Assay Detail
Binding
CHEMBL928295
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Inhibition of GSK3alpha/beta in pig brain
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
9-cyano-1-azapaullone (cazpaullone), a glycogen synthase kinase-3 (GSK-3) inhibitor activating pancreatic beta cell protection and replication.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 6.73 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL50894 | ALSTERPAULLONE | — | 1 | 8.40 |
| CHEMBL259638 | CAZPAULLONE | — | 1 | 8.10 |
| CHEMBL411728 | — | — | 1 | 8.10 |
| CHEMBL260119 | — | — | 1 | 7.89 |
| CHEMBL336961 | AZAKENPAULLONE | — | 1 | 7.75 |
| CHEMBL260045 | — | — | 1 | 7.75 |
| CHEMBL260136 | — | — | 1 | 7.68 |
| CHEMBL296586 | KENPAULLONE | — | 1 | 7.64 |
| CHEMBL260487 | — | — | 1 | 7.60 |
| CHEMBL264177 | — | — | 1 | 7.55 |
| CHEMBL260657 | — | — | 1 | 7.29 |
| CHEMBL406619 | — | — | 1 | 7.28 |
| CHEMBL406748 | — | — | 1 | 7.20 |
| CHEMBL261470 | — | — | 1 | 7.10 |
| CHEMBL258482 | — | — | 1 | 6.92 |
| CHEMBL409492 | — | — | 1 | 6.89 |
| CHEMBL407408 | — | — | 1 | 6.41 |
| CHEMBL411641 | — | — | 1 | 6.40 |
| CHEMBL259697 | — | — | 1 | 6.39 |
| CHEMBL260428 | — | — | 1 | 6.39 |
| CHEMBL411133 | — | — | 1 | 6.10 |
| CHEMBL258700 | — | — | 1 | 6.10 |
| CHEMBL260678 | — | — | 1 | 6.10 |
| CHEMBL260679 | — | — | 1 | 6.10 |
| CHEMBL260656 | — | — | 1 | 6.00 |
| CHEMBL261252 | — | — | 1 | 5.85 |
| CHEMBL407413 | — | — | 1 | 5.75 |
| CHEMBL429329 | — | — | 1 | 5.68 |
| CHEMBL413294 | — | — | 1 | 5.42 |
| CHEMBL412255 | — | — | 1 | 4.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL50894 | ALSTERPAULLONE | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL259638 | CAZPAULLONE | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL411728 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL260119 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL336961 | AZAKENPAULLONE | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL260045 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL260136 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL296586 | KENPAULLONE | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL260487 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL264177 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL260657 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL406619 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL406748 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL261470 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL258482 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL409492 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL407408 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL411641 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL260428 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL259697 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL411133 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL258700 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL260678 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL260679 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL260656 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL261252 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL407413 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL429329 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL413294 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL412255 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL261025 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL410936 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL441733 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL264179 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL411642 | — | IC50 | > | 10000.0 | nM | - |