Assay Detail
Binding
CHEMBL5043166
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Inhibition of CDK12/cyclin K (unknown origin) using 5-FAM-labeled peptide as substrate in presence of ATP by mobility shift assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 7.10 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4791134 | — | — | 1 | 7.82 |
| CHEMBL4786320 | — | — | 1 | 7.62 |
| CHEMBL4555799 | — | — | 1 | 7.54 |
| CHEMBL4782954 | — | — | 1 | 7.48 |
| CHEMBL4786555 | — | — | 1 | 7.44 |
| CHEMBL5083688 | — | — | 1 | 7.22 |
| CHEMBL4779443 | — | — | 1 | 7.16 |
| CHEMBL5088381 | — | — | 1 | 7.12 |
| CHEMBL4786843 | — | — | 1 | 7.02 |
| CHEMBL4786592 | — | — | 1 | 6.99 |
| CHEMBL4790490 | — | — | 1 | 6.95 |
| CHEMBL4800180 | — | — | 1 | 6.87 |
| CHEMBL5080711 | — | — | 1 | 6.81 |
| CHEMBL4798916 | — | — | 1 | 6.67 |
| CHEMBL5090754 | SY-5609 | 1.0 | 1 | 5.77 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4791134 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4786320 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4555799 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4782954 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4786555 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5083688 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4779443 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL5088381 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4786843 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4786592 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL4790490 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL4800180 | — | IC50 | = | 135.0 | nM | 6.87 |
| CHEMBL5080711 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL4798916 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL5090754 | SY-5609 | IC50 | = | 1702.0 | nM | 5.77 |