Assay Detail
Binding
CHEMBL4672956
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full length wild-type CDK2/Cyclin E1 (unknown origin) expressed in baculovirus expression system assessed as reduction in production of ADP using 5-FAM-QSPKKG-CONH2 peptide as substrate preincubated with enzyme for 15 mins followed by further incubation with ATP for 45 mins by fluorescence-based microfluidic mobility shift assay
6
Total Activities
6
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
Novel CDK2 Inhibitors for Treating Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 9.66 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4744945 | — | — | 1 | 10.00 |
| CHEMBL4764153 | — | — | 1 | 9.92 |
| CHEMBL4758192 | — | — | 1 | 9.82 |
| CHEMBL4758595 | — | — | 1 | 9.77 |
| CHEMBL4744114 | — | — | 1 | 9.34 |
| CHEMBL4763408 | — | — | 1 | 9.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4744945 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4764153 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL4758192 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL4758595 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL4744114 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL4763408 | — | Ki | = | 0.77 | nM | 9.11 |