Assay Detail
Binding
CHEMBL4768584
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human full-length N-terminal GST tagged CDK6 (1 to 326 residues)/GST-tagged cyclinD3 (1 to 292 residues) expressed in baculovirus expression system using ULight-elF4E-binding protein 1 peptide as substrate measured after 30 mins by LANCE assay
26
Total Activities
26
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 a novel series of imidazo[1',2':1,6]pyrido[2,3-d]pyrimidin derivatives as potent cyclin-dependent kinase 4/6 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.70 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4778367 | — | — | 1 | 8.70 |
| CHEMBL4792101 | — | — | 1 | 8.60 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 8.49 |
| CHEMBL4783539 | — | — | 1 | 8.43 |
| CHEMBL4779845 | — | — | 1 | 8.42 |
| CHEMBL4780277 | — | — | 1 | 8.37 |
| CHEMBL4776781 | — | — | 1 | 8.32 |
| CHEMBL4784940 | — | — | 1 | 8.29 |
| CHEMBL4782575 | — | — | 1 | 8.25 |
| CHEMBL4781009 | — | — | 1 | 8.23 |
| CHEMBL4794123 | — | — | 1 | 8.15 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 8.14 |
| CHEMBL4777368 | — | — | 1 | 8.05 |
| CHEMBL4785811 | — | — | 1 | 7.99 |
| CHEMBL4786042 | — | — | 1 | 7.65 |
| CHEMBL4791259 | — | — | 1 | 7.64 |
| CHEMBL4785079 | — | — | 1 | 7.59 |
| CHEMBL4781277 | — | — | 1 | 7.48 |
| CHEMBL4797327 | — | — | 1 | 7.47 |
| CHEMBL4787909 | — | — | 1 | 7.06 |
| CHEMBL4788066 | — | — | 1 | 6.96 |
| CHEMBL4793422 | — | — | 1 | 6.95 |
| CHEMBL4792839 | — | — | 1 | 6.82 |
| CHEMBL4777250 | — | — | 1 | 6.55 |
| CHEMBL4778835 | — | — | 1 | 6.03 |
| CHEMBL4787501 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4778367 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4792101 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL189963 | PALBOCICLIB | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4783539 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4779845 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4780277 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4776781 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL4784940 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4782575 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4781009 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL4794123 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4777368 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4785811 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL4786042 | — | IC50 | = | 22.2 | nM | 7.65 |
| CHEMBL4791259 | — | IC50 | = | 23.1 | nM | 7.64 |
| CHEMBL4785079 | — | IC50 | = | 25.7 | nM | 7.59 |
| CHEMBL4781277 | — | IC50 | = | 32.8 | nM | 7.48 |
| CHEMBL4797327 | — | IC50 | = | 33.6 | nM | 7.47 |
| CHEMBL4787909 | — | IC50 | = | 86.6 | nM | 7.06 |
| CHEMBL4788066 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4793422 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4792839 | — | IC50 | = | 150.3 | nM | 6.82 |
| CHEMBL4777250 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4778835 | — | IC50 | = | 923.8 | nM | 6.03 |
| CHEMBL4787501 | — | IC50 | = | 3090.0 | nM | 5.51 |