Assay Detail
Binding
CHEMBL4253389
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Inhibition of CDK4/Cyclin-D1 (unknown origin) using histone-H1 as substrate after 90 mins by ADP-Glo assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Intermediate |
Target
Cyclin-dependent kinase 4/cyclin D1 (CHEMBL1907601) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 7.89 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4288327 | — | — | 1 | 8.52 |
| CHEMBL4277900 | CROZBACICLIB | 2.0 | 1 | 8.52 |
| CHEMBL4276993 | — | — | 1 | 8.40 |
| CHEMBL4284941 | — | — | 1 | 8.40 |
| CHEMBL4288165 | — | — | 1 | 8.22 |
| CHEMBL4281514 | — | — | 1 | 8.22 |
| CHEMBL4279791 | — | — | 1 | 8.10 |
| CHEMBL4277525 | — | — | 1 | 8.10 |
| CHEMBL4285830 | — | — | 1 | 8.10 |
| CHEMBL4292139 | — | — | 1 | 8.00 |
| CHEMBL4289350 | — | — | 1 | 7.92 |
| CHEMBL4284768 | — | — | 1 | 7.89 |
| CHEMBL4294940 | — | — | 1 | 7.82 |
| CHEMBL4284301 | — | — | 1 | 7.80 |
| CHEMBL4280895 | — | — | 1 | 7.80 |
| CHEMBL4287743 | — | — | 1 | 7.77 |
| CHEMBL4286100 | — | — | 1 | 7.75 |
| CHEMBL4279275 | — | — | 1 | 7.75 |
| CHEMBL4288134 | — | — | 1 | 7.55 |
| CHEMBL4282981 | — | — | 1 | 7.48 |
| CHEMBL4284737 | — | — | 1 | 7.46 |
| CHEMBL4289967 | — | — | 1 | 7.38 |
| CHEMBL4280423 | — | — | 1 | 7.36 |
| CHEMBL4283885 | — | — | 1 | 7.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4288327 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4277900 | CROZBACICLIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4276993 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4284941 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4288165 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4281514 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4279791 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4277525 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4285830 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4292139 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4289350 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4284768 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4294940 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4284301 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4280895 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4287743 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4286100 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4279275 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4288134 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4282981 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4284737 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4289967 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4280423 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4283885 | — | IC50 | = | 78.0 | nM | 7.11 |