Assay Detail
Binding
CHEMBL4305804
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full length N-terminal GST-tagged CDK4 (1 to 303 residues)/cyclin D3 (1 to 292 residues) expressed in baculovirus expression system using eIF4E-binding protein 1 peptide and ATP as substrate incubated for 30 mins by LANCE ultra kinase assay
22
Total Activities
22
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 |
Publication
Discovery of 6-(2-(dimethylamino)ethyl)-N-(5-fluoro-4-(4-fluoro-1-isopropyl-2-methyl-1H-benzo[d]imidazole-6-yl)pyrimidin-2-yl)-5,6,7,8-tetrahydro-1,6-naphthyridin-2-amine as a highly potent cyclin-dependent kinase 4/6 inhibitor for treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 8.74 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4448494 | — | — | 1 | 9.15 |
| CHEMBL4550287 | — | — | 1 | 9.02 |
| CHEMBL4463172 | — | — | 1 | 9.00 |
| CHEMBL4438059 | — | — | 1 | 8.99 |
| CHEMBL4446626 | — | — | 1 | 8.98 |
| CHEMBL4462493 | — | — | 1 | 8.97 |
| CHEMBL4439999 | — | — | 1 | 8.87 |
| CHEMBL4463716 | — | — | 1 | 8.87 |
| CHEMBL4463874 | — | — | 1 | 8.82 |
| CHEMBL4461442 | — | — | 1 | 8.81 |
| CHEMBL4466497 | — | — | 1 | 8.80 |
| CHEMBL4453095 | — | — | 1 | 8.79 |
| CHEMBL4449998 | — | — | 1 | 8.79 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 8.74 |
| CHEMBL4542247 | — | — | 1 | 8.73 |
| CHEMBL4455210 | — | — | 1 | 8.71 |
| CHEMBL4438497 | — | — | 1 | 8.70 |
| CHEMBL4445727 | — | — | 1 | 8.63 |
| CHEMBL4593340 | — | — | 1 | 8.51 |
| CHEMBL4458266 | — | — | 1 | 8.37 |
| CHEMBL4525034 | — | — | 1 | 8.32 |
| CHEMBL4461579 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4448494 | — | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL4550287 | — | IC50 | = | 0.96 | nM | 9.02 |
| CHEMBL4463172 | — | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL4438059 | — | IC50 | = | 1.02 | nM | 8.99 |
| CHEMBL4446626 | — | IC50 | = | 1.04 | nM | 8.98 |
| CHEMBL4462493 | — | IC50 | = | 1.08 | nM | 8.97 |
| CHEMBL4439999 | — | IC50 | = | 1.35 | nM | 8.87 |
| CHEMBL4463716 | — | IC50 | = | 1.34 | nM | 8.87 |
| CHEMBL4463874 | — | IC50 | = | 1.52 | nM | 8.82 |
| CHEMBL4461442 | — | IC50 | = | 1.56 | nM | 8.81 |
| CHEMBL4466497 | — | IC50 | = | 1.58 | nM | 8.80 |
| CHEMBL4453095 | — | IC50 | = | 1.61 | nM | 8.79 |
| CHEMBL4449998 | — | IC50 | = | 1.63 | nM | 8.79 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 1.82 | nM | 8.74 |
| CHEMBL4542247 | — | IC50 | = | 1.84 | nM | 8.73 |
| CHEMBL4455210 | — | IC50 | = | 1.94 | nM | 8.71 |
| CHEMBL4438497 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4445727 | — | IC50 | = | 2.35 | nM | 8.63 |
| CHEMBL4593340 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL4458266 | — | IC50 | = | 4.26 | nM | 8.37 |
| CHEMBL4525034 | — | IC50 | = | 4.83 | nM | 8.32 |
| CHEMBL4461579 | — | IC50 | = | 17.7 | nM | 7.75 |