Assay Detail
Binding
CHEMBL4197032
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human CDK4/cyclin D1 using ULight-substrate after 1 hr by LANCE assay
29
Total Activities
29
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/G1/S-specific cyclin-E1 (CHEMBL3885554) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Design, synthesis and biological evaluation of tetrahydronaphthyridine derivatives as bioavailable CDK4/6 inhibitors for cancer therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 8.50 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4210422 | — | — | 1 | 9.00 |
| CHEMBL4207521 | — | — | 1 | 8.92 |
| CHEMBL4203179 | — | — | 1 | 8.85 |
| CHEMBL4213744 | — | — | 1 | 8.85 |
| CHEMBL4214827 | — | — | 1 | 8.82 |
| CHEMBL4208813 | — | — | 1 | 8.82 |
| CHEMBL4206061 | — | — | 1 | 8.80 |
| CHEMBL4202644 | — | — | 1 | 8.74 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 8.70 |
| CHEMBL4204986 | — | — | 1 | 8.70 |
| CHEMBL4210299 | — | — | 1 | 8.68 |
| CHEMBL4212540 | — | — | 1 | 8.68 |
| CHEMBL4212532 | — | — | 1 | 8.66 |
| CHEMBL4205132 | — | — | 1 | 8.64 |
| CHEMBL4210944 | — | — | 1 | 8.60 |
| CHEMBL4216664 | — | — | 1 | 8.55 |
| CHEMBL4213778 | — | — | 1 | 8.51 |
| CHEMBL4213756 | — | — | 1 | 8.49 |
| CHEMBL4213219 | — | — | 1 | 8.44 |
| CHEMBL4202467 | — | — | 1 | 8.42 |
| CHEMBL4218588 | — | — | 1 | 8.28 |
| CHEMBL4214156 | — | — | 1 | 8.19 |
| CHEMBL4217628 | — | — | 1 | 8.17 |
| CHEMBL4205920 | — | — | 1 | 8.11 |
| CHEMBL4209352 | — | — | 1 | 8.08 |
| CHEMBL4203758 | — | — | 1 | 8.08 |
| CHEMBL4204483 | — | — | 1 | 8.01 |
| CHEMBL4207796 | — | — | 1 | 8.00 |
| CHEMBL4210282 | — | — | 1 | 7.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4210422 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4207521 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4203179 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4213744 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4214827 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4208813 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4206061 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4202644 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4204986 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4210299 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4212540 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4212532 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4205132 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4210944 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4216664 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4213778 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4213756 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4213219 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4202467 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4218588 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL4214156 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4217628 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL4205920 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL4209352 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4203758 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL4204483 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL4207796 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4210282 | — | IC50 | = | 16.8 | nM | 7.78 |