Assay Detail
Binding
CHEMBL2350831
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant His6 tagged CDK9/CyclinT1 expressed in Sf21 insect cells after 40 mins by scintillation counting analysis
37
Total Activities
36
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors: synthesis, X-ray crystal structures, structure-activity relationship, and anticancer activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 7.93 | 8.70 |
| IC50 | 1 | 7.85 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2347595 | — | — | 1 | 8.70 |
| CHEMBL2348842 | — | — | 1 | 8.70 |
| CHEMBL46429 | — | — | 1 | 8.70 |
| CHEMBL2348845 | — | — | 1 | 8.52 |
| CHEMBL2348648 | — | — | 1 | 8.52 |
| CHEMBL2348843 | — | — | 1 | 8.52 |
| CHEMBL2348647 | — | — | 1 | 8.40 |
| CHEMBL2347597 | ASNUCICLIB | 2.0 | 1 | 8.40 |
| CHEMBL2348649 | — | — | 1 | 8.40 |
| CHEMBL2348638 | — | — | 1 | 8.30 |
| CHEMBL2348642 | — | — | 1 | 8.30 |
| CHEMBL2348844 | — | — | 1 | 8.30 |
| CHEMBL2348650 | — | — | 1 | 8.30 |
| CHEMBL2312183 | — | — | 1 | 8.22 |
| CHEMBL2348644 | — | — | 1 | 8.22 |
| CHEMBL2312182 | — | — | 1 | 8.22 |
| CHEMBL2348651 | — | — | 1 | 8.15 |
| CHEMBL2312185 | — | — | 2 | 8.15 |
| CHEMBL2348646 | — | — | 1 | 8.15 |
| CHEMBL2348641 | — | — | 1 | 8.15 |
| CHEMBL2348847 | — | — | 1 | 8.10 |
| CHEMBL2348645 | — | — | 1 | 8.05 |
| CHEMBL2348637 | — | — | 1 | 7.96 |
| CHEMBL2348846 | — | — | 1 | 7.80 |
| CHEMBL2348652 | — | — | 1 | 7.72 |
| CHEMBL2348643 | — | — | 1 | 7.66 |
| CHEMBL2348848 | — | — | 1 | 7.18 |
| CHEMBL2348639 | — | — | 1 | 7.01 |
| CHEMBL2348653 | — | — | 1 | 6.87 |
| CHEMBL2348841 | — | — | 1 | 6.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2347595 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL46429 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2348842 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2348648 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2348843 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2348845 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2348647 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2348649 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2347597 | ASNUCICLIB | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2348844 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2348650 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2348642 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2348638 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2312183 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2348644 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2312182 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2348646 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2348651 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2348641 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2312185 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL2348847 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL2348645 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL2348637 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2312185 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2348846 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2348652 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2348643 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2348848 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL2348639 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL2348653 | — | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL2348841 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL2348654 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL2348840 | — | Ki | = | 278.0 | nM | 6.56 |
| CHEMBL2347594 | — | Ki | = | 932.0 | nM | 6.03 |
| CHEMBL2312193 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL2348640 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL2347596 | — | Ki | > | 5000.0 | nM | - |