Assay Detail
Binding
CHEMBL4379571
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) (unknown origin) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr) 4:1 as substrate measured after 150 mins in presence of ATP by ADP-glo reagent based luminescence assay
19
Total Activities
19
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
Identification of a Multitargeted Tyrosine Kinase Inhibitor for the Treatment of Gastrointestinal Stromal Tumors and Acute Myeloid Leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 7.18 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4483070 | — | — | 1 | 7.62 |
| CHEMBL4448198 | — | — | 1 | 7.54 |
| CHEMBL4446778 | — | — | 1 | 7.33 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.32 |
| CHEMBL4521178 | — | — | 1 | 7.31 |
| CHEMBL4550794 | — | — | 1 | 7.31 |
| CHEMBL4438245 | — | — | 1 | 7.28 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.28 |
| CHEMBL4513768 | — | — | 1 | 7.25 |
| CHEMBL4457984 | — | — | 1 | 7.16 |
| CHEMBL4546349 | — | — | 1 | 7.04 |
| CHEMBL3593290 | — | — | 1 | 7.01 |
| CHEMBL4452166 | — | — | 1 | 7.00 |
| CHEMBL4475875 | — | — | 1 | 7.00 |
| CHEMBL4589974 | — | — | 1 | 6.97 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.96 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 6.94 |
| CHEMBL4558996 | — | — | 1 | 6.91 |
| CHEMBL4574485 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4483070 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4448198 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4446778 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL535 | SUNITINIB | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4521178 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4550794 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL4438245 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL941 | IMATINIB | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4513768 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL4457984 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4546349 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3593290 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL4452166 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4475875 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4589974 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL608533 | MIDOSTAURIN | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL1946170 | REGORAFENIB | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL4558996 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL4574485 | — | IC50 | > | 1000.0 | nM | - |