Assay Detail
Binding
CHEMBL5244064
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Inhibition of CDK2/cyclin E (unknown origin) assessed as inhibition constant incubated for 30 to 60 mins presence of dithiothreitol by Cheng-Prusoff equation analysis
12
Total Activities
12
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
2-Anilino-4-(1-methyl-1H-pyrazol-4-yl)pyrimidine-derived CDK2 inhibitors as anticancer agents: Design, synthesis & evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.70 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5286090 | — | — | 1 | 9.00 |
| CHEMBL2347597 | ASNUCICLIB | 2.0 | 1 | 8.52 |
| CHEMBL5281179 | — | — | 1 | 8.15 |
| CHEMBL5285230 | — | — | 1 | 8.10 |
| CHEMBL5277565 | — | — | 1 | 7.80 |
| CHEMBL5286293 | — | — | 1 | 7.75 |
| CHEMBL5286271 | — | — | 1 | 7.68 |
| CHEMBL5286978 | — | — | 1 | 7.64 |
| CHEMBL5277367 | — | — | 1 | 7.16 |
| CHEMBL5273574 | — | — | 1 | 7.06 |
| CHEMBL5287252 | — | — | 1 | 6.77 |
| CHEMBL5277074 | — | — | 1 | 6.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5286090 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2347597 | ASNUCICLIB | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL5281179 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL5285230 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL5277565 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL5286293 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL5286271 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL5286978 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL5277367 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL5273574 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL5287252 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL5277074 | — | Ki | = | 176.0 | nM | 6.75 |