Assay Detail
Binding
CHEMBL5036864
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human GSK-3beta using GS-2 peptide as substrate incubated for 30 mins in presence of ATP by kinase-glo luminescence assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 5.20 | 5.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL284861 | — | — | 1 | 5.85 |
| CHEMBL5083185 | — | — | 1 | 5.60 |
| CHEMBL5086342 | — | — | 1 | 5.55 |
| CHEMBL5092483 | — | — | 1 | 5.40 |
| CHEMBL5083742 | — | — | 1 | 5.32 |
| CHEMBL5085162 | — | — | 1 | 5.31 |
| CHEMBL5084565 | — | — | 1 | 5.24 |
| CHEMBL5073147 | — | — | 1 | 5.22 |
| CHEMBL5091334 | — | — | 1 | 5.21 |
| CHEMBL5092006 | — | — | 1 | 5.21 |
| CHEMBL5089459 | — | — | 1 | 5.19 |
| CHEMBL5079142 | — | — | 1 | 5.18 |
| CHEMBL5071369 | — | — | 1 | 5.18 |
| CHEMBL5088760 | — | — | 1 | 5.17 |
| CHEMBL5091647 | — | — | 1 | 5.12 |
| CHEMBL5089457 | — | — | 1 | 4.82 |
| CHEMBL5091900 | — | — | 1 | 4.82 |
| CHEMBL5091798 | — | — | 1 | 4.77 |
| CHEMBL5083481 | — | — | 1 | 4.70 |
| CHEMBL5084361 | — | — | 1 | - |
| CHEMBL5078092 | — | — | 1 | - |
| CHEMBL5086219 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL284861 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5083185 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5086342 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL5092483 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL5083742 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL5085162 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL5084565 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL5073147 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL5091334 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL5092006 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL5089459 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL5079142 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL5071369 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL5088760 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL5091647 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL5089457 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL5091900 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL5091798 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL5083481 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL5084361 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5078092 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5086219 | — | IC50 | > | 100000.0 | nM | - |