Assay Detail
Binding
CHEMBL666089
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Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 by measuring the phosphorylation of RbING
15
Total Activities
15
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 4/cyclin D1 (CHEMBL1907601) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Aryl[a]pyrrolo[3,4-c]carbazoles as selective cyclin D1-CDK4 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.50 | 7.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL332575 | — | — | 1 | 7.35 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.23 |
| CHEMBL268368 | STAUROSPORINE AGLYCON | — | 1 | 6.85 |
| CHEMBL127532 | — | — | 1 | 6.82 |
| CHEMBL340685 | — | — | 1 | 6.75 |
| CHEMBL126545 | — | — | 1 | 6.66 |
| CHEMBL338264 | — | — | 1 | 6.60 |
| CHEMBL421087 | — | — | 1 | 6.58 |
| CHEMBL125627 | — | — | 1 | 6.39 |
| CHEMBL338289 | — | — | 1 | 6.37 |
| CHEMBL240747 | GRANULATIMIDE | — | 1 | 6.13 |
| CHEMBL16958 | STAUROSPORINONE | — | 1 | 6.08 |
| CHEMBL126447 | — | — | 1 | 5.74 |
| CHEMBL127277 | — | — | 1 | 5.42 |
| CHEMBL341503 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL332575 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL388978 | STAUROSPORINE | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL268368 | STAUROSPORINE AGLYCON | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL127532 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL340685 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL126545 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL338264 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL421087 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL125627 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL338289 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL240747 | GRANULATIMIDE | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL16958 | STAUROSPORINONE | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL126447 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL127277 | — | IC50 | = | 3830.0 | nM | 5.42 |
| CHEMBL341503 | — | IC50 | > | 10000.0 | nM | - |