Assay Detail
Binding
CHEMBL4701416
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged human CDK2/cyclin E1 expressed in insect cells using biotin Ttds-YISPLKSPYKISEG as substrate preincubated for 15 mins followed by ATP and substrate addition and measured after 25 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
Recent Developments in the Biology and Medicinal Chemistry of CDK9 Inhibitors: An Update.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.06 | 6.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4789982 | — | — | 1 | 6.25 |
| CHEMBL4756226 | — | — | 1 | 6.22 |
| CHEMBL4743691 | — | — | 1 | 5.97 |
| CHEMBL4742789 | — | — | 1 | 5.79 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4789982 | — | IC50 | = | 558.0 | nM | 6.25 |
| CHEMBL4756226 | — | IC50 | = | 608.0 | nM | 6.22 |
| CHEMBL4743691 | — | IC50 | = | 1078.0 | nM | 5.97 |
| CHEMBL4742789 | — | IC50 | = | 1608.0 | nM | 5.79 |