Species | Target name | Source | Bibliographic reference |
---|---|---|---|
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 |
---|---|---|---|---|---|
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 | 0.5 |
Schistosoma mansoni | Tr4/Tr2 (homologue) | 0.0016 | 0 | 0.5 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.0016 | 0 | 0.5 |
Echinococcus multilocularis | ecdysone induced protein 78C | 0.0016 | 0 | 0.5 |
Schistosoma mansoni | RAR-like nuclear receptor | 0.0016 | 0 | 0.5 |
Schistosoma mansoni | FTZ-F1 nuclear receptor-like protein | 0.0016 | 0 | 0.5 |
Echinococcus granulosus | FTZ F1 alpha | 0.0016 | 0 | 0.5 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.0016 | 0 | 0.5 |
Echinococcus granulosus | Nuclear hormone receptor family member nhr 41 | 0.0016 | 0 | 0.5 |
Echinococcus granulosus | hepatocyte nuclear factor 4 alpha | 0.0016 | 0 | 0.5 |
Echinococcus granulosus | COUP TF:Svp nuclear hormone receptor | 0.0016 | 0 | 0.5 |
Echinococcus multilocularis | Nuclear hormone receptor family member nhr 41 | 0.0016 | 0 | 0.5 |
Trypanosoma brucei | cytochrome P450, putative | 0.0029 | 1 | 0.5 |
Echinococcus multilocularis | FTZ F1 nuclear receptor protein | 0.0016 | 0 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0016 | 0 | 0.5 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0016 | 0 | 0.5 |
Onchocerca volvulus | Steroid hormone receptor family member cnr14 homolog | 0.0016 | 0 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0016 | 0 | 0.5 |
Onchocerca volvulus | Protein ultraspiracle homolog | 0.0016 | 0 | 0.5 |
Echinococcus multilocularis | FTZ F1 alpha | 0.0016 | 0 | 0.5 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.0016 | 0 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0016 | 0 | 0.5 |
Echinococcus granulosus | ecdysone induced protein 78C | 0.0016 | 0 | 0.5 |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | 0.0016 | 0 | 0.5 |
Schistosoma mansoni | coup transcription factor | 0.0016 | 0 | 0.5 |
Mycobacterium ulcerans | cytochrome P450 185A4 Cyp185A4 | 0.0029 | 1 | 0.5 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.0016 | 0 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0021 | 0.3463 | 0.3463 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0016 | 0 | 0.5 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.0016 | 0 | 0.5 |
Echinococcus multilocularis | hepatocyte nuclear factor 4 alpha | 0.0016 | 0 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0016 | 0 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor nor-1/nor-2 | 0.0016 | 0 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor | 0.0016 | 0 | 0.5 |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.0029 | 1 | 1 |
Leishmania major | cytochrome p450-like protein | 0.0029 | 1 | 0.5 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.0016 | 0 | 0.5 |
Loa Loa (eye worm) | CYP4Cod1 | 0.0029 | 1 | 1 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0029 | 1 | 0.5 |
Brugia malayi | Cytochrome P450 family protein | 0.0029 | 1 | 1 |
Trypanosoma cruzi | cytochrome P450, putative | 0.0029 | 1 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0016 | 0 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0016 | 0 | 0.5 |
Onchocerca volvulus | 0.0016 | 0 | 0.5 | |
Loa Loa (eye worm) | cytochrome P450 family protein | 0.0029 | 1 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (binding) | = 2 nM | Agonist activity at ERalpha (unknown origin) expressed in human HepG2 cells assessed as transcriptional activation after 24 hrs by ERE-luciferase reporter gene assay | ChEMBL. | 24708493 |
Efficacy (binding) | = 6 % | Antagonist activity at ERbeta (unknown origin) expressed in human HepG2 cells assessed as inhibition of 17beta-estradiol-induced transcriptional activation after 24 hrs by ERE-luciferase reporter gene assay relative to 17beta-estradiol | ChEMBL. | 24708493 |
Efficacy (binding) | = 9 % | Agonist activity at ERbeta (unknown origin) expressed in human HepG2 cells assessed as transcriptional activation after 24 hrs by ERE-luciferase reporter gene assay relative to 17beta-estradiol | ChEMBL. | 24708493 |
Efficacy (binding) | = 114 % | Agonist activity at ERalpha (unknown origin) expressed in human HepG2 cells assessed as transcriptional activation after 24 hrs by ERE-luciferase reporter gene assay relative to 17beta-estradiol | ChEMBL. | 24708493 |
Efficacy (binding) | = 138 % | Antagonist activity at ERalpha (unknown origin) expressed in human HepG2 cells assessed as inhibition of transcriptional activation after 24 hrs by ERE-luciferase reporter gene assay relative to 17beta-estradiol | ChEMBL. | 24708493 |
IC50 (binding) | = 9 nM | Antagonist activity at ERbeta (unknown origin) expressed in human HepG2 cells assessed as inhibition of 17beta-estradiol-induced transcriptional activation after 24 hrs by ERE-luciferase reporter gene assay | ChEMBL. | 24708493 |
RBA (binding) | = 49.2 % | Displacement of [3H]-estradiol from human full-length ERalpha after 18 to 24 hrs by competitive radiometric binding assay relative to estradiol | ChEMBL. | 24708493 |
RBA (binding) | = 127 % | Displacement of [3H]-estradiol from human full-length ERbeta after 18 to 24 hrs by competitive radiometric binding assay relative to estradiol | ChEMBL. | 24708493 |
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.