Assay Detail
Binding
CHEMBL5735704
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Assay: The GSK3β kinase assay is run using the Ser/Thr 09 peptide Z-lyte assay kit according to manufacturer's instructions (Life Technologiesa Division of Thermo-Fisher). This is a non-radioactive assay using fluorescence resonance energy transfer (FRET) between coumarin and fluorescein to detect kinase activity which is represented as ratio of coumarin emission/fluorescein emission.Briefly, recombinant GSK3β kinase, ATP and Ser/Thr peptide 09 are prepared in 1× Kinase buffer to final concentrations of 0.04 μg/mL, 46 μM, and 4 μM respectively. The mixture is allowed to incubate with the representative compounds for one hour at room temperature. All reactions were performed in duplicate. Unphosphorylated (0% Control) and phosphorylated (100% control) forms of Ser/Thr 18 serve as control reactions.
60
Total Activities
20
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Indazole containing macrocycles and therapeutic uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 8.00 | 9.00 |
| kon | 20 | - | - |
| k_off | 20 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4753134 | — | — | 3 | 9.00 |
| CHEMBL6017092 | — | — | 3 | 9.00 |
| CHEMBL4793171 | — | — | 3 | 9.00 |
| CHEMBL4800405 | — | — | 3 | 9.00 |
| CHEMBL5817701 | — | — | 3 | 9.00 |
| CHEMBL5883206 | — | — | 3 | 8.70 |
| CHEMBL6008507 | — | — | 3 | 8.40 |
| CHEMBL5741545 | — | — | 3 | 8.40 |
| CHEMBL5904061 | — | — | 3 | 8.15 |
| CHEMBL5849395 | — | — | 3 | 8.00 |
| CHEMBL4784103 | — | — | 3 | 8.00 |
| CHEMBL5910539 | — | — | 3 | 7.96 |
| CHEMBL5866506 | — | — | 3 | 7.85 |
| CHEMBL5856883 | — | — | 3 | 7.82 |
| CHEMBL5914291 | — | — | 3 | 7.32 |
| CHEMBL5956615 | — | — | 3 | 7.21 |
| CHEMBL6010383 | — | — | 3 | 7.06 |
| CHEMBL5969993 | — | — | 3 | 6.31 |
| CHEMBL5817298 | — | — | 3 | 5.73 |
| CHEMBL5902231 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6017092 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4800405 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4793171 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4753134 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5817701 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5883206 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5741545 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL6008507 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5904061 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5849395 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4784103 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5910539 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5866506 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5856883 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5914291 | — | EC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5956615 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL6010383 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5969993 | — | EC50 | = | 494.0 | nM | 6.31 |
| CHEMBL5817298 | — | EC50 | = | 1866.0 | nM | 5.73 |
| CHEMBL5902231 | — | kon | = | - | — | - |
| CHEMBL5856883 | — | k_off | = | - | s-1 | - |
| CHEMBL6008507 | — | k_off | = | - | s-1 | - |
| CHEMBL6008507 | — | kon | = | - | — | - |
| CHEMBL5914291 | — | k_off | = | - | s-1 | - |
| CHEMBL5914291 | — | kon | = | - | — | - |
| CHEMBL5969993 | — | k_off | = | - | s-1 | - |
| CHEMBL5969993 | — | kon | = | - | — | - |
| CHEMBL4753134 | — | k_off | = | - | s-1 | - |
| CHEMBL4753134 | — | kon | = | - | — | - |
| CHEMBL5817701 | — | k_off | = | - | s-1 | - |
| CHEMBL5817701 | — | kon | = | - | — | - |
| CHEMBL5904061 | — | k_off | = | - | s-1 | - |
| CHEMBL5904061 | — | kon | = | - | — | - |
| CHEMBL5902231 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5866506 | — | k_off | = | - | s-1 | - |
| CHEMBL5866506 | — | kon | = | - | — | - |
| CHEMBL6010383 | — | k_off | = | - | s-1 | - |
| CHEMBL6010383 | — | kon | = | - | — | - |
| CHEMBL5817298 | — | k_off | = | - | s-1 | - |
| CHEMBL5817298 | — | kon | = | - | — | - |
| CHEMBL4784103 | — | kon | = | - | — | - |
| CHEMBL5883206 | — | kon | = | - | — | - |
| CHEMBL4784103 | — | k_off | = | - | s-1 | - |
| CHEMBL5956615 | — | k_off | = | - | s-1 | - |
| CHEMBL6017092 | — | k_off | = | - | s-1 | - |
| CHEMBL4800405 | — | kon | = | - | — | - |
| CHEMBL6017092 | — | kon | = | - | — | - |
| CHEMBL5956615 | — | kon | = | - | — | - |
| CHEMBL4800405 | — | k_off | = | - | s-1 | - |
| CHEMBL5883206 | — | k_off | = | - | s-1 | - |