Assay Detail
Binding
CHEMBL4678924
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full length human N-terminal GST-fused CDK9 (1 to 372 residues)/His-tagged CyclinT1 (1 to 726 residues) expressed in baculovirus infected insect cells using FITC-X-GSRTPMY-NH2 as substrate preincubated for 10 mins followed by MgCl2 addition and measured after 90 mins in presence of 5 mM ATP by mobility shift assay
37
Total Activities
35
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
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 |
|---|---|---|---|
| IC50 | 37 | 7.01 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4784117 | — | — | 1 | 8.52 |
| CHEMBL4754081 | — | — | 1 | 8.40 |
| CHEMBL4785242 | — | — | 1 | 8.10 |
| CHEMBL4749175 | — | — | 1 | 7.96 |
| CHEMBL4759074 | — | — | 2 | 7.77 |
| CHEMBL4747227 | — | — | 1 | 7.70 |
| CHEMBL4753076 | — | — | 1 | 7.66 |
| CHEMBL4786995 | — | — | 1 | 7.64 |
| CHEMBL4740254 | — | — | 1 | 7.60 |
| CHEMBL4753256 | — | — | 2 | 7.58 |
| CHEMBL3673434 | — | — | 1 | 7.54 |
| CHEMBL4741063 | — | — | 1 | 7.54 |
| CHEMBL4754399 | — | — | 1 | 7.41 |
| CHEMBL4751230 | — | — | 1 | 7.29 |
| CHEMBL4750372 | — | — | 1 | 7.22 |
| CHEMBL4784363 | — | — | 1 | 7.21 |
| CHEMBL4759053 | — | — | 1 | 7.21 |
| CHEMBL4777517 | — | — | 1 | 7.07 |
| CHEMBL4796500 | — | — | 1 | 6.96 |
| CHEMBL4792521 | — | — | 1 | 6.86 |
| CHEMBL4788016 | — | — | 1 | 6.75 |
| CHEMBL4764361 | — | — | 1 | 6.66 |
| CHEMBL4780912 | — | — | 1 | 6.64 |
| CHEMBL4758821 | — | — | 1 | 6.57 |
| CHEMBL4798156 | — | — | 1 | 6.54 |
| CHEMBL4756050 | — | — | 1 | 6.51 |
| CHEMBL4750648 | — | — | 1 | 6.46 |
| CHEMBL4760601 | — | — | 1 | 6.42 |
| CHEMBL4789009 | — | — | 1 | 6.18 |
| CHEMBL4765079 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4784117 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4754081 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4785242 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4749175 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4759074 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4747227 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4753076 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4786995 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4740254 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4753256 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4753256 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3673434 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4741063 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4754399 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL4751230 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4750372 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4784363 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4759053 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4777517 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4796500 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4792521 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL4788016 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4764361 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL4780912 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4758821 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4798156 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4756050 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4750648 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4760601 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL4789009 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4765079 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL4787309 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4764938 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL4799201 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL4759074 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL4752748 | — | IC50 | < | 3.0 | nM | - |
| CHEMBL4462530 | ZEMIRCICLIB | IC50 | < | 4.0 | nM | - |