Assay Detail
Binding
CHEMBL4032483
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CDK2/cyclin A (unknown origin) using histone H1 as substrate after 30 mins in presence of [33P]-gamma-ATP
30
Total Activities
30
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 |
Publication
Design of Novel 3-Pyrimidinylazaindole CDK2/9 Inhibitors with Potent In Vitro and In Vivo Antitumor Efficacy in a Triple-Negative Breast Cancer Model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.64 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4101278 | — | — | 1 | 9.00 |
| CHEMBL4065940 | — | — | 1 | 8.52 |
| CHEMBL4063017 | — | — | 1 | 8.40 |
| CHEMBL4089950 | — | — | 1 | 8.40 |
| CHEMBL4068858 | — | — | 1 | 8.30 |
| CHEMBL4074567 | — | — | 1 | 8.30 |
| CHEMBL4095226 | — | — | 1 | 8.26 |
| CHEMBL4097680 | — | — | 1 | 8.22 |
| CHEMBL4067806 | — | — | 1 | 8.05 |
| CHEMBL4077931 | — | — | 1 | 8.00 |
| CHEMBL4090021 | — | — | 1 | 8.00 |
| CHEMBL4098661 | — | — | 1 | 8.00 |
| CHEMBL4079646 | — | — | 1 | 8.00 |
| CHEMBL270686 | MERIOLIN 3 | — | 1 | 7.96 |
| CHEMBL4063190 | — | — | 1 | 7.92 |
| CHEMBL4071557 | — | — | 1 | 7.82 |
| CHEMBL4071643 | — | — | 1 | 7.80 |
| CHEMBL4090926 | — | — | 1 | 7.66 |
| CHEMBL4084840 | — | — | 1 | 7.64 |
| CHEMBL4095974 | — | — | 1 | 7.62 |
| CHEMBL4085794 | — | — | 1 | 7.12 |
| CHEMBL405665 | MERIOLIN 1 | — | 1 | 7.05 |
| CHEMBL4098589 | — | — | 1 | 7.04 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 6.97 |
| CHEMBL4068940 | — | — | 1 | 6.80 |
| CHEMBL4103720 | — | — | 1 | 6.74 |
| CHEMBL4060268 | — | — | 1 | 6.64 |
| CHEMBL4082174 | — | — | 1 | 6.52 |
| CHEMBL4105467 | — | — | 1 | 6.46 |
| CHEMBL4093541 | — | — | 1 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4101278 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4065940 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4063017 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4089950 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4068858 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4074567 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4095226 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL4097680 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4067806 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4077931 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4090021 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4098661 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4079646 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL270686 | MERIOLIN 3 | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4063190 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4071557 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4071643 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4090926 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4084840 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4095974 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4085794 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL405665 | MERIOLIN 1 | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL4098589 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL428690 | ALVOCIDIB | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL4068940 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4103720 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL4060268 | — | IC50 | = | 231.0 | nM | 6.64 |
| CHEMBL4082174 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4105467 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4093541 | — | IC50 | = | 1089.0 | nM | 5.96 |