Assay Detail
Binding
CHEMBL4768583
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human full-length N-terminal GST-fused CDK4 (1 to 303 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 | 7.98 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4778367 | — | — | 1 | 9.10 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 8.74 |
| CHEMBL4792101 | — | — | 1 | 8.66 |
| CHEMBL4794123 | — | — | 1 | 8.57 |
| CHEMBL4776781 | — | — | 1 | 8.57 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 8.49 |
| CHEMBL4785811 | — | — | 1 | 8.44 |
| CHEMBL4783539 | — | — | 1 | 8.43 |
| CHEMBL4779845 | — | — | 1 | 8.40 |
| CHEMBL4784940 | — | — | 1 | 8.38 |
| CHEMBL4780277 | — | — | 1 | 8.35 |
| CHEMBL4781009 | — | — | 1 | 8.33 |
| CHEMBL4782575 | — | — | 1 | 8.28 |
| CHEMBL4791259 | — | — | 1 | 8.00 |
| CHEMBL4785079 | — | — | 1 | 8.00 |
| CHEMBL4777368 | — | — | 1 | 7.99 |
| CHEMBL4781277 | — | — | 1 | 7.87 |
| CHEMBL4786042 | — | — | 1 | 7.72 |
| CHEMBL4787909 | — | — | 1 | 7.65 |
| CHEMBL4797327 | — | — | 1 | 7.58 |
| CHEMBL4792839 | — | — | 1 | 7.23 |
| CHEMBL4793422 | — | — | 1 | 7.00 |
| CHEMBL4788066 | — | — | 1 | 6.91 |
| CHEMBL4777250 | — | — | 1 | 6.57 |
| CHEMBL4787501 | — | — | 1 | 6.23 |
| CHEMBL4778835 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4778367 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4792101 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL4794123 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4776781 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL189963 | PALBOCICLIB | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL4785811 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL4783539 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4779845 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4784940 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4780277 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4781009 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4782575 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4791259 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4785079 | — | IC50 | = | 9.9 | nM | 8.00 |
| CHEMBL4777368 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL4781277 | — | IC50 | = | 13.5 | nM | 7.87 |
| CHEMBL4786042 | — | IC50 | = | 18.9 | nM | 7.72 |
| CHEMBL4787909 | — | IC50 | = | 22.3 | nM | 7.65 |
| CHEMBL4797327 | — | IC50 | = | 26.5 | nM | 7.58 |
| CHEMBL4792839 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4793422 | — | IC50 | = | 98.91 | nM | 7.00 |
| CHEMBL4788066 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL4777250 | — | IC50 | = | 270.9 | nM | 6.57 |
| CHEMBL4787501 | — | IC50 | = | 592.3 | nM | 6.23 |
| CHEMBL4778835 | — | IC50 | > | 3333.0 | nM | - |