Assay Detail
Binding
CHEMBL5353310
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of CDK9/CyclinT1 (unknown origin) by ADP-Glo kinase assay
23
Total Activities
23
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
Development and structure-activity relationship of tacrine derivatives as highly potent CDK2/9 inhibitors for the treatment of cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 8.30 | 8.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5436326 | — | — | 1 | 8.73 |
| CHEMBL5431262 | — | — | 1 | 8.73 |
| CHEMBL5440541 | — | — | 1 | 8.66 |
| CHEMBL5435196 | — | — | 1 | 8.66 |
| CHEMBL5432801 | — | — | 1 | 8.65 |
| CHEMBL5416114 | — | — | 1 | 8.62 |
| CHEMBL5416382 | — | — | 1 | 8.56 |
| CHEMBL5402856 | — | — | 1 | 8.54 |
| CHEMBL5431814 | — | — | 1 | 8.53 |
| CHEMBL5406985 | — | — | 1 | 8.47 |
| CHEMBL5419410 | — | — | 1 | 8.39 |
| CHEMBL5426191 | — | — | 1 | 8.24 |
| CHEMBL5421410 | — | — | 1 | 8.19 |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | 8.11 |
| CHEMBL5407954 | — | — | 1 | 8.08 |
| CHEMBL5432535 | — | — | 1 | 6.99 |
| CHEMBL5405290 | — | — | 1 | 6.95 |
| CHEMBL5415697 | — | — | 1 | - |
| CHEMBL5423439 | — | — | 1 | - |
| CHEMBL5394141 | — | — | 1 | - |
| CHEMBL5424301 | — | — | 1 | - |
| CHEMBL5427706 | — | — | 1 | - |
| CHEMBL5438785 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5436326 | — | IC50 | = | 1.87 | nM | 8.73 |
| CHEMBL5431262 | — | IC50 | = | 1.87 | nM | 8.73 |
| CHEMBL5440541 | — | IC50 | = | 2.19 | nM | 8.66 |
| CHEMBL5435196 | — | IC50 | = | 2.18 | nM | 8.66 |
| CHEMBL5432801 | — | IC50 | = | 2.23 | nM | 8.65 |
| CHEMBL5416114 | — | IC50 | = | 2.41 | nM | 8.62 |
| CHEMBL5416382 | — | IC50 | = | 2.77 | nM | 8.56 |
| CHEMBL5402856 | — | IC50 | = | 2.88 | nM | 8.54 |
| CHEMBL5431814 | — | IC50 | = | 2.97 | nM | 8.53 |
| CHEMBL5406985 | — | IC50 | = | 3.36 | nM | 8.47 |
| CHEMBL5419410 | — | IC50 | = | 4.11 | nM | 8.39 |
| CHEMBL5426191 | — | IC50 | = | 5.75 | nM | 8.24 |
| CHEMBL5421410 | — | IC50 | = | 6.39 | nM | 8.19 |
| CHEMBL296468 | BMS-387032 | IC50 | = | 7.821 | nM | 8.11 |
| CHEMBL5407954 | — | IC50 | = | 8.35 | nM | 8.08 |
| CHEMBL5432535 | — | IC50 | = | 101.7 | nM | 6.99 |
| CHEMBL5405290 | — | IC50 | = | 111.2 | nM | 6.95 |
| CHEMBL5415697 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5423439 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5394141 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5424301 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5427706 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5438785 | — | IC50 | > | 500.0 | nM | - |