Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Mycobacterium tuberculosis | Transcriptional regulatory repressor protein (TetR-family) EthR | References |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Mycobacterium leprae | Probable transcriptional regulatory repressor protein (TetR-family) EthR | Get druggable targets OG5_191427 | All targets in OG5_191427 |
Mycobacterium tuberculosis | Transcriptional regulatory repressor protein (TetR-family) EthR | Get druggable targets OG5_191427 | All targets in OG5_191427 |
Mycobacterium ulcerans | AcrR family transcriptional regulator | Get druggable targets OG5_191427 | All targets in OG5_191427 |
Mycobacterium ulcerans | TetR family transcriptional regulator | Get druggable targets OG5_191427 | All targets in OG5_191427 |
Mycobacterium ulcerans | transcriptional regulator | Get druggable targets OG5_191427 | All targets in OG5_191427 |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Onchocerca volvulus | 0.2067 | 1 | 1 | |
Schistosoma mansoni | hypothetical protein | 0.2067 | 1 | 1 |
Onchocerca volvulus | 0.1615 | 0.6009 | 0.2846 | |
Mycobacterium ulcerans | AcrR family transcriptional regulator | 0.1667 | 0.6468 | 0.5 |
Mycobacterium ulcerans | transcriptional regulator | 0.1667 | 0.6468 | 0.5 |
Loa Loa (eye worm) | DOMON domain-containing protein | 0.1434 | 0.4422 | 0.4422 |
Loa Loa (eye worm) | hypothetical protein | 0.2067 | 1 | 1 |
Leishmania major | hypothetical protein, conserved | 0.2067 | 1 | 0.5 |
Brugia malayi | Muscle positioning protein 4 | 0.1615 | 0.6009 | 0.2846 |
Loa Loa (eye worm) | hypothetical protein | 0.1615 | 0.6009 | 0.6009 |
Plasmodium vivax | cysteine repeat modular protein 1, putative | 0.2067 | 1 | 0.5 |
Trypanosoma cruzi | hypothetical protein, conserved | 0.2067 | 1 | 0.5 |
Toxoplasma gondii | kringle domain-containing protein | 0.2067 | 1 | 0.5 |
Mycobacterium ulcerans | TetR family transcriptional regulator | 0.1667 | 0.6468 | 0.5 |
Brugia malayi | Kringle domain containing protein | 0.2067 | 1 | 1 |
Schistosoma mansoni | hypothetical protein | 0.1434 | 0.4422 | 0.4048 |
Loa Loa (eye worm) | hypothetical protein | 0.1434 | 0.4422 | 0.4422 |
Echinococcus granulosus | tissue type plasminogen activator | 0.2067 | 1 | 0.5 |
Loa Loa (eye worm) | TK/ROR protein kinase | 0.2067 | 1 | 1 |
Plasmodium falciparum | cysteine repeat modular protein 1 | 0.2067 | 1 | 0.5 |
Mycobacterium leprae | Probable transcriptional regulatory repressor protein (TetR-family) EthR | 0.1667 | 0.6468 | 0.5 |
Mycobacterium tuberculosis | Transcriptional regulatory repressor protein (TetR-family) EthR | 0.1667 | 0.6468 | 0.5 |
Echinococcus multilocularis | tissue type plasminogen activator | 0.2067 | 1 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
AUC (ADMET) | = 0.1 ug/ml.hr | AUC (0 to infinity) in Swiss mouse at 20 mg/kg, po administered with 100% DMSO by LC-MS/MS analysis | ChEMBL. | 22098589 |
CL (ADMET) | = 4 microL/min/mg | Intrinsic clearance in CD1 mouse liver microsomes by LC-MS-MS analysis | ChEMBL. | 21417236 |
CL (ADMET) | = 4 microL/min/mg | Intrinsic clearance in CD-1 mouse liver microsomes at 1 uM by LC-MS/MS analysis | ChEMBL. | 22098589 |
EC50 (binding) | = 0.4 uM | Inhibition of Mycobacterium tuberculosis H37Rv EthR in Mycobacterium tuberculosis H37Rv expressing GFP infected mouse in RAW264.7 cells assessed as potentiation of ethionamide-induced antitubercular activity after 5 days by SYTO60-based fluorescence microscopy | ChEMBL. | 22098589 |
IC50 (binding) | = 2 uM | Inhibition of EthR binding to ethA promoter in 106-bp biotinylated DNA preincubated for 5 mins measured for 3 mins by surface plasmon resonance assay | ChEMBL. | 22098589 |
IC50 (binding) | = 2 uM | Inhibition of Mycobacterium tuberculosis EthR interaction to ethA promoter after 5 mins by surface plasmon resonance assay | ChEMBL. | 21417236 |
Inhibition (binding) | Inhibition of EthR binding to ethA promoter in 106-bp biotinylated DNA preincubated for 5 mins measured for 3 mins by surface plasmon resonance assay | ChEMBL. | 22098589 | |
T1/2 (ADMET) | = 298 min | Half life in CD1 mouse liver microsomes by LC-MS-MS analysis | ChEMBL. | 21417236 |
T1/2 (ADMET) | = 298 min | Half life in CD-1 mouse liver microsomes at 1 uM by LC-MS/MS analysis | ChEMBL. | 22098589 |
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.