Assay Detail
Binding
CHEMBL4679832
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full length wild-type phosphorylated 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
14
Total Activities
14
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
Potential of Cyclin-Dependent Kinase Inhibitors as Cancer Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 9.34 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4750658 | — | — | 1 | 10.05 |
| CHEMBL4797526 | — | — | 1 | 10.00 |
| CHEMBL4748471 | — | — | 1 | 9.92 |
| CHEMBL4446357 | EBVACICLIB | 2.0 | 1 | 9.92 |
| CHEMBL4745424 | — | — | 1 | 9.80 |
| CHEMBL4798327 | — | — | 1 | 9.70 |
| CHEMBL4752291 | — | — | 1 | 9.70 |
| CHEMBL4747638 | — | — | 1 | 9.60 |
| CHEMBL4757341 | — | — | 1 | 9.55 |
| CHEMBL4753883 | — | — | 1 | 9.54 |
| CHEMBL4796501 | — | — | 1 | 8.85 |
| CHEMBL4800105 | — | — | 1 | 8.76 |
| CHEMBL4763871 | — | — | 1 | 8.13 |
| CHEMBL4755392 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4750658 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL4797526 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4748471 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL4446357 | EBVACICLIB | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL4745424 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL4798327 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4752291 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL4747638 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL4757341 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL4753883 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL4796501 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL4800105 | — | Ki | = | 1.73 | nM | 8.76 |
| CHEMBL4763871 | — | Ki | = | 7.32 | nM | 8.13 |
| CHEMBL4755392 | — | Ki | = | 63.24 | nM | 7.20 |