Assay Detail
Binding
CHEMBL5165830
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant N-terminal GST/His6-fusion tagged human CDK4/Cyclin D3 expressed in Sf9 insect cells using 5-FAM-IPTSPITTTYFFFKKK as substrate preincubated for 10 mins followed by substrate addition and incubated for 3 hrs in presence of ATP by caliper mobility shift analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Novel Src Homology-2 Domain Containing Protein Tyrosine Phosphatase-2 (SHP2) and Cyclin-Dependent Kinase 4 (CDK4) Dual Inhibitor for the Treatment of Triple-Negative Breast Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.45 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 8.82 |
| CHEMBL5200081 | — | — | 1 | 8.17 |
| CHEMBL5200166 | — | — | 1 | 8.15 |
| CHEMBL5179046 | — | — | 1 | 8.09 |
| CHEMBL5177262 | — | — | 1 | 8.06 |
| CHEMBL5176602 | — | — | 1 | 8.04 |
| CHEMBL5195043 | — | — | 1 | 7.79 |
| CHEMBL5179617 | — | — | 1 | 7.74 |
| CHEMBL5205964 | — | — | 1 | 7.29 |
| CHEMBL5194505 | — | — | 1 | 7.02 |
| CHEMBL5196278 | — | — | 1 | 6.86 |
| CHEMBL5172609 | — | — | 1 | 6.67 |
| CHEMBL5184331 | — | — | 1 | 6.35 |
| CHEMBL5204959 | — | — | 1 | 6.35 |
| CHEMBL5199829 | — | — | 1 | 6.29 |
| CHEMBL5180571 | — | — | 1 | - |
| CHEMBL5184558 | — | — | 1 | - |
| CHEMBL5171286 | — | — | 1 | - |
| CHEMBL5178361 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3301610 | ABEMACICLIB | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5200081 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL5200166 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5179046 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL5177262 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL5176602 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL5195043 | — | IC50 | = | 16.1 | nM | 7.79 |
| CHEMBL5179617 | — | IC50 | = | 18.2 | nM | 7.74 |
| CHEMBL5205964 | — | IC50 | = | 51.1 | nM | 7.29 |
| CHEMBL5194505 | — | IC50 | = | 95.9 | nM | 7.02 |
| CHEMBL5196278 | — | IC50 | = | 139.3 | nM | 6.86 |
| CHEMBL5172609 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL5184331 | — | IC50 | = | 445.4 | nM | 6.35 |
| CHEMBL5204959 | — | IC50 | = | 442.5 | nM | 6.35 |
| CHEMBL5199829 | — | IC50 | = | 519.0 | nM | 6.29 |
| CHEMBL5180571 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5184558 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5171286 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5178361 | — | IC50 | > | 1000.0 | nM | - |