Assay Detail
Binding
CHEMBL1840408
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [33P]ATP from human recombinant FLT3 domain after 20 mins by scintillation counting
31
Total Activities
31
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
Receptor-type tyrosine-protein kinase FLT3 (CHEMBL1974) ↗| 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 | 31 | 7.82 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1835746 | — | — | 1 | 9.00 |
| CHEMBL1835870 | — | — | 1 | 8.70 |
| CHEMBL1835867 | — | — | 1 | 8.70 |
| CHEMBL1835740 | — | — | 1 | 8.55 |
| CHEMBL1835871 | — | — | 1 | 8.30 |
| CHEMBL1835869 | — | — | 1 | 8.30 |
| CHEMBL1835749 | — | — | 1 | 8.30 |
| CHEMBL1835747 | — | — | 1 | 8.30 |
| CHEMBL1833992 | — | — | 1 | 8.22 |
| CHEMBL1835750 | — | — | 1 | 8.15 |
| CHEMBL1835748 | — | — | 1 | 8.10 |
| CHEMBL1835866 | — | — | 1 | 8.05 |
| CHEMBL1835864 | — | — | 1 | 8.00 |
| CHEMBL1835736 | — | — | 1 | 7.96 |
| CHEMBL1835863 | — | — | 1 | 7.96 |
| CHEMBL1835751 | — | — | 1 | 7.92 |
| CHEMBL1835865 | — | — | 1 | 7.92 |
| CHEMBL1835743 | — | — | 1 | 7.92 |
| CHEMBL1835744 | — | — | 1 | 7.82 |
| CHEMBL1835741 | — | — | 1 | 7.82 |
| CHEMBL1835742 | — | — | 1 | 7.75 |
| CHEMBL1835745 | — | — | 1 | 7.66 |
| CHEMBL1835662 | — | — | 1 | 7.66 |
| CHEMBL1835663 | — | — | 1 | 7.62 |
| CHEMBL1835661 | — | — | 1 | 7.38 |
| CHEMBL1835739 | — | — | 1 | 7.28 |
| CHEMBL1835660 | — | — | 1 | 7.07 |
| CHEMBL1835664 | — | — | 1 | 6.68 |
| CHEMBL1835738 | — | — | 1 | 6.03 |
| CHEMBL1835737 | — | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1835746 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1835870 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1835867 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL1835740 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL1835871 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1835869 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1835749 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1835747 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1833992 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL1835750 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL1835748 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL1835866 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL1835864 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL1835736 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1835863 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL1835751 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1835865 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1835743 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1835744 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL1835741 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL1835742 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL1835745 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL1835662 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL1835663 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL1835661 | — | Ki | = | 42.0 | nM | 7.38 |
| CHEMBL1835739 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL1835660 | — | Ki | = | 85.0 | nM | 7.07 |
| CHEMBL1835664 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL1835738 | — | Ki | = | 930.0 | nM | 6.03 |
| CHEMBL1835737 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL1835868 | — | Ki | < | 1.0 | nM | - |