Assay Detail
Binding
CHEMBL663524
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Inhibitory activity against Cyclin-dependent kinase 2-cyclin E using Rb21 as substrate
9
Total Activities
9
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 2/cyclin E (CHEMBL2094126) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Synthesis, structure-activity relationship, and biological studies of indolocarbazoles as potent cyclin D1-CDK4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.19 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL293157 | — | — | 1 | 6.85 |
| CHEMBL62253 | — | — | 1 | 6.84 |
| CHEMBL59785 | — | — | 1 | 6.66 |
| CHEMBL291402 | — | — | 1 | 6.56 |
| CHEMBL268368 | STAUROSPORINE AGLYCON | — | 1 | 6.28 |
| CHEMBL64758 | — | — | 1 | 6.28 |
| CHEMBL60564 | — | — | 1 | 5.37 |
| CHEMBL432715 | — | — | 1 | 4.71 |
| CHEMBL293898 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL293157 | — | IC50 | = | 141.0 | nM | 6.85 |
| CHEMBL62253 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL59785 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL291402 | — | IC50 | = | 278.0 | nM | 6.56 |
| CHEMBL268368 | STAUROSPORINE AGLYCON | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL64758 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL60564 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL432715 | — | IC50 | = | 19400.0 | nM | 4.71 |
| CHEMBL293898 | — | IC50 | = | - | nM | - |