Assay Detail
Binding
CHEMBL5609520
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Inhibition of CDK7/CycH/MNAT1 (unknown origin) assessed as change in TR-FRET ratio using Cdk7/9tide as substrate and ATP by in vitro Adapta Eu kinase assay
23
Total Activities
23
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 bivalent small molecule degraders of cyclin-dependent kinase 7 (CDK7).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.91 | 8.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5612636 | — | — | 1 | 8.25 |
| CHEMBL5613276 | — | — | 1 | 8.19 |
| CHEMBL5613200 | — | — | 1 | 8.17 |
| CHEMBL5613393 | — | — | 1 | 8.16 |
| CHEMBL5612049 | — | — | 1 | 8.12 |
| CHEMBL5612354 | — | — | 1 | 8.11 |
| CHEMBL5613342 | — | — | 1 | 8.09 |
| CHEMBL5611964 | — | — | 1 | 8.07 |
| CHEMBL5613703 | — | — | 1 | 8.06 |
| CHEMBL5613991 | — | — | 1 | 8.04 |
| CHEMBL5612986 | — | — | 1 | 8.03 |
| CHEMBL5613579 | — | — | 1 | 7.96 |
| CHEMBL5612749 | — | — | 1 | 7.95 |
| CHEMBL5613917 | — | — | 1 | 7.92 |
| CHEMBL5613656 | — | — | 1 | 7.90 |
| CHEMBL5612598 | — | — | 1 | 7.88 |
| CHEMBL5612241 | — | — | 1 | 7.87 |
| CHEMBL5613012 | — | — | 1 | 7.86 |
| CHEMBL5614037 | — | — | 1 | 7.75 |
| CHEMBL5612001 | — | — | 1 | 7.70 |
| CHEMBL5613124 | — | — | 1 | 7.68 |
| CHEMBL5612073 | — | — | 1 | 7.46 |
| CHEMBL5612364 | — | — | 1 | 6.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5612636 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5613276 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL5613200 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL5613393 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL5612049 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL5612354 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5613342 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL5611964 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL5613703 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL5613991 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL5612986 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL5613579 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL5612749 | — | IC50 | = | 11.3 | nM | 7.95 |
| CHEMBL5613917 | — | IC50 | = | 12.1 | nM | 7.92 |
| CHEMBL5613656 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL5612598 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL5612241 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL5613012 | — | IC50 | = | 13.7 | nM | 7.86 |
| CHEMBL5614037 | — | IC50 | = | 17.7 | nM | 7.75 |
| CHEMBL5612001 | — | IC50 | = | 20.1 | nM | 7.70 |
| CHEMBL5613124 | — | IC50 | = | 21.1 | nM | 7.68 |
| CHEMBL5612073 | — | IC50 | = | 34.4 | nM | 7.46 |
| CHEMBL5612364 | — | IC50 | = | 203.0 | nM | 6.69 |