Assay Detail
Binding
CHEMBL4386485
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of 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 measured after 150 mins in presence of ATP by ADP-glo based luminescence assay
16
Total Activities
16
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 | 16 | 7.15 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3593291 | — | — | 1 | 7.82 |
| CHEMBL3593283 | — | — | 1 | 7.70 |
| CHEMBL4546279 | — | — | 1 | 7.42 |
| CHEMBL4465853 | — | — | 1 | 7.37 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.32 |
| CHEMBL4545864 | — | — | 1 | 7.30 |
| CHEMBL3593293 | — | — | 1 | 7.27 |
| CHEMBL4436208 | — | — | 1 | 7.15 |
| CHEMBL4448433 | — | — | 1 | 7.09 |
| CHEMBL4450651 | — | — | 1 | 7.09 |
| CHEMBL4530082 | — | — | 1 | 7.07 |
| CHEMBL3593290 | — | — | 1 | 7.01 |
| CHEMBL4528798 | — | — | 1 | 7.01 |
| CHEMBL4458373 | — | — | 1 | 6.91 |
| CHEMBL4473755 | — | — | 1 | 6.89 |
| CHEMBL4438683 | — | — | 1 | 6.02 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3593291 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3593283 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4546279 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4465853 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL535 | SUNITINIB | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4545864 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3593293 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4436208 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL4448433 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4450651 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4530082 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL3593290 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4528798 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4458373 | — | IC50 | = | 122.0 | nM | 6.91 |
| CHEMBL4473755 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4438683 | — | IC50 | = | 950.0 | nM | 6.02 |