Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Rattus norvegicus | Estrogen receptor beta | Starlite/ChEMBL | References |
Homo sapiens | estrogen receptor 1 | Starlite/ChEMBL | References |
Homo sapiens | estrogen receptor 2 (ER beta) | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Schistosoma mansoni | retinoic acid receptor RXR | Estrogen receptor beta | 530 aa | 451 aa | 25.5 % |
Loa Loa (eye worm) | hypothetical protein | estrogen receptor 2 (ER beta) | 495 aa | 418 aa | 25.8 % |
Onchocerca volvulus | Estrogen receptor beta | 530 aa | 430 aa | 24.9 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-40 | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-40 | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor nor-1/nor-2 | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-14 | 0.0026 | 0.5 | 0.5 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0026 | 0.5 | 0.5 |
Echinococcus granulosus | COUP TF:Svp nuclear hormone receptor | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | FTZ-F1 nuclear receptor-like protein | 0.0026 | 0.5 | 0.5 |
Echinococcus granulosus | Nuclear hormone receptor family member nhr 41 | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-41 | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0026 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0026 | 0.5 | 0.5 | |
Brugia malayi | Nuclear hormone receptor-like 1 | 0.0026 | 0.5 | 0.5 |
Echinococcus granulosus | hepatocyte nuclear factor 4 alpha | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Steroid receptor seven-up type 2 | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | Tr4/Tr2 (homologue) | 0.0026 | 0.5 | 0.5 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.0026 | 0.5 | 0.5 |
Echinococcus granulosus | ecdysone induced protein 78C | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-1 | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Onchocerca volvulus | Steroid hormone receptor family member cnr14 homolog | 0.0026 | 0.5 | 0.5 |
Onchocerca volvulus | Protein ultraspiracle homolog | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 alpha | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-31 | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-41 | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0026 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | 0.0026 | 0.5 | 0.5 |
Brugia malayi | nuclear hormone receptor | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-3 | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear Hormone Receptor family member | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | COUP TF:Svp nuclear hormone receptor | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | Nuclear hormone receptor family member nhr 41 | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-49 | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | RAR-like nuclear receptor | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | coup transcription factor | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | hepatocyte nuclear factor 4 alpha | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | ecdysone induced protein 78C | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-14 | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-49 | 0.0026 | 0.5 | 0.5 |
Brugia malayi | photoreceptor-specific nuclear receptor | 0.0026 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-1 | 0.0026 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 alpha | 0.0026 | 0.5 | 0.5 |
Brugia malayi | nuclear receptor NHR-88 | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0026 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.0026 | 0.5 | 0.5 |
Brugia malayi | steroid hormone receptor | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | steroid hormone receptor | 0.0026 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-31 | 0.0026 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0026 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 nuclear receptor protein | 0.0026 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = 21 % | Activation of ERalpha in MCF7 cell line transfected with ER responsive luciferase reporter at 1 uM | ChEMBL. | 16219463 |
Activity (functional) | = 21 % | Activation of ERalpha in MCF7 cell line transfected with ER responsive luciferase reporter at 1 uM | ChEMBL. | 16219463 |
Activity (functional) | = 101 % | Activation of ERbeta in rat ovary granulosa cell line transfected with ER responsive luciferase reporter at 1 uM | ChEMBL. | 16219463 |
Activity (functional) | = 101 % | Activation of ERbeta in rat ovary granulosa cell line transfected with ER responsive luciferase reporter at 1 uM | ChEMBL. | 16219463 |
EC50 (functional) | = 40.8 nM | Effect on ERbeta in rat ovary granulosa cell line transfected with ER responsive luciferase reporter | ChEMBL. | 16219463 |
EC50 (functional) | = 40.8 nM | Effect on ERbeta in rat ovary granulosa cell line transfected with ER responsive luciferase reporter | ChEMBL. | 16219463 |
EC50 (functional) | > 1000 nM | Effect on ERalpha in MCF7 cell line transfected with ER responsive luciferase reporter | ChEMBL. | 16219463 |
EC50 (functional) | > 1000 nM | Effect on ERalpha in MCF7 cell line transfected with ER responsive luciferase reporter | ChEMBL. | 16219463 |
IC50 (binding) | = 28.1 nM | Displacement of [3H]17beta-estradiol from recombinant human ERbeta expressed in 293T cells | ChEMBL. | 16219463 |
IC50 (binding) | = 28.1 nM | Displacement of [3H]17beta-estradiol from recombinant human ERbeta expressed in 293T cells | ChEMBL. | 16219463 |
IC50 (binding) | = 2940 nM | Displacement of [3H]17beta-estradiol from recombinant human ERalpha expressed in 293T cells | ChEMBL. | 16219463 |
IC50 (binding) | = 2940 nM | Displacement of [3H]17beta-estradiol from recombinant human ERalpha expressed in 293T cells | ChEMBL. | 16219463 |
Ratio IC50 (binding) | = 105 | Selectivity for human ERbeta over human ERalpha | ChEMBL. | 16219463 |
Ratio IC50 (binding) | = 105 | Selectivity for human ERbeta over human ERalpha | ChEMBL. | 16219463 |
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.