Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | cathepsin A | Starlite/ChEMBL | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Giardia lamblia | Ribonuclease H | 0.0082 | 0.2291 | 0.5 |
Trypanosoma cruzi | ribonuclease H1, putative | 0.0082 | 0.2291 | 1 |
Trypanosoma brucei | ingi protein (ORF1) | 0.0089 | 0.2529 | 0.2529 |
Schistosoma mansoni | phosphoglucomutase | 0.0082 | 0.2291 | 0.2291 |
Onchocerca volvulus | Ribonuclease H1 homolog | 0.0082 | 0.2291 | 1 |
Wolbachia endosymbiont of Brugia malayi | ribonuclease HI | 0.0082 | 0.2291 | 0.5 |
Brugia malayi | RNase H family protein | 0.0082 | 0.2291 | 1 |
Toxoplasma gondii | ribonuclease HI protein | 0.0082 | 0.2291 | 0.5 |
Treponema pallidum | ribonuclease H (rnhA) | 0.0082 | 0.2291 | 0.5 |
Trypanosoma cruzi | ribonuclease H1, putative | 0.0082 | 0.2291 | 1 |
Brugia malayi | RNase H family protein | 0.0082 | 0.2291 | 1 |
Trichomonas vaginalis | ribonuclease H1, putative | 0.0082 | 0.2291 | 0.5 |
Leishmania major | ribonuclease H1, putative | 0.0082 | 0.2291 | 1 |
Trypanosoma brucei | ribonuclease H1 | 0.0082 | 0.2291 | 0.2291 |
Loa Loa (eye worm) | hypothetical protein | 0.0015 | 0 | 0.5 |
Trypanosoma brucei | RNA helicase, putative | 0.0306 | 1 | 1 |
Schistosoma mansoni | phosphoglucomutase | 0.0082 | 0.2291 | 0.2291 |
Trypanosoma brucei | retrotransposon hot spot protein 4 (RHS4), interrupted | 0.0089 | 0.2529 | 0.2529 |
Echinococcus granulosus | ribonuclease H1 | 0.0082 | 0.2291 | 1 |
Trypanosoma brucei | hypothetical protein, conserved | 0.0089 | 0.2529 | 0.2529 |
Trypanosoma brucei | unspecified product | 0.0089 | 0.2529 | 0.2529 |
Brugia malayi | RNase H family protein | 0.0082 | 0.2291 | 1 |
Echinococcus multilocularis | ribonuclease H1 | 0.0082 | 0.2291 | 1 |
Trypanosoma brucei | ingi protein (ORF1) | 0.0089 | 0.2529 | 0.2529 |
Schistosoma mansoni | phosphoglucomutase | 0.0082 | 0.2291 | 0.2291 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 4350 nM | BindingDB_Patents: Inhibition Assay. The activated cathepsin A was diluted in assay buffer (25 mM MES, pH 5.5, containing 5 mM DTT) and mixed with the test compound (dissolved in assay buffer containing (v/v) 3% DMSO) or, in the control experiments, with the vehicle in a multiple assay plate. After incubation for 15 min at room temperature, as substrate then bradykinin carrying an N-terminal ®Bodipy FL (4,4-difluoro-5,7-dimethyl-4-bora-3a,4a-diaza-s-indacene-3-propionyl) label (JPT Peptide Technologies GmbH; dissolved in assay buffer) was added to the mixture. The final concentration of cathepsin A was 833 ng/ml and the final concentration of labeled bradykinin 2 µM. After incubation for 15 min at room temperature the reaction was stopped by the addition of stop buffer (130 mM 2-(4-(2-hydroxy-ethyl)-piperazin-1-yl)-ethanesulfonic acid, pH 7.4, containing (v/v) 0.013% ®Triton X-100, 0.13% Coating Reagent 3 (Caliper Life Sciences), 6.5% DMSO and 20 µM ebelactone B (Sigma, #E0886)). | 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.