Assay Detail
Binding
CHEMBL5551007
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full-length recombinant N-terminal GST-tagged human CDK9 (1 to 372 residues)/His-tagged cyclinT1 (1 to 726 residues) expressed in baculovirus expression system using histone H1 as substrate preincubated for 10 mins followed by substrate and ATP addition and measured after 60 mins by ADP-Glo reagent based microplate reader assay
7
Total Activities
7
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 novel macrocyclic derivatives as potent and selective cyclin-dependent kinase 2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.81 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5569535 | — | — | 1 | 8.57 |
| CHEMBL5574687 | — | — | 1 | 8.24 |
| CHEMBL5570952 | — | — | 1 | 7.89 |
| CHEMBL5571565 | — | — | 1 | 7.79 |
| CHEMBL5574705 | — | — | 1 | 7.58 |
| CHEMBL5573573 | — | — | 1 | 7.36 |
| CHEMBL5574526 | — | — | 1 | 7.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5569535 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL5574687 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL5570952 | — | Ki | = | 12.8 | nM | 7.89 |
| CHEMBL5571565 | — | Ki | = | 16.3 | nM | 7.79 |
| CHEMBL5574705 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL5573573 | — | Ki | = | 43.3 | nM | 7.36 |
| CHEMBL5574526 | — | Ki | = | 60.0 | nM | 7.22 |