Assay Detail
Binding
CHEMBL5534151
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human His-tagged CDK7/cyclin H/MNAT1 expressed in baculovirus infected insect cells preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo kinase assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Insect cell |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery and optimization of thieno[3,2-d]pyrimidine derivatives as highly selective inhibitors of cyclin-dependent kinase 7.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.56 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5090754 | SY-5609 | 1.0 | 1 | 8.60 |
| CHEMBL5574236 | — | — | 1 | 8.21 |
| CHEMBL5574001 | — | — | 1 | 8.19 |
| CHEMBL5569504 | — | — | 1 | 8.14 |
| CHEMBL5573695 | — | — | 1 | 8.14 |
| CHEMBL5573538 | — | — | 1 | 8.06 |
| CHEMBL5594350 | — | — | 1 | 8.06 |
| CHEMBL5570731 | — | — | 1 | 8.05 |
| CHEMBL5542311 | — | — | 1 | 8.00 |
| CHEMBL5572618 | — | — | 1 | 7.99 |
| CHEMBL5594861 | — | — | 1 | 7.96 |
| CHEMBL5574040 | — | — | 1 | 7.65 |
| CHEMBL5564846 | — | — | 1 | 7.60 |
| CHEMBL5569637 | — | — | 1 | 7.58 |
| CHEMBL5592607 | — | — | 1 | 7.46 |
| CHEMBL5571051 | — | — | 1 | 7.42 |
| CHEMBL5572978 | — | — | 1 | 7.40 |
| CHEMBL5590200 | — | — | 1 | 7.28 |
| CHEMBL5567015 | — | — | 1 | 7.24 |
| CHEMBL5570965 | — | — | 1 | 7.24 |
| CHEMBL5569741 | — | — | 1 | 7.19 |
| CHEMBL5568630 | — | — | 1 | 7.14 |
| CHEMBL5592891 | — | — | 1 | 7.11 |
| CHEMBL5575677 | — | — | 1 | 7.06 |
| CHEMBL5595915 | — | — | 1 | 7.05 |
| CHEMBL5573083 | — | — | 1 | 7.02 |
| CHEMBL5562849 | — | — | 1 | 6.86 |
| CHEMBL5572474 | — | — | 1 | 6.85 |
| CHEMBL5572331 | — | — | 1 | 6.66 |
| CHEMBL5562749 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5090754 | SY-5609 | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5574236 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL5574001 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL5569504 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL5573695 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL5573538 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL5594350 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL5570731 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL5542311 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL5572618 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL5594861 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5574040 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL5564846 | — | IC50 | = | 25.2 | nM | 7.60 |
| CHEMBL5569637 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5592607 | — | IC50 | = | 34.9 | nM | 7.46 |
| CHEMBL5571051 | — | IC50 | = | 37.8 | nM | 7.42 |
| CHEMBL5572978 | — | IC50 | = | 39.7 | nM | 7.40 |
| CHEMBL5590200 | — | IC50 | = | 52.4 | nM | 7.28 |
| CHEMBL5567015 | — | IC50 | = | 57.9 | nM | 7.24 |
| CHEMBL5570965 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5569741 | — | IC50 | = | 65.1 | nM | 7.19 |
| CHEMBL5568630 | — | IC50 | = | 72.4 | nM | 7.14 |
| CHEMBL5592891 | — | IC50 | = | 78.3 | nM | 7.11 |
| CHEMBL5575677 | — | IC50 | = | 86.7 | nM | 7.06 |
| CHEMBL5595915 | — | IC50 | = | 89.5 | nM | 7.05 |
| CHEMBL5573083 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL5562849 | — | IC50 | = | 139.0 | nM | 6.86 |
| CHEMBL5572474 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL5572331 | — | IC50 | = | 218.0 | nM | 6.66 |
| CHEMBL5562749 | — | IC50 | > | 2000.0 | nM | - |