Assay Detail
Binding
CHEMBL928296
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Inhibition of recombinant CDK5/p25 expressed in Escherichia coli
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Cyclin-dependent kinase 5/CDK5 activator 1 (CHEMBL1907600) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 | 5.84 | 7.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL260136 | — | — | 1 | 7.50 |
| CHEMBL50894 | ALSTERPAULLONE | — | 1 | 7.40 |
| CHEMBL260119 | — | — | 1 | 6.92 |
| CHEMBL406619 | — | — | 1 | 6.75 |
| CHEMBL260045 | — | — | 1 | 6.68 |
| CHEMBL260657 | — | — | 1 | 6.58 |
| CHEMBL259638 | CAZPAULLONE | — | 1 | 6.52 |
| CHEMBL407408 | — | — | 1 | 6.40 |
| CHEMBL264177 | — | — | 1 | 6.14 |
| CHEMBL296586 | KENPAULLONE | — | 1 | 6.07 |
| CHEMBL258482 | — | — | 1 | 5.70 |
| CHEMBL260656 | — | — | 1 | 5.52 |
| CHEMBL261470 | — | — | 1 | 5.52 |
| CHEMBL258700 | — | — | 1 | 5.40 |
| CHEMBL336961 | AZAKENPAULLONE | — | 1 | 5.38 |
| CHEMBL261252 | — | — | 1 | 5.30 |
| CHEMBL260487 | — | — | 1 | 5.22 |
| CHEMBL260678 | — | — | 1 | 5.05 |
| CHEMBL413294 | — | — | 1 | 5.00 |
| CHEMBL411728 | — | — | 1 | 5.00 |
| CHEMBL261025 | — | — | 1 | 4.52 |
| CHEMBL260679 | — | — | 1 | 4.00 |
| CHEMBL406748 | — | — | 1 | - |
| CHEMBL407413 | — | — | 1 | - |
| CHEMBL409492 | — | — | 1 | - |
| CHEMBL264179 | — | — | 1 | - |
| CHEMBL441733 | — | — | 1 | - |
| CHEMBL410936 | — | — | 1 | - |
| CHEMBL260428 | — | — | 1 | - |
| CHEMBL411133 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL260136 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL50894 | ALSTERPAULLONE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL260119 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL406619 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL260045 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL260657 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL259638 | CAZPAULLONE | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL407408 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL264177 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL296586 | KENPAULLONE | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL258482 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL260656 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL261470 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL258700 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL336961 | AZAKENPAULLONE | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL261252 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL260487 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL260678 | — | IC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL411728 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL413294 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL261025 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL260679 | — | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL412255 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL429329 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL411642 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL259697 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL411641 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL411133 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL260428 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL410936 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL441733 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL264179 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL409492 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL407413 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL406748 | — | IC50 | > | 10000.0 | nM | - |