Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | androgen receptor | Starlite/ChEMBL | References |
Homo sapiens | progesterone receptor | Starlite/ChEMBL | References |
Homo sapiens | nuclear receptor subfamily 3, group C, member 2 | Starlite/ChEMBL | References |
Homo sapiens | nuclear receptor subfamily 3, group C, member 1 (glucocorticoid receptor) | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Brugia malayi | photoreceptor-specific nuclear receptor | 0.004 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-1 | 0.004 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 alpha | 0.004 | 0.5 | 0.5 |
Onchocerca volvulus | Bile acid receptor homolog | 0.004 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-49 | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.004 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.004 | 0.5 | 0.5 |
Schistosoma mansoni | coup transcription factor | 0.004 | 0.5 | 0.5 |
Echinococcus multilocularis | hepatocyte nuclear factor 4 alpha | 0.004 | 0.5 | 0.5 |
Brugia malayi | steroid hormone receptor | 0.004 | 0.5 | 0.5 |
Onchocerca volvulus | Protein ultraspiracle homolog | 0.004 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.004 | 0.5 | 0.5 |
Echinococcus multilocularis | ecdysone induced protein 78C | 0.004 | 0.5 | 0.5 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.004 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor nor-1/nor-2 | 0.004 | 0.5 | 0.5 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.004 | 0.5 | 0.5 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.004 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.004 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.004 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.004 | 0.5 | 0.5 |
Schistosoma mansoni | RAR-like nuclear receptor | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.004 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-31 | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-14 | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-40 | 0.004 | 0.5 | 0.5 |
Onchocerca volvulus | 0.004 | 0.5 | 0.5 | |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.004 | 0.5 | 0.5 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.004 | 0.5 | 0.5 |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | 0.004 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor-like 1 | 0.004 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.004 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-41 | 0.004 | 0.5 | 0.5 |
Echinococcus granulosus | COUP TF:Svp nuclear hormone receptor | 0.004 | 0.5 | 0.5 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.004 | 0.5 | 0.5 |
Schistosoma mansoni | nuclear hormone receptor | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-49 | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-41 | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | steroid hormone receptor | 0.004 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.004 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-14 | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.004 | 0.5 | 0.5 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.004 | 0.5 | 0.5 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.004 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 alpha | 0.004 | 0.5 | 0.5 |
Schistosoma mansoni | thyroid hormone receptor | 0.004 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-40 | 0.004 | 0.5 | 0.5 |
Schistosoma mansoni | Tr4/Tr2 (homologue) | 0.004 | 0.5 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.004 | 0.5 | 0.5 |
Brugia malayi | nuclear receptor NHR-88 | 0.004 | 0.5 | 0.5 |
Brugia malayi | nuclear hormone receptor | 0.004 | 0.5 | 0.5 |
Schistosoma mansoni | FTZ-F1 nuclear receptor-like protein | 0.004 | 0.5 | 0.5 |
Echinococcus granulosus | ecdysone induced protein 78C | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-1 | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.004 | 0.5 | 0.5 |
Echinococcus multilocularis | Nuclear hormone receptor family member nhr 41 | 0.004 | 0.5 | 0.5 |
Echinococcus multilocularis | COUP TF:Svp nuclear hormone receptor | 0.004 | 0.5 | 0.5 |
Echinococcus granulosus | hepatocyte nuclear factor 4 alpha | 0.004 | 0.5 | 0.5 |
Onchocerca volvulus | Steroid hormone receptor family member cnr14 homolog | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.004 | 0.5 | 0.5 |
Echinococcus multilocularis | FTZ F1 nuclear receptor protein | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear Hormone Receptor family member | 0.004 | 0.5 | 0.5 |
Echinococcus granulosus | Nuclear hormone receptor family member nhr 41 | 0.004 | 0.5 | 0.5 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-31 | 0.004 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-3 | 0.004 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.004 | 0.5 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.004 | 0.5 | 0.5 |
Brugia malayi | Steroid receptor seven-up type 2 | 0.004 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | = 0.2 nM | Agonist activity at human GR expressed in CV1 cells by GRE activation assay | ChEMBL. | 17705362 |
EC50 (functional) | = 0.2 nM | Agonist activity at human GR expressed in CV1 cells by GRE activation assay | ChEMBL. | 17705362 |
Efficacy (functional) | = 26 % | Agonist efficacy at human GR expressed in CV1 cells by GRE activation assay relative to dexamethasone | ChEMBL. | 17705362 |
Efficacy (functional) | = 26 % | Agonist efficacy at human GR expressed in CV1 cells by GRE activation assay relative to dexamethasone | ChEMBL. | 17705362 |
Efficacy (functional) | = 29 % | Inhibition of tumor growth in human RPMI8226 cells xenografted nude mouse at 3 mg/kg, po after 4 weeks relative to dexamethasone | ChEMBL. | 17705362 |
Efficacy (functional) | = 29 % | Inhibition of tumor growth in human RPMI8226 cells xenografted nude mouse at 3 mg/kg, po after 4 weeks relative to dexamethasone | ChEMBL. | 17705362 |
Efficacy (functional) | = 80 % | Inhibition of tumor growth in human RPMI8226 cells xenografted nude mouse at 30 mg/kg, po after 4 weeks relative to dexamethasone | ChEMBL. | 17705362 |
Efficacy (functional) | = 80 % | Inhibition of tumor growth in human RPMI8226 cells xenografted nude mouse at 30 mg/kg, po after 4 weeks relative to dexamethasone | ChEMBL. | 17705362 |
Efficacy (binding) | = 94 % | Absolute efficacy at human GR expressed in NHDFneo cells assessed as repression of IL-6 production relative to dexamethasone | ChEMBL. | 17705362 |
Efficacy (binding) | = 94 % | Absolute efficacy at human GR expressed in NHDFneo cells assessed as repression of IL-6 production relative to dexamethasone | ChEMBL. | 17705362 |
Efficacy (functional) | = 97 % | Inhibition of tumor growth in human RPMI8226 cells xenografted nude mouse at 100 mg/kg, po after 4 weeks relative to dexamethasone | ChEMBL. | 17705362 |
Efficacy (functional) | = 97 % | Inhibition of tumor growth in human RPMI8226 cells xenografted nude mouse at 100 mg/kg, po after 4 weeks relative to dexamethasone | ChEMBL. | 17705362 |
Efficacy (functional) | = 99 % | Antiproliferative activity against human RPMI8226 cells after 4 days relative to dexamethasone | ChEMBL. | 17705362 |
Efficacy (functional) | = 99 % | Antiproliferative activity against human RPMI8226 cells after 4 days relative to dexamethasone | ChEMBL. | 17705362 |
IC50 (binding) | = 0.2 nM | Activity at human GR expressed in NHDFneo cells assessed as inhibition of IL-6 production | ChEMBL. | 17705362 |
IC50 (binding) | = 0.2 nM | Activity at human GR expressed in NHDFneo cells assessed as inhibition of IL-6 production | ChEMBL. | 17705362 |
IC50 (functional) | = 4.9 nM | Antiproliferative activity against human RPMI8226 cells after 4 days | ChEMBL. | 17705362 |
IC50 (functional) | = 4.9 nM | Antiproliferative activity against human RPMI8226 cells after 4 days | ChEMBL. | 17705362 |
Ki (binding) | = 0.7 nM | Binding affinity to GR | ChEMBL. | 17705362 |
Ki (binding) | = 0.7 nM | Binding affinity to GR | ChEMBL. | 17705362 |
Ki (binding) | = 290 nM | Binding affinity to AR | ChEMBL. | 17705362 |
Ki (binding) | = 290 nM | Binding affinity to AR | ChEMBL. | 17705362 |
Ki (binding) | = 980 nM | Binding affinity to MR | ChEMBL. | 17705362 |
Ki (binding) | = 980 nM | Binding affinity to MR | ChEMBL. | 17705362 |
Ki (binding) | = 1400 nM | Binding affinity to PR | ChEMBL. | 17705362 |
Ki (binding) | = 1400 nM | Binding affinity to PR | ChEMBL. | 17705362 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 17705362 |
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.