Assay Detail
Binding
CHEMBL4709752
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant GST-tagged human CDK2/GST-tagged cyclin E expressed in sf9 cells using biotinylated peptide biotin-Ttds-YISPLKSPYKISEG as substrate preincubated for 15 mins followed by ATP and substrate addition and measured after 25 mins by TR-FRET assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Cyclin-dependent kinase 2/cyclin E1 (CHEMBL1907605) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.57 | 5.97 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4743691 | — | — | 1 | 5.97 |
| CHEMBL4439321 | ATUVECICLIB | 1.0 | 1 | 5.96 |
| CHEMBL4762845 | — | — | 1 | 5.54 |
| CHEMBL3962241 | — | — | 1 | 5.40 |
| CHEMBL4793497 | — | — | 1 | 4.98 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4743691 | — | IC50 | = | 1078.0 | nM | 5.97 |
| CHEMBL4439321 | ATUVECICLIB | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4762845 | — | IC50 | = | 2920.0 | nM | 5.54 |
| CHEMBL3962241 | — | IC50 | = | 3959.0 | nM | 5.40 |
| CHEMBL4793497 | — | IC50 | = | 10504.0 | nM | 4.98 |