Assay Detail
Binding
CHEMBL4386149
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full-length N-terminal GST-His6 fused CDK5 (M1 to P292 residues)/N-terminal His6-tagged p25 (A104 to R307 residues) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Cyclin-dependent kinase 5/CDK5 activator 1 (CHEMBL1907600) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.21 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4540226 | — | — | 1 | 7.82 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 7.17 |
| CHEMBL518800 | — | — | 1 | 6.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4540226 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2103840 | DINACICLIB | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL518800 | — | IC50 | = | 225.0 | nM | 6.65 |