Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Mus musculus | hydroxysteroid 11-beta dehydrogenase 2 | Starlite/ChEMBL | References |
Homo sapiens | hydroxysteroid (11-beta) dehydrogenase 1 | Starlite/ChEMBL | References |
Homo sapiens | hydroxysteroid (11-beta) dehydrogenase 2 | Starlite/ChEMBL | References |
Mus musculus | hydroxysteroid 11-beta dehydrogenase 1 | 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 % |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 7.8 nM | Inhibition of human 11beta-HSD1 expressed in CHO-K1 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation counting | ChEMBL. | 21334894 |
IC50 (binding) | = 98 nM | Inhibition of mouse 11beta-HSD1 expressed in CHO-K1 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation counting | ChEMBL. | 21334894 |
IC50 (binding) | > 4000 nM | Inhibition of human 11beta-HSD2 | ChEMBL. | 21334894 |
IC50 (binding) | > 4000 nM | Inhibition of mouse 11beta-HSD2 | ChEMBL. | 21334894 |
Inhibition (functional) | = 21 % | Inhibition of 11beta-HSD1 in ICR mouse assessed as conversion of [3H]cortisone to [3H]cortisol at 10 mg/kg, po after 4 hrs by scintillation counting | ChEMBL. | 21334894 |
Inhibition (functional) | = 24 % | 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) | = 24 % | 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) | = 31 % | Inhibition of 11beta-HSD1 in ICR mouse assessed as conversion of [3H]cortisone to [3H]cortisol at 10 mg/kg, po after 1 hr by scintillation counting | ChEMBL. | 21334894 |
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.
2 literature references were collected for this gene.