Assay Detail
Binding
CHEMBL4386487
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of unactivated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 30 mins followed by ATP addition and measured after 120 mins by Kinase Glo based luminescence assay
3
Total Activities
3
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 |
Target
Mast/stem cell growth factor receptor Kit (CHEMBL1936) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of Conformational Control Inhibitors Switching off the Activated c-KIT and Targeting a Broad Range of Clinically Relevant c-KIT Mutants.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 6.79 | 7.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4448433 | — | — | 1 | 7.16 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.10 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4448433 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL535 | SUNITINIB | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL941 | IMATINIB | IC50 | = | 769.0 | nM | 6.11 |