Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | cathepsin A | Starlite/ChEMBL | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | hypothetical protein | 0.0015 | 1 | 0.5 |
Trypanosoma cruzi | serine peptidase, Clan SC, Family S10, putative | 0.0015 | 1 | 0.5 |
Trypanosoma brucei | serine peptidase, Clan SC, Family S10 | 0.0015 | 1 | 0.5 |
Trypanosoma cruzi | serine carboxypeptidase (CBP1), putative | 0.0015 | 1 | 0.5 |
Schistosoma mansoni | family S10 non-peptidase homologue (S10 family) | 0.0015 | 1 | 0.5 |
Onchocerca volvulus | Uncharacterized serine carboxypeptidase homolog | 0.0015 | 1 | 0.5 |
Entamoeba histolytica | protein kinase, putative | 0.0015 | 0.8079 | 0.5 |
Trypanosoma brucei | serine peptidase, Clan SC, Family S10 | 0.0015 | 1 | 0.5 |
Entamoeba histolytica | hypothetical protein | 0.0015 | 0.8079 | 0.5 |
Trypanosoma brucei | serine peptidase, Clan SC, Family S10 | 0.0015 | 1 | 0.5 |
Leishmania major | serine carboxypeptidase (CBP1), putative,serine peptidase, Clan SC, Family S10 | 0.0015 | 1 | 0.5 |
Trypanosoma cruzi | serine peptidase, Clan SC, Family S10, putative | 0.0015 | 1 | 0.5 |
Echinococcus granulosus | lysosomal protective protein | 0.0015 | 1 | 1 |
Trypanosoma cruzi | serine carboxypeptidase (CBP1), putative | 0.0015 | 1 | 0.5 |
Schistosoma mansoni | family S10 unassigned peptidase (S10 family) | 0.0015 | 1 | 0.5 |
Echinococcus multilocularis | lysosomal protective protein | 0.0015 | 1 | 1 |
Entamoeba histolytica | hypothetical protein | 0.0015 | 0.8079 | 0.5 |
Entamoeba histolytica | hypothetical protein | 0.0015 | 0.8079 | 0.5 |
Entamoeba histolytica | leucine-rich repeat domain-containing protein | 0.0015 | 0.8079 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 1020 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.