Assay Detail
Binding
CHEMBL1244477
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to KIT V559D,V654A mutant
7
Total Activities
7
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
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 7 | 7.02 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 9.68 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 7.58 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 7.44 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.62 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.42 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 5.80 |
| CHEMBL1240703 | CGP-52421 | — | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | Kd | = | 0.21 | nM | 9.68 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 26.0 | nM | 7.58 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 36.0 | nM | 7.44 |
| CHEMBL1336 | SORAFENIB | Kd | = | 240.0 | nM | 6.62 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL1240703 | CGP-52421 | Kd | = | 2500.0 | nM | 5.60 |