Assay Detail
Binding
CHEMBL5547018
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length human CDK2 (1 to 298 residues)/N-terminal GST-tagged human Cyclin E1 (1 to 410 residues) expressed in baculovirus expression system preincubated for 10 mins followed by substrate addition and measured after 60 mins in presence of ATP by ADP-Glo reagent based luminescence microtiter plate reader analysis
12
Total Activities
12
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 2/cyclin E1 (CHEMBL1907605) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Design and Synthesis of Novel Macrocyclic Derivatives as Potent and Selective Cyclin-Dependent Kinase 7 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.03 | 8.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5574705 | — | — | 1 | 8.49 |
| CHEMBL5569632 | — | — | 1 | 7.71 |
| CHEMBL4297488 | CT-7001 | 2.0 | 1 | 7.64 |
| CHEMBL5571158 | — | — | 1 | 7.01 |
| CHEMBL5594541 | — | — | 1 | 7.00 |
| CHEMBL5573301 | — | — | 1 | 6.90 |
| CHEMBL5564220 | — | — | 1 | 6.76 |
| CHEMBL5571052 | — | — | 1 | 6.43 |
| CHEMBL5572932 | — | — | 1 | 6.19 |
| CHEMBL5573306 | — | — | 1 | 6.13 |
| CHEMBL5573062 | — | — | 1 | - |
| CHEMBL5573958 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5574705 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL5569632 | — | Ki | = | 19.4 | nM | 7.71 |
| CHEMBL4297488 | CT-7001 | Ki | = | 23.1 | nM | 7.64 |
| CHEMBL5571158 | — | Ki | = | 97.4 | nM | 7.01 |
| CHEMBL5594541 | — | Ki | = | 100.1 | nM | 7.00 |
| CHEMBL5573301 | — | Ki | = | 125.9 | nM | 6.90 |
| CHEMBL5564220 | — | Ki | = | 175.4 | nM | 6.76 |
| CHEMBL5571052 | — | Ki | = | 372.7 | nM | 6.43 |
| CHEMBL5572932 | — | Ki | = | 649.2 | nM | 6.19 |
| CHEMBL5573306 | — | Ki | = | 735.0 | nM | 6.13 |
| CHEMBL5573062 | — | Ki | - | — | - | |
| CHEMBL5573958 | — | Ki | - | — | - |