Assay Detail
Binding
CHEMBL1002020
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Inhibition of GSK3-beta by scintillation proximity assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
Synthesis and evaluation of pyrazolo[1,5-b]pyridazines as selective cyclin dependent kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 6.47 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL526110 | — | — | 1 | 8.70 |
| CHEMBL359794 | — | — | 1 | 8.30 |
| CHEMBL188938 | — | — | 1 | 8.30 |
| CHEMBL497564 | — | — | 1 | 8.10 |
| CHEMBL495696 | GW778894X | — | 1 | 8.00 |
| CHEMBL359963 | GW805758X | — | 1 | 7.80 |
| CHEMBL468963 | GW779439X | — | 1 | 7.80 |
| CHEMBL495751 | — | — | 1 | 7.70 |
| CHEMBL523735 | — | — | 1 | 7.70 |
| CHEMBL359554 | — | — | 1 | 7.50 |
| CHEMBL524059 | — | — | 1 | 7.30 |
| CHEMBL513354 | — | — | 1 | 7.10 |
| CHEMBL495545 | — | — | 1 | 6.70 |
| CHEMBL521871 | — | — | 1 | 6.16 |
| CHEMBL496162 | — | — | 1 | 6.07 |
| CHEMBL525194 | — | — | 1 | 5.80 |
| CHEMBL496779 | — | — | 1 | 5.50 |
| CHEMBL513330 | GW781673X | — | 1 | 5.00 |
| CHEMBL445757 | — | — | 1 | 4.60 |
| CHEMBL497398 | — | — | 1 | 4.60 |
| CHEMBL497196 | — | — | 1 | 4.60 |
| CHEMBL495771 | GW708336X | — | 1 | 4.60 |
| CHEMBL496778 | — | — | 1 | 4.60 |
| CHEMBL523747 | — | — | 1 | 4.60 |
| CHEMBL524901 | GW683109X | — | 1 | 4.50 |
| CHEMBL446024 | GW683003X | — | 1 | - |
| CHEMBL495570 | — | — | 1 | - |
| CHEMBL503212 | — | — | 1 | - |
| CHEMBL522718 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL526110 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL359794 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL188938 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL497564 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL495696 | GW778894X | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL359963 | GW805758X | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL468963 | GW779439X | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL495751 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL523735 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL359554 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL524059 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL513354 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL495545 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL521871 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL496162 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL525194 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL496779 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL513330 | GW781673X | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL445757 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL497398 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL497196 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL495771 | GW708336X | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL496778 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL523747 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL524901 | GW683109X | IC50 | = | 32000.0 | nM | 4.50 |
| CHEMBL446024 | GW683003X | IC50 | > | 32000.0 | nM | - |
| CHEMBL495570 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL503212 | — | IC50 | > | 32000.0 | nM | - |
| CHEMBL522718 | — | IC50 | > | 25000.0 | nM | - |