Assay Detail
Binding
CHEMBL5732370
Review assay metadata, readout intent, target linkage, and publication context from the same page.
GSK 3α Enzyme Inhibition: The GSK3-α protein (500 ng/mL, 2.5 μL) was mixed with the test compound (2.5 μL at either 4 μg/mL, 0.4 μg/mL, 0.04 μg/mL, or 0.004 μg/mL) for 2 hr at RT. The FRET peptide (8 μM, 2.5 μL), which is a phosphorylation target for GSK3α, and ATP (40 μM, 2.5 μL) were then added to the enzyme/compound mixture and the resulting mixture incubated for 1 hr. Development reagent (protease, 5 μL) was added for 1 hr prior to detection in a fluorescence microplate reader (Varioskan® Flash, ThermoFisher Scientific).
108
Total Activities
32
Compounds Tested
4
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
1-pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl) ureas as P38 MAP knase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| kon | 36 | - | - |
| k_off | 36 | - | - |
| IC50 | 34 | 5.87 | 7.35 |
| Kd | 2 | 5.73 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3695569 | — | — | 6 | 7.35 |
| CHEMBL5848716 | — | — | 3 | 5.68 |
| CHEMBL5768918 | — | — | 3 | 5.62 |
| CHEMBL5913904 | — | — | 3 | 5.60 |
| CHEMBL5896412 | — | — | 6 | 5.49 |
| CHEMBL5896806 | — | — | 3 | 5.46 |
| CHEMBL3701217 | — | — | 6 | 4.70 |
| CHEMBL6019442 | — | — | 3 | - |
| CHEMBL5977979 | — | — | 3 | - |
| CHEMBL5896751 | — | — | 6 | - |
| CHEMBL5756167 | — | — | 3 | - |
| CHEMBL5921712 | — | — | 3 | - |
| CHEMBL6007304 | — | — | 3 | - |
| CHEMBL5853055 | — | — | 3 | - |
| CHEMBL5820343 | — | — | 3 | - |
| CHEMBL5797522 | — | — | 3 | - |
| CHEMBL5799669 | — | — | 3 | - |
| CHEMBL5762929 | — | — | 3 | - |
| CHEMBL6014353 | — | — | 3 | - |
| CHEMBL5794070 | — | — | 3 | - |
| CHEMBL5951223 | — | — | 3 | - |
| CHEMBL5830994 | — | — | 3 | - |
| CHEMBL6035491 | — | — | 3 | - |
| CHEMBL5754667 | — | — | 3 | - |
| CHEMBL5988695 | — | — | 3 | - |
| CHEMBL5901318 | — | — | 3 | - |
| CHEMBL5836383 | — | — | 3 | - |
| CHEMBL5758982 | — | — | 3 | - |
| CHEMBL6014943 | — | — | 3 | - |
| CHEMBL5947021 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3695569 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL3695569 | — | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL5848716 | — | IC50 | = | 2108.0 | nM | 5.68 |
| CHEMBL5768918 | — | IC50 | = | 2377.0 | nM | 5.62 |
| CHEMBL5913904 | — | IC50 | = | 2494.0 | nM | 5.60 |
| CHEMBL5896412 | — | IC50 | = | 3260.0 | nM | 5.49 |
| CHEMBL5896806 | — | IC50 | = | 3505.0 | nM | 5.46 |
| CHEMBL3701217 | — | Kd | = | 20000.0 | nM | 4.70 |
| CHEMBL5768918 | — | kon | = | - | — | - |
| CHEMBL5951223 | — | k_off | = | - | s-1 | - |
| CHEMBL5768918 | — | k_off | = | - | s-1 | - |
| CHEMBL3701217 | — | kon | = | - | — | - |
| CHEMBL3701217 | — | k_off | = | - | s-1 | - |
| CHEMBL3695569 | — | kon | = | - | — | - |
| CHEMBL3695569 | — | k_off | = | - | s-1 | - |
| CHEMBL5836383 | — | IC50 | > | 1580.0 | nM | - |
| CHEMBL5830994 | — | kon | = | - | — | - |
| CHEMBL5830994 | — | IC50 | > | 1630.0 | nM | - |
| CHEMBL5848716 | — | kon | = | - | — | - |
| CHEMBL5758982 | — | k_off | = | - | s-1 | - |
| CHEMBL5758982 | — | kon | = | - | — | - |
| CHEMBL5758982 | — | IC50 | > | 1620.0 | nM | - |
| CHEMBL5836383 | — | k_off | = | - | s-1 | - |
| CHEMBL5836383 | — | kon | = | - | — | - |
| CHEMBL5754667 | — | IC50 | > | 1540.0 | nM | - |
| CHEMBL5754667 | — | k_off | = | - | s-1 | - |
| CHEMBL5754667 | — | kon | = | - | — | - |
| CHEMBL5988695 | — | IC50 | > | 1620.0 | nM | - |
| CHEMBL5921712 | — | IC50 | > | 15800.0 | nM | - |
| CHEMBL6019442 | — | IC50 | > | 1590.0 | nM | - |
| CHEMBL5848716 | — | k_off | = | - | s-1 | - |
| CHEMBL5896751 | — | IC50 | > | 15100.0 | nM | - |
| CHEMBL5896751 | — | kon | = | - | — | - |
| CHEMBL5896751 | — | k_off | = | - | s-1 | - |
| CHEMBL5756167 | — | IC50 | > | 16000.0 | nM | - |
| CHEMBL5756167 | — | kon | = | - | — | - |
| CHEMBL5756167 | — | k_off | = | - | s-1 | - |
| CHEMBL5947021 | — | IC50 | > | 1670.0 | nM | - |
| CHEMBL5947021 | — | kon | = | - | — | - |
| CHEMBL5947021 | — | k_off | = | - | s-1 | - |
| CHEMBL5951223 | — | kon | = | - | — | - |
| CHEMBL6019442 | — | kon | = | - | — | - |
| CHEMBL6019442 | — | k_off | = | - | s-1 | - |
| CHEMBL6014353 | — | IC50 | > | 1660.0 | nM | - |
| CHEMBL6014353 | — | kon | = | - | — | - |
| CHEMBL6014353 | — | k_off | = | - | s-1 | - |
| CHEMBL5794070 | — | IC50 | > | 1590.0 | nM | - |
| CHEMBL5794070 | — | kon | = | - | — | - |
| CHEMBL5794070 | — | k_off | = | - | s-1 | - |
| CHEMBL5951223 | — | IC50 | > | 1590.0 | nM | - |