Assay Detail
Binding
CHEMBL5736698
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Characterization of Hits and Compound 15 (MELK-In-1) Derivatives: The top 10 hits from the 1 μM screening and derivatives of MELK-In-1 were subjected to the same assay conditions with varied inhibitor concentrations (0.0005-50 μM) to generate a dose-response curve and IC50. At set time points (0.25, 0.5, 1, 1.5, and 2 min for assays containing 10 nM MELK and 1, 2, 4, 6, and 10 min for assays containing 1 nM MELK), 30 μL aliquots were taken from each reaction and spotted onto 2×2 cm squares of p81 paper. Papers were washed 4 times in 75 mM O-phosphoric acid and once in acetone. Labeled protein was quantified by its associated CPM determined on a Packard 1500 scintillation counter at a sigma value of 2. CPM were translated into nmol 32P incorporated using Equation 1.
33
Total Activities
9
Compounds Tested
3
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
Indolinone derivatives as inhibitors of maternal embryonic leucine zipper kinase
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.31 | 8.52 |
| kon | 11 | - | - |
| k_off | 11 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4062168 | — | — | 6 | 8.52 |
| CHEMBL1908392 | — | — | 3 | 8.44 |
| CHEMBL4089284 | — | — | 3 | 8.28 |
| CHEMBL4083922 | — | — | 6 | 7.75 |
| CHEMBL4081410 | — | — | 3 | 7.62 |
| CHEMBL4075402 | — | — | 3 | 6.45 |
| CHEMBL4099431 | — | — | 3 | 5.94 |
| CHEMBL4061117 | — | — | 3 | 5.57 |
| CHEMBL4062202 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4062168 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL1908392 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4089284 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4083922 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4081410 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4062168 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4083922 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4075402 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL4099431 | — | IC50 | = | 1145.0 | nM | 5.94 |
| CHEMBL4061117 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL4099431 | — | k_off | = | - | s-1 | - |
| CHEMBL4081410 | — | k_off | = | - | s-1 | - |
| CHEMBL4081410 | — | kon | = | - | — | - |
| CHEMBL4075402 | — | k_off | = | - | s-1 | - |
| CHEMBL4075402 | — | kon | = | - | — | - |
| CHEMBL4062168 | — | k_off | = | - | s-1 | - |
| CHEMBL4062168 | — | kon | = | - | — | - |
| CHEMBL1908392 | — | k_off | = | - | s-1 | - |
| CHEMBL1908392 | — | kon | = | - | — | - |
| CHEMBL4062168 | — | k_off | = | - | s-1 | - |
| CHEMBL4062168 | — | kon | = | - | — | - |
| CHEMBL4089284 | — | kon | = | - | — | - |
| CHEMBL4089284 | — | k_off | = | - | s-1 | - |
| CHEMBL4083922 | — | k_off | = | - | s-1 | - |
| CHEMBL4083922 | — | kon | = | - | — | - |
| CHEMBL4083922 | — | k_off | = | - | s-1 | - |
| CHEMBL4083922 | — | kon | = | - | — | - |
| CHEMBL4099431 | — | kon | = | - | — | - |
| CHEMBL4062202 | — | kon | = | - | — | - |
| CHEMBL4062202 | — | IC50 | > | 5000.0 | nM | - |
| CHEMBL4061117 | — | k_off | = | - | s-1 | - |
| CHEMBL4061117 | — | kon | = | - | — | - |
| CHEMBL4062202 | — | k_off | = | - | s-1 | - |