Assay Detail
Binding
CHEMBL3707550
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Assay: The Cdk4 and Cdk6 inhibitory activity of the compounds is measured with a kinase inhibition assay using recombinant Cdk4/CyclinD1 or Cdk6/CyclinD3 protein complexes. The protein substrate used in the assay is the retinoblastoma protein (Rb). The kinase reactions are carried out in a 96-well filter plate (MSDV N6B50, Millipore). Compounds are serially diluted in kinase buffer (20 mM Tris-HCl, pH 7.4, 50 mM NaCl, 1 mM DTT, 1 mg/ml BSA) and added to the reaction mixture containing 2.5 ng/ml Cdk4/CyclinD1 or Cdk6/CyclinD3, 25 μM ATP, 10 μCi/ml [33P]-ATP, 0.1 μg/ml Rb in the kinase buffer. The mixture is incubated at room temperature for 1 hour and the proteins precipitated with an equal volume of 20% TCA. The plates are washed with 10% TCA according to the manufacturer's instruction and dried at room temperature. The amount of the phosphorylated Rb is determined with a TopCount (PerkinElmer).
267
Total Activities
265
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
Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 267 | 7.72 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3698653 | — | — | 1 | 9.44 |
| CHEMBL3698657 | — | — | 1 | 9.39 |
| CHEMBL3698681 | — | — | 1 | 9.12 |
| CHEMBL3237704 | — | — | 1 | 8.96 |
| CHEMBL3698644 | — | — | 1 | 8.96 |
| CHEMBL3698672 | — | — | 1 | 8.92 |
| CHEMBL3698643 | — | — | 1 | 8.89 |
| CHEMBL3698654 | — | — | 1 | 8.82 |
| CHEMBL3702091 | — | — | 1 | 8.70 |
| CHEMBL3702167 | — | — | 1 | 8.66 |
| CHEMBL3698658 | — | — | 1 | 8.60 |
| CHEMBL3702049 | — | — | 1 | 8.59 |
| CHEMBL3698675 | — | — | 1 | 8.59 |
| CHEMBL3698649 | — | — | 1 | 8.59 |
| CHEMBL3698733 | — | — | 1 | 8.59 |
| CHEMBL3702128 | — | — | 1 | 8.57 |
| CHEMBL3702093 | — | — | 1 | 8.55 |
| CHEMBL3702060 | — | — | 1 | 8.55 |
| CHEMBL3698639 | — | — | 1 | 8.54 |
| CHEMBL3702127 | — | — | 1 | 8.52 |
| CHEMBL3698674 | — | — | 1 | 8.51 |
| CHEMBL3642019 | — | — | 1 | 8.51 |
| CHEMBL3702129 | — | — | 1 | 8.51 |
| CHEMBL3702122 | — | — | 1 | 8.48 |
| CHEMBL3698661 | — | — | 1 | 8.46 |
| CHEMBL3702120 | — | — | 1 | 8.44 |
| CHEMBL3698682 | — | — | 1 | 8.43 |
| CHEMBL3641997 | — | — | 1 | 8.42 |
| CHEMBL3702130 | — | — | 1 | 8.41 |
| CHEMBL3698641 | — | — | 1 | 8.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3698653 | — | IC50 | = | 0.36 | nM | 9.44 |
| CHEMBL3698657 | — | IC50 | = | 0.41 | nM | 9.39 |
| CHEMBL3698681 | — | IC50 | = | 0.75 | nM | 9.12 |
| CHEMBL3237704 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3698644 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3698672 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3698643 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3698654 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3702091 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3702167 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3698658 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3698649 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3698675 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3698733 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3702049 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3702128 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3702060 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3702093 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3698639 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3702127 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3702129 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3642019 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3698674 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL3702122 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3698661 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL3702120 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3698682 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3641997 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3702130 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3698641 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL3237444 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3698671 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3237442 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3237702 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3702142 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3702052 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3702092 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3702067 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3642002 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3702050 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3702096 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3702154 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3641992 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3642014 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3642032 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3698659 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3702159 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3702065 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3698683 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL3698664 | — | IC50 | = | 5.7 | nM | 8.24 |