Assay Detail
Binding
CHEMBL4346816
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged CDK2/Cyclin E (unknown origin) expressed in baculovirus expression system using GST-pRb (776 to 928 residues) as substrate measured after 45 mins in presence of [gamma33P]-ATP by liquid scintillation counting method
7
Total Activities
7
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
Cyclin-Dependent Kinase 2 Inhibitors in Cancer Therapy: An Update.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.62 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2377864 | — | — | 1 | 9.05 |
| CHEMBL2377825 | — | — | 1 | 8.96 |
| CHEMBL129396 | — | — | 1 | 8.30 |
| CHEMBL310840 | — | — | 1 | 8.05 |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | 7.42 |
| CHEMBL4573345 | — | — | 1 | 6.77 |
| CHEMBL2377862 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2377864 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL2377825 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL129396 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL310840 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL296468 | BMS-387032 | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4573345 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL2377862 | — | IC50 | = | 15000.0 | nM | 4.82 |