Assay Detail
Binding
CHEMBL5259462
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Inhibition of recombinant human GSK3beta (636 to 661 residues) assessed as reduction in human muscle glycogen synthase type 1 fragment phosphorylation using YRRAAVPPSPSLSRHSSPHQ(pS)EDE as substrate in presence of ATP incubated for 60 mins by ADP-Glo kinase assay
20
Total Activities
20
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
3-Arylidene-2-oxindoles as GSK3β inhibitors and anti-thrombotic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 5.80 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5284455 | — | — | 1 | 8.38 |
| CHEMBL102714 | SB-216763 | — | 1 | 8.08 |
| CHEMBL5284219 | — | — | 1 | 6.81 |
| CHEMBL5276187 | — | — | 1 | 6.63 |
| CHEMBL5272429 | — | — | 1 | 6.46 |
| CHEMBL4440139 | — | — | 1 | 5.91 |
| CHEMBL5202388 | — | — | 1 | 5.76 |
| CHEMBL5274127 | — | — | 1 | 5.75 |
| CHEMBL5266960 | — | — | 1 | 5.36 |
| CHEMBL5289425 | — | — | 1 | 5.25 |
| CHEMBL5270462 | — | — | 1 | 5.17 |
| CHEMBL2347086 | — | — | 1 | 4.89 |
| CHEMBL5274095 | — | — | 1 | 4.87 |
| CHEMBL5266917 | — | — | 1 | 4.70 |
| CHEMBL5285483 | — | — | 1 | 4.46 |
| CHEMBL5185154 | — | — | 1 | 4.30 |
| CHEMBL5271237 | — | — | 1 | - |
| CHEMBL5280912 | — | — | 1 | - |
| CHEMBL5271795 | — | — | 1 | - |
| CHEMBL103307 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5284455 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL102714 | SB-216763 | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5284219 | — | IC50 | = | 155.0 | nM | 6.81 |
| CHEMBL5276187 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL5272429 | — | IC50 | = | 348.0 | nM | 6.46 |
| CHEMBL4440139 | — | IC50 | = | 1231.0 | nM | 5.91 |
| CHEMBL5202388 | — | IC50 | = | 1717.0 | nM | 5.76 |
| CHEMBL5274127 | — | IC50 | = | 1770.0 | nM | 5.75 |
| CHEMBL5266960 | — | IC50 | = | 4343.0 | nM | 5.36 |
| CHEMBL5289425 | — | IC50 | = | 5680.0 | nM | 5.25 |
| CHEMBL5270462 | — | IC50 | = | 6720.0 | nM | 5.17 |
| CHEMBL2347086 | — | IC50 | = | 12750.0 | nM | 4.89 |
| CHEMBL5274095 | — | IC50 | = | 13490.0 | nM | 4.87 |
| CHEMBL5266917 | — | IC50 | = | 20010.0 | nM | 4.70 |
| CHEMBL5285483 | — | IC50 | = | 34440.0 | nM | 4.46 |
| CHEMBL5185154 | — | IC50 | = | 50000.0 | nM | 4.30 |
| CHEMBL5271237 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5280912 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL5271795 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL103307 | — | IC50 | > | 50000.0 | nM | - |