Assay Detail
Binding
CHEMBL4387137
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human full length GST-tagged CDK2 (1 to 298(end) amino acids)/Cyclin E1 (1 to 410(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
4
Total Activities
4
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 |
Target
Cyclin-dependent kinase 2/cyclin E1 (CHEMBL1907605) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 6.03 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1272326 | — | — | 1 | 7.66 |
| CHEMBL4438971 | — | — | 1 | 6.50 |
| CHEMBL4464950 | — | — | 1 | 5.12 |
| CHEMBL4447396 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1272326 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4438971 | — | Ki | = | 320.0 | nM | 6.50 |
| CHEMBL4464950 | — | Ki | = | 7500.0 | nM | 5.12 |
| CHEMBL4447396 | — | Ki | = | 15000.0 | nM | 4.82 |