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 granulosus | retinoic acid receptor rxr beta a | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-14 | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor nor-1/nor-2 | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-40 | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-40 | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0016 | 0.5 | 0.5 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Steroid receptor seven-up type 2 | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | Tr4/Tr2 (homologue) | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor-like 1 | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | hepatocyte nuclear factor 4 alpha | 0.0016 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0016 | 0.5 | 0.5 | |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | Nuclear hormone receptor family member nhr 41 | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-41 | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | FTZ-F1 nuclear receptor-like protein | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | COUP TF:Svp nuclear hormone receptor | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 alpha | 0.0016 | 0.5 | 0.5 |
Onchocerca volvulus | Protein ultraspiracle homolog | 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 |
Brugia malayi | 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 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | ecdysone induced protein 78C | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | COUP TF:Svp nuclear hormone receptor | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | Nuclear hormone receptor family member nhr 41 | 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) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear Hormone Receptor family member | 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-3 | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | 0.0016 | 0.5 | 0.5 |
Brugia malayi | nuclear hormone receptor | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-41 | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-31 | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | RAR-like nuclear receptor | 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 |
Echinococcus multilocularis | hepatocyte nuclear factor 4 alpha | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | coup transcription factor | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-1 | 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 |
Brugia malayi | photoreceptor-specific nuclear receptor | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 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 | FTZ F1 nuclear receptor protein | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-31 | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.0016 | 0.5 | 0.5 |
Brugia malayi | steroid hormone receptor | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | steroid hormone receptor | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 alpha | 0.0016 | 0.5 | 0.5 |
Brugia malayi | nuclear receptor NHR-88 | 0.0016 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
ED50 (functional) | = 0.26 mg kg-1 | Inhibition of estradiol-induced increase in uterine wet weight in orally dosed Sprague-Dawley rat after 3 days | ChEMBL. | 17482463 |
ED50 (functional) | < 1 mg kg-1 | Inhibition of estrogen stimulation in Sprague-Dawley rat at 10 mg/kg | ChEMBL. | 17482463 |
Efficacy (functional) | = 24 % | Increase in estrogen stimulation in human Ishikawa cells by alkaline phosphatase quantitation at 1 uM relative to control | ChEMBL. | 17482463 |
Efficacy (functional) | = 24 % | Increase in estrogen stimulation in human Ishikawa cells by alkaline phosphatase quantitation at 1 uM relative to control | ChEMBL. | 17482463 |
Efficacy (functional) | = 99 % | Inhibition of estrogen stimulation in human Ishikawa cells by alkaline phosphatase quantitation | ChEMBL. | 17482463 |
Efficacy (functional) | = 99 % | Inhibition of estrogen stimulation in human Ishikawa cells by alkaline phosphatase quantitation | ChEMBL. | 17482463 |
IC50 (functional) | = 8 nM | Inhibition of estrogen stimulation in human Ishikawa cells by alkaline phosphatase quantitation | ChEMBL. | 17482463 |
IC50 (functional) | = 8 nM | Inhibition of estrogen stimulation in human Ishikawa cells by alkaline phosphatase quantitation | ChEMBL. | 17482463 |
Inhibition (functional) | = 83 % | Inhibition of estrogen stimulation in Sprague-Dawley rat at 10 mg/kg | ChEMBL. | 17482463 |
Ki (binding) | = 1.09 nM | Displacement of [3H]estradiol from human recombinant ERalpha | ChEMBL. | 17482463 |
Ki (binding) | = 1.09 nM | Displacement of [3H]estradiol from human recombinant ERalpha | ChEMBL. | 17482463 |
Ki (binding) | = 2.69 nM | Displacement of [3H]estradiol from human recombinant ERbeta | ChEMBL. | 17482463 |
Ki (binding) | = 2.69 nM | Displacement of [3H]estradiol from human recombinant ERbeta | ChEMBL. | 17482463 |
Ratio (functional) | = 1.94 | Ratio of estrogen level in Sprague-Dawley rat at dose of 30 times ED50 for 10 days relative to control | ChEMBL. | 17482463 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 17482463 |
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.