Assay Detail
Binding
CHEMBL4180810
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CDK2/cyclin E (unknown origin) expressed in baculovirus infected insect Sf9 cells using histone H1 as substrate in presence of [gamma-33P]ATP
25
Total Activities
25
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 | Intermediate |
Target
Cyclin-dependent kinase 2/cyclin E1 (CHEMBL1907605) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Trisubstituted purine inhibitors of PDGFRα and their antileukemic activity in the human eosinophilic cell line EOL-1.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.28 | 7.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL367625 | — | — | 1 | 7.77 |
| CHEMBL4209971 | — | — | 1 | 6.93 |
| CHEMBL4207053 | — | — | 1 | 6.88 |
| CHEMBL4202703 | — | — | 1 | 6.87 |
| CHEMBL4218867 | — | — | 1 | 6.68 |
| CHEMBL4207048 | — | — | 1 | 6.64 |
| CHEMBL4210919 | — | — | 1 | 6.56 |
| CHEMBL4205769 | — | — | 1 | 6.51 |
| CHEMBL4218356 | — | — | 1 | 6.50 |
| CHEMBL4215315 | — | — | 1 | 6.36 |
| CHEMBL4214362 | — | — | 1 | 6.36 |
| CHEMBL4214422 | — | — | 1 | 6.31 |
| CHEMBL4206527 | — | — | 1 | 6.31 |
| CHEMBL4218779 | — | — | 1 | 6.30 |
| CHEMBL4205604 | — | — | 1 | 6.29 |
| CHEMBL4210474 | — | — | 1 | 6.20 |
| CHEMBL4209694 | — | — | 1 | 6.17 |
| CHEMBL4211413 | — | — | 1 | 6.01 |
| CHEMBL4216607 | — | — | 1 | 6.01 |
| CHEMBL4210897 | — | — | 1 | 5.84 |
| CHEMBL4218942 | — | — | 1 | 5.55 |
| CHEMBL4214781 | — | — | 1 | 5.26 |
| CHEMBL4207999 | — | — | 1 | 5.22 |
| CHEMBL4203120 | — | — | 1 | 5.14 |
| CHEMBL554 | LAPATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL367625 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4209971 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL4207053 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4202703 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4218867 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL4207048 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL4210919 | — | IC50 | = | 275.0 | nM | 6.56 |
| CHEMBL4205769 | — | IC50 | = | 306.0 | nM | 6.51 |
| CHEMBL4218356 | — | IC50 | = | 319.0 | nM | 6.50 |
| CHEMBL4215315 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL4214362 | — | IC50 | = | 433.0 | nM | 6.36 |
| CHEMBL4214422 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL4206527 | — | IC50 | = | 485.0 | nM | 6.31 |
| CHEMBL4218779 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4205604 | — | IC50 | = | 513.0 | nM | 6.29 |
| CHEMBL4210474 | — | IC50 | = | 627.0 | nM | 6.20 |
| CHEMBL4209694 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4211413 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL4216607 | — | IC50 | = | 965.0 | nM | 6.01 |
| CHEMBL4210897 | — | IC50 | = | 1441.0 | nM | 5.84 |
| CHEMBL4218942 | — | IC50 | = | 2830.0 | nM | 5.55 |
| CHEMBL4214781 | — | IC50 | = | 5504.0 | nM | 5.26 |
| CHEMBL4207999 | — | IC50 | = | 5967.0 | nM | 5.22 |
| CHEMBL4203120 | — | IC50 | = | 7170.0 | nM | 5.14 |
| CHEMBL554 | LAPATINIB | IC50 | > | 20000.0 | nM | - |