Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | estrogen receptor 1 | Starlite/ChEMBL | References |
Homo sapiens | estrogen receptor 2 (ER beta) | 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 |
---|---|---|---|---|
Onchocerca volvulus | 0.0016 | 0.5 | 0.5 | |
Echinococcus multilocularis | FTZ F1 nuclear receptor protein | 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 | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.0016 | 0.5 | 0.5 |
Brugia malayi | nuclear receptor NHR-88 | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 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-25 | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 alpha | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 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 |
Brugia malayi | steroid hormone receptor | 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 |
Echinococcus multilocularis | Nuclear hormone receptor family member nhr 41 | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | ecdysone induced protein 78C | 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 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | COUP TF:Svp nuclear hormone receptor | 0.0016 | 0.5 | 0.5 |
Onchocerca volvulus | Steroid hormone receptor family member cnr14 homolog | 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-1 | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | COUP TF:Svp 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-14 | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor-like 1 | 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) | 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 | FTZ-F1 nuclear receptor-like protein | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | hepatocyte nuclear factor 4 alpha | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-41 | 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-14 | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | coup transcription factor | 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-41 | 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 |
Loa Loa (eye worm) | hypothetical protein | 0.0016 | 0.5 | 0.5 |
Onchocerca volvulus | Protein ultraspiracle homolog | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-40 | 0.0016 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | hepatocyte nuclear factor 4 alpha | 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-49 | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.0016 | 0.5 | 0.5 |
Brugia malayi | photoreceptor-specific nuclear receptor | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | Tr4/Tr2 (homologue) | 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 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-1 | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0016 | 0.5 | 0.5 |
Schistosoma mansoni | RAR-like nuclear receptor | 0.0016 | 0.5 | 0.5 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | 0.0016 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-31 | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 alpha | 0.0016 | 0.5 | 0.5 |
Echinococcus granulosus | ecdysone induced protein 78C | 0.0016 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Decrease (functional) | = 45.9 % | Percent decrease in serum cholesterol relative to OVX control at 0.1 mg/kg in rat was determined (in vivo) | ChEMBL. | 9003514 |
Decrease (functional) | = 55.3 % | Percent decrease in serum cholesterol relative to OVX control at 10 mg/kg in rat was determined (in vivo) | ChEMBL. | 9003514 |
Decrease (functional) | = 59.2 % | Percent decrease in serum cholesterol relative to OVX control at 1 mg/kg in rat | ChEMBL. | 9003514 |
ED50 (functional) | = 0.4 mg kg-1 | Dose required to reduce serum cholesterol by 50% relative to OVX controls was determined (in vivo) | ChEMBL. | 9003514 |
IC50 (functional) | = 0.3 nM | Antagonism of estrogen action in a mammary tumor cell line was assayed via inhibition of MCF-7 cell proliferation stimulated by 10 e-11 M 17-beta-estradiol (in vitro) | ChEMBL. | 9003514 |
IC50 (functional) | = 0.3 nM | Antagonism of estrogen action in a mammary tumor cell line was assayed via inhibition of MCF-7 cell proliferation stimulated by 10 e-11 M 17-beta-estradiol (in vitro) | ChEMBL. | 9003514 |
IC50 (functional) | = 0.3 nM | Antiproliferative activity against human MCF7 cells | ChEMBL. | 22405286 |
Increase (functional) | = 34.3 % | Minimum effective dose at which significant increase in uterine weight/body weight in rat was determined (in vivo); expressed as % increase relative to ovariectomized (OVX) controls | ChEMBL. | 9003514 |
MED (functional) | = 0.1 mg kg-1 | Minimum effective dose at which significant increase in uterine weight/body weight in rat was determined (in vivo) | ChEMBL. | 9003514 |
MED (functional) | > 10 mg kg-1 | Minimum effective dose at which significant increase in uterine eosinophil peroxidase (EPO) activity in rat was determined (in vivo) | ChEMBL. | 9003514 |
Protection (functional) | = 34.1 % | Percent protection of bone mineral density in the distal femur of OVX rat at a dose of 0.1 mg/kg/day | ChEMBL. | 9003514 |
Protection (functional) | = 34.5 % | Percent protection of bone mineral density in the distal femur of OVX rat at a dose of 0.01 mg/kg/day | ChEMBL. | 9003514 |
Protection (functional) | = 68 % | Percent protection of bone mineral density in the distal femur of OVX rat at a dose of 1 mg/kg/day | ChEMBL. | 9003514 |
Protection (functional) | = 69.8 % | Percent protection of bone mineral density in the distal femur of OVX rat at a dose of 10 mg/kg/day | ChEMBL. | 9003514 |
RBA (binding) | = 0.2 | In vitro relative binding affinity by competition with [3H]-17-beta-estradiol for estrogen receptor in MCF-7 cell lysate | ChEMBL. | 9003514 |
RBA (binding) | = 0.2 | Relative binding affinity to estrogen receptor | ChEMBL. | 22405286 |
RBA (binding) | = 0.2 | In vitro relative binding affinity by competition with [3H]-17-beta-estradiol for estrogen receptor in MCF-7 cell lysate | ChEMBL. | 9003514 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 22405286 |
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.
2 literature references were collected for this gene.