Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | hydroxysteroid (11-beta) dehydrogenase 1 | Starlite/ChEMBL | References |
Mus musculus | hydroxysteroid 11-beta dehydrogenase 2 | Starlite/ChEMBL | References |
Mus musculus | hydroxysteroid 11-beta dehydrogenase 1 | Starlite/ChEMBL | References |
Homo sapiens | hydroxysteroid (11-beta) dehydrogenase 2 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Mycobacterium tuberculosis | Probable oxidoreductase | Get druggable targets OG5_132866 | All targets in OG5_132866 |
Mycobacterium ulcerans | short chain dehydrogenase | Get druggable targets OG5_132866 | All targets in OG5_132866 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Plasmodium falciparum | steroid dehydrogenase, putative | hydroxysteroid 11-beta dehydrogenase 1 | 292 aa | 246 aa | 25.2 % |
Plasmodium falciparum | steroid dehydrogenase, putative | hydroxysteroid (11-beta) dehydrogenase 1 | 292 aa | 250 aa | 24.8 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Onchocerca volvulus | Bile acid receptor homolog | 0.0493 | 0.5476 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-41 | 0.0493 | 0.5476 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0493 | 0.5476 | 1 |
Schistosoma mansoni | nuclear receptor 2DBD-gamma | 0.0493 | 0.5476 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-19 | 0.0493 | 0.5476 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-49 | 0.0493 | 0.5476 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0493 | 0.5476 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-1 | 0.0493 | 0.5476 | 1 |
Schistosoma mansoni | RAR-like nuclear receptor | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-14 | 0.0493 | 0.5476 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-14 | 0.0493 | 0.5476 | 1 |
Schistosoma mansoni | thyroid hormone receptor | 0.0493 | 0.5476 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-25 | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-41 | 0.0493 | 0.5476 | 1 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-31 | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | nuclear Hormone Receptor family member | 0.0493 | 0.5476 | 1 |
Echinococcus granulosus | retinoic acid receptor rxr beta a | 0.0493 | 0.5476 | 1 |
Echinococcus multilocularis | COUP TF:Svp nuclear hormone receptor | 0.0493 | 0.5476 | 1 |
Schistosoma mansoni | FTZ-F1 nuclear receptor-like protein | 0.0493 | 0.5476 | 1 |
Echinococcus granulosus | ecdysone induced protein 78C | 0.0493 | 0.5476 | 1 |
Schistosoma mansoni | photoreceptor-specific nuclear receptor related | 0.0493 | 0.5476 | 1 |
Brugia malayi | steroid hormone receptor | 0.0493 | 0.5476 | 1 |
Echinococcus multilocularis | thyroid hormone receptor alpha | 0.0493 | 0.5476 | 1 |
Echinococcus granulosus | Nuclear hormone receptor family member nhr 41 | 0.0493 | 0.5476 | 1 |
Schistosoma mansoni | thyroid hormone receptor | 0.0493 | 0.5476 | 1 |
Brugia malayi | nuclear hormone receptor | 0.0493 | 0.5476 | 1 |
Brugia malayi | Steroid receptor seven-up type 2 | 0.0493 | 0.5476 | 1 |
Schistosoma mansoni | nuclear hormone receptor | 0.0493 | 0.5476 | 1 |
Echinococcus multilocularis | FTZ F1 alpha | 0.0493 | 0.5476 | 1 |
Echinococcus multilocularis | FTZ F1 nuclear receptor protein | 0.0493 | 0.5476 | 1 |
Schistosoma mansoni | coup transcription factor | 0.0493 | 0.5476 | 1 |
Echinococcus granulosus | COUP TF:Svp nuclear hormone receptor | 0.0493 | 0.5476 | 1 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-40 | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0493 | 0.5476 | 1 |
Brugia malayi | photoreceptor-specific nuclear receptor | 0.0493 | 0.5476 | 1 |
Onchocerca volvulus | 0.0493 | 0.5476 | 0.5 | |
Echinococcus multilocularis | ecdysone induced protein 78C | 0.0493 | 0.5476 | 1 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0493 | 0.5476 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-3 | 0.0493 | 0.5476 | 1 |
Brugia malayi | Ligand-binding domain of nuclear hormone receptor family protein | 0.0493 | 0.5476 | 1 |
Echinococcus granulosus | hepatocyte nuclear factor 4 alpha | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | steroid hormone receptor | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-49 | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0493 | 0.5476 | 1 |
Echinococcus granulosus | nuclear receptor 2DBD gamma | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0493 | 0.5476 | 1 |
Brugia malayi | nuclear receptor NHR-88 | 0.0493 | 0.5476 | 1 |
Schistosoma mansoni | retinoic acid receptor RXR | 0.0493 | 0.5476 | 1 |
Brugia malayi | Nuclear hormone receptor family member nhr-40 | 0.0493 | 0.5476 | 1 |
Brugia malayi | ecdysteroid receptor | 0.0493 | 0.5476 | 1 |
Echinococcus multilocularis | hepatocyte nuclear factor 4 alpha | 0.0493 | 0.5476 | 1 |
Onchocerca volvulus | Protein ultraspiracle homolog | 0.0493 | 0.5476 | 0.5 |
Brugia malayi | Nuclear hormone receptor family member nhr-31 | 0.0493 | 0.5476 | 1 |
Brugia malayi | Nuclear hormone receptor-like 1 | 0.0493 | 0.5476 | 1 |
Echinococcus granulosus | FTZ F1 alpha | 0.0493 | 0.5476 | 1 |
Mycobacterium ulcerans | short chain dehydrogenase | 0.0685 | 1 | 0.5 |
Schistosoma mansoni | steroid hormone receptor ad4bp | 0.0493 | 0.5476 | 1 |
Echinococcus granulosus | FTZ F1 nuclear receptor protein | 0.0493 | 0.5476 | 1 |
Schistosoma mansoni | Tr4/Tr2 (homologue) | 0.0493 | 0.5476 | 1 |
Schistosoma mansoni | nuclear hormone receptor nor-1/nor-2 | 0.0493 | 0.5476 | 1 |
Loa Loa (eye worm) | nuclear hormone receptor family member nhr-1 | 0.0493 | 0.5476 | 1 |
Onchocerca volvulus | Steroid hormone receptor family member cnr14 homolog | 0.0493 | 0.5476 | 0.5 |
Echinococcus multilocularis | nuclear receptor 2DBD gamma | 0.0493 | 0.5476 | 1 |
Echinococcus multilocularis | Nuclear hormone receptor family member nhr 41 | 0.0493 | 0.5476 | 1 |
Schistosoma mansoni | retinoid-x-receptor (RXR) | 0.0493 | 0.5476 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (functional) | = -0.3 % | Reduction in hBA1c in type 2 diabetic patient | ChEMBL. | 24294985 |
AUC (ADMET) | = 4.68 microM.hr/mg/kg | Normalized AUC (0 to 24 hrs) in C57B6 mouse at 10 mg/kg, iv | ChEMBL. | 18440812 |
AUC (ADMET) | = 4.68 microM.hr/mg/kg | Normalized AUC (0 to 24 hrs) in C57B6 mouse at 10 mg/kg, iv | ChEMBL. | 18440812 |
AUC (ADMET) | = 5.44 microM.hr/mg/kg | Normalized AUC (0 to 24 hrs) in C57B6 mouse at 10 mg/kg, po | ChEMBL. | 18440812 |
AUC (ADMET) | = 5.44 microM.hr/mg/kg | Normalized AUC (0 to 24 hrs) in C57B6 mouse at 10 mg/kg, po | ChEMBL. | 18440812 |
CL (ADMET) | = 10.7 ml/min.kg | Plasma concentration in C57B6 mouse at 10 mg/kg | ChEMBL. | 18440812 |
CL (ADMET) | = 10.7 ml/min.kg | Plasma concentration in C57B6 mouse at 10 mg/kg | ChEMBL. | 18440812 |
F (ADMET) | = 100 % | Oral bioavailability in C57B6 mouse at 10 mg/kg | ChEMBL. | 18440812 |
F (ADMET) | = 100 % | Oral bioavailability in C57B6 mouse at 10 mg/kg | ChEMBL. | 18440812 |
IC50 (binding) | = 5 nM | Inhibition of human 11betaHSD1 by SPA assay | ChEMBL. | 18440812 |
IC50 (binding) | = 5 nM | Inhibition of human 11betaHSD1 by SPA assay | ChEMBL. | 18440812 |
IC50 (binding) | = 16 nM | Inhibition of mouse 11betaHSD1 by SPA assay | ChEMBL. | 18440812 |
IC50 (binding) | = 16 nM | Inhibition of mouse 11betaHSD1 by SPA assay | ChEMBL. | 18440812 |
IC50 (binding) | > 4000 nM | Inhibition of human 11betaHSD2 by SPA assay | ChEMBL. | 18440812 |
IC50 (binding) | > 4000 nM | Inhibition of mouse 11betaHSD2 by SPA assay | ChEMBL. | 18440812 |
IC50 (binding) | > 4000 nM | Inhibition of human 11betaHSD2 by SPA assay | ChEMBL. | 18440812 |
IC50 (binding) | > 4000 nM | Inhibition of mouse 11betaHSD2 by SPA assay | ChEMBL. | 18440812 |
Inhibition (functional) | = 91 % | Inhibition of 11betaHSD1 in mouse phamacodynamic model assessed as inhibition of [3H]cortisone to [3H]cortisol at 10 mg/kg, po after 4 hrs | ChEMBL. | 18440812 |
Inhibition (functional) | = 91 % | Inhibition of 11betaHSD1 in mouse phamacodynamic model assessed as inhibition of [3H]cortisone to [3H]cortisol at 10 mg/kg, po after 4 hrs | ChEMBL. | 18440812 |
Inhibition (functional) | = 92 % | Inhibition of 11betaHSD1 in mouse phamacodynamic model assessed as inhibition of [3H]cortisone to [3H]cortisol at 10 mg/kg, po after 1 hr | ChEMBL. | 18440812 |
Inhibition (functional) | = 92 % | Inhibition of 11betaHSD1 in mouse phamacodynamic model assessed as inhibition of [3H]cortisone to [3H]cortisol at 10 mg/kg, po after 1 hr | ChEMBL. | 18440812 |
t1/2 (ADMET) | = 1.5 hr | Half life in C57B6 mouse at 10 mg/kg | ChEMBL. | 18440812 |
T1/2 (ADMET) | = 1.5 hr | Half life in C57B6 mouse at 10 mg/kg | ChEMBL. | 18440812 |
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.