG5_134341 | All targets in OG5_134341 |
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 % |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | RAR-related orphan receptor B | 459 aa | 403 aa | 24.6 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Onchocerca volvulus | Bile acid receptor homolog | 0.0244 | 1 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0244 | 1 | 1 |
Echinococcus granulosus | thyroid hormone receptor alpha | 0.0196 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | Agonist activity at human GAL4-fused LXRbeta expressed in HEK293 cells assessed as transcriptional activity after 5 hrs by luciferase reporter gene assay | ChEMBL. | 24685544 | |
EC50 (binding) | = 0.36 uM | Inverse agonist activity at an N-terminal 6xHis-GST-tag human RORc-LBD assessed as inhibition of recruitment of the SRC1 co-activator peptide after 3 hrs by time-resolved FRET assay | ChEMBL. | 24685544 |
EC50 (binding) | = 1.9 uM | Inverse agonist activity at human GAL4-fused LXRbeta expressed in HEK293 cells assessed as inhibition of T0901317-induced transcriptional activity after 5 hrs by luciferase reporter gene assay | ChEMBL. | 24685544 |
EC50 (binding) | = 2.4 uM | Inverse agonist activity at human GAL4-fused RORc expressed in HEK293 cells after 5 hrs by luciferase reporter gene based transcriptional assay | ChEMBL. | 24685544 |
EC50 (binding) | = 2.7 uM | Inverse agonist activity at human GAL4-fused LXRalpha expressed in HEK293 cells assessed as inhibition of T0901317-induced transcriptional activity after 5 hrs by luciferase reporter gene assay | ChEMBL. | 24685544 |
EC50 (binding) | = 4.2 uM | Inverse agonist activity at human GAL4-fused RORa expressed in HEK293 cells after 5 hrs by luciferase reporter gene based transcriptional assay | ChEMBL. | 24685544 |
EC50 (binding) | = 5 uM | Inverse agonist activity at human GAL4-fused RORb expressed in HEK293 cells after 5 hrs by luciferase reporter gene based transcriptional assay | ChEMBL. | 24685544 |
Efficacy (binding) | = 60 % | Inverse agonist activity at an N-terminal 6xHis-GST-tag human RORc-LBD assessed as inhibition of recruitment of the SRC1 co-activator peptide after 3 hrs by time-resolved FRET assay relative to control | ChEMBL. | 24685544 |
IC50 (binding) | = 0.37 uM | Displacement of [3H2]25-hydroxycholesterol from human RORc-LBD after 3 hrs by scintillation counting | ChEMBL. | 24685544 |
IC50 (binding) | = 0.45 uM | Displacement of [3H]T0901317 from LXRbeta (unknown origin) | ChEMBL. | 24685544 |
IC50 (binding) | = 29 uM | Displacement of [3H]T0901317 from LXRalpha (unknown origin) | ChEMBL. | 24685544 |
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.