Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | nuclear receptor subfamily 1, group H, member 2 | Starlite/ChEMBL | References |
Homo sapiens | nuclear receptor subfamily 1, group H, member 3 | Starlite/ChEMBL | References |
Homo sapiens | RAR-related orphan receptor B | Starlite/ChEMBL | References |
Homo sapiens | nuclear receptor subfamily 1, group I, member 2 | Starlite/ChEMBL | References |
Homo sapiens | peroxisome proliferator-activated receptor gamma | Starlite/ChEMBL | References |
Homo sapiens | RAR-related orphan receptor C | Starlite/ChEMBL | References |
Homo sapiens | nuclear receptor subfamily 1, group H, member 4 | Starlite/ChEMBL | References |
Homo sapiens | RAR-related orphan receptor A | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Onchocerca volvulus | Bile acid receptor homolog | Get druggable targets OG5_134445 | All targets in OG5_134445 |
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 |
Brugia malayi | steroid hormone receptor | Get druggable targets OG5_134341 | All targets in OG5_134341 |
Echinococcus granulosus | thyroid hormone receptor alpha | Get druggable targets OG5_134341 | All targets in OG5_134341 |
Brugia malayi | ecdysteroid receptor | Get druggable targets OG5_134445 | All targets in OG5_134445 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus granulosus | FTZ F1 nuclear receptor protein | RAR-related orphan receptor B | 459 aa | 403 aa | 24.6 % |
Brugia malayi | photoreceptor-specific nuclear receptor | nuclear receptor subfamily 1, group H, member 3 | 387 aa | 321 aa | 28.0 % |
Echinococcus granulosus | ecdysone induced protein 78C | peroxisome proliferator-activated receptor gamma | 477 aa | 447 aa | 28.2 % |
Brugia malayi | ecdysteroid receptor | nuclear receptor subfamily 1, group I, member 2 | 434 aa | 427 aa | 25.1 % |
Echinococcus granulosus | ecdysone induced protein 78C | nuclear receptor subfamily 1, group H, member 4 | 476 aa | 402 aa | 28.1 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.0277 | 1 | 1 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0277 | 1 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
%max (functional) | = 73 % | Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA relative to control | ChEMBL. | 26048793 |
EC50 (binding) | = 0.002 uM | Inverse agonist activity at N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486) expressed in bacterial expression system assessed as inhibition of SRC1 co-activator peptide recruitment after 3 hrs by TR-FRET analysis | ChEMBL. | 26048793 |
EC50 (binding) | = 0.013 uM | Inverse agonist activity at GAL4-fused human RORc expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay | ChEMBL. | 26048793 |
EC50 (functional) | = 0.03 uM | Antiinflammatory activity in human PBMC assessed as inhibition of IL-17 production after 48 hrs by Sandwich ELISA | ChEMBL. | 26048793 |
EC50 (binding) | > 10 uM | Inverse agonist activity at GAL4-fused human RORb expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay | ChEMBL. | 26048793 |
EC50 (binding) | > 10 uM | Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay | ChEMBL. | 26048793 |
EC50 (binding) | > 10 uM | Agonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay | ChEMBL. | 26048793 |
EC50 (binding) | > 10 uM | Agonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay | ChEMBL. | 26048793 |
EC50 (binding) | > 10 uM | Agonist activity at GAL4-fused human LXRalpha expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay | ChEMBL. | 26048793 |
EC50 (binding) | > 10 uM | Agonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as activation of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay | ChEMBL. | 26048793 |
Efficacy (binding) | = -99 % | Inverse agonist activity at N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486) expressed in bacterial expression system assessed as inhibition of SRC1 co-activator peptide recruitment after 3 hrs by TR-FRET analysis relative to apo-RORc ligand binding domain | ChEMBL. | 26048793 |
IC50 (binding) | = 3.4 uM | Displacement of fluormone PPARgamma green from GST-tagged human PPARgamma-LBD after 2 hrs by fluorescence polarization assay | ChEMBL. | 26048793 |
Inhibition (binding) | Antagonist activity at GAL4-fused human FXR expressed in HEK293T cells assessed as inhibition of T0901317-induced basal transcriptional activity up to 10 uM after 20 hrs by dual-glo luciferase reporter gene assay | ChEMBL. | 26048793 | |
Inhibition (binding) | Antagonist activity at GAL4-fused human PXR expressed in HEK293T cells assessed as inhibition of T0901317-induced basal transcriptional activity up to 10 uM after 20 hrs by dual-glo luciferase reporter gene assay | ChEMBL. | 26048793 | |
Inhibition (binding) | Antagonist activity at GAL4-fused human LXRbeta expressed in HEK293T cells assessed as inhibition of T0901317-induced basal transcriptional activity up to 10 uM after 20 hrs by dual-glo luciferase reporter gene assay | ChEMBL. | 26048793 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 26048793 |
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.