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 |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_134445 | All targets in OG5_134445 |
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 | photoreceptor-specific nuclear receptor | nuclear receptor subfamily 1, group H, member 3 | 387 aa | 321 aa | 28.0 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus granulosus | hepatocyte nuclear factor 4 alpha | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor nor-1/nor-2 | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | ecdysone induced protein 78C | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | Nuclear hormone receptor family member nhr 41 | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | ecdysone induced protein 78C | 0.0022 | 0 | 0.5 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0207 | 1 | 1 |
Echinococcus multilocularis | FTZ F1 nuclear receptor protein | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | FTZ F1 alpha | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | Nuclear hormone receptor family member nhr 41 | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | COUP TF:Svp nuclear hormone receptor | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | Tr4/Tr2 (homologue) | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | FTZ F1 alpha | 0.0022 | 0 | 0.5 |
Echinococcus granulosus | COUP TF:Svp nuclear hormone receptor | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | FTZ-F1 nuclear receptor-like protein | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | coup transcription factor | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.0022 | 0 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0207 | 1 | 1 |
Echinococcus multilocularis | hepatocyte nuclear factor 4 alpha | 0.0022 | 0 | 0.5 |
Schistosoma mansoni | RAR-like nuclear receptor | 0.0022 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | = 0.35 uM | Induction of [3H]cholesterol efflux in human HepG2 cells loaded with ac-LDL assessed as lipid accumulation | ChEMBL. | 20350005 |
EC50 (functional) | = 0.9 uM | Induction of ABCA1 expression in human THP1 cells | ChEMBL. | 20350005 |
EC50 (binding) | = 2.02 uM | Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay | ChEMBL. | 20350005 |
EC50 (binding) | = 3.59 uM | Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay | ChEMBL. | 20350005 |
Efficacy (binding) | = 13 % | Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay relative to TO901317 | ChEMBL. | 20350005 |
Efficacy (functional) | = 32 % | Induction of [3H]cholesterol efflux in human HepG2 cells loaded with ac-LDL assessed as lipid accumulation relative to T0901317 | ChEMBL. | 20350005 |
Efficacy (functional) | = 65 % | Induction of ABCA1 expression in human THP1 cells relative to T0901317 | ChEMBL. | 20350005 |
Efficacy (binding) | = 70 % | Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay relative to TO901317 | ChEMBL. | 20350005 |
FC (functional) | = 9 | Antiatherosclerotic activity against high fat/high cholesterol fed LDLR-deficient mouse assessed as lipg gene regulation at 0.6 mg/kg administered with diet for 7 days by Experion chip analysis | ChEMBL. | 20350005 |
IC50 (binding) | = 0.018 uM | Displacement of [3H]T0901317 from human LXRbeta ligand binding domain | ChEMBL. | 20350005 |
IC50 (binding) | = 0.165 uM | Displacement of [3H]T0901317 from human LXRalpha ligand binding domain | ChEMBL. | 20350005 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 20350005 |
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.