Assay Detail
Binding
CHEMBL3707641
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Assay: To evaluate the in-vitro kinase potency of the compounds, they were screened against CDK 2 and CDK9. Kinase assays were performed in 96-well plates using recombinant CDK/cyclins generated at Cyclacel. Ltd Dundee, UK.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Trisubstituted purine derivatives
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.05 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3655764 | — | — | 1 | 7.22 |
| CHEMBL3655765 | — | — | 1 | 7.10 |
| CHEMBL3655762 | CYC-065 | 2.0 | 1 | 7.00 |
| CHEMBL3655772 | — | — | 1 | 6.60 |
| CHEMBL3655767 | — | — | 1 | 6.57 |
| CHEMBL3655768 | — | — | 1 | 6.42 |
| CHEMBL3655769 | — | — | 1 | 6.30 |
| CHEMBL3655770 | — | — | 1 | 6.21 |
| CHEMBL3655771 | — | — | 1 | 5.98 |
| CHEMBL3655773 | — | — | 1 | 5.69 |
| CHEMBL3655777 | — | — | 1 | 5.67 |
| CHEMBL3655763 | — | — | 1 | 5.44 |
| CHEMBL3655774 | — | — | 1 | 5.23 |
| CHEMBL3655775 | — | — | 1 | 5.18 |
| CHEMBL3655776 | — | — | 1 | 5.13 |
| CHEMBL3655766 | — | — | 1 | 5.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3655764 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL3655765 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL3655762 | CYC-065 | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3655772 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3655767 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3655768 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3655769 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3655770 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL3655771 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL3655773 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL3655777 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL3655763 | — | IC50 | = | 3630.0 | nM | 5.44 |
| CHEMBL3655774 | — | IC50 | = | 5840.0 | nM | 5.23 |
| CHEMBL3655775 | — | IC50 | = | 6530.0 | nM | 5.18 |
| CHEMBL3655776 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL3655766 | — | IC50 | = | 7890.0 | nM | 5.10 |