Assay Detail
Binding
CHEMBL911174
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Inhibition of CDK2/Cyclin E in presence of 15 uM ATP
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 E (CHEMBL2094126) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 4.90 | 5.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL386422 | — | — | 1 | 5.60 |
| CHEMBL215205 | — | — | 1 | 5.46 |
| CHEMBL280074 | OLOMOUCINE | — | 1 | 5.30 |
| CHEMBL214475 | — | — | 1 | 5.22 |
| CHEMBL387068 | — | — | 1 | 5.21 |
| CHEMBL425089 | — | — | 1 | 5.00 |
| CHEMBL215072 | — | — | 1 | 4.82 |
| CHEMBL428639 | — | — | 1 | 4.77 |
| CHEMBL384625 | — | — | 1 | 4.66 |
| CHEMBL217734 | — | — | 1 | 4.64 |
| CHEMBL425975 | — | — | 1 | 4.55 |
| CHEMBL217836 | — | — | 1 | 4.40 |
| CHEMBL216673 | — | — | 1 | 4.04 |
| CHEMBL383939 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL386422 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL215205 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL280074 | OLOMOUCINE | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL214475 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL387068 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL425089 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL215072 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL428639 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL384625 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL217734 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL425975 | — | IC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL217836 | — | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL216673 | — | IC50 | = | 92000.0 | nM | 4.04 |
| CHEMBL383939 | — | IC50 | > | 100000.0 | nM | - |