Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | maternal embryonic leucine zipper kinase | Starlite/ChEMBL | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus granulosus | maternal embryonic leucine zipper kinase | 0.0099 | 0.3581 | 1 |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Trichomonas vaginalis | CAMK family protein kinase | 0.0148 | 1 | 1 |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Onchocerca volvulus | Dopamine\/Ecdysteroid receptor homolog | 0.0072 | 0 | 0.5 |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Echinococcus multilocularis | maternal embryonic leucine zipper kinase | 0.0099 | 0.3581 | 1 |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Schistosoma mansoni | serine/threonine kinase | 0.0148 | 1 | 1 |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Onchocerca volvulus | 0.0072 | 0 | 0.5 | |
Loa Loa (eye worm) | CAMK/CAMKL/MELK protein kinase | 0.0148 | 1 | 1 |
Onchocerca volvulus | Neuropeptide F receptor homolog | 0.0072 | 0 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 2.2 nM | BindingDB_Patents: Kinase Assay. MELK activity was determined in the presence or absence of compounds using fluorescein isothiocyanate-labeled (FITC-labeled) histone H3 peptide as a substrate. The extent of FITC-labeled histone H3 peptide phosphorylation was measured by immobilized metal ion affinity-based fluorescence polarization (IMAP) technology (Sportsman J R, et al., Assay Drug Dev. Technol. 2: 205-14, 2004) using IMAP FP Progressive Binding System (Molecular Devices Corporation). Test compounds were dissolved in DMSO at 12.5 mM and then serially diluted as the DMSO concentration in the assays to be 1%. The serially diluted compounds, 0.8 ng/micro-L PBK (Carna Biosciences) and 100 nM FITC-labeled histone H3 peptide were reacted in a reaction buffer (20 mM HEPES, 0.01% Tween-20, 0.3 mM MgCl2, 2 mM dithiothreitol, 50 micro-M ATP, pH 7.4) at room temperature for 1 hour. The reaction was stopped by the addition of three fold assay volume of progressive binding solution. Following 0.5 hour incubation at room temperature. | 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.