Assay Detail
Binding
CHEMBL4387134
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Inhibition of human full length GST-tagged CDK6 (1 to 326(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 | 7.57 | 8.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4564687 | — | — | 1 | 8.80 |
| CHEMBL4589135 | — | — | 1 | 8.77 |
| CHEMBL4545456 | — | — | 1 | 8.66 |
| CHEMBL4529532 | — | — | 1 | 8.48 |
| CHEMBL4560219 | — | — | 1 | 8.37 |
| CHEMBL4440980 | — | — | 1 | 8.31 |
| CHEMBL4546255 | — | — | 1 | 8.10 |
| CHEMBL4539133 | — | — | 1 | 8.00 |
| CHEMBL4466797 | — | — | 1 | 7.75 |
| CHEMBL4561999 | — | — | 1 | 7.72 |
| CHEMBL4578267 | — | — | 1 | 7.68 |
| CHEMBL4588989 | — | — | 1 | 7.62 |
| CHEMBL4536835 | — | — | 1 | 7.50 |
| CHEMBL4520067 | — | — | 1 | 7.43 |
| CHEMBL4435669 | — | — | 1 | 7.42 |
| CHEMBL4569666 | — | — | 1 | 7.40 |
| CHEMBL1272326 | — | — | 1 | 6.35 |
| CHEMBL4438971 | — | — | 1 | 6.14 |
| CHEMBL4447396 | — | — | 1 | 5.72 |
| CHEMBL4464950 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4564687 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL4589135 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL4545456 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL4529532 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL4560219 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL4440980 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL4546255 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL4539133 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4466797 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL4561999 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL4578267 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4588989 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL4536835 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4520067 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL4435669 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4569666 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL1272326 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL4438971 | — | Ki | = | 720.0 | nM | 6.14 |
| CHEMBL4447396 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL4464950 | — | Ki | = | 7400.0 | nM | 5.13 |