Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | hydroxysteroid (11-beta) dehydrogenase 1 | No references |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Mycobacterium ulcerans | short chain dehydrogenase | Get druggable targets OG5_132866 | All targets in OG5_132866 |
Mycobacterium tuberculosis | Probable oxidoreductase | 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 | 250 aa | 24.8 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Mycobacterium leprae | NADH-DEPENDENT ENOYL-[ACYL-CARRIER-PROTEIN] REDUCTASE INHA (NADH-DEPENDENT ENOYL-ACP REDUCTASE) | 0.0162 | 0.4542 | 0.5 |
Mycobacterium ulcerans | phosphotyrosine protein phosphatase PtpB | 0.018 | 0.5085 | 0.5085 |
Entamoeba histolytica | hypothetical protein, conserved | 0.0052 | 0.1117 | 0.5 |
Plasmodium vivax | enoyl-acyl carrier protein reductase | 0.0162 | 0.4542 | 0.5 |
Mycobacterium ulcerans | enoyl-(acyl carrier protein) reductase | 0.0162 | 0.4542 | 0.4542 |
Entamoeba histolytica | phosphatidylinositol-3,4,5-trisphosphate 3-phosphatase, putative | 0.0052 | 0.1117 | 0.5 |
Toxoplasma gondii | enoyl-acyl carrier reductase ENR | 0.0162 | 0.4542 | 1 |
Leishmania major | hypothetical protein, unknown function | 0.0052 | 0.1117 | 0.2197 |
Plasmodium falciparum | enoyl-acyl carrier reductase | 0.0162 | 0.4542 | 0.5 |
Trichomonas vaginalis | conserved hypothetical protein | 0.018 | 0.5085 | 1 |
Trypanosoma brucei | oxidoreductase-like protein | 0.0016 | 0 | 0.5 |
Leishmania major | phosphoinositide phosphatase | 0.018 | 0.5085 | 1 |
Onchocerca volvulus | 0.0016 | 0 | 0.5 | |
Mycobacterium ulcerans | short chain dehydrogenase | 0.0338 | 1 | 1 |
Chlamydia trachomatis | enoyl-acyl-carrier protein reductase | 0.0162 | 0.4542 | 0.5 |
Mycobacterium tuberculosis | NADH-dependent enoyl-[acyl-carrier-protein] reductase InhA (NADH-dependent enoyl-ACP reductase) | 0.0162 | 0.4542 | 0.4542 |
Wolbachia endosymbiont of Brugia malayi | enoyl-ACP reductase | 0.0162 | 0.4542 | 0.5 |
Mycobacterium tuberculosis | Phosphotyrosine protein phosphatase PTPB (protein-tyrosine-phosphatase) (PTPase) | 0.018 | 0.5085 | 0.5085 |
Trypanosoma cruzi | tyrosine phosphatase, putative | 0.0052 | 0.1117 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 330 nM | BindingDB_Patents: Homogeneous Time-Resolved Fluorescence Assay. In vitro inhibition of 11beta -HSD1 by test compounds is determined with HTRF (Homogeneous Time-Resolved Fluorescence) technology (cisbio international, France) detecting cortisol generated from cortisterone by human liver microsomes. Briefly, compounds are incubated for 1 hour at 37C. in Tris buffer (20 mM tris, 5 mM EDTA, pH 6.0) containing NADPH (200 uM) and cortisone (80 nM). Cortisol generated in the reaction is then detected with a competitive immunoassay, involving two HTRF conjugates: cortisol linked to XL665 and anti-cortisol antibody labeled with Europium cryptate. The incubation period for detection reaction is typically 2 hours. The amount of cortisol is determined by reading the time-resolved fluorescence of the wells (Ex 320/75 nm; Em 615/8.5 nm and 665/7.5 nm). The ratio of the two emission signals is then calculated (Em665X10000/Em615). | ChEMBL. | No reference |
IC50 (binding) | = 330 nM | BindingDB_Patents: Homogeneous Time-Resolved Fluorescence Assay. In vitro inhibition of 11beta -HSD1 by test compounds is determined with HTRF (Homogeneous Time-Resolved Fluorescence) technology (cisbio international, France) detecting cortisol generated from cortisterone by human liver microsomes. Briefly, compounds are incubated for 1 hour at 37C. in Tris buffer (20 mM tris, 5 mM EDTA, pH 6.0) containing NADPH (200 uM) and cortisone (80 nM). Cortisol generated in the reaction is then detected with a competitive immunoassay, involving two HTRF conjugates: cortisol linked to XL665 and anti-cortisol antibody labeled with Europium cryptate. The incubation period for detection reaction is typically 2 hours. The amount of cortisol is determined by reading the time-resolved fluorescence of the wells (Ex 320/75 nm; Em 615/8.5 nm and 665/7.5 nm). The ratio of the two emission signals is then calculated (Em665X10000/Em615). | ChEMBL. | No reference |
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.