Assay Detail
Binding
CHEMBL3707754
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Kinase Assay: The compounds from the examples below were investigated for their CDK2/cyclin E, CDK1/cyclin B, CDK4/cyclin D1 and CDK7/cyclin H, ERK-2, and PKA inhibitory activity. His6-tagged recombinant human cyclin-dependent kinases CDK1/cyclin B1, CDK2/cyclin E, CDK4 and CDK7/cyclin H were expressed in sf9 cells using a baculovirus expression system. Recombinant cyclin D1 was expressed in E. coli. Proteins were purified by metal chelate affinity chromatography to greater than 90% homogeneity. Kinase assays were performed in 96-well plates using recombinant CDK/cyclins, recombinant active ERK-2 (Upstate Biotechnology), or cyclic AMP-dependent kinase (PKA) catalytic subunit (Calbiochem Cat. 539487). Assays were performed in assay buffer (25 mM beta -glycerophosphate, 20 mM MOPS, 5 mM EGTA, 1 mM DTT, 1 mM Na3VO3, pH 7.4), into which were added 2-4 ug of active enzyme with appropriate substrates (purified histone H1 for CDK2, recombinant GST-retinoblastoma protein (residues 773-928) for CDK4.
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Purine derivatives
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.00 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1922219 | — | — | 1 | 5.66 |
| CHEMBL1922212 | — | — | 1 | 5.36 |
| CHEMBL1922218 | — | — | 1 | 5.31 |
| CHEMBL1922123 | — | — | 1 | 5.21 |
| CHEMBL1922120 | — | — | 1 | 4.92 |
| CHEMBL1922209 | — | — | 1 | 4.89 |
| CHEMBL1922121 | — | — | 1 | 4.70 |
| CHEMBL1922211 | — | — | 1 | 4.68 |
| CHEMBL1922210 | — | — | 1 | 4.66 |
| CHEMBL1922122 | — | — | 1 | 4.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1922219 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL1922212 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL1922218 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL1922123 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL1922120 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1922209 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1922121 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL1922211 | — | IC50 | = | 21000.0 | nM | 4.68 |
| CHEMBL1922210 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL1922122 | — | IC50 | = | 23000.0 | nM | 4.64 |