Assay Detail
Binding
CHEMBL3889223
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Caliper Assay: Selected compounds disclosed herein were tested in CDK4/cyclinD1, CDK6/CycD3 CDK2/CycA and CDK2/cyclinE kinase assays by Nanosyn (Santa Clara, Calif.) to determine their inhibitory effect on these CDKs. The assays were performed using microfluidic kinase detection technology (Caliper Assay Platform). The compounds were tested in 12-point dose-response format in singlicate at Km for ATP. Phosphoacceptor substrate peptide concentration used was 1 μM for all assays and Staurosporine was used as the reference compound for all assays. Specifics of each assay are as described below:CDK2/CyclinA: Enzyme concentration: 0.2 nM; ATP concentration: 50 μM; Incubation time: 3 hr.CDK2/CyclinE: Enzyme concentration: 0.28 nM; ATP concentration: 100 μM; Incubation time: 1 hr.CDK4/CyclinD1: Enzyme concentration: 1 nM; ATP concentration: 200 μM; Incubation time: 10 hr.CDK6/CyclinD3: Enzyme concentration: 1 nM; ATP concentration: 300 μM; Incubation time: 3 hr.
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 6 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Publication
Transient protection of normal cells during chemotherapy
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.29 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3890528 | — | — | 1 | 8.36 |
| CHEMBL3904602 | LEROCICLIB | 3.0 | 1 | 8.33 |
| CHEMBL3894860 | TRILACICLIB | 4.0 | 1 | 8.25 |
| CHEMBL3919361 | — | — | 1 | 8.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3890528 | — | IC50 | = | 4.38 | nM | 8.36 |
| CHEMBL3904602 | LEROCICLIB | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3894860 | TRILACICLIB | IC50 | = | 5.64 | nM | 8.25 |
| CHEMBL3919361 | — | IC50 | = | 5.99 | nM | 8.22 |