Assay Detail
Binding
CHEMBL5043164
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Binding affinity to full length CDK7 (1 to 346 residues) /N-terminal TEV cleavable 6His tagged full length cyclinH (1 to 323 residues) (unknown origin) expressed in baculovirus infected Sf9 cells by Surface plasmon resonance assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Cyclin-dependent kinase 7/ cyclin H (CHEMBL2111288) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 15 | 9.93 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5088381 | — | — | 1 | 10.52 |
| CHEMBL5080711 | — | — | 1 | 10.22 |
| CHEMBL4791134 | — | — | 1 | 10.15 |
| CHEMBL5090754 | SY-5609 | 1.0 | 1 | 10.15 |
| CHEMBL4786592 | — | — | 1 | 10.10 |
| CHEMBL4782954 | — | — | 1 | 10.10 |
| CHEMBL5083688 | — | — | 1 | 10.05 |
| CHEMBL4779443 | — | — | 1 | 10.00 |
| CHEMBL4790490 | — | — | 1 | 10.00 |
| CHEMBL4786320 | — | — | 1 | 9.82 |
| CHEMBL4798916 | — | — | 1 | 9.82 |
| CHEMBL4786555 | — | — | 1 | 9.68 |
| CHEMBL4555799 | — | — | 1 | 9.48 |
| CHEMBL4786843 | — | — | 1 | 9.47 |
| CHEMBL4800180 | — | — | 1 | 9.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5088381 | — | Kd | = | 0.03 | nM | 10.52 |
| CHEMBL5080711 | — | Kd | = | 0.06 | nM | 10.22 |
| CHEMBL4791134 | — | Kd | = | 0.07 | nM | 10.15 |
| CHEMBL5090754 | SY-5609 | Kd | = | 0.07 | nM | 10.15 |
| CHEMBL4786592 | — | Kd | = | 0.08 | nM | 10.10 |
| CHEMBL4782954 | — | Kd | = | 0.08 | nM | 10.10 |
| CHEMBL5083688 | — | Kd | = | 0.09 | nM | 10.05 |
| CHEMBL4779443 | — | Kd | = | 0.1 | nM | 10.00 |
| CHEMBL4790490 | — | Kd | = | 0.1 | nM | 10.00 |
| CHEMBL4786320 | — | Kd | = | 0.15 | nM | 9.82 |
| CHEMBL4798916 | — | Kd | = | 0.15 | nM | 9.82 |
| CHEMBL4786555 | — | Kd | = | 0.21 | nM | 9.68 |
| CHEMBL4555799 | — | Kd | = | 0.33 | nM | 9.48 |
| CHEMBL4786843 | — | Kd | = | 0.34 | nM | 9.47 |
| CHEMBL4800180 | — | Kd | = | 0.4 | nM | 9.40 |