Assay Detail
Binding
CHEMBL3705547
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.
20
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 | 20 | 6.95 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3655764 | — | — | 2 | 8.00 |
| CHEMBL3655762 | CYC-065 | 2.0 | 2 | 7.70 |
| CHEMBL3655765 | — | — | 2 | 7.70 |
| CHEMBL3655770 | — | — | 1 | 7.40 |
| CHEMBL3655772 | — | — | 1 | 7.40 |
| CHEMBL3655768 | — | — | 1 | 7.40 |
| CHEMBL3655771 | — | — | 1 | 7.30 |
| CHEMBL3655767 | — | — | 1 | 7.30 |
| CHEMBL3655773 | — | — | 1 | 7.30 |
| CHEMBL3655777 | — | — | 1 | 7.05 |
| CHEMBL3655769 | — | — | 1 | 6.80 |
| CHEMBL3655775 | — | — | 1 | 6.54 |
| CHEMBL3655763 | — | — | 2 | 6.28 |
| CHEMBL3655776 | — | — | 1 | 6.24 |
| CHEMBL3655774 | — | — | 1 | 6.11 |
| CHEMBL3655766 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3655764 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3655762 | CYC-065 | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3655765 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3655768 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3655770 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3655772 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3655771 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3655773 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3655767 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3655777 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3655762 | CYC-065 | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3655764 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3655765 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3655769 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3655775 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3655763 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3655776 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL3655774 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL3655766 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL3655763 | — | IC50 | = | 3250.0 | nM | 5.49 |