Assay Detail
Binding
CHEMBL4387133
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human full length GST-tagged CDK4 (1 to 303(end) amino acids)/Cyclin D3 (1 to 292(end) amino acids) expressed in baculovirus expression system assessed as inhibition constant using Ulight-4E-BP1 as substrate preincubated for 30 mins followed by substrate addition and incubated for 90 mins by TR-FRET assay
20
Total Activities
20
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
Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 8.48 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4546255 | — | — | 1 | 9.40 |
| CHEMBL4560219 | — | — | 1 | 9.40 |
| CHEMBL4466797 | — | — | 1 | 9.10 |
| CHEMBL4539133 | — | — | 1 | 9.00 |
| CHEMBL4578267 | — | — | 1 | 9.00 |
| CHEMBL4520067 | — | — | 1 | 8.89 |
| CHEMBL4561999 | — | — | 1 | 8.85 |
| CHEMBL4588989 | — | — | 1 | 8.74 |
| CHEMBL4536835 | — | — | 1 | 8.57 |
| CHEMBL4569666 | — | — | 1 | 8.44 |
| CHEMBL4435669 | — | — | 1 | 8.42 |
| CHEMBL1272326 | — | — | 1 | 7.75 |
| CHEMBL4438971 | — | — | 1 | 7.70 |
| CHEMBL4447396 | — | — | 1 | 7.21 |
| CHEMBL4464950 | — | — | 1 | 6.68 |
| CHEMBL4440980 | — | — | 1 | - |
| CHEMBL4589135 | — | — | 1 | - |
| CHEMBL4564687 | — | — | 1 | - |
| CHEMBL4529532 | — | — | 1 | - |
| CHEMBL4545456 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4546255 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4560219 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4466797 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL4539133 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4578267 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4520067 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL4561999 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL4588989 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL4536835 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL4569666 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL4435669 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL1272326 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4438971 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4447396 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL4464950 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL4440980 | — | Ki | < | 0.3 | nM | - |
| CHEMBL4589135 | — | Ki | < | 0.3 | nM | - |
| CHEMBL4564687 | — | Ki | < | 0.3 | nM | - |
| CHEMBL4529532 | — | Ki | < | 0.3 | nM | - |
| CHEMBL4545456 | — | Ki | < | 0.3 | nM | - |