Assay Detail
Binding
CHEMBL3706362
Review assay metadata, readout intent, target linkage, and publication context from the same page.
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.
113
Total Activities
112
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Maternal embryonic leucine zipper kinase (CHEMBL4578) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
1,5-naphthyridine derivatives and MELK inhibitors containing the same
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 113 | 8.48 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3688376 | — | — | 1 | 9.52 |
| CHEMBL3688335 | — | — | 1 | 9.52 |
| CHEMBL3688339 | — | — | 2 | 9.40 |
| CHEMBL3692787 | — | — | 1 | 9.40 |
| CHEMBL3692824 | — | — | 1 | 9.34 |
| CHEMBL3688337 | — | — | 1 | 9.30 |
| CHEMBL3688348 | — | — | 1 | 9.30 |
| CHEMBL3692797 | — | — | 1 | 9.30 |
| CHEMBL3692807 | — | — | 1 | 9.30 |
| CHEMBL3688380 | — | — | 1 | 9.22 |
| CHEMBL3692796 | — | — | 1 | 9.22 |
| CHEMBL3692806 | — | — | 1 | 9.22 |
| CHEMBL3692815 | — | — | 1 | 9.22 |
| CHEMBL3692820 | — | — | 1 | 9.22 |
| CHEMBL3688360 | — | — | 1 | 9.15 |
| CHEMBL3688342 | — | — | 1 | 9.15 |
| CHEMBL3688338 | — | — | 1 | 9.10 |
| CHEMBL3692789 | — | — | 1 | 9.10 |
| CHEMBL3688347 | — | — | 1 | 9.05 |
| CHEMBL3692788 | — | — | 1 | 9.05 |
| CHEMBL3692823 | — | — | 1 | 9.03 |
| CHEMBL3688345 | — | — | 1 | 9.00 |
| CHEMBL3688381 | — | — | 1 | 9.00 |
| CHEMBL3692801 | — | — | 1 | 9.00 |
| CHEMBL3692809 | — | — | 1 | 9.00 |
| CHEMBL3692819 | — | — | 1 | 8.96 |
| CHEMBL3692835 | — | — | 1 | 8.96 |
| CHEMBL3688336 | — | — | 1 | 8.92 |
| CHEMBL3688372 | — | — | 1 | 8.92 |
| CHEMBL3692783 | — | — | 1 | 8.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3688376 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3688335 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3688339 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3692787 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL3692824 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL3688337 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3692797 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3692807 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3688348 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3692815 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3692806 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3692796 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3688380 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3692820 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3688360 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3688342 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3688338 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3692789 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3688347 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3692788 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3692823 | — | IC50 | = | 0.93 | nM | 9.03 |
| CHEMBL3688381 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3688345 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3692809 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3692801 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3692835 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3688339 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3692819 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3692783 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3688336 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3692790 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3688372 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3692795 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3692793 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3692828 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3692826 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3692836 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3688340 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3688346 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3692832 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3688343 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3688341 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3688385 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3692825 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3692805 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3688364 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3692834 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3692829 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3688373 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3692839 | — | IC50 | = | 1.8 | nM | 8.74 |