Assay Detail
Binding
CHEMBL1840409
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [33P]ATP from human recombinant c-KIT domain after 20 mins by scintillation counting
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Design, synthesis, and evaluation of a novel dual FMS-like tyrosine kinase 3/stem cell factor receptor (FLT3/c-KIT) inhibitor for the treatment of acute myelogenous leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 7.34 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1835740 | — | — | 1 | 8.05 |
| CHEMBL1835864 | — | — | 1 | 8.00 |
| CHEMBL1835741 | — | — | 1 | 7.92 |
| CHEMBL1835747 | — | — | 1 | 7.75 |
| CHEMBL1835863 | — | — | 1 | 7.68 |
| CHEMBL1835743 | — | — | 1 | 7.43 |
| CHEMBL1835749 | — | — | 1 | 7.42 |
| CHEMBL1833992 | — | — | 1 | 7.22 |
| CHEMBL1835866 | — | — | 1 | 6.75 |
| CHEMBL1835745 | — | — | 1 | 6.69 |
| CHEMBL1835865 | — | — | 1 | 6.62 |
| CHEMBL1835746 | — | — | 1 | 6.57 |
| CHEMBL1835751 | — | — | 1 | - |
| CHEMBL1835871 | — | — | 1 | - |
| CHEMBL1835870 | — | — | 1 | - |
| CHEMBL1835869 | — | — | 1 | - |
| CHEMBL1835868 | — | — | 1 | - |
| CHEMBL1835867 | — | — | 1 | - |
| CHEMBL1835750 | — | — | 1 | - |
| CHEMBL1835744 | — | — | 1 | - |
| CHEMBL1835742 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1835740 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL1835864 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1835741 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1835747 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL1835863 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL1835743 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL1835749 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL1833992 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL1835866 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL1835745 | — | Ki | = | 205.0 | nM | 6.69 |
| CHEMBL1835865 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL1835746 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL1835751 | — | Ki | < | 50.0 | nM | - |
| CHEMBL1835871 | — | Ki | - | — | - | |
| CHEMBL1835870 | — | Ki | < | 1.0 | nM | - |
| CHEMBL1835869 | — | Ki | < | 50.0 | nM | - |
| CHEMBL1835868 | — | Ki | < | 50.0 | nM | - |
| CHEMBL1835867 | — | Ki | < | 0.001 | nM | - |
| CHEMBL1835750 | — | Ki | < | 50.0 | nM | - |
| CHEMBL1835744 | — | Ki | - | — | - | |
| CHEMBL1835742 | — | Ki | - | — | - |