Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | nuclear receptor subfamily 3, group C, member 2 | Starlite/ChEMBL | References |
Homo sapiens | progesterone receptor | Starlite/ChEMBL | References |
Homo sapiens | nuclear receptor subfamily 3, group C, member 1 (glucocorticoid receptor) | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | FTZ-F1 nuclear receptor-like protein | 0.0031 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 nuclear receptor protein | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | steroid hormone receptor | 0.0031 | 0.5 | 0.5 |
Brugia malayi | photoreceptor-specific nuclear receptor | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0031 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-49 | 0.0031 | 0.5 | 0.5 |
Brugia malayi | nuclear receptor NHR-88 | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-40 | 0.0031 | 0.5 | 0.5 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.0031 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 alpha | 0.0031 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.0031 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 alpha | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0031 | 0.5 | 0.5 |
Echinococcus granulosus | Nuclear hormone receptor family member nhr 41 | 0.0031 | 0.5 | 0.5 |
Echinococcus multilocularis | hepatocyte nuclear factor 4 alpha | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-14 | 0.0031 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.0031 | 0.5 | 0.5 |
Echinococcus multilocularis | Nuclear hormone receptor family member nhr 41 | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0031 | 0.5 | 0.5 |
Schistosoma mansoni | RAR-like nuclear receptor | 0.0031 | 0.5 | 0.5 |
Schistosoma mansoni | coup transcription factor | 0.0031 | 0.5 | 0.5 |
Brugia malayi | nuclear hormone receptor | 0.0031 | 0.5 | 0.5 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear Hormone Receptor family member | 0.0031 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor | 0.0031 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-1 | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-31 | 0.0031 | 0.5 | 0.5 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-41 | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-3 | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Steroid receptor seven-up type 2 | 0.0031 | 0.5 | 0.5 |
Echinococcus granulosus | COUP TF:Svp nuclear hormone receptor | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0031 | 0.5 | 0.5 |
Echinococcus multilocularis | COUP TF:Svp nuclear hormone receptor | 0.0031 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-40 | 0.0031 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-14 | 0.0031 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-1 | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0031 | 0.5 | 0.5 |
Onchocerca volvulus | 0.0031 | 0.5 | 0.5 | |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0031 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-31 | 0.0031 | 0.5 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0031 | 0.5 | 0.5 |
Echinococcus multilocularis | ecdysone induced protein 78C | 0.0031 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor nor-1/nor-2 | 0.0031 | 0.5 | 0.5 |
Onchocerca volvulus | Steroid hormone receptor family member cnr14 homolog | 0.0031 | 0.5 | 0.5 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.0031 | 0.5 | 0.5 |
Onchocerca volvulus | Bile acid receptor homolog | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0031 | 0.5 | 0.5 |
Echinococcus granulosus | hepatocyte nuclear factor 4 alpha | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-49 | 0.0031 | 0.5 | 0.5 |
Schistosoma mansoni | Tr4/Tr2 (homologue) | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor-like 1 | 0.0031 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-41 | 0.0031 | 0.5 | 0.5 |
Echinococcus granulosus | ecdysone induced protein 78C | 0.0031 | 0.5 | 0.5 |
Onchocerca volvulus | Protein ultraspiracle homolog | 0.0031 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0031 | 0.5 | 0.5 |
Brugia malayi | steroid hormone receptor | 0.0031 | 0.5 | 0.5 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.0031 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | = 16 nM | Agonist activity at GR expressed in african green monkey CV1 cells transfected with luciferase gene linked to MMTV promoter assessed as induction of luciferase transactivation activity | ChEMBL. | 21349714 |
EC50 (functional) | = 182 nM | Agonist activity at GR expressed in rat H4IIEC3 cells assessed as induction of PEPCK transactivation by luciferase reporter gene assay | ChEMBL. | 21349714 |
Efficacy (functional) | = 44 % | Agonist activity at GR expressed in rat H4IIEC3 cells assessed as induction of PEPCK transactivation by luciferase reporter gene assay relative to Dexamethasone | ChEMBL. | 21349714 |
Efficacy (binding) | = 95 % | Transrepression activity at GR expressed in NHDF cells assessed as IL-1beta-mediated IL-6 transcription by ELISA relative to Dexamethasone | ChEMBL. | 21349714 |
Efficacy (binding) | = 98 % | Transrepression activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay relative to Dexamethasone | ChEMBL. | 21349714 |
Efficacy (functional) | = 155 % | Agonist activity at GR expressed in african green monkey CV1 cells transfected with luciferase gene linked to MMTV promoter assessed as induction of luciferase transactivation activity relative to Dexamethasone | ChEMBL. | 21349714 |
IC50 (binding) | = 23 nM | Transrepression activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay | ChEMBL. | 21349714 |
IC50 (binding) | = 31 nM | Transrepression activity at GR expressed in NHDF cells assessed as IL-1beta-mediated IL-6 transcription by ELISA | ChEMBL. | 21349714 |
Ki (binding) | = 2.9 nM | Displacement of radiolabeled Dexamethasone from GR | ChEMBL. | 21349714 |
Ki (binding) | = 231 nM | Binding affinity to progesterone receptor | ChEMBL. | 21349714 |
Ki (binding) | = 1115 nM | Binding affinity to mineralocorticoid receptor | ChEMBL. | 21349714 |
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.