Assay Detail
Binding
CHEMBL4678926
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Inhibition of CDK9 in human MV4-11 cells assessed as induction of caspase-3/7 activation measured after 6 hrs followed by Caspase-glo reagent based assay
30
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MV4-11 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 6.76 | 7.86 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4462530 | ZEMIRCICLIB | 2.0 | 1 | 7.86 |
| CHEMBL4784117 | — | — | 1 | 7.82 |
| CHEMBL4752748 | — | — | 1 | 7.82 |
| CHEMBL4754081 | — | — | 1 | 7.54 |
| CHEMBL4740254 | — | — | 1 | 7.42 |
| CHEMBL4785242 | — | — | 1 | 7.41 |
| CHEMBL4749175 | — | — | 1 | 7.27 |
| CHEMBL4759074 | — | — | 2 | 7.17 |
| CHEMBL4753076 | — | — | 1 | 7.13 |
| CHEMBL4753256 | — | — | 2 | 7.11 |
| CHEMBL4741063 | — | — | 1 | 7.00 |
| CHEMBL4754399 | — | — | 1 | 6.89 |
| CHEMBL4784363 | — | — | 1 | 6.85 |
| CHEMBL4759053 | — | — | 1 | 6.82 |
| CHEMBL4751230 | — | — | 1 | 6.80 |
| CHEMBL4786995 | — | — | 1 | 6.75 |
| CHEMBL3673434 | — | — | 1 | 6.66 |
| CHEMBL4796500 | — | — | 1 | 6.58 |
| CHEMBL4788016 | — | — | 1 | 6.48 |
| CHEMBL4798156 | — | — | 1 | 6.38 |
| CHEMBL4780912 | — | — | 1 | 6.36 |
| CHEMBL4758821 | — | — | 1 | 6.25 |
| CHEMBL4760601 | — | — | 1 | 6.18 |
| CHEMBL4750648 | — | — | 1 | 6.17 |
| CHEMBL4756050 | — | — | 1 | 6.16 |
| CHEMBL4764361 | — | — | 1 | 6.04 |
| CHEMBL4789009 | — | — | 1 | 5.92 |
| CHEMBL4787309 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4462530 | ZEMIRCICLIB | EC50 | = | 13.7 | nM | 7.86 |
| CHEMBL4784117 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4752748 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4754081 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4740254 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4785242 | — | EC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4749175 | — | EC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4759074 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4753076 | — | EC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4753256 | — | EC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4753256 | — | EC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4741063 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4754399 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4784363 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4759053 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4751230 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4786995 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3673434 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4796500 | — | EC50 | = | 260.0 | nM | 6.58 |
| CHEMBL4788016 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL4798156 | — | EC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4780912 | — | EC50 | = | 440.0 | nM | 6.36 |
| CHEMBL4758821 | — | EC50 | = | 560.0 | nM | 6.25 |
| CHEMBL4760601 | — | EC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4750648 | — | EC50 | = | 670.0 | nM | 6.17 |
| CHEMBL4756050 | — | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL4764361 | — | EC50 | = | 910.0 | nM | 6.04 |
| CHEMBL4789009 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4787309 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4759074 | — | EC50 | = | 4800.0 | nM | 5.32 |