Assay Detail
Binding
CHEMBL2350830
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant His6 tagged CDK1/Cyclin B 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 |
Target
Cyclin-dependent kinase 1/cyclin B1 (CHEMBL1907602) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
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 | 7.53 | 9.30 |
| IC50 | 1 | 6.73 | 6.73 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2348843 | — | — | 1 | 9.30 |
| CHEMBL2348844 | — | — | 1 | 9.00 |
| CHEMBL2348842 | — | — | 1 | 8.82 |
| CHEMBL2348847 | — | — | 1 | 8.70 |
| CHEMBL2348845 | — | — | 1 | 8.40 |
| CHEMBL2347597 | ASNUCICLIB | 2.0 | 1 | 8.40 |
| CHEMBL46429 | — | — | 1 | 8.30 |
| CHEMBL2312182 | — | — | 1 | 8.22 |
| CHEMBL2347595 | — | — | 1 | 8.22 |
| CHEMBL2312183 | — | — | 1 | 7.92 |
| CHEMBL2348846 | — | — | 1 | 7.75 |
| CHEMBL2348648 | — | — | 1 | 7.75 |
| CHEMBL2348637 | — | — | 1 | 7.72 |
| CHEMBL2348647 | — | — | 1 | 7.62 |
| CHEMBL2348646 | — | — | 1 | 7.58 |
| CHEMBL2348645 | — | — | 1 | 7.46 |
| CHEMBL2348642 | — | — | 1 | 7.38 |
| CHEMBL2348641 | — | — | 1 | 7.37 |
| CHEMBL2348643 | — | — | 1 | 7.35 |
| CHEMBL2348650 | — | — | 1 | 7.33 |
| CHEMBL2348638 | — | — | 1 | 7.21 |
| CHEMBL2348644 | — | — | 1 | 7.10 |
| CHEMBL2348649 | — | — | 1 | 7.06 |
| CHEMBL2348651 | — | — | 1 | 7.04 |
| CHEMBL2312185 | — | — | 2 | 7.03 |
| CHEMBL2348841 | — | — | 1 | 6.81 |
| CHEMBL2348848 | — | — | 1 | 6.75 |
| CHEMBL2348652 | — | — | 1 | 6.71 |
| CHEMBL2348840 | — | — | 1 | 6.48 |
| CHEMBL2348654 | — | — | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2348843 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL2348844 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL2348842 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL2348847 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2348845 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL2347597 | ASNUCICLIB | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL46429 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2312182 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2347595 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL2312183 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2348648 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2348846 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2348637 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL2348647 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2348646 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL2348645 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL2348642 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL2348641 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL2348643 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL2348650 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL2348638 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL2348644 | — | Ki | = | 79.0 | nM | 7.10 |
| CHEMBL2348649 | — | Ki | = | 88.0 | nM | 7.06 |
| CHEMBL2348651 | — | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL2312185 | — | Ki | = | 94.0 | nM | 7.03 |
| CHEMBL2348841 | — | Ki | = | 154.0 | nM | 6.81 |
| CHEMBL2348848 | — | Ki | = | 176.0 | nM | 6.75 |
| CHEMBL2312185 | — | IC50 | = | 188.0 | nM | 6.73 |
| CHEMBL2348652 | — | Ki | = | 195.0 | nM | 6.71 |
| CHEMBL2348840 | — | Ki | = | 334.0 | nM | 6.48 |
| CHEMBL2348654 | — | Ki | = | 556.0 | nM | 6.25 |
| CHEMBL2348639 | — | Ki | = | 788.0 | nM | 6.10 |
| CHEMBL2347594 | — | Ki | = | 1424.0 | nM | 5.85 |
| CHEMBL2348640 | — | Ki | - | — | - | |
| CHEMBL2347596 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL2312193 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL2348653 | — | Ki | > | 5000.0 | nM | - |