Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | glutaminyl-peptide cyclotransferase | Starlite/ChEMBL | No references |
Species | Potential target | Known druggable target/s | Ortholog Group |
---|---|---|---|
Echinococcus multilocularis | glutaminyl peptide cyclotransferase | 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 |
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 |
Echinococcus granulosus | glutaminyl peptide cyclotransferase | Get druggable targets OG5_129821 | All targets in OG5_129821 |
Onchocerca volvulus | Glutaminyl cyclase homolog | 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 |
---|---|---|---|---|
Brugia malayi | Calcitonin receptor-like protein seb-1 | 0.0047 | 0.2192 | 0.2192 |
Echinococcus granulosus | glutaminyl peptide cyclotransferase | 0.0136 | 1 | 1 |
Trypanosoma cruzi | glutaminyl cyclase, putative | 0.0022 | 0 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0047 | 0.2192 | 0.2192 |
Loa Loa (eye worm) | hypothetical protein | 0.0136 | 1 | 1 |
Toxoplasma gondii | peptidase, M28 family protein | 0.0022 | 0 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0032 | 0.09 | 0.09 |
Mycobacterium ulcerans | lipoprotein aminopeptidase LpqL | 0.0022 | 0 | 0.5 |
Loa Loa (eye worm) | pigment dispersing factor receptor c | 0.0047 | 0.2192 | 0.2192 |
Mycobacterium ulcerans | hypothetical protein | 0.0022 | 0 | 0.5 |
Leishmania major | glutaminyl cyclase, putative | 0.0022 | 0 | 0.5 |
Trypanosoma brucei | glutaminyl cyclase, putative | 0.0022 | 0 | 0.5 |
Echinococcus multilocularis | glutaminyl peptide cyclotransferase | 0.0136 | 1 | 1 |
Trypanosoma cruzi | glutaminyl cyclase, putative | 0.0022 | 0 | 0.5 |
Brugia malayi | Corticotropin releasing factor receptor 2 precursor, putative | 0.0047 | 0.2192 | 0.2192 |
Schistosoma mansoni | hypothetical protein | 0.0032 | 0.09 | 0.09 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0022 | 0 | 0.5 |
Mycobacterium tuberculosis | Conserved protein | 0.0022 | 0 | 0.5 |
Toxoplasma gondii | hypothetical protein | 0.0022 | 0 | 0.5 |
Leishmania major | hypothetical protein, conserved | 0.0022 | 0 | 0.5 |
Onchocerca volvulus | Glutaminyl cyclase homolog | 0.0136 | 1 | 1 |
Brugia malayi | latrophilin 2 splice variant baaae | 0.0032 | 0.09 | 0.09 |
Schistosoma mansoni | glutaminyl cyclase (M28 family) | 0.0136 | 1 | 1 |
Trichomonas vaginalis | Clan MH, family M28, aminopeptidase S-like metallopeptidase | 0.0022 | 0 | 0.5 |
Mycobacterium tuberculosis | Probable lipoprotein aminopeptidase LpqL | 0.0022 | 0 | 0.5 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0022 | 0 | 0.5 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0022 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 9830 nM | BindingDB_Patents: Inhibition Assay. Fluorometric Assays: All measurements were performed with a BioAssay Reader HTS-7000Plus for microplates (Perkin Elmer) at 30 C. 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 30 C. utilizing the NOVOStar reader for microplates (BMG labtechnology). | ChEMBL. | No reference |
Ki (binding) | = 971 nM | BindingDB_Patents: Inhibition Assay. Fluorometric Assays: All measurements were performed with a BioAssay Reader HTS-7000Plus for microplates (Perkin Elmer) at 30 C. 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 30 C. utilizing the NOVOStar reader for microplates (BMG labtechnology). | 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.