Assay Detail
Binding
CHEMBL5734552
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In-Vitro Kinase Inhibition Assay: Compounds 2-4 and cabozantinib were each tested for binding of c-Met, VEGFR2, TIE2 and the control compound, staurosporine. Specifically, each compound was tested at a 3-fold serial dilution starting at 10 microMolar (μM) in a 10-dose IC50 mode into an enzyme/substrate mixture using acoustic technology, and pre-incubated for 20 minutes to ensure compounds were equilibrated and bound to the enzyme. Staurosporine was used as a control and was tested at a 4-fold serial dilution starting at 20 μM. Next, 5 concentrations of ATP were added to initiate the reaction. The activity was monitored every 5-15 min for a time course study.
30
Total Activities
10
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Multi-tyrosine kinase inhibitors derivatives and methods of use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 8.85 | 10.46 |
| kon | 10 | - | - |
| k_off | 10 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 3 | 10.46 |
| CHEMBL1289926 | AXITINIB | 4.0 | 3 | 9.70 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 3 | 9.30 |
| CHEMBL1171837 | PONATINIB | 4.0 | 3 | 8.82 |
| CHEMBL1230609 | FORETINIB | 2.0 | 3 | 8.55 |
| CHEMBL254760 | — | — | 3 | 8.52 |
| CHEMBL572881 | MOTESANIB | 3.0 | 3 | 8.52 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 3 | 8.38 |
| CHEMBL1289494 | TIVOZANIB | 4.0 | 3 | 8.19 |
| CHEMBL535 | SUNITINIB | 4.0 | 3 | 8.05 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105717 | CABOZANTINIB | Ki | = | 0.035 | nM | 10.46 |
| CHEMBL1289926 | AXITINIB | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL491473 | CEDIRANIB | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL1171837 | PONATINIB | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1230609 | FORETINIB | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL254760 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL572881 | MOTESANIB | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL1946170 | REGORAFENIB | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL1289494 | TIVOZANIB | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL535 | SUNITINIB | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL1230609 | FORETINIB | k_off | = | - | s-1 | - |
| CHEMBL1230609 | FORETINIB | kon | = | - | — | - |
| CHEMBL1171837 | PONATINIB | k_off | = | - | s-1 | - |
| CHEMBL1171837 | PONATINIB | kon | = | - | — | - |
| CHEMBL491473 | CEDIRANIB | k_off | = | - | s-1 | - |
| CHEMBL491473 | CEDIRANIB | kon | = | - | — | - |
| CHEMBL1289926 | AXITINIB | k_off | = | - | s-1 | - |
| CHEMBL1289926 | AXITINIB | kon | = | - | — | - |
| CHEMBL2105717 | CABOZANTINIB | k_off | = | - | s-1 | - |
| CHEMBL2105717 | CABOZANTINIB | kon | = | - | — | - |
| CHEMBL254760 | — | kon | = | - | — | - |
| CHEMBL254760 | — | k_off | = | - | s-1 | - |
| CHEMBL572881 | MOTESANIB | kon | = | - | — | - |
| CHEMBL572881 | MOTESANIB | k_off | = | - | s-1 | - |
| CHEMBL1946170 | REGORAFENIB | kon | = | - | — | - |
| CHEMBL1946170 | REGORAFENIB | k_off | = | - | s-1 | - |
| CHEMBL535 | SUNITINIB | k_off | = | - | s-1 | - |
| CHEMBL1289494 | TIVOZANIB | kon | = | - | — | - |
| CHEMBL535 | SUNITINIB | kon | = | - | — | - |
| CHEMBL1289494 | TIVOZANIB | k_off | = | - | s-1 | - |