Assay Detail
Binding
CHEMBL4686308
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human FLT3 ITD mutant EAIYAAPFAKKK peptide as substrate in presence of 33P-gamma ATP by hotspot kinase assay
9
Total Activities
9
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
A series of novel aryl-methanone derivatives as inhibitors of FMS-like tyrosine kinase 3 (FLT3) in FLT3-ITD-positive acute myeloid leukemia.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.99 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4790597 | — | — | 1 | 9.14 |
| CHEMBL4745937 | — | — | 1 | 8.64 |
| CHEMBL4765060 | — | — | 1 | 8.41 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 8.38 |
| CHEMBL4755980 | — | — | 1 | 7.96 |
| CHEMBL4754982 | — | — | 1 | 7.92 |
| CHEMBL4740264 | — | — | 1 | 7.47 |
| CHEMBL4751666 | — | — | 1 | 7.07 |
| CHEMBL4764595 | — | — | 1 | 6.88 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4790597 | — | IC50 | = | 0.73 | nM | 9.14 |
| CHEMBL4745937 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4765060 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL576982 | QUIZARTINIB | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4755980 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4754982 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4740264 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4751666 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4764595 | — | IC50 | = | 133.0 | nM | 6.88 |