Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | glutaminyl-peptide cyclotransferase-like | Starlite/ChEMBL | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | NNMT/PNMT/TEMT family protein | 0.0315 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0315 | 0.5 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0315 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 230 nM | BindingDB_Patents: Fluorometric Assay. All measurements were performed with a BioAssay Reader HTS-7000Plus for microplates (Perkin Elmer) at 30C. QC activity was evaluated fluorometrically using H-Gln-beta NA. The samples consisted of 0.2 mM fluorogenic substrate, 0.25 U pyroglutamyl aminopeptidase (Unizyme, Horsholm, Denmark) in 0.2 M Tris/HCl, pH 8.0 containing 20 mM EDTA and an appropriately diluted aliquot of QC in a final volume of 250 ul. Excitation/emission wavelengths were 320/410 nm. The assay reactions were initiated by addition of glutaminyl cyclase. QC activity was determined from a standard curve of beta -naphthylamine under assay conditions. One unit is defined as the amount of QC catalyzing the formation of 1 umol pGlu-beta NA from H-Gln-beta NA per minute under the described conditions. In a second fluorometric assay, QC was activity determined using H-Gln-AMC as substrate. Reactions were carried out at 30C. utilizing the NOVOStar reader for microplates (BMG labtechnologies). | ChEMBL. | No reference |
Ki (binding) | = 41 nM | BindingDB_Patents: Fluorometric Assay. All measurements were performed with a BioAssay Reader HTS-7000Plus for microplates (Perkin Elmer) at 30C. QC activity was evaluated fluorometrically using H-Gln-beta NA. The samples consisted of 0.2 mM fluorogenic substrate, 0.25 U pyroglutamyl aminopeptidase (Unizyme, Horsholm, Denmark) in 0.2 M Tris/HCl, pH 8.0 containing 20 mM EDTA and an appropriately diluted aliquot of QC in a final volume of 250 ul. Excitation/emission wavelengths were 320/410 nm. The assay reactions were initiated by addition of glutaminyl cyclase. QC activity was determined from a standard curve of beta -naphthylamine under assay conditions. One unit is defined as the amount of QC catalyzing the formation of 1 umol pGlu-beta NA from H-Gln-beta NA per minute under the described conditions. In a second fluorometric assay, QC was activity determined using H-Gln-AMC as substrate. Reactions were carried out at 30C. utilizing the NOVOStar reader for microplates (BMG labtechnologies). | 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.