Assay Detail
Binding
CHEMBL4386142
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged CDK2/Cyclin-E1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured in presence of [gamma-33P]ATP
39
Total Activities
39
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
3,5,7-Substituted Pyrazolo[4,3- d]pyrimidine Inhibitors of Cyclin-Dependent Kinases and Their Evaluation in Lymphoma Models.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 39 | 7.49 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4540226 | — | — | 1 | 8.70 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 8.70 |
| CHEMBL4524274 | — | — | 1 | 8.52 |
| CHEMBL4592599 | — | — | 1 | 8.52 |
| CHEMBL4450602 | — | — | 1 | 8.00 |
| CHEMBL4455558 | — | — | 1 | 7.96 |
| CHEMBL4453838 | — | — | 1 | 7.92 |
| CHEMBL4555088 | — | — | 1 | 7.92 |
| CHEMBL4439587 | — | — | 1 | 7.89 |
| CHEMBL4457612 | — | — | 1 | 7.75 |
| CHEMBL4445057 | — | — | 1 | 7.72 |
| CHEMBL4466439 | — | — | 1 | 7.72 |
| CHEMBL4451181 | — | — | 1 | 7.70 |
| CHEMBL4476075 | — | — | 1 | 7.68 |
| CHEMBL4436621 | — | — | 1 | 7.66 |
| CHEMBL4443897 | — | — | 1 | 7.57 |
| CHEMBL4524174 | — | — | 1 | 7.52 |
| CHEMBL4441727 | — | — | 1 | 7.52 |
| CHEMBL4471164 | — | — | 1 | 7.51 |
| CHEMBL4466975 | — | — | 1 | 7.50 |
| CHEMBL4563510 | — | — | 1 | 7.41 |
| CHEMBL4460642 | — | — | 1 | 7.39 |
| CHEMBL3775479 | — | — | 1 | 7.32 |
| CHEMBL4548100 | — | — | 1 | 7.28 |
| CHEMBL4535735 | — | — | 1 | 7.28 |
| CHEMBL4520596 | — | — | 1 | 7.23 |
| CHEMBL518800 | — | — | 1 | 7.21 |
| CHEMBL4534893 | — | — | 1 | 7.11 |
| CHEMBL4470943 | — | — | 1 | 7.11 |
| CHEMBL4559997 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4540226 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2103840 | DINACICLIB | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4592599 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4524274 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4450602 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4455558 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4453838 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4555088 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4439587 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4457612 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4466439 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4445057 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4451181 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4476075 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4436621 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4443897 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4524174 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4441727 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4471164 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4466975 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4563510 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4460642 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3775479 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4548100 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4535735 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4520596 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL518800 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4534893 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4470943 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4559997 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4465254 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4476377 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL4467247 | — | IC50 | = | 134.0 | nM | 6.87 |
| CHEMBL4435304 | — | IC50 | = | 138.0 | nM | 6.86 |
| CHEMBL4454328 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4557625 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL4441506 | — | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL4574449 | — | IC50 | = | 558.0 | nM | 6.25 |
| CHEMBL1873475 | IBRUTINIB | IC50 | > | 25000.0 | nM | - |