Assay Detail
Binding
CHEMBL871040
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Inhibition of Cdk4/Cyclin D1
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Cyclin-dependent kinase 4/cyclin D1 (CHEMBL1907601) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
CA224, a non-planar analogue of fascaplysin, inhibits Cdk4 but not Cdk2 and arrests cells at G0/G1 inhibiting pRB phosphorylation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 4.41 | 6.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL211632 | — | — | 1 | 6.39 |
| CHEMBL213805 | — | — | 1 | 5.21 |
| CHEMBL378617 | — | — | 1 | 4.43 |
| CHEMBL213302 | — | — | 1 | 4.42 |
| CHEMBL209433 | — | — | 1 | 4.34 |
| CHEMBL209467 | — | — | 1 | 4.31 |
| CHEMBL213449 | — | — | 1 | 4.23 |
| CHEMBL377131 | — | — | 1 | 4.20 |
| CHEMBL209972 | — | — | 1 | 4.13 |
| CHEMBL376003 | — | — | 1 | 4.11 |
| CHEMBL213036 | — | — | 1 | 4.10 |
| CHEMBL213032 | — | — | 1 | 4.09 |
| CHEMBL211622 | — | — | 1 | 4.06 |
| CHEMBL212768 | — | — | 1 | 4.06 |
| CHEMBL211636 | — | — | 1 | 4.02 |
| CHEMBL214188 | — | — | 1 | - |
| CHEMBL214008 | — | — | 1 | - |
| CHEMBL374207 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL211632 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL213805 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL378617 | — | IC50 | = | 37000.0 | nM | 4.43 |
| CHEMBL213302 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL209433 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL209467 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL213449 | — | IC50 | = | 59000.0 | nM | 4.23 |
| CHEMBL377131 | — | IC50 | = | 63000.0 | nM | 4.20 |
| CHEMBL209972 | — | IC50 | = | 74000.0 | nM | 4.13 |
| CHEMBL376003 | — | IC50 | = | 78000.0 | nM | 4.11 |
| CHEMBL213036 | — | IC50 | = | 79000.0 | nM | 4.10 |
| CHEMBL213032 | — | IC50 | = | 81000.0 | nM | 4.09 |
| CHEMBL211622 | — | IC50 | = | 88000.0 | nM | 4.06 |
| CHEMBL212768 | — | IC50 | = | 88000.0 | nM | 4.06 |
| CHEMBL211636 | — | IC50 | = | 95000.0 | nM | 4.02 |
| CHEMBL214188 | — | IC50 | = | 109000.0 | nM | - |
| CHEMBL214008 | — | IC50 | = | 113000.0 | nM | - |
| CHEMBL374207 | — | IC50 | = | 103000.0 | nM | - |