Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | estrogen receptor 2 (ER beta) | Starlite/ChEMBL | References |
Homo sapiens | estrogen receptor 1 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | estrogen receptor 2 (ER beta) | 495 aa | 418 aa | 25.8 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | COUP TF:Svp nuclear hormone receptor | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | hepatocyte nuclear factor 4 alpha | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | Nuclear hormone receptor family member nhr 41 | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 nuclear receptor protein | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear Hormone Receptor family member | 0.0016 | 0.5 | 0.5 |
Onchocerca volvulus | Steroid hormone receptor family member cnr14 homolog | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | Nuclear hormone receptor family member nhr 41 | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-31 | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Steroid receptor seven-up type 2 | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-3 | 0.0016 | 0.5 | 0.5 |
Brugia malayi | nuclear hormone receptor | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | FTZ-F1 nuclear receptor-like protein | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | ecdysone induced protein 78C | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-1 | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | steroid hormone receptor | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-14 | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 alpha | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | Tr4/Tr2 (homologue) | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-40 | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0016 | 0.5 | 0.5 |
Brugia malayi | nuclear receptor NHR-88 | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0016 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0016 | 0.5 | 0.5 | |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-41 | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | COUP TF:Svp nuclear hormone receptor | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor-like 1 | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-49 | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-41 | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | RAR-like nuclear receptor | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-40 | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-31 | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-14 | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | ecdysone induced protein 78C | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor nor-1/nor-2 | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | hepatocyte nuclear factor 4 alpha | 0.0016 | 0.5 | 0.5 |
Brugia malayi | steroid hormone receptor | 0.0016 | 0.5 | 0.5 |
Onchocerca volvulus | Protein ultraspiracle homolog | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-1 | 0.0016 | 0.5 | 0.5 |
Brugia malayi | photoreceptor-specific nuclear receptor | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 alpha | 0.0016 | 0.5 | 0.5 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | coup transcription factor | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-49 | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = 16 % | Estrogenic activity in Sprague-Dawley rat assessed as effect on uterine weight at 1 ug/kg, sc | ChEMBL. | 17289385 |
IC50 (binding) | = 8 nM | Displacement of [3H]estradiol from full length human recombinant ERalpha after 3 hrs by scintillation proximity assay | ChEMBL. | 17289385 |
IC50 (binding) | = 8 nM | Displacement of [3H]estradiol from full length human recombinant ERalpha after 3 hrs by scintillation proximity assay | ChEMBL. | 17289385 |
IC50 (functional) | = 42.7 nM | Antiproliferative activity against estrogen depleted MCF7 cells after 8 to 10 days | ChEMBL. | 17289385 |
IC50 (functional) | = 42.7 nM | Antiproliferative activity against estrogen depleted MCF7 cells after 8 to 10 days | ChEMBL. | 17289385 |
IC50 (binding) | = 1231 nM | Displacement of [3H]estradiol from full length human recombinant ERbeta after 3 hrs by scintillation proximity assay | ChEMBL. | 17289385 |
IC50 (binding) | = 1231 nM | Displacement of [3H]estradiol from full length human recombinant ERbeta after 3 hrs by scintillation proximity assay | ChEMBL. | 17289385 |
Inhibition (functional) | = 23 % | Antiestrogenic activity in Sprague-Dawley rat assessed as inhibition of 17beta estradiol-induced immature uterine weight at 1 ug/kg, sc | ChEMBL. | 17289385 |
Ratio IC50 (binding) | = 153.8 | Selectivity for human recombinant ERalpha over human recombinant ERbeta | ChEMBL. | 17289385 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 17289385 |
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.