Assay Detail
Binding
CHEMBL4032485
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CDK9/cyclin T (unknown origin) using YSPTSPSYSPTSPSYSPTSPKKK 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 | 7.16 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 8.43 |
| CHEMBL270686 | MERIOLIN 3 | — | 1 | 8.22 |
| CHEMBL4098661 | — | — | 1 | 7.70 |
| CHEMBL4089950 | — | — | 1 | 7.66 |
| CHEMBL4095226 | — | — | 1 | 7.62 |
| CHEMBL4068858 | — | — | 1 | 7.57 |
| CHEMBL4097680 | — | — | 1 | 7.55 |
| CHEMBL405665 | MERIOLIN 1 | — | 1 | 7.52 |
| CHEMBL4101278 | — | — | 1 | 7.46 |
| CHEMBL4063017 | — | — | 1 | 7.42 |
| CHEMBL4071557 | — | — | 1 | 7.40 |
| CHEMBL4065940 | — | — | 1 | 7.38 |
| CHEMBL4074567 | — | — | 1 | 7.38 |
| CHEMBL4095974 | — | — | 1 | 7.35 |
| CHEMBL4077931 | — | — | 1 | 7.33 |
| CHEMBL4079646 | — | — | 1 | 7.28 |
| CHEMBL4090021 | — | — | 1 | 7.28 |
| CHEMBL4090926 | — | — | 1 | 7.23 |
| CHEMBL4067806 | — | — | 1 | 7.21 |
| CHEMBL4063190 | — | — | 1 | 7.09 |
| CHEMBL4084840 | — | — | 1 | 7.03 |
| CHEMBL4098589 | — | — | 1 | 6.84 |
| CHEMBL4103720 | — | — | 1 | 6.80 |
| CHEMBL4085794 | — | — | 1 | 6.67 |
| CHEMBL4071643 | — | — | 1 | 6.47 |
| CHEMBL4068940 | — | — | 1 | 6.35 |
| CHEMBL4093541 | — | — | 1 | 6.20 |
| CHEMBL4060268 | — | — | 1 | 6.19 |
| CHEMBL4105467 | — | — | 1 | 6.16 |
| CHEMBL4082174 | — | — | 1 | 6.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL428690 | ALVOCIDIB | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL270686 | MERIOLIN 3 | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4098661 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4089950 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4095226 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4068858 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4097680 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL405665 | MERIOLIN 1 | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4101278 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4063017 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4071557 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4065940 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4074567 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4095974 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4077931 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4079646 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4090021 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4090926 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4067806 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4063190 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4084840 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4098589 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL4103720 | — | IC50 | = | 159.0 | nM | 6.80 |
| CHEMBL4085794 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL4071643 | — | IC50 | = | 342.0 | nM | 6.47 |
| CHEMBL4068940 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL4093541 | — | IC50 | = | 625.0 | nM | 6.20 |
| CHEMBL4060268 | — | IC50 | = | 642.0 | nM | 6.19 |
| CHEMBL4105467 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4082174 | — | IC50 | = | 800.0 | nM | 6.10 |