Assay Detail
Binding
CHEMBL5136664
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 Sf9 cells using histone H1 as substrate in presence of ATP and [gamma33-P]ATP by radioisotope filter binding assay
29
Total Activities
29
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-<i>d</i>]Pyrimidine Inhibitors of Cyclin-Dependent Kinases and Cyclin K Degraders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 7.75 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5171387 | — | — | 1 | 8.70 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 8.52 |
| CHEMBL5182767 | — | — | 1 | 8.40 |
| CHEMBL5187378 | — | — | 1 | 8.40 |
| CHEMBL5194202 | — | — | 1 | 8.40 |
| CHEMBL5209068 | — | — | 1 | 8.30 |
| CHEMBL5169449 | — | — | 1 | 8.30 |
| CHEMBL5184795 | — | — | 1 | 8.30 |
| CHEMBL5207899 | — | — | 1 | 8.30 |
| CHEMBL5191136 | — | — | 1 | 8.22 |
| CHEMBL5187158 | — | — | 1 | 8.22 |
| CHEMBL5183669 | — | — | 1 | 8.22 |
| CHEMBL5169627 | — | — | 1 | 8.10 |
| CHEMBL5195127 | — | — | 1 | 8.05 |
| CHEMBL5176463 | — | — | 1 | 7.96 |
| CHEMBL5194833 | — | — | 1 | 7.92 |
| CHEMBL5179519 | — | — | 1 | 7.92 |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | 7.75 |
| CHEMBL5205821 | — | — | 1 | 7.72 |
| CHEMBL5208001 | — | — | 1 | 7.62 |
| CHEMBL5173574 | — | — | 1 | 7.60 |
| CHEMBL5176720 | — | — | 1 | 7.43 |
| CHEMBL5201329 | — | — | 1 | 7.37 |
| CHEMBL5187017 | — | — | 1 | 7.28 |
| CHEMBL5201069 | — | — | 1 | 7.12 |
| CHEMBL5171541 | — | — | 1 | 6.59 |
| CHEMBL5198145 | — | — | 1 | 6.33 |
| CHEMBL5199692 | — | — | 1 | 6.01 |
| CHEMBL5181131 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5171387 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL2103840 | DINACICLIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5182767 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5187378 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5194202 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5209068 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5169449 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5184795 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5207899 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5191136 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5187158 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5183669 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5169627 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5195127 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5176463 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5194833 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5179519 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL14762 | SELICICLIB | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5205821 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5208001 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5173574 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5176720 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5201329 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5187017 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5201069 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL5171541 | — | IC50 | = | 256.0 | nM | 6.59 |
| CHEMBL5198145 | — | IC50 | = | 464.0 | nM | 6.33 |
| CHEMBL5199692 | — | IC50 | = | 978.0 | nM | 6.01 |
| CHEMBL5181131 | — | IC50 | = | 2302.0 | nM | 5.64 |