Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | glutaminyl-peptide cyclotransferase | Starlite/ChEMBL | No references |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Onchocerca volvulus | Glutaminyl cyclase homolog | Get druggable targets OG5_129821 | All targets in OG5_129821 |
Echinococcus granulosus | glutaminyl peptide cyclotransferase | Get druggable targets OG5_129821 | All targets in OG5_129821 |
Brugia malayi | Peptidase family M28 containing protein | Get druggable targets OG5_129821 | All targets in OG5_129821 |
Schistosoma mansoni | glutaminyl cyclase (M28 family) | Get druggable targets OG5_129821 | All targets in OG5_129821 |
Loa Loa (eye worm) | hypothetical protein | Get druggable targets OG5_129821 | All targets in OG5_129821 |
Schistosoma japonicum | ko:K00683 glutaminyl-peptide cyclotransferase [EC2.3.2.5], putative | Get druggable targets OG5_129821 | All targets in OG5_129821 |
Echinococcus multilocularis | glutaminyl peptide cyclotransferase | Get druggable targets OG5_129821 | All targets in OG5_129821 |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Echinococcus granulosus | endoplasmic reticulum metallopeptidase 1 | glutaminyl-peptide cyclotransferase | 361 aa | 292 aa | 21.9 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | glutaminyl cyclase (M28 family) | 0.0136 | 0.5 | 0.5 |
Echinococcus multilocularis | glutaminyl peptide cyclotransferase | 0.0136 | 0.5 | 0.5 |
Echinococcus granulosus | glutaminyl peptide cyclotransferase | 0.0136 | 0.5 | 0.5 |
Onchocerca volvulus | Glutaminyl cyclase homolog | 0.0136 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0136 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 48 nM | BindingDB_Patents: Spectrophotometric Assay. This novel assay was used to determine the kinetic parameters for most of the QC substrates. QC activity was analyzed spectrophotometrically using a continuous method, that was derived by adapting a previous discontinuous assay (Bateman, R. C. J. 1989 J Neurosci Methods 30, 23-28) utilizing glutamate dehydrogenase as auxiliary enzyme. Samples consisted of the respective QC substrate, 0.3 mM NADH, 14 mM alpha-Ketoglutaric acid and 30 U/ml glutamate dehydrogenase in a final volume of 250 ul. Reactions were started by addition of QC and persued by monitoring of the decrease in absorbance at 340 nm for 8-15 min. The initial velocities were evaluated and the enzymatic activity was determined from a standard curve of ammonia under assay conditions. All samples were measured at 30 C., using either the SPECTRAFluor Plus or the Sunrise (both from TECAN) reader for microplates. Kinetic data was evaluated using GraFit software. | ChEMBL. | No reference |
Ki (binding) | = 4.13 nM | BindingDB_Patents: Spectrophotometric Assay. This novel assay was used to determine the kinetic parameters for most of the QC substrates. QC activity was analyzed spectrophotometrically using a continuous method, that was derived by adapting a previous discontinuous assay (Bateman, R. C. J. 1989 J Neurosci Methods 30, 23-28) utilizing glutamate dehydrogenase as auxiliary enzyme. Samples consisted of the respective QC substrate, 0.3 mM NADH, 14 mM alpha-Ketoglutaric acid and 30 U/ml glutamate dehydrogenase in a final volume of 250 ul. Reactions were started by addition of QC and persued by monitoring of the decrease in absorbance at 340 nm for 8-15 min. The initial velocities were evaluated and the enzymatic activity was determined from a standard curve of ammonia under assay conditions. All samples were measured at 30 C., using either the SPECTRAFluor Plus or the Sunrise (both from TECAN) reader for microplates. Kinetic data was evaluated using GraFit software. | 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.