Assay Detail
Binding
CHEMBL5376182
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Inhibition of human CDK7/Cyclin H preincubated for 20 mins followed by 32P-ATP addition and measured after 2 hrs
19
Total Activities
19
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 |
Target
Cyclin-dependent kinase 7/ cyclin H (CHEMBL2111288) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9 for MYC-Dependent Cancers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.66 | 6.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5440829 | — | — | 1 | 6.58 |
| CHEMBL5421527 | — | — | 1 | 6.52 |
| CHEMBL5438063 | — | — | 1 | 5.89 |
| CHEMBL5199065 | ISTISOCICLIB | 2.0 | 1 | 5.82 |
| CHEMBL5440226 | — | — | 1 | 5.73 |
| CHEMBL5428866 | — | — | 1 | 5.68 |
| CHEMBL5424203 | — | — | 1 | 5.12 |
| CHEMBL5405502 | — | — | 1 | 5.11 |
| CHEMBL5440331 | — | — | 1 | 5.05 |
| CHEMBL5419691 | — | — | 1 | 5.05 |
| CHEMBL5425977 | — | — | 1 | - |
| CHEMBL5406720 | — | — | 1 | - |
| CHEMBL5409162 | — | — | 1 | - |
| CHEMBL5411270 | — | — | 1 | - |
| CHEMBL5413258 | — | — | 1 | - |
| CHEMBL5419772 | — | — | 1 | - |
| CHEMBL5439995 | — | — | 1 | - |
| CHEMBL5421587 | — | — | 1 | - |
| CHEMBL5396123 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5440829 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL5421527 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5438063 | — | IC50 | = | 1298.0 | nM | 5.89 |
| CHEMBL5199065 | ISTISOCICLIB | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL5440226 | — | IC50 | = | 1880.0 | nM | 5.73 |
| CHEMBL5428866 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5424203 | — | IC50 | = | 7545.0 | nM | 5.12 |
| CHEMBL5405502 | — | IC50 | = | 7735.0 | nM | 5.11 |
| CHEMBL5440331 | — | IC50 | = | 8805.0 | nM | 5.05 |
| CHEMBL5419691 | — | IC50 | = | 8990.0 | nM | 5.05 |
| CHEMBL5425977 | — | IC50 | - | — | - | |
| CHEMBL5406720 | — | IC50 | - | — | - | |
| CHEMBL5409162 | — | IC50 | - | — | - | |
| CHEMBL5411270 | — | IC50 | - | — | - | |
| CHEMBL5413258 | — | IC50 | - | — | - | |
| CHEMBL5419772 | — | IC50 | - | — | - | |
| CHEMBL5439995 | — | IC50 | - | — | - | |
| CHEMBL5421587 | — | IC50 | - | — | - | |
| CHEMBL5396123 | — | IC50 | > | 10000.0 | nM | - |