Assay Detail
Binding
CHEMBL2350828
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant His6 tagged CDK7/CyclinH/MAT1 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 7/ cyclin H (CHEMBL2111288) ↗| 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 | 6.59 | 7.40 |
| IC50 | 1 | 7.04 | 7.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2348845 | — | — | 1 | 7.40 |
| CHEMBL2312185 | — | — | 2 | 7.34 |
| CHEMBL2348842 | — | — | 1 | 7.33 |
| CHEMBL2348844 | — | — | 1 | 7.27 |
| CHEMBL2348843 | — | — | 1 | 7.19 |
| CHEMBL2348642 | — | — | 1 | 7.17 |
| CHEMBL2348644 | — | — | 1 | 7.15 |
| CHEMBL2347597 | ASNUCICLIB | 2.0 | 1 | 7.04 |
| CHEMBL2348641 | — | — | 1 | 7.04 |
| CHEMBL2348650 | — | — | 1 | 6.96 |
| CHEMBL2312183 | — | — | 1 | 6.94 |
| CHEMBL2348649 | — | — | 1 | 6.81 |
| CHEMBL2348647 | — | — | 1 | 6.71 |
| CHEMBL2348651 | — | — | 1 | 6.68 |
| CHEMBL2348847 | — | — | 1 | 6.59 |
| CHEMBL2312182 | — | — | 1 | 6.58 |
| CHEMBL2348846 | — | — | 1 | 6.56 |
| CHEMBL2348645 | — | — | 1 | 6.54 |
| CHEMBL2348646 | — | — | 1 | 6.52 |
| CHEMBL2348643 | — | — | 1 | 6.50 |
| CHEMBL46429 | — | — | 1 | 6.38 |
| CHEMBL2348652 | — | — | 1 | 6.36 |
| CHEMBL2348648 | — | — | 1 | 6.33 |
| CHEMBL2348848 | — | — | 1 | 6.33 |
| CHEMBL2348637 | — | — | 1 | 6.16 |
| CHEMBL2348638 | — | — | 1 | 5.93 |
| CHEMBL2348639 | — | — | 1 | 5.89 |
| CHEMBL2348840 | — | — | 1 | 5.81 |
| CHEMBL2347595 | — | — | 1 | 5.71 |
| CHEMBL2348841 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2348845 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL2312185 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL2348842 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL2348844 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL2348843 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL2348642 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL2348644 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL2347597 | ASNUCICLIB | Ki | = | 91.0 | nM | 7.04 |
| CHEMBL2312185 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL2348641 | — | Ki | = | 92.0 | nM | 7.04 |
| CHEMBL2348650 | — | Ki | = | 111.0 | nM | 6.96 |
| CHEMBL2312183 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL2348649 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL2348647 | — | Ki | = | 193.0 | nM | 6.71 |
| CHEMBL2348651 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL2348847 | — | Ki | = | 255.0 | nM | 6.59 |
| CHEMBL2312182 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL2348846 | — | Ki | = | 273.0 | nM | 6.56 |
| CHEMBL2348645 | — | Ki | = | 286.0 | nM | 6.54 |
| CHEMBL2348646 | — | Ki | = | 302.0 | nM | 6.52 |
| CHEMBL2348643 | — | Ki | = | 316.0 | nM | 6.50 |
| CHEMBL46429 | — | Ki | = | 417.0 | nM | 6.38 |
| CHEMBL2348652 | — | Ki | = | 433.0 | nM | 6.36 |
| CHEMBL2348648 | — | Ki | = | 473.0 | nM | 6.33 |
| CHEMBL2348848 | — | Ki | = | 464.0 | nM | 6.33 |
| CHEMBL2348637 | — | Ki | = | 685.0 | nM | 6.16 |
| CHEMBL2348638 | — | Ki | = | 1176.0 | nM | 5.93 |
| CHEMBL2348639 | — | Ki | = | 1285.0 | nM | 5.89 |
| CHEMBL2348840 | — | Ki | = | 1543.0 | nM | 5.81 |
| CHEMBL2347595 | — | Ki | = | 1960.0 | nM | 5.71 |
| CHEMBL2348841 | — | Ki | = | 1984.0 | nM | 5.70 |
| CHEMBL2348654 | — | Ki | = | 3474.0 | nM | 5.46 |
| CHEMBL2312193 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL2348653 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL2348640 | — | Ki | - | — | - | |
| CHEMBL2347596 | — | Ki | > | 5000.0 | nM | - |
| CHEMBL2347594 | — | Ki | > | 5000.0 | nM | - |